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Patent Searching and Data


Title:
COMPOUNDS
Document Type and Number:
WIPO Patent Application WO/2023/115165
Kind Code:
A1
Abstract:
The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

Inventors:
BANISTER SAMUEL (AU)
JORGENSEN WILLIAM (AU)
TAN JINLONG (AU)
Application Number:
PCT/AU2022/051591
Publication Date:
June 29, 2023
Filing Date:
December 23, 2022
Export Citation:
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Assignee:
PSYLO PTY LTD (AU)
International Classes:
C07D471/04; A61K31/407; A61K31/416; A61K31/423; A61P25/00; A61P25/18; A61P25/24; C07D231/56; C07D261/20
Domestic Patent References:
WO2013063492A12013-05-02
WO2022120181A12022-06-09
Foreign References:
EP0870768A11998-10-14
Other References:
COMANITA BOGDAN ET AL: "Synthesis and Reactivity of Some Mannich Bases. VII. Synthesis of 3-(2-dialkylaminoethyl)-1,2-benzioxazoles", HETEROCYCLES, JAPAN INSTITUTE OF HETEROCYCLIC CHEMISTRY, JP, vol. 51, no. 9, 30 November 1998 (1998-11-30), JP , pages 2139 - 2146, XP009547152, ISSN: 0385-5414, DOI: 10.3987/COM-99-8556
MANIK PULLAGURLA ET AL: "5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS", MEDICINAL CHEMISTRY RESEARCH, BIRKHÄUSER-VERLAG, BOSTON, vol. 14, no. 1, 1 January 2005 (2005-01-01), Boston , pages 1 - 18, XP019202365, ISSN: 1554-8120, DOI: 10.1007/s00044-004-0121-8
ZHU, J. ET AL.: "An effective procedure for the preparation of 3-substituted-4- or 6- azaindoles from ortho-methyl nitro pyridines", TETRAHEDRON LETTERS, vol. 47, 2006, pages 5653 - 5656, XP025004602, DOI: 10.1016/j.tetlet.2006.06.017
Attorney, Agent or Firm:
FPA PATENT ATTORNEYS PTY LTD (AU)
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Claims:
CLAIMS 1. A compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R1 and R2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4 and SO2R4, said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; alternatively R1 and R2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR4, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4, SO2R4, C1-6 alkyl, C1-6 haloalkyl, C2- 6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; R3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3 and one of R1 and R2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4, SO2R4, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; each R4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR5, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R5, C(O)N(R5)2, OR5, N(R5)2, NO2, SR5 and SO2R5, said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR5; each R5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X1 is N, NR6, O or S; X2 is CR7, N, O or S; Z1 is CR8 or N; Z2 is CR9 or N; Z3 is CR10 or N; Z4 is CR11 or N; R6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR12)2, C(O)R12, CO2R12, C(O)N(R12)2, S(O)R12 and SO2R12, C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12 and SO2R12, said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR12; each R12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R7, R8, R9, R10 and R11 are each independently selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13 and SO2R13, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X2 is CR7, R7 and one of R1, R2, or R3 may be combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; alternatively, when X1 is NR6 and X2 is CR7, R6 and R7 may be combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; alternatively, when Z1 is CR8 and Z2 is CR9, or when Z2 is CR9 and Z3 is CR10, or when Z3 is CR10 and Z4 is CR11, then R8 and R9, or R9 and R10, or R10 and R11 may be combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; each R14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3- 10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X2, Z1, Z2, Z3 and Z4 are heteroatoms; and wherein the compound of formula (I) is not one of the following: 2. The compound of claim 1, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein one of X2, Z1, Z2, Z3 and Z4 is a heteroatom. 3. The compound of claim 1 or 2, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein X1, X2, Z1, Z2, Z3 and Z4 are defined by embodiments 1-6: Embodiment X1 X2 Z1 Z2 Z3 Z4 No. 1 NR6 CR7 N CR9 CR10 CR11 2 NR6 CR7 CR8 CR9 CR10 N

4. The compound of claim 3, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein X1, X2, Z1, Z2, Z3 and Z4 are according to any one of embodiments 1-4. 5. The compound of any one of claims 1 to 4, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein X1 is NR6. 6. The compound of any one of claims 1-5, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R6 (if present) is H. 7. The compound of any one of claims 1-6, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein one of R8 and R9 (if present) is selected from halogen, OR13, N(R13)2, SR13, C1-6 alkyl and C1-6 haloalkyl, the other (if present) is hydrogen. 8. The compound of claim 7, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein each R13 (if present) is independently selected from hydrogen and C1-6 alkyl. 9. The compound of claim 7 or 8, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R7, R10 and R11 (if present) are hydrogen. 10. The compound of any one of claims 1-9, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R1 and R2 are each independently selected from C1-4 alkyl.

11. The compound of any one of claims 1-10, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R1 and R2, together with the nitrogen to which they are attached, form any one of the following: 12. The compound of any one of claims 1-10, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R3 is hydrogen. 13. The compound of any one of claims 1-12, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein L is methylene. 14. The compound of any one of claims 1-13, selected from: Code Structure P-1 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 15. A medicament comprising a compound of any one of claims 1-14 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 16. A pharmaceutical composition comprising a compound of any one of claims 1-14 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, and a pharmaceutically acceptable excipient. 17. A method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R1 and R2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4 and SO2R4, said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C4-C14 alkyleneheterocycloalkyl, C3- C8 heterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; alternatively R1 and R2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR4, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4, SO2R4, C1-6 alkyl, C1-6 haloalkyl, C2- 6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; R3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3 and one of R1 and R2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R4, C(O)N(R4)2, OR4, N(R4)2, NO2, SR4, SO2R4, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR4; each R4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR5, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R5, C(O)N(R5)2, OR5, N(R5)2, NO2, SR5 and SO2R5, said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR5; each R5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X1 is N, NR6, O or S; X2 is CR7, N, O or S; Z1 is CR8 or N; Z2 is CR9 or N; Z3 is CR10 or N; Z4 is CR11 or N; R6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR12)2, C(O)R12, CO2R12, C(O)N(R12)2, S(O)R12 and SO2R12, C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12 and SO2R12, said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR12; each R12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R7, R8, R9, R10 and R11 are each independently selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13 and SO2R13, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X2 is CR7, R7 and one of R1, R2, or R3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; alternatively, when X1 is NR6 and X2 is CR7, R6 and R7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; alternatively, when Z1 is CR8 and Z2 is CR9, or when Z2 is CR9 and Z3 is CR10, or when Z3 is CR10 and Z4 is CR11, then R8 and R9, or R9 and R10, or R10 and R11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R14, C(O)N(R14)2, OR14, N(R14)2, NO2, SR14, SO2R14, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR14; each R14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3- 10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X2, Z1, Z2, Z3 and Z4 are heteroatoms. 19. A method of treating a mental illness, comprising administering to a subject in need thereof an effective amount of a compound defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof,.

20. A method of treating a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof an effective amount of a compound defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 21. A method for increasing neuronal plasticity and/or increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound as defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 22. The method of any one of claims 17-21, wherein the compound of formula (I), or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, is a compound of any one of claims 1-14, optionally administered in the form of the medicament of claim 15 or the pharmaceutical composition of claim 16.

Description:
Compounds This application claims priority to Australian provisional application no.2021904268 (filed on 24 December 2021), the entire contents of which is incorporated herein by reference. Field of the invention The present disclosure relates generally to novel compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders. Background of the invention Mental illness covers many neuropsychiatric disorders which cause enormous burden to the lives of their sufferers. Diagnoses such as treatment resistant depression, major depressive disorder, eating disorders, substance abuse disorders, post-traumatic stress disorder, obsessive compulsive disorder, attention deficit disorders, schizophrenia, and others can cause such devastating symptoms that many sufferers lose the capability of leading a normal life. A variety of serotonergic drugs such as antidepressants, serotonin reuptake inhibitors, monoamine oxidase inhibitors, selective serotonin reuptake inhibitors, and others are commercially available to treat mental illnesses. Unfortunately, in many indications, these therapeutics provide limited benefit when compared to a placebo. Additionally, these therapeutics can result in a wide range of side effects including loss of libido, insomnia, fatigue, weight gain, and others. In spite of their limited efficacy, these drugs continue to be used to treat neuropsychiatric conditions as well as a broad range of auxiliary medical indications. There have been limited advances in new treatment options since many of these drugs were released, and the pharmaceutical industry has come under increased financial pressure to de-emphasise neuroscience programmes entirely. The unmet need for more efficacious mental health treatment is on the rise, and the global COVID-19 pandemic is likely to increase disease burden around the world. In the 1950s and 1960s, the use of psychedelic drugs to treat various mental illnesses was extensively explored, and these substances showed promise as treatments for many diseases of the central nervous system (CNS). Following decades of prohibition, scientific research into the application of psychedelics as treatments for mental illnesses has been gaining momentum. The serotonergic psychedelic agent psilocybin has been designated a Breakthrough Therapy by the FDA for the treatment of major depressive disorder (2019) and treatment-resistant depression (2018). Psilocybin is the prodrug compound produced by many species of mushrooms known collectively as psilocybin mushrooms or “magic mushrooms”. Psilocybin is rapidly metabolized to the bioactive compound psilocin, which produces a state of altered consciousness including changes in perception, visual hallucinations, and distorted sense of space, time, and self. Many patients report spiritual or “mystical” experiences which have profound and lasting impact on the patients’ mood and behaviour. Psilocybin has shown promise in more than 50 clinical trials for neuropsychiatric indications, including numerous anxiety disorders, obsessive-compulsive disorder, anorexia nervosa, alcohol dependence, and tobacco addiction. Psilocybin and other psychedelic compounds such as N,N- dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) have both immediate and persistent effects on mental state, with the latter extending far beyond the duration of action, possibly as a result of their ability to incite increased neuroplasticity, promote neural outgrowth, and increase spine density of the synaptic neurons in the brain. To date, psilocybin remains classified as a controlled substance and/or drug of abuse in most countries under national drug laws. However, clinical investigations have recently led to increased awareness of the potential for psychedelic drugs as breakthrough therapies to treat CNS diseases of enormous unmet medical need. Despite its therapeutic potential, psilocybin and other psychedelics remain scheduled drugs of abuse in most countries and the commercial path to market for these drugs as medicines is uncertain. As an adjunct to psychotherapy, the long duration of action of psilocybin and LSD make treatment sessions costly and impractical for broad implementation. In spite of a long history of safe human use, several adverse events have been reported in clinical trials, and it is possible that these may be attributed to signalling bias at 5-HT2A (the primary target) or off-target activity at, for example, 5- HT2B receptors (a cardiac liability antitarget) or 5-HT1A (an anxiolytic target) or 5-HT2C receptors (a disease-relevant target for obesity and some genetic epilepsies, for example). Naturally-occurring psychedelics provide important lead structures for a new generation of neurotherapeutic agents with novel mechanisms of action and/or superior clinical efficacy to currently available neuropsychiatric medications. In view of the foregoing there is an ongoing need to develop new compounds which may be useful in the treatment of mental illness or central nervous system disorders. Reference to any prior art in the specification is not an acknowledgment or suggestion that this prior art forms part of the common general knowledge in any jurisdiction or that this prior art could reasonably be expected to be understood, regarded as relevant, and/or combined with other pieces of prior art by a skilled person in the art. Summary of the invention In one aspect the present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 together with the nitrogen atom to which they are attached form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 together the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C 3 -C 7 cycloalkyl and C 3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X 1 is N, NR 6 , O or S; X 2 is CR 7 , N, O or S; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR 12 )2, C(O)R 12 , CO2R 12 , C(O)N(R 12 )2, S(O)R 12 and SO2R 12 , C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C 1-6 alkyl, C 2 - 6 alkenyl, C 2 - 6 alkynyl, C 3 - 6 cycloalkyl, C 6 - 9 alkylenecycloalkyl, C 3 - 6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 12 , C(O)N(R 12 )2, OR 12 , N(R 12 )2, NO2, SR 12 and SO2R 12 , said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 12 ; each R 12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 , R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 ) 2 , SO 2 R 13 , N(R 13 ) 2 , N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 ) 2 , NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X 2 is CR 7 , R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C 5 - 8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when X 1 is NR 6 and X 2 is CR 7 , R 6 and R 7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C 1 - 8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms; and wherein the compound of formula (I) is not one of the following: . In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following:

In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In any one of the herein disclosed embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- alkyleneP(O)(OR 13 ) S(O)R 13 S(O)N(R 13 ) SO R 13 N(R 13 ) N(R 13 )C(O)R 13 N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C 4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 7 (if present) is selected from H and C1-6alkyl, preferably R 7 (if present) is H. In some embodiments, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO 2 H, CO 2 CH 3 , C(O)NH 2 , C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C 5-8 heterocycloalkyl or C 5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, L is C1-4 alkylene. In some embodiments, L is methylene. In any one of the herein disclosed embodiments, R 6 is selected from hydrogen and C1-6 alkyl. In any one of the herein disclosed embodiments, R 6 is hydrogen. In some embodiments, X 1 is NH or N. In some embodiments, the compound of formula (I) has the formula (II): wherein R 1 , R 2 , R 3 , R 7 , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. In some embodiments the compound of formula (I) has the formula (IIa): wherein R 1 , R 2 , R 3 , R 7 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments the compound of formula (II) has the formula (IIb): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (IIc): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (IId): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 10 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (III): wherein R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (IIIa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (IV): wherein X2 is O or S, and R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (IVa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In any one of the herein disclosed embodiments X 1 is O. In some embodiments, the compound of formula (I) has the formula (V): wherein R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) has the formula (Va): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments, the compound of formula (I) is selected from any one of the following:

or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In another aspect the present disclosure provides a medicament comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In another aspect the present disclosure provides a pharmaceutical composition comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, and a pharmaceutically acceptable excipient. In another aspect the present disclosure provides a pharmaceutical composition comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, an additional therapeutic agent, and a pharmaceutically acceptable excipient. In another aspect the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C4-C14 alkyleneheterocycloalkyl, C3-C8 heterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO 2 , N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C 1 - 6 alkyl, C 2 - 6 alkenyl, C 2 - 6 alkynyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, C 5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X 1 is N, NR 6 , O or S; X 2 is CR 7 , N, O or S; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR 12 )2, C(O)R 12 , CO2R 12 , C(O)N(R 12 )2, S(O)R 12 and SO2R 12 , C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3- 6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 12 , C(O)N(R 12 )2, OR 12 , N(R 12 )2, NO2, SR 12 and SO2R 12 , said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C 7-18 alkylenearyl, C 5-10 heteroaryl, and C 6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 12 ; each R 12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 , R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C 1 - 8 alkylamino, C 1-8 alkylsulfonyl, CO 2 R 13 , C(O)N(R 13 ) 2 , OR 13 , NO 2 , N(R 13 ) 2 , SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X 2 is CR 7 , R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when X 1 is NR 6 and X 2 is CR 7 , R 6 and R 7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C 4-10 heterocycloalkyl and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms. In some embodiments of the method, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C 4-14 alkylenecycloalkyl. In some embodiments of the method, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments of the method, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: In some embodiments of the method, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments of the method, R 3 is hydrogen. In some embodiments of the method, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, SR 4 , NO2, SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments of the method, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2- 6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments of the method, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2- 6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 -C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments of the method, 1 or 2 of R 7 , R 8 R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 R 9 , R 10 and R 11 are each hydrogen.In some embodiments of the method, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments of the method, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments of the method, R 8 and R 9 are combined to form a C 5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments of the method, L is C1-4 alkylene. In some embodiments of the method, L is methylene. In some embodiments of the method, R 6 is selected from hydrogen and C1-6 alkyl. In some embodiments of the method, R 6 is hydrogen. In some embodiments of the method, X 1 is NH or N. In some embodiments of the method, the compound of formula (I) has the formula (II): wherein R 1 , R 2 , R 3 , , R 7 , , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. In some embodiments of the method, the compound of formula (I) has the formula (IIa): wherein R 1 , R 2 , R 3 , R 7 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IIb): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IIc): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IId): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 10 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (III): wherein R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IIIa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IV): wherein X2 is O or S, and R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (IVa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has X 1 as O. In some embodiments of the method, the compound of formula (I) has the formula (V): wherein R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) has the formula (Va): ( a) wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are defined as in any one of the foregoing paragraphs. In some embodiments of the method, the compound of formula (I) is selected from any one of the following: , or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In another aspect the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in combination with another known agent useful for treatment of a disease, disorder or condition by activation of a serotonin receptor. In another aspect the present disclosure provides a method of treating a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In some embodiments, the mental illness is selected from anxiety disorders; depression; mood disorders; psychotic disorders; impulse control and addiction disorders; drug addiction; obsessive-compulsive disorder (OCD); post-traumatic stress disorder (PTSD); stress response syndromes; dissociative disorders; depersonalization disorder; factitious disorders; sexual and gender disorders; somatic symptom disorders; hallucinations; delusions; psychosis; and combinations thereof In another aspect the present disclosure provides a method for treating a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In some embodiments, the CNS disease, disorder or condition and/or neurological disease, disorder or condition is selected from neurological diseases including neurodevelopmental diseases and neurodegenerative diseases such as Alzheimer’s disease; presenile dementia; senile dementia; vascular dementia; Lewy body dementia; cognitive impairment, Parkinson’s disease and Parkinsonian related disorders such as Parkinson dementia, corticobasal degeneration, and supranuclear palsy; epilepsy; CNS trauma; CNS infections; CNS inflammation; stroke; multiple sclerosis; Huntington’s disease; mitochondrial disorders; Fragile X syndrome; Angelman syndrome; hereditary ataxias; neuro-otological and eye movement disorders; neurodegenerative diseases of the retina amyotrophic lateral sclerosis; tardive dyskinesias; hyperkinetic disorders; attention deficit hyperactivity disorder and attention deficit disorders; restless leg syndrome; Tourette's syndrome; schizophrenia; autism spectrum disorders; tuberous sclerosis; Rett syndrome; cerebral palsy; disorders of the reward system including eating disorders such as anorexia nervosa and bulimia nervosa; binge eating disorder, trichotillomania, dermotillomania, nail biting; migraine; fibromyalgia; and peripheral neuropathy of any etiology, and combinations thereof. In another aspect the present disclosure provides a method for increasing neuronal plasticity and/or increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N- oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in an amount sufficient to increase neuronal plasticity and/or increase dendritic spine density of the neuronal cell. In another aspect the present disclosure provides methods of treating weight, comprising administering an effective amount of a compound of the invention to a subject in need thereof. Treatment of weight may include treating weight gain; weight loss; metabolic disorder; weight gain associated with pharmaceutical intervention; weight gain associated with a mental illness (including those described herein); eating disorders such as anorexia, bulimia, cachexia, etc.; eating behaviour; obesity; diabetes; insulin resistance; pre-diabetes; glucose intolerance; hyperlipidemia; and cardiovascular disease. In another aspect the present disclosure provides a method for activating a serotonin receptor in a cell either in a biological sample or in a patient comprising administering a compound of formula (I) as defined in any one of the herein disclosed embodiments to the cell. Any embodiment herein shall be taken to apply mutatis mutandis to any other embodiment unless specifically stated otherwise. The present disclosure is not to be limited in scope by the specific embodiments described herein, which are intended for the purpose of exemplification only. Functionally-equivalent products, compositions and methods are clearly within the scope of the invention, as described herein. Further aspects of the present invention and further embodiments of the aspects described in the preceding paragraphs will become apparent from the following description, given by way of example and with reference to the accompanying drawings. Brief description of the drawings Figure 1: Plasma concentrations of a subset of exemplar compounds P-8, P-5, P-3, and P-1 in male C57BL/6 mice following IP administration at 10 mg/kg described in Example 49. Figure 2: Time binned and mean ± SD (n = 3) HTR counts of a subset of exemplar compounds P-4, P-3, and P-1 in male C57BL/6 mice following SC administration over several doses as described in Example 50. Figure 3: Temperature results displayed as mean ± SD (n = 3) HTR counts of a subset of exemplar compounds P-4, P-3, and P-1 in male C57BL/6 mice following SC administration over several doses as described in Example 50. Figure 4: Locomotor results (total distance) displayed as mean ± SD (n = 3) HTR counts of a subset of exemplar compounds P-4, P-3, and P-1 in male C57BL/6 mice following SC administration over several doses as described in Example 50. Figure 5: Locomotor results (distance/time) displayed as mean ± SD (n = 3) HTR counts of a subset of exemplar compounds P-4, P-3, and P-1 in male C57BL/6 mice following SC administration over several doses as described in Example 50. Figure 6: Time immobilisation results from tail suspension test (TST) experiments described in Example 51 for compounds P-3.2HCl (3mg/kg; 10mg/kg) and P-8.2HCl (3mg/kg; 10mg/kg; 30mg/kg) compared with ketamine (10mg/kg) and vehicle. Detailed description of the embodiments It will be understood that the invention disclosed and defined in this specification extends to all alternative combinations of two or more of the individual features mentioned or evident from the text or drawings. All of these different combinations constitute various alternative aspects of the invention. Definitions For purposes of interpreting this specification, terms used in the singular will also include the plural and vice versa. As used herein, except where the context requires otherwise, the term "comprise" and variations of the term, such as "comprising", "comprises" and "comprised", are not intended to exclude further additives, components, integers or steps. The terms "treatment" or "treating" of a subject includes delaying, slowing, stabilizing, curing, healing, alleviating, relieving, altering, remedying, less worsening, ameliorating, improving, or affecting the disease or condition, the sign or symptom of the disease or condition, or the risk of (or susceptibility to) the disease or condition. The term "treating" refers to any indication of success in the treatment or amelioration of an injury, pathology or condition, including any objective or subjective parameter such as abatement; remission; lessening of the rate of worsening; lessening severity of the disease; stabilization, diminishing of signs or symptoms or making the injury, pathology or condition more tolerable to the individual; slowing in the rate of degeneration or decline; making the final point of degeneration less debilitating. In particularly preferred embodiments, the methods of the present invention can be to prevent or reduce the severity, or inhibit or minimise progression, of a sign or symptom of a disease or condition as described herein. As such, the methods of the present invention have utility as treatments as well as prophylaxes. As used herein, "preventing" or "prevention" is intended to refer to at least the reduction of likelihood of the risk of (or susceptibility to) acquiring a disease or disorder (ie causing at least one of the clinical signs or symptoms of the disease not to develop in an individual that may be exposed to or predisposed to the disease but does not yet experience or display signs or symptoms of the disease). Biological and physiological parameters for identifying such patients are provided herein and are also well known by physicians. Herein, the term “subject” or “patient" can be used interchangeably with each other. The term “individual” or “patient” refers to an animal that is treatable by the compound and/or method, respectively, including but not limited to, for example, dogs, cats, horses, sheep, pigs, cows, and the like, as well as human, non-human primates. Unless otherwise specified, the “subject” or “patient” may include both male and female genders. Further, it also includes a subject or patient, preferably a human, suitable for receiving treatment with a pharmaceutical composition and/or method of the present invention. The term "selective" means a greater activity against a first target (e.g., a 5-HT receptor subtype) relative to a second target (e.g., a second 5-HT receptor subtype). In some embodiments a compound has a selectivity of at least 1.25-fold, at least 1.5 fold, at least 2- fold, at least 3-fold, at least 4-fold, at least 5-fold, at least 6-fold, at least 10-fold or at least 100-fold greater towards a first target relative to a second target. In some embodiments, a compound described herein is selective towards the 5-HT2A receptor relative to one or more other 5-HT receptor subtypes such as 5-HT2B and/or 5-HT2C, preferably 5-HT2B. In some embodiments, a compound described herein is selective towards the 5-HT2c receptor relative to one or more other 5-HT receptor subtypes such as 5-HT2A and/or 5-HT2B, preferably 5-HT2B. "About" as used herein when referring to a measurable value such as an amount, a temporal duration, and the like, is meant to encompass variations of ±20% or ±10%, in some instances ±5%, in some instances ±1%, and in some instances ±0.1% from the specified value, as such variations are appropriate to perform the disclosed methods. Ranges: throughout this disclosure, various aspects of the invention can be presented in a range format. It should be understood that the description in range format is merely for convenience and brevity and should not be construed as an inflexible limitation on the scope of the invention. Accordingly, the description of a range should be considered to have specifically disclosed all the possible subranges as well as individual numerical values within that range. For example, description of a range such as from 1 to 6 should be considered to have specifically disclosed subranges such as from 1 to 3, from 1 to 4, from 1 to 5, from 2 to 4, from 2 to 6, from 3 to 6 etc., as well as individual numbers within that range, for example, 1, 2, 2.7, 3, 4, 5, 5.3, and 6. This applies regardless of the breadth of the range. As used herein the term "alkyl" refers to a straight or branched chain hydrocarbon radical having from one to twelve carbon atoms, or any range between, i.e. it contains 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 carbon atoms. The alkyl group is optionally substituted with substituents. Examples of "alkyl" as used herein include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, n-pentyl, isopentyl, and the like. As used herein, the terms "C1-C2 alkyl", "C1-C3 alkyl" and "C1-C6 alkyl" refer to an alkyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (eg alkyl groups containing 2-5 carbon atoms are also within the range of C1-C6). The term “alkylene” refers to a straight or branched, saturated, aliphatic radical having the number of carbon atoms indicated, and linking at least two other groups, i.e., a divalent hydrocarbon radical. The two moieties linked to the alkylene can be linked to the same atom or different atoms of the alkylene group. For instance, a straight chain alkylene can be the bivalent radical of –(CH2)n–, where n is 1, 2, 3, 4, 5 or 6. Representative alkylene groups include, but are not limited to, methylene, ethylene, propylene, isopropylene, butylene, isobutylene, sec-butylene, pentylene and hexylene. The term “alkenyl” whether it is used alone or as part of another group, means a straight or branched chain, saturated alkylene group, that is, a saturated carbon chain that contains substituents on two of its ends. The number of carbon atoms that are possible in the referenced alkylene group are indicated by the prefix “Cn1-n2”. For example, the term C2-6 alkylene means an alkylene group having 2, 3, 4, 5 or 6 carbon atoms. Examples of alkenyl groups include, but are not limited to, vinyl (ethenyl), propenyl, isopropenyl, 1-butenyl, 2-butenyl, isobutenyl, butadienyl, 1-pentenyl, 2-pentenyl, isopentenyl, 1,3-pentadienyl, 1,4-pentadienyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 1,3- hexadienyl, 1 ,4-hexadienyl, 1,5-hexadienyl, 2,4-hexadienyl, or 1,3,5-hexatrienyl. The term “alkynyl” as used herein, whether it is used alone or as part of another group, means straight or branched chain, unsaturated alkynyl groups containing at least one triple bond. The number of carbon atoms that are possible in the referenced alkyl group are indicated by the prefix “Cn1-n2”. For example, the term C2-6 alkynyl means an alkynyl group having 2, 3, 4, 5 or 6 carbon atoms. Examples of alkynyl groups include, but are not limited to, acetylenyl, propynyl, 1-butynyl, 2-butynyl, butadiynyl, 1-pentynyl, 2- pentynyl, isopentynyl, 1,3-pentadiynyl, 1,4-pentadiynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 1,3-hexadiynyl, 1,4-hexadiynyl, 1,5-hexadiynyl, 2,4-hexadiynyl, or 1,3,5-hexatriynyl. The term "cycloalkyl" is intended to include mono-, bi- or tricyclic alkyl groups. The number of carbon atoms that are possible in the referenced cycloalkyl group are indicated by the prefix “Cn1-n2”. For example, the term C3-8 cycloalkyl means an cycloalkyl group having 3, 4, 5, 6, 7 or 8 carbon atoms. In some embodiments, cycloalkyl groups have from 3 to 12, from 3 to 10, from 3 to 8, from 3 to 6, from 3 to 5 carbon atoms in the ring(s). In some embodiments, cycloalkyl groups have 5 or 6 ring carbon atoms. Examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. In some embodiments, the cycloalkyl group has from 3 to 8, from 3 to 7, from 3 to 6, from 4 to 6, from 3 to 5, or from 4 to 5 ring carbon atoms. Bi- and tricyclic ring systems include bridged, spiro, and fused cycloalkyl ring systems. Examples of bi- and tricyclic ring cycloalkyl systems include, but are not limited to, bicyclo[2.1.1]hexanyl, bicyclo[2.2.1]heptanyl, adamantyl, and decalinyl. The term "alkylenecycloalkyl" refers to a radical having an alkyl component and a cycloalkyl component, where the alkyl component links the cycloalkyl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the cycloalkyl component and to the point of atachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The cycloalkyl component is as defined herein. The numerical range from x to y in “Cx-y alkylenecycloalkyl” relates to the total number of alkyl carbons and cycloalkyl ring atoms. Exemplary alkylenecycloalkyl groups include, but are not limited to, methylenecyclopropyl, methylenecyclobutyl, methylenecyclopentyl and methylenecyclohexyl. The term “aryl” refers to an aromatic ring system having any suitable number of ring atoms and any suitable number of rings. The number of carbon atoms that are possible in the referenced aryl group are indicated by the prefix “C n1-n2 ”. For example, the term C6-12 aryl means an aryl group having 6, 7, 8, 9, 10, 11 or 12 carbon atoms. Aryl groups can include any suitable number of ring atoms, such as, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 16 ring atoms, as well as from 6 to 10, 6 to 12, or 6 to 14 ring members. Aryl groups can be monocyclic, fused to form bicyclic or tricyclic groups, or linked by a bond to form a biaryl group. Representative aryl groups include phenyl, naphthyl and biphenyl. Other aryl groups include benzyl, having a methylene linking group. Some aryl groups have from 6 to 12 ring members, such as phenyl, naphthyl or biphenyl. Other aryl groups have from 6 to 10 ring members, such as phenyl or naphthyl. Some other aryl groups have 6 ring members, such as phenyl. The term “alkylenearyl” refers to a radical having an alkyl component and an aryl component, where the alkyl component links the aryl component to the point of attachment. The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the aryl component and to the point of attachment. The alkyl component can include any number of carbons, such as C1-6, C1- 2, C1-3, C1-4, C1-5, C1-6, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. In some instances, the alkyl component can be absent. The aryl component is as defined above. The numerical range from x to y in “Cx-y alkylenearyl” relates to the total number of alkyl carbons and aryl ring atoms. Examples of alkylenearyl groups include, but are not limited to, benzyl and ethylenephenyl. As used herein, the term “alkoxy” refers to an alkyl group as defined herein covalently bound via an O linkage. The alkoxy group is optionally substituted with substituents. Examples of “alkoxy” as used herein include, but are not limited to methoxy, ethoxy, propoxy, isoproxy, butoxy, iso-butoxy, tert-butoxy and pentoxy. As used herein, the terms "C1-C2 alkoxy", "C1-C3 alkoxy" and "C1-C6 alkoxy" refer to an alkoxy group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (eg alkoxy groups containing 2-5 carbon atoms are also within the range of C1-C6). As used herein, the term “alkylamine” refers to an alkyl group as defined herein having one or more amino groups. The amino groups can be primary, secondary or tertiary. The alkyl amine can be further substituted with a hydroxy group to form an amino- hydroxy group. Examples of alkylamines include, but are not limited to, ethyl amine, propyl amine, isopropyl amine, ethylene diamine and ethanolamine. The amino group can link the alkyl amine to the point of attachment with the rest of the compound, be at the omega position of the alkyl group, or link together at least two carbon atoms of the alkyl group. As used herein, the terms "C1-C2 alkylamine", "C1-C3 alkylamine" and "C1-C6 alkylamine " refer to an alkylamine group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g., alkylamine groups containing 2-5 carbon atoms are also within the range of C1-C6). As used herein, the term “alkylsulfonyl” refers to an alkyl group as defined herein having one or more sulfonyl groups. The sulfonyl group can link the alkylsulfonyl to the point of attachment with the rest of the compound, be at the omega position of the alkyl group, or link together at least two carbon atoms of the alkyl group. As used herein, the terms "C1-C2 alkylsulfonyl", "C1-C3 alkylsulfonyl" and "C1-C6 alkylsulfonyl" refer to an alkylsulfonyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g., alkylsulfonyl groups containing 2-5 carbon atoms are also within the range of C1-C6). The term "heteroatom" as used herein means an atom of any element other than carbon or hydrogen. Examples of heteroatoms include nitrogen, oxygen, sulfur and phosphorus. Preferred heteroatoms include N, O and S, preferably N and O. The term “heteromoiety" as used herein means a chemical group comprising a heteroatom. Examples of heteromoieties include O, S, S(O), SO2, N and NH. A "substituent" as used herein, refers to a molecular moiety that is covalently bonded to an atom within a molecule of interest. For example, a "ring substituent" may be a moiety such as a halogen, alkyl group, or other substituent described herein that is covalently bonded to an atom, preferably a carbon or nitrogen atom, that is a ring member. The term "substituted," as used herein, means that any one or more hydrogens on the designated atom is replaced with a selection from the indicated substituents, provided that the designated atom's normal valence is not exceeded, and that the substitution results in a stable compound, ie, a compound that can be isolated, characterized and tested for biological activity. The terms "optionally substituted" or “may be substituted” and the like, as used throughout the specification, denotes that the group may or may not be further substituted or fused (so as to form a polycyclic system), with one or more non-hydrogen substituent groups. Suitable chemically viable substituents for a particular functional group will be apparent to those skilled in the art. Examples of substituents include but are not limited to C1-C6 alkyl, C1-C6 haloalkyl, C1- C6 haloalkoxy, C1-C6 hydroxyalkyl, C3-C7 heterocyclyl, C3-C7 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylsulfanyl, C1-C6 alkylsulfenyl, C1-C6 alkylsulfonyl, C1-C6 alkylsulfonylamino, arylsulfonoamino, alkylcarboxy, alkylcarboxyamide, oxo, hydroxy, mercapto, amino, acyl, carboxy, carbamoyl, aryl, aryloxy, heteroaryl, aminosulfonyl, aroyl, aroylamino, heteroaroyl, acyloxy, aroyloxy, heteroaroyloxy, alkoxycarbonyl, nitro, cyano, halo, ureido, C1-C6 perfluoroalkyl. Preferably the substituents include amino, halo, C1-C6 alkyl, amido, hydroxyl. As used herein, the term "halogen" refers to fluorine (F), chlorine (Cl), bromine (Br), or iodine (I) and the term "halo" refers to the halogen radicals fluoro (-F), chloro (-Cl), bromo (-Br), and iodo (-I). Preferably, ‘halo’ is fluoro or chloro. As used herein, the term “haloalkyl” refers to an alkyl group as defined herein in which one or more (up to all) of the available hydrogen atoms have been replacd with a halogen. In some instances, the term“perfluoro” can be used to define a compound or radical where all the hydrogens are replaced with fluorine. For example, perfluoromethyl refers to 1,1,1 -trifluoromethyl. As used herein, the terms "C1-C2 haloalkyl", "C1-C3 haloalkyl" and "C1-C6 haloalkyl" refer to a haloalkyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g. haloalkyl groups containing 2- 5 carbon atoms are also within the range of C1-C6). For example a C1 haloalkyl group could be, but is not limited to, fluoromethyl, or difluoromethyl, or trifluoromethyl. As used herein, the term “haloalkenyl” refers to an alkenyl group as defined above in which one or more of the available hydrogen atoms have been replaced with a halogen. Thus, for example, “C 1 - 6 haloalkenyl” (or “C 1 -C 6 haloalkenyl”) refers to a C 1 to C 6 linear or branched alkenyl group as defined above with one or more halogen substituents. As used herein, the term “haloalkynyl” refers to an alkynyl group as defined above in which one or more of the available hydrogen atoms have been replaced with a halogen. Thus, for example, “C1-6 haloalkynyl” (or “C1-C6 haloalkynyl”) refers to a C1 to C6 linear or branched alkynyl group as defined above with one or more halogen substituents. As used herein the term haloalkoxy refers to an alkoxy group as defined herein substituted with at least one halogen. The term “amino” or “amine” refers to the group -NH2. The term “substituted amino” or “secondary amino” refers to an amino group having a hydrogen replaced with, for example a C1-C6 alkyl group (“C1-C6 alkylamino”), an aryl or aralkyl group (“arylamino”, “aralkylamino”) and so on. C1-C3 alkylamino groups are preferred, such as for example, methylamino (NHMe), ethylamino (NHEt) and propylamino (NHPr). The term “disubstituted amino” or “tertiary amino” refers to an amino group having the two hydrogens replaced with, for example a C1-C6alkyl group, which may be the same or different (“dialkylamino”), an aryl and alkyl group (“aryl(alkyl)amino”) and so on. Di(C1-C3alkyl)amino groups are preferred, such as for example, dimethylamino (NMe2), diethylamino (NEt2), dipropylamino (NPr2) and variations thereof (eg N(Me)(Et) and so on). The term “nitro” refers to the group –NO2. The term “cyano” and “nitrile” refer to the group –CN. The term “amido” or “amide” refers to the group -C(O)NH2. The term “substituted amido” or “substituted amide” refers to an amido group having a hydrogen replaced with, for example a C1-C6 alkyl group (“C1-C6 alkylamido” or “C1-C6 alkylamide”), an aryl (“arylamido”), aralkyl group (“aralkylamido”) and so on. C1-C3 alkylamide groups are preferred, such as for example, methylamide (-C(O)NHMe), ethylamide (-C(O)NHEt) and propylamide (-C(O)NHPr) and includes reverse amides thereof (eg NHMeC(O)-, -NHEtC(O)- and –NHPrC(O)-). The term “disubstituted amido” or “disubstituted amide” refers to an amido group having the two hydrogens replaced with, for example a C1-C6alkyl group (“di(C1-C6 alkyl)amido” or “di(C1-C6 alkyl)amide”), an aralkyl and alkyl group (“alkyl(aralkyl)amido”) and so on. Di(C1-C3 alkyl)amide groups are preferred, such as for example, dimethylamide (- C(O)NMe2), diethylamide (-C(O)NEt2) and dipropylamide ((-C(O)NPr2) and variations thereof (eg C(O)N(Me)Et and so on) and includes reverse amides thereof. The term “sulfonyl” refers to the group -SO2H. The term “substituted sulfonyl” refers to a sulfonyl group having the hydrogen replaced with, for example a C1-C6 alkyl group (“sulfonylC1-C6 alkyl”), an aryl (“arylsulfonyl”), an aralkyl (“aralkylsulfonyl”) and so on. Sulfonyl C1-C3 alkyl groups are preferred, such as for example, -SO2Me, -SO2Et and -SO2Pr. The term “sulfonylamido” or “sulfonamide” refers to the group -SO2NH2. The term “substituted sulfonamido” or “substituted sulphonamide” refers to an sulfonylamido group having a hydrogen replaced with, for example a C1-C6 alkyl group (“sulfonylamidoC1-C6 alkyl”), an aryl (“arylsulfonamide”), aralkyl (“aralkylsulfonamide”) and so on. SulfonylamidoC1-C3 alkyl groups are preferred, such as for example, SO2NHMe, SO2NHEt and -SO2NHPr and includes reverse sulfonamides thereof (e.g. - NHSO2Me, NHSO2Et and -NHSO2Pr). The term “disubstituted sufonamido” or “disubstituted sulphonamide” refers to an sulfonylamido group having the two hydrogens replaced with, for example a C1-C6 alkyl group, which may be the same or different (“sulfonylamidodi(C1-C6 alkyl)”), an aralkyl and alkyl group (“sulfonamido(aralkyl)alkyl”) and so on. Sulfonylamidodi(C1-C3 alkyl) groups are preferred, such as for example, -SO2NMe2, -SO2NEt2 and -SO2NPr2 and variations thereof (eg SO2N(Me)Et and so on) and includes reserve sulfonamides thereof (eg –N(Me)SO2Me and so on). The term “sulfate” refers to the group OS(O)2OH and includes groups having the hydrogen replaced with, for example a C1-C6 alkyl group (“alkylsulfates”), an aryl (“arylsulfate”), an aralkyl (“aralkylsulfate”) and so on. C1-C3 alkylsulfates are preferred, such as for example, OS(O)2OMe, OS(O)2OEt and OS(O)2OPr. The term “sulfonate” refers to the group SO 3 H and includes groups having the hydrogen replaced with, for example a C1-C6 alkyl group (“alkylsulfonate”), an aryl (“arylsulfonate”), an aralkyl (“aralkylsulfonate”) and so on. C1-C3 alkylsulfonates are preferred, such as for example, SO3Me, SO3Et and SO3Pr. The term “amino acid” as herein defined refers to a moiety containing an amino group and a carboxyl group linked by at least one carbon. An amino acid may refer a natural or non-natural amino acid, preferably a natural amino acid such as alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine, preferably the amino acid is arginine, lysine or histidine, most preferably lysine. The term “carboxylate” or “carboxyl” refers to the group -COO- or -COOH. The term “carbamate” or “carbomyl” refers to the group –OC(O)NH2. The carbamate may be substituted, or may be disubstituted, for example with an alkyl group such as but not limited to C1-C6 alkyl. The term “carbonate” refers to the group –OC(O)O- or –OC(O)OH. The term “alkylcarbonate” as herein defined refers to a carbonate group having the hydrogen replaced with, for example a C1-C6 alkyl group, an aryl or aralkyl group (“arylcarbonate” or “aralkylcarbonate”) and so on. CO3C1-C3alkyl groups are preferred, such as for example, methylcarbonate (CO3Me), ethylcarbonate (CO3Et) and propylcarbonate (CO3Pr). The term “ester” refers to a carboxyl group having the hydrogen replaced with, for example a C1-C6 alkyl group (“carboxylC1-C6 alkyl” or “alkylester”), an aryl or aralkyl group (“arylester” or “aralkylester”) and so on. CO2C1-C3 alkyl groups are preferred, such as for example, methylester (CO2Me), ethylester (CO2Et) and propylester (CO2Pr) and includes reverse esters thereof (eg –OC(O)Me, -OC(O)Et and –OC(O)Pr). The term “heterocyclyl” refers to a moiety obtained by removing a hydrogen atom from a ring atom of a heterocyclic compound which moiety has from 3 to 12 ring atoms (unless otherwise specified), of which 1, 2, 3, 4 or more are ring heteroatoms, for example independently selected from O, S and N, or ring heteromoieties, for example independently selected from O, S, S(O), SO 2 , N and NH. When a heterocyclyl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding carbocyclic group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom or heteromoiety. In this context, the prefixs 3-, 4-, 5-, 6-, 7-, 8-, 9- and 10- membered denote the number of ring atoms, or range of ring atoms, whether carbon atoms or heteroatoms. For example, the term “C3-10 heterocyclyl” or “3-10 membered heterocylyl”, as used herein, pertains to a heterocyclyl group having 3, 4, 5, 6, 7, 8, 9 or 10 ring atoms. Examples of heterocylyl groups include 5-6-membered monocyclic heterocyclyls and 9-10 membered fused bicyclic heterocyclyls. Examples of monocyclic heterocyclyl groups include, but are not limited to, those containing one nitrogen atom such as aziridine (3-membered ring), azetidine (4- membered ring), pyrrolidine (tetrahydropyrrole), pyrroline (eg 3-pyrroline, 2,5- dihydropyrrole), 2Hpyrrole or 3H-pyrrole (isopyrrole, isoazole) or pyrrolidinone (5- membered rings), piperidine, dihydropyridine, tetrahydropyridine (6-membered rings), and azepine (7membered ring); those containing two nitrogen atoms such as imidazoline, pyrazolidine (diazolidine), imidazoline, pyrazoline (dihydropyrazole) (5- membered rings), piperazine (6membered ring); those containing one oxygen atom such as oxirane (3-membered ring), oxetane (4-membered ring), oxolane (tetrahydrofuran), oxole (dihydrofuran) (5-membered rings), oxane (tetrahydropyran), dihydropyran, pyran (6-membered rings), oxepin (7membered ring); those containing two oxygen atoms such as dioxolane (5-membered ring), dioxane (6-membered ring), and dioxepane (7-membered ring); those containing three oxygen atoms such as trioxane (6-membered ring); those containing one sulfur atom such as thiirane (3- membered ring), thietane (4-membered ring), thiolane (tetrahydrothiophene) (5- membered ring), thiane (tetrahydrothiopyran) (6-membered ring), thiepane (7- membered ring); those containing one nitrogen and one oxygen atom such as tetrahydrooxazole, dihydrooxazole, tetrahydroisoxazole, dihydroisoxazole (5-membered rings), morpholine, tetrahydrooxazine, dihydrooxazine, oxazine (6-membered rings); those containing one nitrogen and one sulfur atom such as thiazoline, thiazolidine (5- membered rings), thiomorpholine (6-membered ring); those containing two nitrogen and one oxygen atom such as oxadiazine (6-membered ring); those containing one oxygen and one sulfur such as: oxathiole (5-membered ring) and oxathiane (thioxane) (6- membered ring); and those containing one nitrogen, one oxygen and one sulfur atom such as oxathiazine (6-membered ring). Heterocyclyls also encompass heteroaryl (aromatic heterocyclyls) and heterocycloalkyl (non-aromatic heterocyclyls). Such groups may be substituted or unsubstituted. The term “aromatic heterocyclyl” may be used interchangeably with the term “heteroaromatic” or the term “heteroaryl” or “hetaryl”. The heteroatoms in the aromatic heterocyclyl group may be independently selected from N, S and O. The aromatic heterocyclyl groups may comprise 1, 2, 3, 4 or more ring heteroatoms. When a heteroaryl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding aryl group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom. In the case of fused aromatic heterocyclyl groups, only one of the rings may contain a heteroatom and not all rings must be aromatic. “Heteroaryl” is used herein to denote a heterocyclic group having aromatic character and embraces aromatic monocyclic ring systems and polycyclic (eg bicyclic) ring systems containing one or more aromatic rings. The term aromatic heterocyclyl also encompasses pseudoaromatic heterocyclyls. The term “pseudoaromatic” refers to a ring system which is not strictly aromatic, but which is stabilized by means of delocalization of electrons and behaves in a similar manner to aromatic rings. The term aromatic heterocyclyl therefore covers polycyclic ring systems in which all of the fused rings are aromatic as well as ring systems where one or more rings are non-aromatic, provided that at least one ring is aromatic. In polycyclic systems containing both aromatic and non-aromatic rings fused together, the group may be attached to another moiety by the aromatic ring or by a non-aromatic ring. Examples of heteroaryl groups are monocyclic and bicyclic groups containing from five to ten ring members. The heteroaryl group can be, for example, a five membered or six membered monocyclic ring or a bicyclic structure formed from fused five and six membered rings or two fused six membered rings or two fused five membered rings. Each ring may contain up to about four heteroatoms typically selected from nitrogen, sulphur and oxygen. The heteroaryl ring will contain up to 4 heteroatoms, more typically up to 3 heteroatoms, more usually up to 2, for example a single heteroatom. In one embodiment, the heteroaryl ring contains at least one ring nitrogen atom. The nitrogen atoms in the heteroaryl rings can be basic, as in the case of an imidazole or pyridine, or essentially non-basic as in the case of an indole or pyrrole nitrogen. In general the number of basic nitrogen atoms present in the heteroaryl group, including any amino group substituents of the ring, will be less than five. Aromatic heterocyclyl groups may be 5-membered or 6-membered mono-cyclic aromatic ring systems. Examples of 5-membered monocyclic heteroaryl groups include but are not limited to furanyl, thienyl, pyrrolyl, oxazolyl, oxadiazolyl (including 1,2,3 and 1,2,4 oxadiazolyls and furazanyl i.e.1,2,5-oxadiazolyl), thiazolyl, isoxazolyl, isothiazolyl, pyrazolyl, imidazolyl, triazolyl (including 1,2,3, 1,2,4 and 1,3,4 triazolyls), oxatriazolyl, tetrazolyl, thiadiazolyl (including 1,2,3 and 1,3,4 thiadiazolyls) and the like. Examples of 6-membered monocyclic heteroaryl groups include but are not limited to pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, pyranyl, oxazinyl, dioxinyl, thiazinyl, thiadiazinyl and the like. Examples of 6-membered aromatic heterocyclyls containing nitrogen include pyridyl (1 nitrogen), pyrazinyl, pyrimidinyl and pyridazinyl (2 nitrogens). Aromatic heterocyclyl groups may also be bicyclic or polycyclic heteroaromatic ring systems such as fused ring systems (including purine, pteridinyl, napthyridinyl, 1H thieno[2,3-c]pyrazolyl, thieno[2,3-b]furyl and the like) or linked ring systems (such as oligothiophene, polypyrrole and the like). Fused ring systems may also include aromatic 5-membered or 6-membered heterocyclyls fused to carbocyclic aromatic rings such as phenyl, napthyl, indenyl, azulenyl, fluorenyl, anthracenyl and the like, such as 5- membered aromatic heterocyclyls containing nitrogen fused to phenyl rings, 5- membered aromatic heterocyclyls containing 1 or 2 nitrogens fused to phenyl ring. A bicyclic heteroaryl group may be, for example, a group selected from: a) a benzene ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; b) a pyridine ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; c) a pyrimidine ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; d) a pyrrole ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; e) a pyrazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; f) an imidazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; g) an oxazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; h) an isoxazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; i) a thiazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; j) an isothiazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; k) a thiophene ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; I) a furan ring fused to a 5- or 6membered ring containing 1, 2 or 3 ring heteroatoms; m) a cyclohexyl ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; and n) a cyclopentyl ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms. Particular examples of bicyclic heteroaryl groups containing a five membered ring fused to another five membered ring include but are not limited to imidazothiazole (e.g. imidazo[2,1-b]thiazole) and imidazoimidazole (e.g. imidazo[1,2-a]imidazole). Particular examples of bicyclic heteroaryl groups containing a six membered ring fused to a five membered ring include but are not limited to benzofuran, benzothiophene, benzimidazole, benzoxazole, isobenzoxazole, benzisoxazole, benzothiazole, benzisothiazole, isobenzofuran, indole, isoindole, indolizine, indoline, isoindoline, purine (e.g., adenine, guanine), indazole, pyrazolopyrimidine (e.g. pyrazolo[1 ,5-a]pyrimidine), benzodioxole and pyrazolopyridine (e.g. pyrazolo[1,5-a]pyridine) groups. A further example of a six membered ring fused to a five membered ring is a pyrrolopyridine group such as a pyrrolo[2,3-b]pyridine group. Particular examples of bicyclic heteroaryl groups containing two fused six membered rings include but are not limited to quinoline, isoquinoline, chroman, thiochroman, chromene, isochromene, isochroman, benzodioxan, quinolizine, benzoxazine, benzodiazine, pyridopyridine, quinoxaline, quinazoline, cinnoline, phthalazine, naphthyridine and pteridine groups. Examples of heteroaryl groups containing an aromatic ring and a non-aromatic ring include tetrahydronaphthalene, tetrahydroisoquinoline, tetrahydroquinoline, dihydrobenzothiophene, dihydrobenzofuran, 2,3-dihydro- benzo[1,4]dioxine, benzo[1,3]dioxole, 4,5,6,7-tetrahydrobenzofuran, indoiine, isoindoline and indane groups. Examples of aromatic heterocyclyls fused to carbocyclic aromatic rings may therefore include but are not limited to benzothiophenyl, indolyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzimidazolyl, indazolyl, benzoxazolyl, benzisoxazolyl, isobenzoxazoyl, benzothiazolyl, benzisothiazolyl, quinolinyl, isoquinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, benzotriazinyl, phthalazinyl, carbolinyl and the like. The term “heterocycloalkyl” or “non-aromatic heterocyclyl” encompasses optionally substituted saturated and unsaturated rings which contain at least one heteroatom such as N, S and O, or a heteromoiety such as O, S, S(O), SO2, N and NH. The ring may contain 1, 2, 3, 4 or more heteroatoms or heteromoieties. When a heterocycloalkyl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding carbocyclic group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom or heteromoiety. The ring may be a monocyclic ring or part of a polycyclic ring system. Polycyclic ring systems include fused rings and spirocycles. Not every ring in a non-aromatic heterocyclic polycyclic ring system must contain a heteroatom, provided at least one ring contains one or more heteroatoms. Non-aromatic heterocyclyls may be 3-8 membered mono-cyclic rings. Examples of 5-membered non-aromatic heterocyclyl rings include 2H-pyrrolyl, 1pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3- pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrazolinyl, 2-pyrazolinyl, 3- pyrazolinyl, pyrazolidinyl, 2-pyrazolidinyl, 3-pyrazolidinyl, imidazolidinyl, 3-dioxalanyl, thiazolidinyl, isoxazolidinyl, 2-imidazolinyl and the like. Examples of 6-membered non-aromatic heterocyclyls include piperidinyl, piperidinonyl, pyranyl, dihyrdopyranyl, tetrahydropyranyl, 2H pyranyl, 4H pyranyl, thianyl, thianyl oxide, thianyl dioxide, piperazinyl, diozanyl, 1,4-dioxinyl, 1,4-dithianyl, 1,3,5triozalanyl, 1,3,5-trithianyl, 1,4-morpholinyl, thiomorpholinyl, 1,4-oxathianyl, triazinyl, 1,4thiazinyl and the like. Examples of 7-membered non-aromatic heterocyclyls include azepanyl, oxepanyl, thiepanyl and the like. Non-aromatic heterocyclyl rings may also be bicyclic heterocyclyl rings such as linked ring systems (for example uridinyl and the like) or fused ring systems. Fused ring systems include non-aromatic 5-membered, 6-membered or 7-membered heterocyclyls fused to carbocyclic aromatic rings such as phenyl, napthyl, indenyl, azulenyl, fluorenyl, anthracenyl and the like. Examples of non-aromatic 5-membered, 6-membered or 7membered heterocyclyls fused to carbocyclic aromatic rings include indolinyl, benzodiazepinyl, benzazepinyl, dihydrobenzofuranyl and the like. The term “alkyleneheteroaryl” refers to a radical having an alkyl component and a heteroaryl component, where the alkyl component links the heteroaryl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the heteroaryl component and to the point of atachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The heteroaryl component is as defined herein. The numerical range from x to y in “Cx-y alkylenecycloalkyl” relates to the total number of alkyl carbons and heteroaryl ring atoms (carbon and heteroatoms together). The term “alkyleneheterocycloalkyl” refers to a radical having an alkyl component and a heterocycloalkyl component, where the alkyl component links the heterocycloalkyl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the heterocycloalkyl component and to the point of atachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The heterocycloalkyl component is as defined herein. The numerical range from x to y in “Cx- y alkyleneheterocycloalkyl” relates to the total number of alkyl carbons and heterocycloalkyl ring atoms (carbon and heteroatoms together). As used herein, the term solvate refers to a complex of the compound and either stoichiometric or non-stoichiometric amounts of a solvent. Solvates are often formed during the process of crystallization with pharmaceutically acceptable solvents such as water, ethanol, and the like. Hydrates are formed when the solvent is water, or alcoholates are formed when the solvent is alcohol. As used herein, the term polymorph refers to the different crystal packing arrangements of the same elemental composition of a compound. Polymorphs usually have different X-ray diffraction patterns, infrared spectra, melting points, density, hardness, crystal shape, optical and electrical properties, stability, and solubility. Various factors such as the recrystallization solvent, rate of crystallization, and storage temperature may cause a single crystal form to dominate. As used herein, the term “metabolite” refers to a derivative of a compound that is formed when the compound is metabolized. The term "active metabolite" refers to a biologically active derivative of a compound that is formed when the compound is metabolized. The term "metabolized," as used herein, refers to the sum of the processes (including, but not limited to, hydrolysis reactions and reactions catalyzed by enzymes) by which a particular substance is changed by an organism. Thus, enzymes may produce specific structural alterations to a compound. Metabolites of the compounds disclosed herein are optionally identified either by administration of compounds to a host and analysis of tissue samples from the host, or by incubation of compounds with hepatic cells in vitro and analysis of the resulting compounds. Stereochemical definitions and conventions used herein generally follow S. P. Parker, Ed., McGraw-Hill Dictionary of Chemical Terms (1984) McGraw-Hill Book Company, New York; and Eliel, E. and Wilen, S., “Stereochemistry of Organic Compounds”, John Wiley & Sons, Inc., New York, 1994. The compounds of the invention may contain asymmetric or chiral centers, and therefore exist in different stereoisomeric forms. The term “stereoisomers” refers to compounds which have identical chemical constitution, but differ with regard to the arrangement of the atoms or groups in space. As used herein, the term “stereoisomer” includes but is not limited to diastereomers, enantiomers and atropisomers, as well as mixtures thereof such as racemic mixtures. As used herein, the term "pharmaceutically acceptable salt" refers to those salts which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of humans and lower animals without undue toxicity, irritation, allergic response and the like, and are commensurate with a reasonable benefit/risk ratio. Pharmaceutically acceptable salts are well known in the art. For example, S. M. Berge et al., describe pharmaceutically acceptable salts in detail in J. Pharmaceutical Sciences, 1977, 66, 1–19, incorporated herein by reference. Pharmaceutically acceptable salts of the compounds of this invention include those derived from suitable inorganic and organic acids and bases. Examples of pharmaceutically acceptable, nontoxic acid addition salts are salts of an amino group formed with inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid and perchloric acid or with organic acids such as acetic acid, oxalic acid, maleic acid, tartaric acid, citric acid, succinic acid or malonic acid or by using other methods used in the art such as ion exchange. Other pharmaceutically acceptable salts include adipate, alginate, ascorbate, aspartate, benzenesulfonate, benzoate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, citrate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, formate, fumarate, glucoheptonate, glycerophosphate, gluconate, hemisulfate, heptanoate, hexanoate, hydroiodide, 2–hydroxy– ethanesulfonate, lactobionate, lactate, laurate, lauryl sulfate, malate, maleate, malonate, methanesulfonate, 2–naphthalenesulfonate, nicotinate, nitrate, oleate, oxalate, palmitate, pamoate, pectinate, persulfate, 3–phenylpropionate, phosphate, pivalate, propionate, stearate, succinate, sulfate, tartrate, thiocyanate, p–toluenesulfonate, undecanoate, valerate salts, and the like. Compounds The present disclosure provides compounds of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C 1 - 8 alkylamino, C 1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X 1 is N, NR 6 , O or S; X 2 is CR 7 , N, O or S; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR 12 )2, C(O)R 12 , CO2R 12 , C(O)N(R 12 )2, S(O)R 12 and SO2R 12 , C3- 6 cycloalkyl, C 6 - 9 alkylenecycloalkyl, C 3 - 6 heterocyclyl, C 6 - 9 alkyleneheterocycloalkyl, C 4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3- 6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 12 , C(O)N(R 12 )2, OR 12 , N(R 12 )2, NO2, SR 12 and SO2R 12 , said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 12 ; each R 12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 , R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO 2 R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO 2 , N, NH and NCH 3 ; alternatively, when X 2 is CR 7 , R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when X 1 is NR 6 and X 2 is CR 7 , R 6 and R 7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms. In some embodiments, the compound of formula (I) is not one of the following: In some embodiments, one of X 2 , Z 1 , Z 2 , Z 3 and Z 4 is a heteroatom. The remainder will all denote a ring carbon atom as defined for each variable herein. In these embodiments, the 6,5-fused bicyclic core of the compounds of formula (I) possess 2 heteroatoms. In some embodiments, X 1 , X 2 , Z 1 , Z 2 , Z 3 and Z 4 are defined by embodiments 1-6: In some embodiments, X 1 , X 2 , Z 1 , Z 2 , Z 3 and Z 4 are according to any one of the above embodiments 1-4. In some embodiments, X 1 is NR 6 . In some embodiments, R 6 (if present) is H. In some embodiments, R 6 (if present) is C1-6alkyl, preferably C1-4alkyl. In some embodiments, X 1 is NR 6 and R 6 is H. In some embodiments, one of R 8 and R 9 (if present) is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl and C1-6 haloalkyl, the other (if present) being hydrogen. In some embodiments, R 8 (if present) is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1- 6 alkyl and C1-6 haloalkyl, and R 9 (if present) is hydrogen. In some embodiments, R 9 (if present) is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1- 6 alkyl and C1-6 haloalkyl, and R 8 (if present) is hydrogen. In some embodiments, R 8 (if present) is selected from halogen, OR 13 and C1-6 alkyl, and R 9 (if present) is hydrogen. In some embodiments, R 9 (if present) is selected from halogen, OR 13 and C1-6 alkyl, and R 8 (if present) is hydrogen. In some embodiments, Z 1 is CR 8 . In some embodiments, Z 2 is CR 9 . In some embodiments, Z 1 is CR 8 and R 8 is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl and C1-6 haloalkyl. In some embodiments, Z 2 is CR 9 and R 9 is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl and C1-6 haloalkyl. In some embodiments, Z 1 is CR 8 and R 8 is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl and C1-6 haloalkyl, and Z 2 is N or CH. In some embodiments, Z 2 is CR 9 and R 9 is selected from halogen, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl and C1-6 haloalkyl, and Z 1 is N or CH. In some embodiments, Z 3 is CR 10 , and preferably R 10 is H. In some embodiments, one of R 8 and R 9 is OR 13 . In some embodiments, one or both of Z 1 is CR 8 and/or Z 2 is CR 9 . In some embodiments, each R 13 (if present) is independently selected from hydrogen and C1-6 alkyl. In some embodiments, each R 13 (if present) is H. In some embodiments, each R 13 (if present) is C1-6alkyl, preferably C1-4alkyl, more preferably methyl. In some embodiments, X 2 is CR 7 . In some embodiments, R 7 (if present) is hydrogen. In some embodiments, Z 1 is CR 8 . In some embodiments, R 8 (if present) is hydrogen. In some embodiments, Z 2 is CR 9 . In some embodiments, R 9 (if present) is hydrogen. In some embodiments, Z 3 is CR 10 . In some embodiments, R 10 (if present) is hydrogen. In some embodiments, Z 4 is CR 11 . In some embodiments, R 11 (if present) is hydrogen. In some embodiments, R 7 , R 10 and R 11 (if present) are each hydrogen. In some embodiments, R 6 , R 7 , R 10 and R 11 (if present) are each hydrogen. In some embodiments, only one of R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 8 of R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 9 of R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 10 of R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 11 of R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only one of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 6 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 7 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 8 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 9 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 10 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, only R 11 of R 6 , R 7 , R 8 , R 9 , R 10 and R 11 (if present) is other than hydrogen. In some embodiments, at least one of R 1 and R 2 is not methyl. In some embodiments, both of R 1 and R 2 are not methyl. In some embodiments, the compound of formula (I) has the formula (II): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO 2 , N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl, or C 4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH NH2 N(CH3)2 NHCH3 NO2 SH SCH3 SO2CH3 SOCH3 C1-6 alkyl C1-6 haloalkyl C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH 3 ; R 7 is selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH 3 , OH, NH 2 , N(CH 3 ) 2 , NHCH 3 , NO 2 , SH, SCH 3 , SO 2 CH 3, SOCH 3 , C 1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl C3-10 heterocycloalkyl C4-16 alkyleneheterocycloalkyl C6-12 aryl C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C 1 - 8 alkylamino, C 1-8 alkylsulfonyl, CO 2 R 13 , C(O)N(R 13 ) 2 , OR 13 , N(R 13 ) 2 , NO 2 , SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C 1 - 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C 1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C 3-8 cycloalkyl, C 3 - 14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C 1-6 alkyl and C 1-6 haloalkyl, and the other of R 7 , R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments the compound of formula (I) has the formula (IIa): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O S N S(O) SO and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C 3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 is selected from hydrogen, halogen, CN, OR 13 , N(R 13 ) 2 , SR 13 , C 1-6 alkyl, C 1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C 3 - 6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH 2 , N(CH 3 ) 2 , NO 2 , NHCH 3 , SH, SCH 3 , SO 2 CH 3, SOCH 3 , C 1-6 alkyl, C 1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: , In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C 1-8 alkoxy, C 1 - 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 9 , R 10 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 9 , R 10 and R 11 are each hydrogen. In some embodiments the compound of formula (II) has the formula (IIb): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 8 cycloalkyl, C 4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 ) 2 , OR 4 , N(R 4 ) 2 , NO 2 , SR 4 , SO 2 R 4 , C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 is selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 ) 2 , NO 2 , C 3-8 cycloalkyl, C 3 - 14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C 5 - 8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; R 8 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C 7 - 18 alkylenearyl, C 5-10 heteroaryl, and C 6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C 1-6 alkyl, C 1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: , In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO 2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C 5-10 heteroaryl, C 4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 8 , R 10 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 , R 10 and R 11 are each hydrogen. In some embodiments, the compound of formula (I) has the formula (IIc): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C 1 - 6 alkyl, C 1 - 6 haloalkyl, C 2 - 6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 is selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 -C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO 2 R 14 , C(O)N(R 14 ) 2 , OR 14 , N(R 14 ) 2 , NO 2 , SR 14 , SO 2 R 14 , C 1-6 alkyl, C 1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; R 8 , R 9 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C 5-10 heteroaryl, and C 6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 9 and R 9 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: , In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 9 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 9 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C 7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 8 , R 9 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 , R 9 and R 11 are each hydrogen. In some embodiments, the compound of formula (I) has the formula (IId): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C 1 - 8 alkylamino, C 1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 is selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C 1 - 8 alkylamino, C 1-8 alkylsulfonyl, CO 2 R 13 , C(O)N(R 13 ) 2 , OR 13 , N(R 13 ) 2 , NO 2 , SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; R 8 , R 9 and R 10 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO 2 R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO 2 , N, NH and NCH 3 ; alternatively, R 8 and R 9 or R 9 and R 10 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following:

In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C 4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 7 , R 8 , R 9 and R 10 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 , R 9 and R 10 are each hydrogen. In some embodiments, the compound of formula (I) has the formula (III): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO 2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C 1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C 3-8 cycloalkyl, C 3 - 14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C 1-6 alkyl and C 1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, the compound of formula (I) has the formula (IIIa): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C 3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH 3 , OH, NH 2 , N(CH 3 ) 2 , NHCH 3 , NO 2 , SH, SCH 3 , SO 2 CH 3, SOCH 3 , C 1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C 7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C 5-8 heterocycloalkyl and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, the compound of formula (I) has the formula (IV): wherein X2 is O or S, R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C 3 - 8 cycloalkyl, C 4-14 alkylenecycloalkyl, C 3 -C 8 heterocycloalkyl, C 4 -C 14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO 2 R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C 4-8 cycloalkyl, C 5-8 heterocycloalkyl, C 6-12 aryl, and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following:

In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C 4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO 2 CH 3, SOCH 3 , C 1-6 alkyl and C 1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments X 2 is O. In some embodiments, the compound of formula (I) has the formula (IVa): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C 1 - 6 alkyl, C 2 - 6 alkenyl, C 2 - 6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO 2 , N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: , In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C 1-8 alkoxy, C 1 - 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C 5-8 heterocycloalkyl or C 5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C 5-8 heterocycloalkyl and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, the compound of formula (I) has the formula (V): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C 3 -C 8 heterocycloalkyl, C 4 -C 14 alkyleneheterocycloalkyl, C 6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO 2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 ) 2 , SR 13 , C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 -C 6 haloalkenyl, C 2 - 6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 1 - 6 alkylamine, C 1 - 6 alkoxy, C 1 - 6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C 7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C 5-8 heterocycloalkyl and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, the compound of formula (I) has the formula (Va): wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C 3 - 8 cycloalkyl, C 4-14 alkylenecycloalkyl, C 3 -C 8 heterocycloalkyl, C 4 -C 14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO 2 R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO 2 R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. In some embodiments, R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, R 1 and R 2 are each independently selected from C1-4 alkyl. In some embodiments, R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: , In some embodiments, R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1- 8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO 2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments R 3 is hydrogen. In some embodiments, R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1- 8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is defined as in any one of the foregoing paragraphs. In some embodiments, R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C 3 - 6 cycloalkyl and C 3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in any one of the foregoing paragraphs. In some embodiments, R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2- C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1- 6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined as in any one of the foregoing paragraphs. In some embodiments, 1 or 2 of R 8 , R 9 , R 10 and R 11 are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 8 R 9 , R 10 and R 11 are each hydrogen. In some embodiments, R 8 and R 9 are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C 5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3.. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. In some embodiments, R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. In some embodiments, the compound of formula (I) is a compound of formula (IIaa) wherein L, R 1 , R 2 , R 3 and R 9 are as defined for any aspect or embodiment herein. In some embodiments of the compounds of formula (IIaa), one or both of R 1 and R 2 is not methyl. In some embodiments, the compound of formula (I) is a compound of formula (IIba) wherein L, R 1 , R 2 , R 3 and R 8 are as defined for any aspect or embodiment herein. In some embodiments, the compound of formula (I) is a compound of formula (IIda) wherein L, R 1 , R 2 , R 3 , R 8 and R 9 are as defined for any aspect or embodiment herein. In some embodiments, the compound of formula (I) is a compound of formula (IIIb) wherein L, R 1 , R 2 , R 3 , R 8 and R 9 are as defined for any aspect or embodiment herein. In some embodiments, the compound of formula (I) is a compound of formula (IIaa) wherein R 1 , R 2 , and R 9 are as defined for any aspect or embodiment herein. In some embodiments of the compounds of formula (IIaa), one or both of R 1 and R 2 is not methyl. In some embodiments, the compound of formula (I) is a compound of formula (IIbb) wherein R 1 , R 2 and R 8 are as defined for any aspect or embodiment herein. In some embodiments, the compound of formula (I) is a compound of formula (IIdb) wherein R 1 , R 2 , R 8 and R 9 are as defined for any aspect or embodiment herein. In some embodiments, the compound of formula (I) is a compound of formula (IIIc) wherein R 1 , R 2 , R 8 and R 9 are as defined for any aspect or embodiment herein. In any one of formulae (II), (IIa), (IIaa), (IIab), (IIb), (IIba), (IIbb), (IIc), (IId), (IIda), (IIdb), (III), (IIIa), (IIIb), (IIIc) (IV), (IVa), (V) and (Va), the compound is not one of the following: . In some embodiments, the compound of any of formulae (I), (II), (IIa), (IIaa), (IIab), (IIb), (IIba), (IIbb), (IIc), (IId), (IIda), (IIdb), (III), (IIIa), (IIIb), (IIIc) (IV), (IVa), (V) and (Va) may be selected from compounds P-1 to P-56. In some embodiments, the compound is selected from P-13, P-20, P-21, P-37 and P-45. Forms of the compound In the case of compounds that are solids, it will be understood by those skilled in the art that the inventive compounds, agents and salts may exist in different crystalline or polymorphic forms, all of which are intended to be within the scope of the present invention and specified formulae. The invention includes all crystalline forms of a compound of Formula (I) including anhydrous crystalline forms, hydrates, solvates and mixed solvates. If any of these crystalline forms demonstrates polymorphism, all polymorphs are within the scope of this invention. Formula (I) is intended to cover, where applicable, solvated as well as unsolvated forms of the compounds. Thus, Formula (I) includes compounds having the indicated structures, including the hydrated or solvated forms, as well as the non-hydrated and non-solvated forms. The compounds of Formula (I) or salts, tautomers, N-oxides, polymorphs or prodrugs thereof may be provided in the form of solvates. Solvates contain either stoichiometric or non-stoichiometric amounts of a solvent, and may be formed during the process of crystallization with pharmaceutically acceptable solvents such as water, alcohols such as methanol, ethanol or isopropyl alcohol, DMSO, acetonitrile, dimethyl formamide (DMF), acetic acid, and the like with the solvate forming part of the crystal lattice by either non-covalent binding or by occupying a hole in the crystal lattice. Hydrates are formed when the solvent is water, alcoholates are formed when the solvent is alcohol. Solvates of the compounds of the present invention can be conveniently prepared or formed during the processes described herein. In general, the solvated forms are considered equivalent to the unsolvated forms for the purposes of the invention. Basic nitrogen-containing groups may be quarternised with such agents as C1-6alkyl halide, such as methyl, ethyl, propyl, and butyl chlorides, bromides and iodides; dialkyl sulfates like dimethyl and diethyl sulfate; and others. Nitrogen containing groups may also be oxidised to form an N-oxide. The compound of Formula (I) or salts, tautomers, N-oxides, solvates and/or prodrugs thereof that form crystalline solids may demonstrate polymorphism. All polymorphic forms of the compounds, salts, tautomers, N-oxides, solvates and/or prodrugs are within the scope of the invention. The compound of Formula (I) may demonstrate tautomerism. Tautomers are two interchangeable forms of a molecule that typically exist within an equilibrium. Any tautomers of the compounds of Formula (I) are to be understood as being within the scope of the invention. The compound of Formula (I) may contain one or more stereocentres. All stereoisomers of the compounds of formula (I) are within the scope of the invention. Stereoisomers include enantiomers, diastereomers, geometric isomers (E and Z olephinic forms and cis and trans substitution patterns) and atropisomers. In some embodiments, the compound is a stereoisomerically enriched form of the compound of formula (I) at any stereocentre. The compound may be enriched in one stereoisomer over another by at least about 60, 70, 80, 90, 95, 98 or 99%. The compound of Formula (I) or its salts, tautomers, solvates, N-oxides, and/or stereoisomers, may be isotopically enriched with one or more of the isotopes of the atoms present in the compound. For example, the compound may be enriched with one or more of the following minor isotopes: 2 H, 3 H, 13 C, 14 C, 15 N and/or 17 O, preferably 2 H. An isotope may be considered enriched when its abundance is greater than its natural abundance. A "prodrug" is a compound that may not fully satisfy the structural requirements of the compounds provided herein, but is modified in vivo, following administration to a subject or patient, to produce a compound of formula (I) provided herein. For example, a prodrug may be an acylated derivative of a compound as provided herein. Prodrugs include compounds wherein hydroxy, carboxy, amine or sulfhydryl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxy, carboxy, amino, or sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, phosphate and benzoate derivatives of alcohol and amine functional groups within the compounds provided herein. Prodrugs of the compounds provided herein may be prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved in vivo to generate the parent compounds. Prodrugs include compounds wherein an amino acid residue, or a polypeptide chain of two or more (eg, two, three or four) amino acid residues which are covalently joined to free amino, and amido groups of compounds of Formula (I). The amino acid residues include the 20 naturally occurring amino acids commonly designated by three letter symbols and also include, 4-hydroxyproline, hydroxylysine, demosine, isodemosine, 3- methylhistidine, norvlin, beta-alanine, gamma-aminobutyric acid, citrulline, homocysteine, homoserine, ornithine and methionine sulfone. Prodrugs also include compounds wherein carbonates, carbamates, amides and alkyl esters which are covalently bonded to the above substituents of Formula (I) through the carbonyl carbon prodrug sidechain. Compositions, formulations and modes of administration The compounds of formula (I) can be administered alone or in the form of a pharmaceutical composition. In practice, the compounds of formula (I) are usually administered in the form of pharmaceutical compositions, that is, in admixture with at least one pharmaceutically acceptable excipient. The proportion and nature of any pharmaceutically acceptable excipient(s) are determined by the properties of the selected compound of the invention, the chosen route of administration, and standard pharmaceutical practice. In another embodiment, there is provided a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph thereof, and at least one pharmaceutically acceptable excipient. Pharmaceutical compositions of the disclosure typically include a therapeutically effective amount of one or more active ingredients in admixture with one or more pharmaceutically and physiologically acceptable formulation materials. Suitable formulation materials include, but are not limited to, antioxidants, preservatives, coloring, flavoring and diluting agents, emulsifying agents, suspending agents, solvents, fillers, bulking agents, buffers, delivery vehicles, diluents, excipients and/or pharmaceutical adjuvants. For example, a suitable vehicle may be water for injection, physiological saline solution, or artificial perilymph, possibly supplemented with other materials common in compositions for parenteral administration. Neutral buffered saline or saline mixed with serum albumin are further exemplary vehicles. Pharmaceutical compositions of the present disclosure additionally comprise a pharmaceutically acceptable carrier, which, as used herein, includes any and all solvents, diluents, or other liquid vehicle, dispersion or suspension aids, surface active agents, isotonic agents, thickening or emulsifying agents, preservatives, solid binders, lubricants and the like, as suited to the particular dosage form desired. Remington's Pharmaceutical Sciences, Sixteenth Edition, E. W. Martin (Mack Publishing Co., Easton, Pa., 1980) discloses various carriers used in formulating pharmaceutical compositions and known techniques for the preparation thereof. Except insofar as any conventional carrier medium is incompatible with the compounds of the invention, such as by producing any undesirable biological effect or otherwise interacting in a deleterious manner with any other component(s) of the pharmaceutical composition, its use is contemplated to be within the scope of this disclosure. Some examples of materials which can serve as pharmaceutically acceptable carriers include, but are not limited to, sugars such as lactose, glucose and sucrose; starches such as corn starch and potato starch; cellulose and its derivatives such as sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; powdered tragacanth; malt; gelatine; talc; excipients such as cocoa butter and suppository waxes; oils such as peanut oil, cottonseed oil; safflower oil, sesame oil; olive oil; corn oil and soybean oil; glycols; such as propylene glycol; esters such as ethyl oleate and ethyl laurate; agar; buffering agents such as magnesium hydroxide and aluminium hydroxide; alginic acid; pyrogenfree water; isotonic saline; Ringer's solution; ethyl alcohol, and phosphate buffer solutions, as well as other non-toxic compatible lubricants such as sodium lauryl sulfate and magnesium stearate, as well as colouring agents, releasing agents, coating agents, sweetening, flavouring and perfuming agents, preservatives and antioxidants can also be present in the composition, according to the judgment of the formulator. Various dosage units are each preferably provided as a discrete dosage tablet, capsules, lozenge, dragee, gum, or other type of solid formulation. Capsules may encapsulate a powder, liquid, or gel. The solid formulation may be swallowed, or may be of a suckable or chewable type (either frangible or gum-like). The present invention contemplates dosage unit retaining devices other than blister packs; for example, packages such as bottles, tubes, canisters, packets. The dosage units may further include conventional excipients well-known in pharmaceutical formulation practice, such as binding agents, gellants, fillers, tableting lubricants, disintegrants, surfactants, and colorants; and for suckable or chewable formulations. A compound of formula (I) may be administered in any form and route which makes the compound bioavailable. Compositions described herein may be administered systemically or directly to the site of condition or disease. Compositions described herein may be formulated from compounds according to Formula (I) for any appropriate route of administration including, for example, oral, rectal, nasal, vaginal, topical (including transdermal, buccal, ocular and sublingual), parenteral (including subcutaneous, intraperitoneal, intradermal, intravascular (for example, intravenous), intramuscular, spinal, intracranial, intrathecal, intraocular, periocular, intraorbital, intrasynovial and intraperitoneal injection, intracisternal injection as well as any other similar injection or infusion techniques), inhalation, insufflation, infusion or implantation techniques (e.g., as sterile injectable aqueous or non-aqueous solutions or suspensions). In some embodiments, compositions described herein may be administered orally, nasally, intravenously, intramuscularly, topically, subcutaneously, rectally, vaginally or by urethral application. Compositions intended for oral use may further comprise one or more components such as sweetening agents, flavouring agents, colouring agents and/or preserving agents in order to provide appealing and palatable preparations. Tablets contain the active ingredient in admixture with physiologically acceptable excipients that are suitable for the manufacture of tablets. Such excipients include, for example, inert diluents such as calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate, granulating and disintegrating agents such as corn starch or alginic acid, binding agents such as starch, gelatine or acacia, and lubricating agents such as magnesium stearate, stearic acid or talc. The tablets may be uncoated or they may be coated by known techniques to delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period. For example, a time delay material such as glyceryl monosterate or glyceryl distearate may be employed. Formulations for oral use may also be presented as hard gelatine capsules wherein the active ingredient is mixed with an inert solid diluent such as calcium carbonate, calcium phosphate or kaolin, or as soft gelatine capsules wherein the active ingredient is mixed with water or an oil medium such as peanut oil, liquid paraffin or olive oil. Oily suspensions may be formulated by suspending the active ingredients in a vegetable oil such as arachis oil, olive oil, sesame oil or coconut oil, or in a mineral oil such as liquid paraffin. The oily suspensions may contain a thickening agent such as beeswax, hard paraffin or cetyl alcohol. Sweetening agents such as those set forth above, and/or flavouring agents may be added to provide palatable oral preparations. Such suspensions may be preserved by the addition of an antioxidant such as ascorbic acid. Dispersible powders and granules suitable for preparation of an aqueous suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent, suspending agent and one or more preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified by those already mentioned above. Additional excipients, such as sweetening, flavouring and colouring agents, may also be present. Pharmaceutical compositions may also be in the form of oil-in-water emulsions. The oily phase may be a vegetable oil such as olive oil or arachis oil, a mineral oil such as liquid paraffin, or a mixture thereof. Suitable emulsifying agents include naturally-occurring gums such as gum acacia or gum tragacanth, naturally-occurring phosphatides such as soy bean lecithin, and esters or partial esters derived from fatty acids and hexitol, anhydrides such as sorbitan monoleate, and condensation products of partial esters derived from fatty acids and hexitol with ethylene oxide such as polyoxyethylene sorbitan monoleate. An emulsion may also comprise one or more sweetening and/or flavouring agents. Syrups and elixirs may be formulated with sweetening agents, such as glycerol, propylene glycol, sorbitol or sucrose. Such Formulations may also comprise one or more demulcents, preservatives, flavouring agents and/or colouring agents. A composition may further include one or more components adapted to improve the stability or effectiveness of the applied formulation, such as stabilizing agents, suspending agents, emulsifying agents, viscosity adjusters, gelling agents, preservatives, antioxidants, skin penetration enhancers, moisturizers and sustained release materials. Examples of such components are described in Martindale – The Extra Pharmacopoeia (Pharmaceutical Press, London 1993) and Martin (ed.), Remington's Pharmaceutical Sciences. Formulations may comprise microcapsules, such as hydroxymethylcellulose or gelatine-microcapsules, liposomes, albumin microspheres, microemulsions, nanoparticles or nanocapsules. Preservatives include, but are not limited to, antimicrobials such as methylparaben, propylparaben, sorbic acid, benzoic acid, and formaldehyde, as well as physical stabilizers and antioxidants such as vitamin E, sodium ascorbate/ascorbic acid and propyl gallate. Suitable moisturizers include, but are not limited to, lactic acid and other hydroxy acids and their salts, glycerine, propylene glycol, and butylene glycol. Suitable emollients include lanolin alcohol, lanolin, lanolin derivatives, cholesterol, petrolatum, isostearyl neopentanoate and mineral oils. Suitable fragrances and colours include, but are not limited to, FD&C Red No.40 and FD&C Yellow No.5. Other suitable additional ingredients that may be included in a topical Formulation include, but are not limited to, abrasives, absorbents, anticaking agents, antifoaming agents, antistatic agents, astringents (such as witch hazel), alcohol and herbal extracts such as chamomile extract, binders/excipients, buffering agents, chelating agents, film forming agents, conditioning agents, propellants, opacifying agents, pH adjusters and protectants. Liquid dosage forms for oral administration include, but are not limited to, pharmaceutically acceptable emulsions, microemulsions, solutions, suspensions, syrups and elixirs. In addition to the active compounds, the liquid dosage forms may contain inert diluents commonly used in the art such as, for example, water or other solvents, solubilizing agents and emulsifiers such as ethyl alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3- butylene glycol, dimethylformamide, oils (in particular, cottonseed, groundnut, corn, germ, olive, castor, and sesame oils), glycerol, tetrahydrofurfuryl alcohol, polyethylene glycols and fatty acid esters of sorbitan, and mixtures thereof. Besides inert diluents, the oral compositions can also include adjuvants such as wetting agents, emulsifying and suspending agents, sweetening, flavoring, and perfuming agents. Injectable preparations, for example, sterile injectable aqueous or oleaginous suspensions may be formulated according to the known art using suitable dispersing or wetting agents and suspending agents. The sterile injectable preparation may also be a sterile injectable solution, suspension or emulsion in a nontoxic parenterally acceptable diluent or solvent, for example, as a solution in 1,3-butanediol. Among the acceptable vehicles and solvents that may be employed are water, Ringer's solution, U.S. P. and isotonic sodium chloride solution. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium. For this purpose any bland fixed oil can be employed including synthetic mono-or diglycerides. In addition, fatty acids such as oleic acid are used in the preparation of injectables. The injectable formulations can be sterilized, for example, by filtration through a bacterial-retaining filter, or by incorporating sterilizing agents in the form of sterile solid compositions which can be dissolved or dispersed in sterile water or other sterile injectable medium prior to use. A pharmaceutical composition may be formulated as inhaled formulations, including sprays, mists, or aerosols. For inhalation formulations, the composition or combination provided herein may be delivered via any inhalation methods known to a person skilled in the art. Such inhalation methods and devices include, but are not limited to, metered dose inhalers with propellants such as CFC or HFA or propellants that are physiologically and environmentally acceptable. Other suitable devices are breath operated inhalers, multidose dry powder inhalers and aerosol nebulizers. Aerosol formulations for use in the subject method typically include propellants, surfactants and co-solvents and may be filled into conventional aerosol containers that are closed by a suitable metering valve. Inhalant compositions may comprise liquid or powdered compositions containing the active ingredient that are suitable for nebulization and intrabronchial use, or aerosol compositions administered via an aerosol unit dispensing metered doses. Suitable liquid compositions comprise the active ingredient in an aqueous, pharmaceutically acceptable inhalant solvent such as isotonic saline or bacteriostatic water. The solutions are administered by means of a pump or squeeze-actuated nebulized spray dispenser, or by any other conventional means for causing or enabling the requisite dosage amount of the liquid composition to be inhaled into the patient's lungs. Suitable Formulations, wherein the carrier is a liquid, for administration, as for example, a nasal spray or as nasal drops, include aqueous or oily solutions of the active ingredient. Compositions suitable for rectal administration are preferably presented as unit dose suppositories. These may be prepared by at least partially dispersing the active in one or more lipophilic bases and then shaping the mixture. Pharmaceutical compositions may be formulated as sustained release formulations such as a capsule that creates a slow release of active following administration. Such formulations may generally be prepared using well-known technology and administered by, for example, oral, rectal or subcutaneous implantation, or by implantation at the desired target site. Carriers for use within such formulations are biocompatible, and may also be biodegradable. Preferably, the formulation provides a relatively constant level of active release. The amount of active contained within a sustained release formulation depends upon, for example, the site of implantation, the rate and expected duration of release and the nature of the condition to be treated. One skilled in the art can readily select the proper form and route of administration depending on the particular characteristics of the compound selected, the disease or condition to be treated, the stage of the disease or condition, and other relevant circumstances. It will be understood, that the specific dose level for any particular patient will depend upon a variety of factors including the activity of the specific compound employed, the age, body weight, general health, sex, diet, time of administration, route of administration, number of doses, and rate of excretion, drug combination (i.e. other drugs being used to treat the patient), and the severity of the particular disorder undergoing therapy. The phrase “therapeutically effective amount” generally refers to an amount of one or more active ingredients of the invention that (i) treats the particular disease, condition, or disorder, (ii) attenuates, ameliorates, or eliminates one or more sign or symptoms of the particular disease, condition, or disorder, or (iii) delays the onset of one or more sign or symptoms of the particular disease, condition, or disorder described herein. Typically, a therapeutically effective dosage is formulated to contain a concentration (by weight) of at least about 0.1% up to about 50% or more, and all combinations and sub- combinations of ranges therein. The compositions can be formulated to contain one or more actives described herein in a concentration of from about 0.1 to less than about 50%, for example, about 49, 48, 47, 46, 45, 44, 43, 42, 41 or 40%, with concentrations of from greater than about 0.1%, for example, about 0.2, 0.3, 0.4 or 0.5%, to less than about 40%, for example, about 39, 38, 37, 36, 35, 34, 33, 32, 31 or 30%. Exemplary compositions may contain from about 0.5% to less than about 30%, for example, about 29, 28, 27, 26, 25, 25, 24, 23, 22, 21 or 20%, with concentrations of from greater than about 0.5%, for example, about 0.6, 0.7, 0.8, 0.9 or 1%, to less than about 20%, for example, about 19, 18, 17, 16, 15, 14, 13, 12, 11 or 10%. The compositions can contain from greater than about 1% for example, about 2%, to less than about 10%, for example about 9 or 8%, including concentrations of greater than about 2%, for example, about 3 or 4%, to less than about 8%, for example, about 7 or 6%. The active agent can, for example, be present in a concentration of about 5%. In all cases, amounts may be adjusted to compensate for differences in amounts of active ingredients actually delivered to the treated cells or tissue. The frequency of administration may be once daily, 2, 3 or 4 times daily. The treatment period may be for the duration of the detectable disease. In some embodiments, the pharmaceutical composition comprises a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, an additional therapeutic agent, and a pharmaceutically acceptable excipient. The additional agent may be any suitable agent described herein. In some embodiments, the additional agent is a psychoactive drug, including those described herein. In some embodiments, the additional agent is useful for treatment of a disease, disorder or condition by activation of a serotonin receptor, including those described herein. In some embodiments, the additional agent is selected from any one of the following, including those described herein: an agent for a mental illness and/or a neuropsychiatric condition; an agent for psychosis and/or psychotic symptoms; an agent for attention deficit hyperactivity disorder and/or attention deficit disorder; an agent for dementia and/or Alzheimer’s disease; and an agent for an addiction disorder. Applications The present disclosure provides methods of using the compounds of formula (I) and compositions as described in any one of the foregoing paragraphs. The present disclosure also provides methods of delivering to a subject in need thereof a compound of formula (I) or a composition (e.g., an effective amount of the compound or composition) of the present disclosure. In another aspect, the present disclosure provides methods of treating a disease in a subject in need thereof comprising administering to the subject in need thereof an effective amount (e.g., therapeutically effective amount) of a compound or composition (e.g., pharmaceutical composition) of the present disclosure. In another aspect, the present disclosure provides methods of preventing a disease in a subject in need thereof comprising administering to the subject in need thereof an effective amount (e.g., therapeutically effective amount) of a compound of formula (I) or composition (e.g., pharmaceutical composition) of the present disclosure. In another aspect, provided herein are uses of the compounds of formula (I) or compositions of the present disclosure in the manufacture of a medicament for use in a method (e.g., method of delivering an active agent to a subject in need thereof, method of treating a disease in a subject in need thereof, method of preventing a disease in a subject in need thereof) of the present disclosure. In another aspect, provided herein are uses of the compounds of formula (I) or compositions of the present disclosure in a method (e.g., method of delivering an active agent to a subject in need thereof, method of treating a disease in a subject in need thereof, method of preventing a disease in a subject in need thereof) of the present disclosure. In certain embodiments, the effective amount is effective in treating the disease. In certain embodiments, the effective amount is effective in preventing the disease. In another aspect, the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method of preventing a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein, in combination with another known agent useful for treatment of a disease, disorder or condition by activation of a serotonin receptor. The other known agents useful for treatment of a disease, disorder or condition by activation of a serotonin receptor may be any suitable agents known in the art, including those described herein. In another aspect, the present disclosure provides method of preventing a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein, in combination with another known agent useful for prevention of a disease, disorder or condition by activation of a serotonin receptor. In certain embodiments, the serotonin receptor is 5-HT2A. In certain embodiments, the serotonin receptor is one or both of 5-HT2A and 5-HT2C. Additionally, or alternatively, in some embodiments, the serotonin receptor is not 5- HT2B. In some embodiments, the compound of formula (I) of the present disclosure is selective towards the 5-HT2A receptor over one or both of the 5-HT2C receptor and the 5-HT2B receptor, preferably over the 5-HT2B receptor. In some embodiments, the compound of formula (I) is selective towards the 5-HT2C receptor over one or both of the 5-HT2A receptor and the 5-HT2B receptor, preferably over the 5-HT2B receptor. In some embodiments, the compound of formula (I) is selective toward the 5-HT2A receptor and 5-HT2C receptor over the 5-HT2B receptor. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2A receptor of less than about 1 mM, less than about 100 µM, less than about 10 µM, less than about 1 µM, or less than about 100 nM, or less than about 10 nM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the compound of formula (I) exhibits an EC50 for the 5-HT2A receptor of less than about 1 mM, less than about 900 µM, less than about 800 µM, less than about 700 µM, less than about 600 µM, less than about 500 µM, less than about 400 µM, less than about 300 µM, less than about 200 µM, less than about 100 µM, less than about 90 µM, less than about 80 µM, less than about 70 µM, less than about 60 µM, less than about 50 µM, less than about 40 µM, less than about 30 µM, less than about 20 µM, less than about 10 µM, less than about 9 µM, less than about 8 µM, less than about 7 µM, less than about 6 µM, less than about 5 µM, less than about 4 µM, less than about 3 µM, less than about 2 µM, less than about 1 µM, less than about 900 nM, less than about 800 nM, less than about 700 nM, less than about 600 nM, less than about 500 nM, less than about 400 nM, less than about 300 nM, less than about 200 nM, or less than about 100 nM, or any equivalent unit of measure (e.g., mol/L), as determined by an assay of calcium flux activity. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2C receptor of less than about 1 mM, less than about 100 µM, less than about 10 µM, less than about 1 µM, or less than about 100 nM, or less than about 10 nM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the compound of formula (I) exhibits an EC50 for the 5-HT2C receptor of less than about 1 mM, less than about 900 µM, less than about 800 µM, less than about 700 µM, less than about 600 µM, less than about 500 µM, less than about 400 µM, less than about 300 µM, less than about 200 µM, less than about 100 µM, less than about 90 µM, less than about 80 µM, less than about 70 µM, less than about 60 µM, less than about 50 µM, less than about 40 µM, less than about 30 µM, less than about 20 µM, less than about 10 µM, less than about 9 µM, less than about 8 µM, less than about 7 µM, less than about 6 µM, less than about 5 µM, less than about 4 µM, less than about 3 µM, less than about 2 µM, less than about 1 µM, less than about 900 nM, less than about 800 nM, less than about 700 nM, less than about 600 nM, less than about 500 nM, less than about 400 nM, less than about 300 nM, less than about 200 nM, or less than about 100 nM, or any equivalent unit of measure (e.g., mol/L), as determined by an assay of calcium flux activity. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2B receptor of greater than about 1 µM, greater than about 10 µM, or greater than about 100 µM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a mental illness or a neuropsychiatric condition. Accordingly, the present application also includes a method of treating a mental illness or a neuropsychiatric condition comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of a mental illness or a neuropsychiatric condition, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of a mental illness or a neuropsychiatric condition. The application further includes a compound of formula (I) of the present disclosure for use in treating a mental illness or a neuropsychiatric condition. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a mental illness or a neuropsychiatric condition and compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for a mental illness or a neuropsychiatric condition. The one or more additional agents for a mental illness or a neuropsychiatric condition may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for a mental illness or a neuropsychiatric condition is selected from antipsychotics, including typical antipsychotics and atypical antipsychotics; antidepressants including selective serotonin reuptake inhibitors (SSRIs) and selective norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants and monoamine oxidase inhibitors (MAOIs) (e.g. bupropion); anti-anxiety medication including benzodiazepines such as alprazolam; agents for an addiction disorder such as alcohol addiction (e.g., disulfiram), nicotine dependence (e.g., varenicline) and opioid use disorder (e.g., methadone, buprenorphine, buprenorphine-naloxone and buprenorphine long-acting injection); mood stabilizers such as lithium and anticonvulsants such carbamazepine, divalproex (valproic acid), lamotrigine, gabapentin and topiramate. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is neurodegeneration. Accordingly, the present application also includes a method of treating neurodegeneration comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of neurodegeneration, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment neurodegeneration. The application further includes a compound of formula (I) of the present disclosure for use in treating neurodegeneration. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is reduced brain- derived neurotrophic factor (BDNF), mammalian target of rapamycin (mTOR) activation and/or inflammation. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor comprises cognitive impairment; ischemia including stroke; neurodegeneration; refractory substance use disorders; sleep disorders; pain, such as social pain, acute pain, cancer pain, chronic pain, breakthrough pain, bone pain, soft tissue pain, nerve pain, referred pain, phantom pain, neuropathic pain, cluster headaches and migraine; obesity and eating disorders; epilepsies and seizure disorders; neuronal cell death; excitotoxic cell death; or a combination thereof. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is psychosis or psychotic symptoms. Accordingly, the present application also includes a method of treating psychosis or psychotic symptoms comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of psychosis or psychotic symptoms, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of psychosis or psychotic symptoms. The application further includes a compound of formula (I) of the present disclosure for use in treating psychosis or psychotic symptoms. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is psychosis or psychotic symptoms and the the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for psychosis or psychotic symptoms. The one or more additional agents for psychosis or psychotic symptoms may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for psychosis or psychotic symptoms are selected typical antipsychotics and atypical antipsychotics. The typical antipsychotics may be selected from acepromazine, acetophenazine, benperidol, bromperidol, butaperazine, carfenazine, chlorproethazine, chlorpromazine, chlorprothixene, clopenthixol, cyamemazine, dixyrazine, droperidol, fluanisone, flupentixol, fluphenazine, fluspirilene, haloperidol, levomepromazine, lenperone, loxapine, mesoridazine, metitepine, molindone, moperone, oxypertine, oxyprotepine, penfluridol, perazine, periciazine, perphenazine, pimozide, pipamperone, piperacetazine, pipotiazine, prochlorperazine, promazine, prothipendyl, spiperone, sulforidazine, thiopropazate, thioproperazine, thioridazine, thiothixene, timiperone, trifluoperazine, trifluperidol, triflupromazine and zuclopenthixol and combinations thereof. The atypical antipsychotics may be selected from amoxapine, amisulpride, aripiprazole, asenapine, blonanserin, brexpiprazole, cariprazine, carpipramine, clocapramine, clorotepine, clotiapine, clozapine, iloperidone, levosulpiride, lurasidone, melperone, mosapramine, nemonapride, olanzapine, paliperidone, perospirone, quetiapine, remoxipride, reserpine, risperidone, sertindole, sulpiride, sultopride, tiapride, veralipride, ziprasidone and zotepine, and combinations thereof. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compound of formula (I) of the present disclosure does not result in a worsening of psychosis or psychotic symptoms such as, but not limited to, hallucinations and delusions. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compound of formula (I) results in an improvement of psychosis or psychotic symptoms such as, but not limited to, hallucinations and delusions. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compounds of formula (I) results in an improvement of psychosis or psychotic symptoms. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition. Accordingly, the present application also includes a method of treating a CNS disease, disorder or condition and/or a neurological disease, disorder or condition comprising administering a therapeutically effective amount of compound of formula (I) or a composition of the present disclosure to a subject in need thereof. The present application also includes a use of compound of formula (I) of the present disclosure for treatment a CNS disease, disorder or condition and/or a neurological disease, disorder or condition, as well as a use of compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of a CNS disease, disorder or condition and/or a neurological disease, disorder or condition. The application further includes a compound of formula (I) of the present disclosure of the application for use in treating a CNS disease, disorder or condition and/or a neurological disease, disorder or condition. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition. The one or more additional agents for a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition are selected from lithium, olanzapine, quetiapine, risperidone, ariprazole, ziprasidone, clozapine, divalproex sodium, lamotrigine, valproic acid, carbamazepine, topiramate, levomilnacipran, duloxetine, venlafaxine, citalopram, fluvoxamine, escitalopram, fluoxetine, paroxetine, sertraline, clomipramine, amitriptyline, desipramine, imipramine, nortriptyline, phenelzine, tranylcypromine, diazepam, alprazolam, clonazepam, or any combination thereof. Non limiting examples of standard of care therapy for depression are sertraline, fluoxetine, escitalopram, venlafaxine, or aripiprazole. Non-limiting examples of standard of care therapy for depression are citralopram, escitalopram, fluoxetine, paroxetine, diazepam, or sertraline. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is selected from attention deficit hyperactivity disorder and attention deficit disorder and a combination thereof. Accordingly, the present application also includes a method of treating attention deficit hyperactivity disorder and/or attention deficit disorder comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of attention deficit hyperactivity disorder and/or attention deficit disorder, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of attention deficit hyperactivity disorder and/or attention deficit disorder. The application further includes a compound of formula (I) of the present disclosure for use in treating attention deficit hyperactivity disorder and/or attention deficit disorder. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is attention deficit hyperactivity disorder and/or attention deficit disorder and a combination thereof and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for attention deficit hyperactivity disorder and/or attention deficit disorder and a combination thereof. The one or more additional agents for attention deficit hyperactivity disorder and/or attention deficit disorder may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for attention deficit hyperactivity disorder and/or attention deficit disorder and a combination thereof are selected from methylphenidate, dexamphetamine, lisdexamfetine, atomoxetine and amphetamine and a combination thereof. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is selected from dementia and Alzheimer’s disease and a combination thereof. Accordingly, the present application also includes a method of treating dementia and/or Alzheimer’s disease comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of dementia and/or Alzheimer’s disease, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of dementia and/or Alzheimer’s disease. The application further includes a compound of formula (I) of the present disclosure for use in treating dementia and/or Alzheimer’s disease. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is dementia or Alzheimer’s disease and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for dementia or Alzheimer’s disease. The one or more additional agents for dementia or Alzheimer’s disease may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for dementia and Alzheimer’s disease are selected from acetylcholinesterase inhibitors, NMDA antagonists and nicotinic agonists. The acetylcholinesterase inhibitors may be selected from donepezil, galantamine, rivastigmine, and phenserine, and combinations thereof. The NMDA antagonists may be selected from MK-801, ketamine, phencyclidine, and memantine, and combinations thereof. The nicotinic agonists may be selected from nicotine, nicotinic acid, nicotinic alpha7 agonists, or alpha2 beta4 agonists or a combination thereof. In another aspect, the present disclosure provides a method of treating a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method of preventing a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. The mental illness may be a neuropsychiatric condition. In certain embodiments, the mental illness is selected from anxiety disorders such as generalized anxiety disorder, panic disorder, social anxiety disorder and specific phobias; depression such as, hopelessness, loss of pleasure, fatigue and suicidal thoughts; mood disorders, such as depression, bipolar disorder, cancer-related depression, anxiety and cyclothymic disorder; psychotic disorders, such as hallucinations, delusions, mania, schizophrenia, schizoaffective disorder, schizophreniform Disorder; impulse control and addiction disorders, such as pyromania (starting fires), kleptomania (stealing) and compulsive gambling; alcohol addiction; drug addiction, such as opioid addiction/dependence, nicotine dependence, cocaine dependence, marijuana abuse and so on; smoking cessation; personality disorders, such as antisocial personality disorder, aggression, obsessive-compulsive personality disorder and paranoid personality disorder; obsessive-compulsive disorder (OCD), such as thoughts or fears that cause a subject to perform certain rituals or routines; post- traumatic stress disorder (PTSD); stress response syndromes (formerly called adjustment disorders); dissociative disorders, formerly called multiple personality disorder, or "split personality," and depersonalization disorder; factitious disorders; sexual and gender disorders, such as sexual dysfunction, gender identity disorder and the paraphilias; somatic symptom disorders, formerly known as a psychosomatic disorder or somatoform disorder. In certain embodiments, the mental illness is selected from hallucinations and delusions and a combination thereof. In these embodiments, the hallucinations may be selected from visual hallucinations, auditory hallucinations, olfactory hallucinations, gustatory hallucinations, tactile hallucinations, proprioceptive hallucinations, equilibrioceptive hallucinations, nociceptive hallucinations, thermoceptive hallucinations and chronoceptive hallucinations, and a combination thereof. In another aspect, the present disclosure provides a method for treating a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method for preventing a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In some embodiments, the CNS disease, disorder or condition and/or neurological disease, disorder or condition is selected from neurological diseases including neurodevelopmental diseases and neurodegenerative diseases such as Alzheimer’s disease; presenile dementia; senile dementia; vascular dementia; Lewy body dementia; cognitive impairment, Parkinson’s disease and Parkinsonian related disorders such as Parkinson dementia, corticobasal degeneration, and supranuclear palsy; epilepsy; CNS trauma; CNS infections; CNS inflammation; stroke; multiple sclerosis; Huntington’s disease; mitochondrial disorders; Fragile X syndrome; Angelman syndrome; hereditary ataxias; neuro-otological and eye movement disorders; neurodegenerative diseases of the retina amyotrophic lateral sclerosis; tardive dyskinesias; hyperkinetic disorders; attention deficit hyperactivity disorder and attention deficit disorders; restless leg syndrome; Tourette's syndrome; Tic disorder; schizophrenia; autism spectrum disorders; tuberous sclerosis; Rett syndrome; cerebral palsy; disorders of the reward system including eating disorders such as anorexia nervosa and bulimia nervosa; binge eating disorder, trichotillomania, dermotillomania, nail biting; migraine; fibromyalgia; and peripheral neuropathy of any etiology, and combinations thereof. In another aspect, the present disclosure provides a method for increasing neuronal plasticity, the method comprising contacting a neuronal cell with a compound of formula (I) or a pharmaceutical composition as described herein, in an amount sufficient to increase neuronal plasticity of the neuronal cell. “Neuronal plasticity” refers to the ability of the brain to change its structure and/or function continuously throughout a subject’s life. Examples of the changes to the brain include, but are not limited to, the ability to adapt or respond to internal and/or external stimuli, such as due to an injury, and the ability to produce new neurites, dendritic spines, and synapses. Increasing neuronal plasticity includes, but is not limited to, promoting neuronal growth, promoting neuritogenesis, promoting synaptogenesis, promoting dendritogenesis, increasing dendritic arbor complexity, increasing dendritic spine density, and increasing excitatory synapsis in the brain. In some embodiments, increasing neuronal plasticity comprises promoting neuronal growth, promoting neuritogenesis, promoting synaptogenesis, promoting dendritogenesis, increasing dendritic arbor complexity, and increasing dendritic spine density. In some embodiments, increasing neuronal plasticity can treat neurodegenerative disorder, Alzheimer’s, Parkinson’s disease, psychological disorder, depression, addiction, anxiety, post-traumatic stress disorder, treatment resistant depression, suicidal ideation, major depressive disorder, bipolar disorder, schizophrenia, stroke, traumatic brain injury, or substance use disorder. In another aspect the present disclosure provides methods of treating weight, comprising administering an effective amount of a compound of the invention to a subject in need thereof. Treatment of weight may include treating weight gain; weight loss; metabolic disorder; weight gain associated with pharmaceutical intervention; weight gain associated with a mental illness (including those described herein); eating disorders such as anorexia, bulimia, cachexia, etc.; eating behaviour; obesity; diabetes; insulin resistance; pre-diabetes; glucose intolerance; hyperlipidemia; and cardiovascular disease. In another aspect, the present disclosure provides a method for increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound of formula (I) or a pharmaceutical composition as described herein, in an amount sufficient to increase dendritic spine density of the neuronal cell. In certain embodiments, the compound of formula (I) produces a maximum number of dendritic crossings with an increase of greater than 1.0 fold by a Sholl Analysis. In another aspect the present disclosure provides a method for activating a serotonin receptor in a cell, either in a biological sample or in a patient, comprising administering a compound of formula (I) as defined in any one of the herein disclosed embodiments to the cell. The serotonin receptor may be a 5-HT receptor subtype, preferably one or both of 5-HT2A and 5-HT2C. In some embodiments, effective amounts vary according to factors such as the disease state, age, sex and/or weight of the subject or species. In some embodiments, the amount of a given compound or compounds that will correspond to an effective amount will vary depending upon factors, such as the given drug(s) or compound(s), the pharmaceutical formulation, the route of administration, the type of condition, disease or disorder, the identity of the subject being treated and the like, but can nevertheless be routinely determined by one skilled in the art. In some embodiments, the compounds of formula (I) of the present disclosure are administered one, two, three or four times a year. In some embodiments, the compounds of the present disclosure are administered at least once a week. However, in another embodiment, the compounds are administered to the subject from about one time per two weeks, three weeks or one month. In another embodiment, the compounds are administered about one time per week to about once daily. In another embodiment, the compounds are administered 1, 2, 3, 4, 5 or 6 times daily. The length of the treatment period depends on a variety of factors, such as the severity of the disease, disorder or condition, the age of the subject, the concentration and/or the activity of the compounds of the application and/or a combination thereof. It will also be appreciated that the effective dosage of the compound used for the treatment may increase or decrease over the course of a particular treatment regime. Changes in dosage may result and become apparent by standard diagnostic assays known in the art. In some instances, chronic administration is required. For example, the compounds are administered to the subject in an amount and for duration sufficient to treat the subject. In some embodiments, the compounds of the application are administered at doses that are hallucinogenic or psychotomimetic and taken in conjunction with psychotherapy or therapy and may occur once, twice, three, or four times a year. However, in some embodiments, the compounds are administered to the subject once daily, once every two days, once every 3 days, once a week, once every two weeks, once a month, once every two months, or once every three months at doses that are not hallucinogenic or psychotomimetic. A compound of formula (I) of the present disclosure may be either used alone or in combination with other known agents useful for treating diseases, disorders or conditions by activation of a serotonin receptor, such as the compounds of the present disclosure. When used in combination with other known agents useful in treating diseases, disorders by activation of a serotonin receptor, it is an embodiment that a compound of formu;a (I) is administered contemporaneously with those agents. As used herein, "contemporaneous administration" of two substances to a subject means providing each of the two substances so that they are both active in the individual at the same time. The exact details of the administration will depend on the pharmacokinetics of the two substances in the presence of each other and can include administering the two substances within a few hours of each other, or even administering one substance within 24 hours of administration of the other, if the pharmacokinetics are suitable. Design of suitable dosing regimens is routine for one skilled in the art. In particular embodiments, two substances will be administered substantially simultaneously, i.e., within minutes of each other, or in a single composition that contains both substances. It is a further embodiment of the present application that a combination of agents is administered to a subject in a non-contemporaneous fashion. In some embodiments, a compound of formula (I) of the present disclosure is administered with another therapeutic agent simultaneously or sequentially in separate unit dosage forms or together in a single unit dosage form. Accordingly, the present application provides a single unit dosage form comprising one or more compounds of formula (I) as described herein, an additional therapeutic agent and a pharmaceutically acceptable carrier. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that are devoid of clinically meaningful psychedelic/ psychotomimetic actions. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that provide clinical effects similar to those exhibited by a human plasma psilocin Cmax of 4 ng/mL or less and/or human 5-HT2A human CNS receptor occupancy of 40% or less or those exhibited by a human plasma psilocin Cmax of 1 ng/mL or less and/or human 5- HT2A human CNS receptor occupancy of 30% or less. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that provide clinical effects similar to those exhibited by a human plasma psilocin Tmax in excess of 60 minutes, in excess of 120 minutes or in excess of 180 minutes. Kit In another embodiment there is provided a kit or article of manufacture including one or more compounds, pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph, and/or pharmaceutical compositions as described above. In other embodiments there is provided a kit for use in a therapeutic application mentioned above, the kit including: a container holding one or more compounds, pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph and/or pharmaceutical compositions as described herein; a label or package insert with instructions for use. It will be understood that the invention disclosed and defined in this specification extends to all alternative combinations of two or more of the individual features mentioned or evident from the text or drawings. All of these different combinations constitute various alternative aspects of the invention. Examples Scheme 1: Compounds of general formula (I) can be synthesised from the appropriately substituted aza-indole following the outlined sequence of steps in Scheme 1 or similar as one skilled in the art may consider. A similar sequence of synthetic transformations as outlined in Scheme 1 proved to be a viable method of accessing compounds of general formula (I). Friedel-Crafts acylation of aza-indole starting material 1 provides access to intermediate 2 which can be subjected to chemoselective silane reduction conditions to provide the alkylchloride intermediate 3. Nucleophilic displacement of the alkylchloride with a substituted amine provides compounds of general formula (I) (exemplified by P-1). One skilled in the art will recognise that utilising differentially substituted amines would allow access to compounds of general formula (I) disclosed herein. Example 1: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethyletha n-1- amine (P-1): Step 1: 2-chloro-1-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1- one (2) To a solution of 5-methoxy-1H-pyrrolo[3,2-b]pyridine (2.00 g, 13.5 mmol) in CH2Cl2 (40 mL) 0 °C under N2 was added AlCl3 (9.00 g, 67.5 mmol), followed by a solution of chloroacetyl chloride (7.62 g, 67.5 mmol) in CH2Cl2 (6 mL). The mixture was stirred at 0 °C for 1.5 h, then quenched with H2O (50 mL). The pH was adjusted to 10 with saturated aqueous Na2CO3 solution. The mixture was filtered through celite, and the filter cake was washed with EtOAc (50 mL × 2). The filtrate was separated and washed with brine (30 mL), dried over anhydrous Na2SO4, and concentrated. The filter cake was stirred in EtOAc/THF (1:1, 200 mL) for 12 h. The mixture was filtered, and the filtrate was evaporated, combined with the preceding organic layer to give the 2-chloro- 1-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-one (2.00 g, 64%) as an off-white solid. 1 H NMR (400 MHz, DMSO-d6): ^^ 12.28 (br, 1H), 8.25 (d, J = 3.2 Hz, 1H), 7.84 (d, J = 8.8 Hz, 1H), 6.70 (d, J = 8.8 Hz, 1H), 5.21 (s, 2H), 3.94 (s, 3H). LCMS (ESI+): m/z 225.1, 227.1 [M+H] + . Step 2: 3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[3,2-b]pyridine (3) To a solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1- one (2.00 g, 8.90 mmol) in TFA (14 mL) was added Et3SiH (7.25 g, 62.3 mmol). The reaction mixture was stirred at 25 °C for 12 h. The solvent was evaporated, and the crude product was purified by column chromatography (SiO2, petroleum ether/EtOAc, v/v, 20/1 to 5/1).3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[3,2-b]pyridine was obtained as an off-white solid (2.00 g, crude). 1 H NMR (400 MHz, DMSO-d6): ^^ 10.97 (br, 1H), 7.66 (d, J = 8.4 Hz, 1H), 7.39 (s, 1H), 6.53 (d, J = 8.8 Hz, 1H), 3.95 (t, J = 7.4 Hz, 2H), 3.86 (s, 3H), 3.14 (t, J = 7.4 Hz, 2H). LCMS (ESI+): m/z 211.1, 213.1 [M+H] + . Step 3: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine (P-1) To a mixture of crude 3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[3,2-b]pyridine (2.00 g) and 2 M Me 2 NH in THF (40 mL) was added NaI (1.42 g, 9.49 mmol). The mixture was stirred at 90 °C for 12 h. The mixture was filtered, and the filter cake was washed with THF (10 mL). The filtrate was evaporated, and the crude product was purified by preparative HPLC (column: Waters Xbridge BEH C18 (250*50 mm*10 µm); mobile phase: [water (NH3 + NH4HCO3)-MeCN]; B: 1-30%, 10 min). 2-(5-Methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan-1-amine (P-1, 406 mg, 20%) was obtained as an off-white solid. 1 H NMR (400 MHz, MeOD-d4): ^^ 7.59 (d, J = 8.8 Hz, 1H), 7.20 (s, 1H), 6.54 (d, J = 8.8 Hz, 1H), 3.93 (s, 3H), 2.99 - 2.95 (m, 2H), 2.78 - 2.74 (m, 2H), 2.35 (s, 6H). LCMS (ESI+): m/z 220.2 [M+H] + . HPLC Purity (220 nm): 100%. Step 4: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine hydrochloride (P-1·HCl) A solution of 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine (200 mg, 0.91 mmol) in anhydrous Et2O (5 mL) and abs. EtOH (1 mL) was made acidic by dropwise addition of HCl (2 M in Et2O) at 0 °C. The resulting precipitate was collected by filtration and dried overnight in a vacuum desiccator to afford the 2-(5-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan-1-amine hydrochloride (100 mg, 43%) which was a white solid. 1H NMR (400 MHz, DMSO-d 6 ): ^ 11.65 (br s, 1H), 10.54 – 10.49 (m, 1H), 7.97 (d, J = 8.8 Hz, 1H), 7.59 (s, 1H), 6.78 (d, J = 8.8 Hz, 1H), 3.98 (s, 3H), 3.45 – 3.35 (m, 2H), 3.19 – 3.15 (m, 2H), 2.83 (d, J = 4.8 Hz, 6H). HPLC Purity (220 nm): 99.3%. Scheme 2: Compounds of general formula (I) can be synthesised from the appropriately substituted aza-indole following the outlined sequence of steps in Scheme 2 or similar as one skilled in the art may consider. A similar sequence of synthetic transformations as outlined in Scheme 2 proved to be a viable method of accessing compounds of general formula (I). Phthalimide formation of alkylamine 31 provides access to intermediate 32 which can be implemented in a Fischer-type indole synthesis to provide aza-indole intermediate 33. Hydrazinolysis of 33 provides access to intermediate 34 bearing the primary amine. Reductive alkylation of the amine with an appropriate aldehyde and reducing agent provides compounds of general formula (I) (exemplified by P-10). One skilled in the art will recognise that utilising different aldehydes would allow access to compounds of general formula (I) disclosed herein. Example 2: 2-(5-Methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-diethylethan -1- amine (P-10)

Step 1: 2-(4,4-Diethoxybutyl)-1H-isoindole-1,3(2H)-dione (32) To a solution of 4,4-diethoxybutan-1-amine (6.80 g, 42.2 mmol) and ethyl 1,3-dioxo- 2,3-dihydro-1H-isoindole-2-carboxylate (9.24 g, 42.2 mmol) in THF (130 mL) was added Et3N (4.27 g, 42.2 mmol) and the mixture was stirred at 20 °C for 16 h. The reaction mixture was concentrated in vacuo to obtain crude product which was purified by column chromatography (SiO2, Petroleum ether/EtOAc, v/v, 50/1 to 1/1) to give 2- (4,4-diethoxybutyl)-1H-isoindole-1,3(2H)-dione (11.6 g, 94%) as a colourless solid. 1 H NMR (400 MHz, CDCl3): ^ 7.88 - 7.80 (m, 2H), 7.76 - 7.66 (m, 2H), 4.52 (t, J = 5.6 Hz, 1H), 3.72 (t, J = 7.2 Hz, 2H), 3.64 - 3.61 (m, 2H), 3.54 - 3.45 (m, 2H), 1.81 - 1.74 (m, 2H), 1.70 - 1.62 (m, 2H), 1.19 (t, J = 7.2 Hz, 6H). Step 2: 2-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)isoindol ine-1,3-dione (33) To a solution of 2-(4,4-diethoxybutyl)-1H-isoindole-1,3(2H)-dione (10.0 g, 34.3 mmol) and 5-hydrazinyl-2-methoxypyridine (4.00 g, 28.7 mmol) in EtOH (64 mL) was added 4% v/v aqueous H 2 SO 4 (400 mL) at ambient temperature, and the mixture was then stirred at 95 °C for 4 h. The pH of the reaction mixture was adjusted to 8 by addition of saturated aqueous NH4OH solution before extraction with EtOAc (300 mL × 3). The combined organics were washed with brine (300 mL), dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was triturated with CH2Cl2, filtered, and dried under reduced pressure to give 2-(2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)ethyl)isoindoline-1,3-dione (6.8 g, 62%) as a brown solid. 1 H NMR (400 MHz, CDCl3): ^ 7.92 (br s, 1H), 7.81 – 7.77 (m, 2H), 7.69 – 7.66 (m, 2H), 7.49 (d, J = 8.8 Hz, 1H), 7.17 (d, J = 2.8 Hz, 1H), 6.52 (d, J = 8.8 Hz, 1H), 4.12 (t, J = 7.2 Hz, 2H), 3.92 (s, 3H), 3.21 (t, J = 7.2 Hz, 2H). LCMS (ESI+): m/z 322.2 [M+H] + . Step 3: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (34) To a solution of 2-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)isoindol ine-1,3-dione (4.00 g, 12.4 mmol) in EtOH (40 mL) was added 80% hydrazine hydrate (7.79 g, 124 mmol) and the mixture was stirred at 80 °C for 12 h. The reaction mixture was filtered and concentrated under reduced pressure to provide crude 2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)ethan-1-amine (3.00 g) as a brown oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 192.2 [M+H] + . Step 4: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-diethylethan -1-amine (P-10) To a solution of crude 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (400 mg) in MeOH (6 mL) at 0 °C was added NaBH(OAc)3 (2.22 g, 10.5 mmol), Et3N (1.06 g, 10.5 mmol) and 40% v/v aqueous acetaldehyde (575 mg, 5.22 mmol), and the mixture was then stirred at 20 °C for 12 h. The reaction mixture was concentrated under reduced pressure and the crude product was purified by preparative HPLC (column: Waters Xbridge C18 (250 x 50 mm x 10 µm); mobile phase: [water (NH4HCO3)-ACN]; B: 10-40%, 10 min) to provide 2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)-N,N-diethylethan-1-amine (20.7 mg, 3% over 2 steps) as a yellow solid. 1 H NMR (400 MHz, DMSO-d 6 ): ^^ 10.79 (br s, 1H), 7.62 (d, J = 8.8 Hz, 1H), 7.28 (d, J = 2.8 Hz, 1H), 6.50 (d, J = 8.8 Hz, 1H), 3.86 (s, 3H), 2.76 (s, 4H), 2.55 (q, J = 7.2 Hz, 4H), 1.02 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 248.1 [M+H] + . HPLC Purity (220 nm): 99.8%. Example 3: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dipropyletha n-1- amine (P-11):

To a solution of crude 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (200 mg) in MeOH (3 mL) at 0 °C was added NaBH(OAc)3 (1.11 g, 5.24 mmol), Et3N (529 mg, 5.23 mmol) and propanal (151 mg, 2.6 mmol), and the mixture was then stirred at 20 °C for 12 h. The reaction mixture was concentrated under reduced pressure and the residue was purified by preparative HPLC (column - Water Xbridge C18 (150*40 mm*10 µm); mobile phase: [water (NH4HCO3)-ACN]; B: 20-50%, 8 min) to provide 2- (5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dipropylethan- 1-amine (20.5 mg, 5% over 2 steps) as an off-white solid. 1 H NMR (400 MHz, DMSO-d 6 ): ^ 10.78 (br, 1H), 7.61 (d, J = 8.8 Hz, 1H), 7.27 (d, J = 2.8 Hz, 1H), 6.49 (d, J = 8.8 Hz, 1H), 3.86 (s, 3H), 2.76 (s, 4H), 2.43 (t, J = 7.6 Hz, 4 H), 1.46 (sext, J = 7.2 Hz, 4H), 0.85 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 276.1 [M+H] + . HPLC Purity (220 nm): 98.3%. Example 4: N-isopropyl-N-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3- yl)ethyl)propan-2-amine (P-12) To a solution of crude 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (300 mg) in MeOH (5 mL) and acetone (5 mL) was added NaBH3CN (2.96 g, 47.1 mmol) and the reaction mixture was stirred at 20 °C for 12 h. The reaction mixture was then concentrated in vacuo to obtain the crude product which was purified by preparative HPLC (column - Phenomenex Luna (80*30 mm*3 µm); mobile phase: [water (TFA)- ACN]; B: 1-30%, 8 min) to provide N-isopropyl-N-(2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)ethyl)propan-2-amine (20.7 mg, 0.4% over 2 steps) as a yellow solid. 1 H NMR (400 MHz, MeOD-d 4 ): ^ 7.74 (d, J = 8.8 Hz, 1H), 7.40 (s, 1H), 6.67 (d, J = 8.8 Hz, 1H), 3.97 (s, 3H), 3.84 (hept, J = 6.8 Hz, 2H), 3.49-3.55 (m, 2H), 3.18-3.24 (m, 2H), 1.46 (d, J = 6.8 Hz, 12H). LCMS (ESI+): RT = 2.22 min, m/z 276.2 [M+H] + . HPLC Purity (220 nm): 96.1%. Scheme 3: Compounds of general formula (I) can be synthesised from the appropriately substituted 2-(1-ethanamine)aza-indole following the outlined sequence of steps in Scheme 3 or similar as one skilled in the art may consider. A similar sequence of synthetic transformations as outlined in Scheme 3 proved to be a viable method of accessing compounds of general formula (I). Addition of a tert-butoxy carbonyl group to the primary amine of 2-(1-ethanamine)aza-indole starting material 34 provides access to intermediate 35 which can be subjected to chemoselective reduction conditions to provide the N-methylated intermediate 36. Further N-alkylation can be achieved with an appropriate aldehyde and reducing agent to provide compounds of general formula (I) (exemplified by P-13). One skilled in the art will recognise that utilising different aldehydes would allow access to compounds of general formula (I) disclosed herein. Example 4: N-ethyl-2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N-methyl ethan-1- amine (P-13): Step 1: tert-butyl (2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)carbamate (35) To a solution of 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (1.40 g) in THF (10 mL) was added di-tert-butyl dicarbonate (1.68 g, 7.70 mmol) at 0 °C and the mixture was stirred at 20 °C for 2 h. The mixture was concentrated under reduced pressure and purified by column chromatography (SiO2, Petroleum ether/EtOAc, v/v, 50/1 to 0/1) to afford tert-butyl (2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3- yl)ethyl)carbamate (1.14 g, 18% over two steps) as a brown oil. 1 H NMR (400 MHz, CDCl3): ^^ 8.05 (br, 1H), 7.59 (d, J = 8.8 Hz, 1H), 7.14 (d, J = 2.4 Hz, 1H), 6.64 (d, J = 8.8 Hz, 1H), 4.07 (s, 3H), 3.45-3.47 (m, 2H), 2.95-2.98 (m, 2H), 1.44 (s, 9H). Step 2: 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N-methylethan-1- amine (36) To a solution of LiAlH4 (390 mg, 10.3 mmol) in THF (2.5 mL) was added tert-butyl (2- (5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)carbamate (0.60 g, 2.06 mmol) portionwise at 0 °C under nitrogen. The reaction mixture was stirred at 0 °C for 6 min and then at 70 °C for 3 h under N2. The reaction mixture was cooled to 0 °C and quenched by dropwise addition of H2O (10 mL), and then extracted with EtOAc (10 mL × 4). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure to provide crude 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)- N-methylethan-1-amine (300 mg) as a brown oil. LCMS (ESI+): m/z 206.0 [M+H] + . Step 3: N-ethyl-2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N-methyl ethan-1-amine (P-13) To a solution of crude 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)-N-methylethan-1- amine (400 mg) in MeOH (6 mL) was added NaBH(OAc)3 (2.07 g, 9.77 mmol), acetaldehyde (103 mg, 2.34 mmol) and Et3N (985 mg, 9.73 mmol) at 0 °C and the mixture was stirred at 20 °C for 12 h. The reaction mixture was concentrated under reduced pressure to obtain the crude product which was purified by preparative HPLC (column: Waters Xbridge prep OBD C18 (150*40 mm*10 µm); mobile phase: [water (NH4HCO3)-ACN]; B: 2-30%, 8 min) to obtain N-ethyl-2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)-N-methylethan-1-amine (23.3 mg, 3% over 2 steps) as a yellow solid. 1 H NMR (400 MHz, MeOD-d 4 ): ^^ 7.60 (d, J = 8.8 Hz, 1H), 7.19 (s, 1H), 6.54 (d, J = 8.8 Hz, 1H), 3.93 (s, 3H), 2.95-3.31 (m, 2H), 2.82-2.86 (m, 2H), 2.60 (q, J = 7.2 Hz, 2H), 2.37 (s, 3H), 1.15 (t, J = 7.2 Hz, 3H). LCMS (ESI+): RT = 1.3 min, m/z 234.1 [M+H] + . HPLC Purity (220 nm): 99.7% Example 5: N-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)-N- methylpropan-2-amine (P-14): Step 1: N-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)propan-2 -amine (98) To a solution of 2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethan-1-amine (200 mg) in MeOH (3 mL) was added NaBH(OAc)3 (1.11 g, 5.24 mmol), Et3N (529 mg, 5.23 mmol) and acetone (151 mg, 2.60 mmol) at 0 °C and the reaction was stirred at 20 °C for 12 h. The reaction mixture was concentrated under reduced pressure to give crude N-(2- (5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)propan-2-amin e (300 mg) as yellow oil. LCMS (ESI+): m/z 234.1 [M+H] + . Step 2: N-(2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)-N-methy lpropan-2-amine (P-14) To a solution of crude (2-(5-methoxy-1H-pyrrolo[3,2-b]pyridin-3-yl)ethyl)(propan-2- yl)amine (100 mg) in MeOH (1.5 mL) was added NaBH(OAc)3 (454 mg, 2.14 mmol), formaldehyde (32.1 mg, 1.07 mmol) and Et3N (216 mg, 2.13 mmol) which was then stirred at 20 °C for 12 h. The reaction mixture was concentrated under reduced pressure and the crude product was purified by preparative HPLC (column: Waters Xbridge prep OBD C18 column (150*40 mm, 10 µm); mobile phase: [water (NH4HCO3)-ACN]; B: 5-50%, 8 min) to obtain N-(2-(5-methoxy-1H-pyrrolo[3,2- b]pyridin-3-yl)ethyl)-N-methylpropan-2-amine P-14 (20.6 mg, 18% over 3 steps as a yellow solid. 1 H NMR (400 MHz, MeOD-d4): ^^ 7.65 (d, J = 8.8 Hz, 1H), 7.27 (s, 1H), 6.59 (d, J = 8.8 Hz, 1H), 3.94 (s, 1H), 3.25-3.28 (m, 1H), 3.11-3.15 (m, 4H), 2.60 (s, 3H), 1.20 (d, J = 6.8 Hz, 6H). LCMS (ESI+): m/z 248.1 [M+H] + . HPLC Purity (220 nm): 100% Scheme 4: Compounds of general formula (I) can be synthesised from the appropriately substituted aza-indole following the outlined sequence of steps in Scheme 4 or similar as one skilled in the art may consider. A similar sequence of synthetic transformations as outlined in Scheme 4 proved to be a viable method of accessing compounds of general formula (I). Friedel-crafts acylation of aza-indole starting material 7 provides access to intermediate 8 which can be subjected to chemoselective silane reduction conditions to provide the alkyl chloride intermediate 9. Nucleophilic displacement of the alkyl chloride with a substituted amine provides compounds of general formula (I) (exemplified by P-3). One skilled in the art will recognise that utilising differentially substituted amines would allow access to compounds of general formula (I) as disclosed herein. Example 8: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1- amine (P-3): Step 1: 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (8) To a solution of 5-methoxy-1H-pyrrolo[2,3-b]pyridine (2.40 g, 16.2 mmol) in CH2Cl2 (48 mL) at 0 °C under N2 was added AlCl3 (10.8 g, 81.0 mmol), and then a solution of chloroacetyl chloride (9.15 g, 81.0 mmol) in CH2Cl2 (7 mL). The reaction mixture was stirred at 0 °C for 1 h, and quenched by the addition of H2O (50 mL). The pH was adjusted to 10 with saturated aqueous Na2CO3 solution. The mixture was filtered through celite, and the filter cake was washed with EtOAc (50 mL × 2). The filtrate was separated, and the organic layer was washed with brine (30 mL), dried over anhydrous Na 2 SO 4 , filtered, and concentrated under reduced pressure. The filter cake was stirred in EtOAc/THF (1:1, 200 mL) for 12 h.I The mixture was filtered, and the filtrate was concentrated, and combined with preceding organic layer to give 2-chloro-1-(5- methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (2.80 g, 77%) as an off-white solid. 1 H NMR (400 MHz, DMSO-d6): ^^ 12.58 (br, 1H), 8.53 (s, 1H), 8.10 (d, J = 2.8 Hz, 1H), 7.96 (d, J = 2.8 Hz, 1H), 4.90 (s, 2H), 3.86 (s, 3H). LCMS (ESI+): m/z 225.1, 227.1 [M+H] + . HPLC Purity (220 nm): 100%. Step 2: 3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[2,3-b]pyridine (9) To a solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one 8 (1.40 g, 6.23 mmol) in TFA (10 mL) was added Et3SiH (5.07 g, 43.6 mmol). The reaction mixture was stirred at 25 °C for 12 h. The reaction mixture was adjusted to pH 9 with saturated aqueous Na2CO3 solution and extracted with EtOAc (80 mL × 2). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and concentrated in vacuo to give crude 3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[2,3- b]pyridine 9 (1.40 g) as an off-white solid. 1 H NMR (400 MHz, DMSO-d6): ^^11.29 (br, 1H), 7.94 (d, J = 2.8 Hz, 1H), 7.60 (d, J = 2.4 Hz, 1H), 7.32 (d, J = 2.4 Hz, 1H), 3.82 – 3.87 (m, 5H), 3.12 (t, J = 7.4 Hz, 2H). LCMS (ESI+): m/z 211.1, 213.1 [M+H]+. HPLC Purity (220 nm): 98.5% Step 3: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine (P-3) To a mixture of crude 3-(2-chloroethyl)-5-methoxy-1H-pyrrolo[2,3-b]pyridine (1.40 g) in Me2NH (2.0 M in THF, 28 mL) was added NaI (996 mg, 6.65 mmol) and the mixture was stirred at 90 °C for 12 h. The mixture was filtered, and the filter cake was washed with THF (10 mL). The filtrate was evaporated, and the crude product was purified by preparative HPLC (column: Waters Xbridge BEH C18 (250*50 mm*10 µm); mobile phase: [water (NH3 aq.+NH4HCO3)-ACN]; B: 1 – 30%, 10 min) to afford 2-(5-methoxy- 1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan-1-amine P-3 (397 mg, 29% over 2 steps) as a brown solid. 1 H NMR (400 MHz, MeOD-d4): ^^ 7.91 (d, J = 2.8 Hz, 1H), 7.56 (d, J = 2.8 Hz, 1H), 7.19 (s, 1H), 3.89 (s, 3H), 2.89 – 2.93 (m, 2H), 2.63 – 2.67 (m, 2H), 2.35 (s, 6H). LCMS (ESI+): RT = 0.79 min, m/z 220.2 [M+H] + . HPLC Purity (220 nm): 100%. Step 3a: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine hydrochloride (P-3·HCl) To an ice cold (0 °C) solution of 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N- dimethylethan-1-amine (100 mg, 0.45 mmol) in anhydrous Et2O (5 mL) and abs. EtOH (1 mL) was added 2 M HCl in Et2O dropwise over 10 min until the pH of the reaction solution was acidic. The resulting precipitate was collected by filtration and dried overnight in a vacuum desiccator to afford 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)- N,N-dimethylethan-1-amine as the hydrochloride salt (78 mg, 68%) which was a white solid. 1 H NMR (400 MHz, MeOD-d4): ^ 7.91 (d, J = 2.8 Hz, 1H), 7.56 (d, J = 2.8 Hz, 1H), 7.19 (s, 1H), 3.89 (s, 3H), 2.96 – 2.87 (m, 2H), 2.69 – 2.60 (m, 2H), 2.35 (s, 6H). HPLC Purity (220nm): 99.7%. Scheme 5: In some circumstances, an alternative synthesis for compounds of general formula (I) was utilised as outlined in Scheme 5. Nucleophilic displacement of the chloride of intermediate 8 by appropriately substituted amines generated aminoethan- 1-ones. Subsequent two-step reductions allowed access to compounds of general formula (I) (exemplified by P-17). One skilled in the art will recognise that utilising differentially substituted amines would allow access to compounds of general formula (I) as disclosed herein. Example 9: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-diethylethan -1- amine (P-17): Step 1: 2-(diethylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl) ethan-1-one (40) A solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (250 mg, 1.11 mmol), NaI (250 mg, 1.67 mmol), and Et 2 NH (814 mg, 11.1 mmol) in DMAc (7 mL) was stirred at ambient temperature for 2 h at which point the reaction was diluted with water (30 mL) and then extracted with EtOAc (10 mL × 2). The combined organics were washed with brine (40 mL), dried over anhydrous Na2SO4, filtered and concentrated concentrated under reduced pressure to give crude 2-(diethylamino)-1- (5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (281 mg) as a yellow solid which was used in the subsequent step without purification. LCMS (ESI+): m/z 262.2 [M+H] + . Step 2: 2-(diethylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl) ethan-1-ol (41) To a solution of crude 2-(diethylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3- yl)ethan-1-one (189 mg) in MeOH (5 mL) and H2O (1.6 mL) at ambient temperature was added NaBH4 (3.00 g, 79.3 mmol) and the mixture was stirred overnight. The reaction was quenched with water (10 mL) and then extracted withCH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (15 mL), dried over Na2SO4 and concentrated in vacuo to give crude 2-(diethylamino)-1-(5-methoxy- 1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-ol (170 mg) as an off-white solid which was used without further purification. LCMS (ESI+): m/z 264.2 [M+H] + . Step 3: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-diethylethan -1-amine (P-17) To a stirred solution of crude 2-(diethylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin- 3-yl)ethan-1-one (170 mg) and Et3SiH (0.20 mL, 1.25 mmol) in MeCN (4 mL) at ambient temperature was added BF3·Et2O (0.10 mL, 0.80 mmol) and the mixture was stirred overnight. The reaction was quenched with water (5 mL) and extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The resulting residue was purified by preparative thin layer chromatography (SiO2, CH2Cl2/MeOH, v/v, 8/1) to afford 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)- N,N-diethylethan-1-amine (60 mg, 22% over 3 steps) as an off white solid. 1 H NMR (300 MHz, MeOD-d 4 ): ^^ 7.95 (d, J = 2.7 Hz, 1 H), 7.62 (d, J = 2.2 Hz, 1H) 7.33 (s, 1H), 3.89 (s, 3H), 3.36-3.41 (m, 2H), 3.12-3.18 (m, 2H), 1.31 (t, J = 7.3 Hz, 6H). LCMS (ESI+): RT = 3.33 min, m/z 248.3 [M+H] + . HPLC Purity (220 nm): 98.6%. Example 10: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dipropyletha n-1- amine (P-18): Step 1: 2-(dipropylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl )ethan-1-one (42) A solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (250 mg, 1.11 mmol), NaI (250 mg, 1.67 mmol) in DMAc (7 mL) was added dipropylamine (1.13 g, 11.1 mmol) and the mixture was stirred at room temperature for 2 h.w The reaction was quenched with water (30 mL) and then extracted with EtOAc (10 mL × 2). The combined organic layers were washed with brine (40 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to give crude 2-(dipropylamino)-1- (5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (350 mg) as a yellow solid which was used in the subsequent step without purification. LCMS (ESI+): m/z 290.4 [M+H] + . Step 2: 2-(dipropylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl )ethan-1-ol (43) To a solution of crude 2-(dipropylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3- yl)ethan-1-one (350 mg) in MeOH (5 mL) at ambient temperature was added NaBH4 (3.00 g, 79.3 mmol) and the mixture was stirred overnight. The reaction was quenched with water (10 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na2SO4 and concentrated in vacuo to give crude 2-(dipropylamino)-1-(5-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-ol (280 mg) that was used without further purification. LCMS (ESI+): m/z 292.3 [M+H] + . Step 3: 2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dipropyletha n-1-amine (P-18) To a stirred solution of crude 2-(dipropylamino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin- 3-yl)ethan-1-ol (280 mg) and Et3SiH (0.40 mL, 2.50 mmol) in MeCN (6 mL) at ambient temperature was added BF3·Et2O (0.30 mL, 2.43 mmol) and the mixture was stirred at room temperature overnight. The reaction was quenched with H2Or (5 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (15 mL) before being dried over anhydrous Na2SO4 and concentrated under reduced pressure. The resulting residue was purified by preparative thin layer chromatography (SiO2, CH2Cl2/MeOH, v/v, 8/1) to afford 2-(5- methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dipropylethan-1-a mine (80 mg, 26% over 3 steps) as an off white solid. 1 H NMR (300 MHz, MeOD-d4): ^^ 7.95 (d, J = 2.6 Hz, 1H), 7.64 (d, J = 2.6 Hz, 1H), 7.34 (s, 1H), 3.89 (s, 3H), 3.41-3.47 (m, 2H), 3.15-3.21 (m, 6H), 1.75 (sext, J = 7.3 Hz, 4H),1.00 (t, J = 7.3 Hz, 6H). LCMS (ESI+): m/z 276.3 [M+H] + . HPLC Purity (220 nm): 97.8%. Scheme 6: In some circumstances, access to compounds of general formula (I) via Scheme 5 required the introduction of an appropriate protecting group for the reactive pyrrolo amine. Base mediated SEM protection of common intermediate 8 generated the protected aza-indole 44. This intermediate proved amenable to the previously described synthetic route (Scheme 5) involving nucleophilic displacement of the chloride of intermediate 44 by appropriately substituted amines. Subsequent two-step reductions simultaneously removed the SEM protecting group providing access to compounds of general formula (I) (exemplified by P-19). One skilled in the art will recognise that utilising differentially substituted amines would allow access to alternative derivatives of general formula (I) as disclosed herein.

Example 11: N-isopropyl-N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3- yl)ethyl)propan-2-amine (P-19): Step 1: 2-chloro-1-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1 H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-one (44) A solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (1 g, 4.45 mmol) and DIPEA (3.00 mL, 22.0 mmol) in DMAc (10 mL) was treated with (2- (chloromethoxy)ethyl)trimethylsilane (2.50 mL, 14.1 mmol) at 0 °C and then stirred at ambient temperature for 5 h. The reaction was then quenched with H2O (30 mL) and extracted with EtOAc (10 mL × 2). The combined organic layer was washed with brine (40 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was subjected to column chromatography (SiO2, Petroleum ether:EtOAc - 7:1) to afford crude 2-chloro-1-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1 H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (420 mg) which was used in the subsequent step without further purification. LCMS (ESI+): m/z 355.3, 357.2 [M+H] + . Step 2: 2-(diisopropylamino)-1-(5-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (45) A solution of crude 2-chloro-1-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1 H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (410 mg), NaI (410 mg, 2.74 mmol), and diisopropylamine (2.07 mL, 14.8 mmol) in DMAc (5 mL) was stirred at ambient temperature for 3 h. The reaction was quenched with water (30 mL) and then extracted with EtOAc (10 mL × 2). The combined organics were washed with brine (40 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash column chromatography (SiO2, petroleum ether/EtOAc, v/v, 3/1) to give crude 2-(diisopropylamino)-1-(5-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (146 mg) LCMS (ESI+): m/z 420.5 [M+H] + . Step 3: 2-(diisopropylamino)-1-(5-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-ol (46) To a solution of crude 2-(diisopropylamino)-1-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[2,3-b]pyridin-3-yl )ethan-1-one (145 mg) in MeOH (2 mL) and H2O (0.4 mL) at ambient temperature was added NaBH4 (3.00 g, 79.3 mmol) which was stirred overnight. The reaction was quenched with water (10 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (30 mL), dried over anhydrous Na2SO4 and concentrated in vacuo to give crude 2-(diisopropylamino)-1-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[2,3-b]pyridin-3-yl )ethan-1-ol (110 mg) which was used in the subsequent step without further purification. LCMS (ESI+): m/z 422.4 [M+H] + . Step 4: N-isopropyl-N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)et hyl)propan-2- amine (P-19) To a stirred solution of crude 2-(diisopropylamino)-1-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[2,3-b]pyridin-3-yl )ethan-1-ol (110 mg) and Et3SiH (300 mg, 2.58 mmol) in MeCN (2 mL) at ambient temperature was added BF3·Et2O (0.20 mL,1.62 mmol) and the mixture was stirred overnight. The reaction was quenched with H2O (5 mL) and extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The resulting residue was purified by preparative thin layer chromatography (SiO2, CH2Cl2:MeOH, v/v, 8/1) to afford N- isopropyl-N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethy l)propan-2-amine (20 mg, 2% over 4 steps) as an off white solid. 1 H-NMR (300 MHz, MeOD-d4): ^^ 7.96 (d, J = 2.5 Hz, 1H), 7.55 (d, J = 2.4 Hz, 1H), 7.36 (s, 1H), 3.89 (s, 3H), 3.79-3.83 (m, 2H), 3.36-3.41 (m, 2H), 3.13-3.18 (m, 2H), 1.42 (d, J = 6.6 Hz, 12H). LCMS (ESI+): m/z 276.4 [M+H] + . HPLC Purity (220 nm): 97.4%. Example 12: N-ethyl-2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N-methyl ethan- 1-amine (P-20): Step 1: 2-(ethyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin -3-yl)ethan-1- one (47) A solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (250 mg, 1.11 mmol), NaI (250 mg, 1.67 mmol), and ethyl(methyl)amine (658 mg, 11.1 mmol) in DMAc (7 mL) was stirred at ambient temperature for 2 h. The reaction was diluted with water (30 mL) and then extracted with EtOAc (10 mL × 2).The combined organics were washed with brine (40 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to give crude 2-(ethyl(methyl)amino)-1-(5- methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (216 mg) as a yellow solid that was used in the subsequent step without purification. LCMS (ESI+): m/z 248.3 [M+H] + . Step 2: 2-(ethyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin -3-yl)ethan-1-ol (48) To a solution of crude 2-(ethyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin - 3-yl)ethan-1-one (205 mg) in MeOH/H2O (6/2 v/v, 8 mL) at ambient temperature was added NaBH4 (3.00 g, 79.3 mmol) and the mixture was stirred overnight. The reaction was quenched with water (10 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organics were washed with brine (30 mL), dried over anhydrous Na2SO4 and concentrated in vacuo to give crude 2-(dipropylamino)-1-(5-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-ol (185 mg) as awhite solid that was used in the next step without further purification. LCMS (ESI+): m/z 250.2 [M+H] + . Step 3: N-ethyl-2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N-methyl ethan-1-amine (P-20·HCl) To a stirred solution of crude 2-(ethyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-ol (185 mg) and Et3SiH (0.40 mL, 2.5 mmol) in MeCN (4 mL) at ambient temperature was added BF3·Et2O (0.50 mL, 4.05 mmol) and the mixture was stirred overnight. The reaction was quenched with sat. aq. Na2CO3 (5 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (15 mL) before being dried over anhydrous Na2SO4 and concentrated under reduced pressure. The resulting residue was purified by preparative thin layer chromatography (SiO2, CH2Cl2/MeOH, v/v, 8/1). The HCl salt was recovered after treatment with HCl/MeOH (1 mL) to provide N-ethyl-2-(5-methoxy- 1H-pyrrolo[2,3-b]pyridin-3-yl)-N-methylethan-1-amine hydrochloride as an off-white solid (30 mg, 12% over 3 steps). 1 H NMR (300 MHz, MeOD-d4): ^^ 8.56 (d, J = 2.1 Hz, 1H), 8.25 (d, J = 2.0 Hz, 1H), 7.66 (s, 1H), 4.00 (s, 3H), 3.33 - 3.55 (m, 4H), 3.13 - 3.22 (m, 2H), 2.92 (s, 3H),1.34 (t, J = 7.3 Hz, 3H).. LCMS (ESI+): m/z 234.2 [M+H] + . HPLC Purity (220 nm): 98.6%. Example 13: N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethyl)-N- methylpropan-2-amine (P-21): Step 1: 2-(isopropyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyr idin-3-yl)ethan- 1-one (49) A solution of 2-chloro-1-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (300 mg, 1.33 mmol), NaI (300 mg, 2.00 mmol), and methyl(propan-2-yl)amine (977 mg, 13.4 mmol) in DMAc (8 mL) was stirred at ambient temperature for 2 h. The reaction was quenched with water (30 mL) and then extracted with EtOAc (10 mL × 2). The combined organic layers were washed with brine (20 mL), dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure to give crude 2- (isopropyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyrid in-3-yl)ethan-1-one (275 mg) as a yellow solid that was used in the subsequent step without purification. LCMS (ESI+): m/z 262.2 [M+H] + . Step 2: 2-(isopropyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3-b]pyr idin-3-yl)ethan- 1-ol (50) To a solution of crude 2-(isopropyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-one (275 mg, 1.05 mmol) in MeOH/H2O (8 mL, v/v, 6/2) at ambient temperature was added NaBH4 (3.00 g, 79.3 mmol). The resulting mixture was stirred at ambient temperature overnight. The reaction was quenched with water (10 mL) and extracted withCH2Cl2:MeOH (10:1 v/v, 5 mL × 2). The combined organic layers were washed with brine (30 mL), dried over anhydrous Na2SO4 and concentrated in vacuo to give crude 2-(isopropyl(methyl)amino)-1-(5-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-ol (207 mg) as a white solid that was used in the next step without further purification. LCMS (ESI+): m/z 264.3 [M+H] + . Step 3: N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethyl)-N-methy lpropan-2-amine (P-21) To a stirred solution of crude 2-(isopropyl(methyl)amino)-1-(5-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-ol (207 mg) and Et3SiH (0.40 mL, 2.50 mmol) in MeCN (4 mL) at ambient temperature was added BF3·Et2O (0.30 mL, 2.43 mmol) and the mixture was stirred overnight. The reaction was quenched with sat. aq. Na2CO3 (5 mL) and then extracted with CH2Cl2:MeOH (10:1 v/v, 2 x 5 mL). The combined organic layers were washed with brine (10 mL), dried over anhydrous Na2SO4 and concentrated in vacuo. The resulting residue was purified by preparative thin layer chromatography (SiO2, CH2Cl2/MeOH, v/v, 8/1) to afford N-(2-(5-methoxy-1H-pyrrolo[2,3-b]pyridin-3- yl)ethyl)-N-methylpropan-2-amine (32 mg, 10% over 3 steps) as an off white solid. 1 H NMR (300 MHz, MeOD-d4): ^^ 7.95 (d, J = 2.4 Hz, 1H), 7.65 (d, J = 2.5 Hz, 1H), 7.34 (s, 1H), 3.89 (s, 3H), 3.64-3.72 (m, 1H), 3.34-3.44 (m, 2H), 3.12-3.23 (m, 2H), 2.85 (s, 3H), 1.32 (d, J = 6.0 Hz, 6H). LCMS (ESI+): m/z 248.3 [M+H] + . HPLC Purity (220 nm): 96%. Example 14: N,N-dimethyl-2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1- amine (P-22): Step 1: 2-chloro-1-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (52) A mixture of 5-methyl-1H-pyrrolo[2,3-b]pyridine (500 mg, 3.78 mmol) in CH2Cl2 (15 mL) was degassed and purged with N2 three times before adding AlCl3 (2.52 g, 18.9 mmol) at 0 °C under N2. After stirring at 0 °C for 5 min, was added 2-chloroacetyl chloride (1.28 g, 11.3 mmol) at 0 °C and then the mixture was stirred at ambient temperature for 2 h. The reaction was quenched with water (15 mL) at 0 °C and then adjusted to pH 9 with aqueous Na2CO3, filtered and the filter cake washed with EtOAc (30 mL × 4). The aqueous phase was separated and extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (10 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure to provide crude 2-chloro-1-(5-methyl-1H- pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (650 mg) as a yellow solid which was used in the next step without purification. Step 2: 3-(2-chloroethyl)-5-methyl-1H-pyrrolo[2,3-b]pyridine (53) To a solution of 2-chloro-1-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (650 mg) in TFA (10 mL) was added Et3SiH (5.10 g, 43.9 mmol) and the reaction was stirred at 70 °C for 12 h. The reaction mixture was then concentrated under reduced pressure and the residue was adjusted to pH 9 with saturated Na2CO3 solution and then extracted with EtOAc (10 mL × 3). The combined organics were washed with brine (10 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by column chromatography (SiO2, Petroleum ether/ EtOAc, v/v, 10:1 to 1:1) to afford 3-(2-chloroethyl)-5-methyl-1H-pyrrolo[2,3-b]pyridine (350 mg) as an off-white solid. LCMS (ESI+): m/z 195.1 [M+H] + . Step 3: 2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan -1-amine (P-22) To a solution of 3-(2-chloroethyl)-5-methyl-1H-pyrrolo[2,3-b]pyridine (200 mg) in THF (3 mL) was added NaI (462 mg, 3.08 mmol) and 2 M Me2NH in THF (1.03 mL, 2.06 mmol) which was stirred at 90 °C for 12 h in a sealed tube. The reaction mixture was diluted with water (20 mL) and then extracted with EtOAc (5 mL × 3). The combined organics were washed with brine (5 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm* 5 µm); mobile phase: [water (NH3)-ACN]; B: 12-42%, 9 min) to provide 2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N- dimethylethan-1-amine (25 mg, 6% over 3 steps) as an off-white solid. 1 H NMR (400 MHz, CDCl3): ^ 9.11 (br s, 1H), 8.13 (d, J = 2.0 Hz, 1H), 7.71 (s, 1H), 7.10 (s, 1H), 2.89-2.93 (m, 2H), 2.62-2.66 (m, 2H), 2.44 (s, 3H), 2.36 (s, 6H). LCMS (ESI+): m/z 204.0 [M+H] + . HPLC Purity (220 nm): 96.5% Example 15: N-ethyl-N-methyl-2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1- amine (P-23): Step 1: N-ethyl-N-methyl-2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1-amine (P- 23) To a solution of 3-(2-chloroethyl)-5-methyl-1H-pyrrolo[2,3-b]pyridine (200 mg, 1.03 mmol) in DMF (3 mL) was added K2CO3 (213 mg, 1.54 mmol) and ethyl(methyl)amine (182 mg, 3.08 mmol) which was stirred at 50 °C for 12 h. The reaction mixture was diluted with water (20 mL) and then extracted with EtOAc (5 mL × 3). The combined organics were washed with brine (5 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm* 5 μm); mobile phase: [water (NH4HCO3)-ACN]; B: 12-42%, 9 min) to provide N-ethyl-N-methyl-2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3- yl)ethan-1-amine (25 mg, 5% over 3 steps) as a yellow oil. 1 H NMR (400 MHz, CDCl3): ^ 9.08 (br s, 1H), 8.14 (d, J = 1.6 Hz, 1H), 7.72 (s, 1H), 7.11 (s, 1H), 2.99 - 2.86 (m, 2H), 2.76 - 2.67 (m, 2H), 2.57 (q, J = 7.2 Hz, 2H), 2.45 (s, 3H), 2.38 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H). LCMS (ESI+): m/z 218.0 [M+H] + . HPLC Purity (220 nm): 98.2%. Example 16: N,N-dimethyl-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1- amine (P-24): Step 1: 2-chloro-1-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (55) A mixture of 5-fluoro-1H-pyrrolo[2,3-b]pyridine (1.00 g, 7.35 mmol) in CH2Cl2 (7 mL) was degassed and purged with N2 three times before adding AlCl3 (4.90 g, 36.8 mmol) at 0 °C under N2. After stirring at 0 °C for 5 min, 2-chloroacetyl chloride (4.15 g, 36.7 mmol) was added at 0 °C and then the mixture was stirred at ambient temperature for 3 h. The reaction was then quenched with water (20 mL) at 0 °C and the pH adjusted 9 with aqueous Na2CO3 and then filtered. The filter cake was washed with EtOAc (30 mL × 4) and the aqueous phase separated, diluted with H2O (30 mL) and further extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and the filtrate concentrated under reduced pressure to provide crude 2-chloro-1-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (1.16 g) as a yellow solid which was used in the next step without purification. Step 2: 3-(2-chloroethyl)-5-fluoro-1H-pyrrolo[2,3-b]pyridine (56) To a solution of 2-chloro-1-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (1.16 g, 5.46 mmol) in TFA (10 mL) was added Et3SiH (3.64 g, 31.3 mmol) and the reaction was stirred at ambient temperature for 12 h. The reaction mixture was adjusted to pH 9 with saturated Na2CO3 solution, diluted with H2O (50 mL) and then extracted with EtOAc (75 mL × 3). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and the filtrate concentrated under reduced pressure. The residue triturated with MTBE:Petroleum ether (1:5 v/v, 20 mL) at ambient temperature for 30 min and filtered to afford 3-(2-chloroethyl)-5-fluoro-1H-pyrrolo[2,3- b]pyridine (389 mg) as a yellow solid. LCMS (ESI+): m/z 199.0 [M+H] + Step 3: 2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan -1-amine (P-24) To a solution of 3-(2-chloroethyl)-5-fluoro-1H-pyrrolo[2,3-b]pyridine (50.0 mg, 0.25 mmol) in THF (5 mL) was added NaI (56.6 mg, 0.39 mmol) and 2 M Me2NH in THF (0.5 mL, 1.01 mmol) which was stirred at 100 °C for 12 h in a sealed tube. The reaction mixture was then diluted with water (20 mL) and then extracted with EtOAc (20 mL × 5). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and the filtrate concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm * 5 μm); mobile phase: [water (NH3)-ACN]; B: 18-48%, 10 min) to provide 2-(5-fluoro-1H- pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan-1-amine (10.3 mg, 5% over 3 steps) as a yellow solid. 1 H NMR (400 MHz, CDCl3): ^ 9.11 (br, 1H), 8.17 (t, J = 2.2 Hz, 1H), 7.60 (dd, J = 8.9, 2.7 Hz, 1H), 7.21 (d, J = 2.4 Hz, 1H), 2.89 (t, J = 7.6 Hz, 2H), 2.62 (t, J = 6.9 Hz, 2H), 2.35 (s, 6H). 19 F NMR (400 MHz, CDCl3): ^ -139.4. LCMS (ESI+): m/z 208.2 [M+H] + . HPLC Purity (220 nm): 98.0%. Example 17: N-ethyl-N-methyl-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1- amine (P-25): Step 1: N-ethyl-N-methyl-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1-amine (P- 25) To a solution of 3-(2-chloroethyl)-5-fluoro-1H-pyrrolo[2,3-b]pyridine (200 mg, 1.01 mmol) in DMF (5 mL) was added K2CO3 (306 mg, 2.21 mmol) and ethyl(methyl)amine (238 mg, 4.03 mmol) which was stirred at 50 °C for 12 h in a sealed tube. The reaction mixture was then diluted with water (20 mL) and extracted with EtOAc (20 mL × 5). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and the filtrate concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm* 5 μm); mobile phase: [water (aq. NH3)-ACN]; B: 18-48%, 10 min) to provide N-ethyl-N-methyl-2-(5- fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-amine (57.0 mg, 7% over 3 steps) as a yellow solid. 1 H NMR (400 MHz, CDCl3): ^ 9.19 (br s, 1H), 8.16 (t, J = 2.2 Hz, 1H), 7.61 (dd, J = 8.9, 2.6 Hz, 1H), 7.20 (d, J = 2.1 Hz, 1H), 2.87-2.91 (m, 2H), 2.66-2.70 (m, 2H), 2.53 (q, J = 7.2 Hz, 2H), 2.34 (s, 3H), 1.11 (t, J = 7.2 Hz, 3H). 19 F NMR (400 MHz, CDCl3): ^ -139.4. LCMS (ESI+): m/z 222.2 [M+H] + . HPLC Purity (220 nm): 98.0%. Scheme 7: Compounds of general formula (I) can be synthesised from the appropriately substituted aza-indole following the outlined sequence of steps in Scheme 7 or similar as one skilled in the art may consider. In a similar fashion to the steps outlined in Scheme 7, Friedel-crafts acylation of aza-indole starting material 10 provides access to intermediate 11 which can be subjected to chemoselective silane reduction conditions to provide the alkyl chloride intermediate 12. Nucleophilic displacement of the alkyl chloride with a substituted amine provides compounds of general formula (I) (exemplified by P-4). Example 18: 2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1- amine (P-4): Step 1: 2-chloro-1-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (11) To a solution of 4-methoxy-1H-pyrrolo[2,3-b]pyridine (2.20 g, 14.8 mmol) in CH2Cl2 (14 mL) was added AlCl3 (9.90 g, 74.2 mmol) and chloroacetyl chloride (8.39 g, 74.2 mmol). The mixture was stirred at 0 °C for 1.5 h. The reaction mixture was quenched by addition of H2O (20 mL) at 0 °C, and then adjusted to pH 9 with saturated aqueous Na2CO3 solution. The mixture was filtered and extracted with EtOAc (50 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na2SO4, filtered, and set aside. The filter cake was triturated with THF/EtOAc (1:1, 100 mL) at 20 °C for 2 h. The filter liquor was combined with organic layers and concentrated in vacuo to give the title compound (3.10 g, 93%) as a light-yellow solid. 1 H NMR: (400 MHz, DMSO-d 6 ): δ 12.5 (br s, 1H), 8.27 (s, 1H), 8.21 (d, J = 5.6 Hz, 1H), 6.84 (d, J = 5.6 Hz, 1H), 4.97 (s, 2H), 3.95 (s, 3H). LCMS (ESI+): m/z 225.1 [M+H] + . Step 2: 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (12) To a solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1- one (2.26 g, 10.1 mmol) in TFA (13.2 mL) was added Et3SiH (8.19 g, 70.4 mmol). The mixture was stirred at 20 °C for 16 h. The reaction mixture was adjusted to pH = 9 with saturated aqueous Na2CO3 solution, then extracted with EtOAc (50 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na 2 SO 4 , filtered, and concentrated in vacuum to give 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3- b]pyridine (12) (2.00 g, 94%) as red solid. 1 H NMR: (400 MHz, DMSO-d6): ^ 8.06 (d, J = 5.6 Hz, 1H), 7.14 (d, J = 1.6 Hz, 1H), 6.63 (d, J = 5.6 Hz, 1H), 5.20 (br s, 1H), 3.93 (s, 3H), 3.81 (t, J = 7.4 Hz, 2H), 3.16 (t, J = 7.4 Hz, 2H). LCMS (ESI+): m/z 211.1 [M+H] + . Step 3: 2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine (P-4) A solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (1.6 g, 7.6 mmol) in 2 M Me2NH in THF (32.3 mL, 8.5 eq., 64.6 mmol) was treated with sodium iodide (1.14 g, 7.6 mmol) and stirred under reflux for 24 h. Upon completion, the reaction mixture was filtered, and the filter cake was eluted with THF (20 mL). The combined filtrate was concentrated in vacuo and the residue was purified by preparative HPLC (column: Waters Xbridge Prep OBD C18 150*40 mm*10µm; mobile phase: [water(NH4HCO3)-ACN]; B: 1%-30%, 8 min) to afford 2-(4-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)-N,N-dimethylethan-1-amine (0.6 g, 2.74 mmol) as a light yellow solid (600 mg, 36%). 1 H-NMR (400 MHz, MeOD-d 4 ): δ 8.03 (d, J = 5.6 Hz, 1H), 7.00 (s, 1H), 6.64 (d, J = 5.6 Hz, 1H), 4.00 (s, 3H), 2.96 – 3.03 (m, 2H), 2.60 – 2.68 (m, 2H), 2.34 (s, 6H). LCMS (ESI+): m/z 220.2 [M+H] + . HPLC purity (220 nm): 100%. Step 3a: 2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethyletha n-1-amine hydrochloride (P-4·HCl) To an ice cold (0 °C) solution of 2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N- dimethylethan-1-amine (0.2 g, 0.91 mmol) in anhydrous Et2O (5 mL) and abs. EtOH (1 mL) was added 2 M HCl in Et2O dropwise over 10 min until the pH of the reaction solution was acidic. The resulting precipitate was collected by filtration and dried overnight in a vacuum desiccator to afford 2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)- N,N-dimethylethan-1-amine as the hydrochloride salt (120 mg, 52%) which was a white solid. 1 H NMR (400 MHz, DMSO-d 6 ): δ 12.47 (s, 1H), 10.55 (br. s, 1H), 8.38 (d, J = 6.6 Hz, 1H), 7.40 (d, J = 2.2 Hz, 1H), 7.07 (d, J = 6.6 Hz, 1H), 4.15 (s, 3H), 3.30 – 3.16 (m, 4H), 2.81 (d, J = 4.8 Hz, 6H). 13 C NMR (100 MHz, DMSO-d 6 ): δ 164.3, 142.3, 138.8, 124.1, 111.1, 110.1, 99.1, 57.2, 57.1, 42.1, 21.0. HPLC Purity (220nm): 96.7%. Example 19: N,N-diethyl-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1- amine (P-26) To a solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (500 mg, 2.37 mmol) in THF (5 mL) was added NaI (534 mg, 3.56 mmol) and Et2NH (1.74 g, 23.8 mmol) and the mixture was stirred at 100 °C for 48 h. The mixture was then filtered and the filter cake was washed with THF (5 mL). The filtrate was concentrated under reduced pressure and the residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH4HCO3)-ACN]; B: 5-35%, 9 min) to afford N,N- diethyl-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-a mine (P-26) (100 mg, 17%) as a light yellow solid. 1 H NMR (400 MHz, MeOD-d 4 ): δ 8.05 (d, J = 5.7 Hz, 1H), 7.02 (s, 1H), 6.66 (d, J = 5.7 Hz, 1H), 4.02 (s, 3H), 2.97-3.02 (m, 2H), 2.81-2.85 (m, 2H), 2.74 (q, J = 7.2 Hz, 4H), 1.16 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 248.1 [M+H] + . HPLC Purity (220 nm): 96.9%. Example 20: N-isopropyl-N-(2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3- yl)ethyl)propan-2-amine (P-27) To a solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (500 mg, 2.37 mmol) in THF (5 mL) was added NaI (534 mg, 3.56 mmol) and diisopropyl amine (2.40 g, 23.7 mmol) and the mixture was stirred at 100 °C for 48 h. The mixture was then filtered, and the filter cake was washed with THF (5 mL). The filtrate was concentrated under reduced pressure and the residue was purified by preparative HPLC (Column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH4HCO3)-ACN]; B: 10-40%, 9 min) to afford N-isopropyl-N-(2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)et hyl)propan-2- amine (P-27) (14.4 mg, 2%) as a light yellow solid. 1 H NMR (400 MHz, MeOD-d4): δ 8.04 (br d, J = 3.2 Hz, 1H), 7.00 (s, 1H), 6.65 (d, J = 5.7 Hz, 1H), 4.00 (s, 3 H), 3.16 (hept, J = 6.5 Hz, 2H), 2.90-2.94 (m, 2H), 2.72-2.77 (m, 2H), 1.14 (d, J = 6.5 Hz, 12H). LCMS (ESI+): m/z 276.1 [M+H] + . HPLC Purity (220 nm): 97.1%. Example 21: N-ethyl-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-N-methyl ethan- 1-amine (P-28) To a solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (200 mg, 0.95 mmol) in THF (2 mL) was added NaI (213 mg, 1.42 mmol) and ethyl(methyl)amine (561 mg, 9.49 mmol) and the mixture was stirred at 100 °C for 48 h. The mixture was then filtered, and the filter cake was washed with THF (2 mL). The filtrate was concentrated under reduced pressure and the residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH4HCO3)- ACN]; B: 5-35%, 9 min) to afford N-ethyl-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)- N-methylethan-1-amine (P-28) (64.0 mg, 29%) as a light yellow solid. 1 H NMR (400 MHz, MeOD-d4): δ 8.07 (d, J = 5.7 Hz, 1H), 7.08 (s, 1H), 6.68 (d, J = 5.7 Hz, 1H), 4.03 (s, 3H), 3.06-3.14 (m, 2H), 2.96-3.03 (m, 2H), 2.87 (q, J = 7.2 Hz, 2H), 2.60 (s, 3H), 1.23 (t, J = 7.2 Hz, 3H). LCMS (ESI+): m/z 233.15 [M+H] + . HPLC Purity (220 nm): 96.9%. Example 22: N-(2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethyl)-N- methylpropan-2-amine (P-29) To a solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine (150 mg, 0.71 mmol) in THF (2 mL) was added NaI (160 mg, 1.07 mmol) and methyl(propan-2- yl)amine (521 mg, 7.12 mmol) and the mixture was stirred at 100 °C for 48 h. The mixture was filtered, and the filter cake was washed with THF (1.5 mL). The filtrate was concentrated under reduced pressure and the residue was purified by preparative HPLC (column: Waters Xbridge Prep OBD C18 (150*40 mm*10 μm); mobile phase: [water (NH4HCO3)-ACN]; B: 0-30%, 15 min) to afford N-(2-(4-methoxy-1H-pyrrolo[2,3- b]pyridin-3-yl)ethyl)-N-methylpropan-2-amine (P-29) (120 mg, 68%) as a light yellow solid. 1 H NMR (400 MHz, MeOD-d 4 ): δ 8.04 (d, J = 5.7 Hz, 1H), 7.01 (s, 1 H), 6.65 (d, J = 5.7 Hz, 1H), 4.01 (s, 3H), 2.95-3.00 (m, 3H), 2.71-2.76 (m, 2H), 2.37 (s, 3H), 1.10 (d, J = 6.5 Hz, 6H). LCMS (ESI+): m/z 248.1 [M+H] + . HPLC Purity (220 nm): 96.2%. Example 23: N,N-dimethyl-2-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1- amine (P-30): Step 1: 2-chloro-1-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (58) A mixture of 4-methyl-1H-pyrrolo[2,3-b]pyridine (500 mg, 3.78 mmol) in CH2Cl2 (15 mL) was degassed and purged with N2 three times before adding AlCl3 (2.52 g, 18.9 mmol) at 0 °C under N 2 . After stirring at 0 °C for 5 min, 2-chloroacetyl chloride (1.28 g, 11.3 mmol) was added at 0 °C and then the mixture was stirred at room temperature for 2 h under N2. The reaction was then cooled to 0 °C before being quenched with water (20 mL) followed by addition of sat. aq. Na2CO3 until the solution was at pH 9. The mixture was then filtered and the filter cake was washed with EtOAc (30 mL × 4) and the aqueous phase separated and extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (15 mL × 2), dried over anhydrous Na2SO4, filtered and the filtrate concentrated under reduced pressure to provide crude 2-chloro-1-(4- methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one (58) (850 mg) as a yellow solid which was used in the next step without purification. Step 2: 3-(2-chloroethyl)-4-methyl-1H-pyrrolo[2,3-b]pyridine (59) To a solution of 2-chloro-1-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (800 mg) in TFA (10 mL) was added Et3SiH (4.11 g, 35.3 mmol) and the reaction was stirred at 70 °C for 12 h. The reaction mixture was then concentrated under reduced pressure and the residue was adjusted to pH 9 with sat. aq. Na 2 CO 3 solution and then extracted with EtOAc (10 mL × 3). The combined organics were washed with brine (10 mL × 2), dried with anhydrous Na2SO4 before being filtered and the filtrate concentrated under reduced pressure. The residue was purified by column chromatography (SiO2, petroleum ether:EtOAc 10:1 to 1:2) to afford 3-(2-chloroethyl)-4-methyl-1H-pyrrolo[2,3- b]pyridine (59) (310 mg, 42% over 2 steps) as a white solid. LCMS (ESI+): m/z 195.0 Step 3: N,N-dimethyl-2-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1-amine (P-30) A mixture of 3-(2-chloroethyl)-4-methyl-1H-pyrrolo[2,3-b]pyridine (50.0 mg, 257 µmol), K2CO3 (53.3 mg, 0.39 mmol) and Me2NH (23.3 mg, 0.52 mmol) in THF (4 mL) and DMF (2 mL) was stirred at 50 °C for 12 h in a sealed tube. The reaction mixture was then diluted with water (20 mL) and then extracted with EtOAc (5 mL × 3). The combined organics were washed with brine (5 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH3)-ACN]; B: 18-48%, 10 min) to provide N,N-dimethyl-2-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1-amine (P-30) (15.0 mg, 14%) as a white solid. 1 H NMR (400 MHz, CDCl3): ^ 8.84 (br s., 1H), 8.13 (d, J = 4.8 Hz, 1H), 7.08 (br s, 1H), 6.82 (d, J = 4.8 Hz, 1H), 3.07-3.11 (m, 2H), 2.70 (s, 3H) 2.65-2.69 (m, 2H), 2.39 (s, 6H). LCMS (ESI+): m/z 204.0. HPLC Purity (220 nm): 99.6%. Example 24: N-ethyl-N-methyl-2-(4-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1- amine (P-31): Step 1: N-ethyl-N-methyl-2-(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1-amine (P- 31) To a solution of 3-(2-chloroethyl)-4-methyl-1H-pyrrolo[2,3-b]pyridine (150 mg, 771 µmol) in DMF (3 mL) was added K2CO3 (160 mg, 1.16 mmol) and ethyl(methyl)amine (137 mg, 2.32 mmol) which was stirred at 50 °C for 12 h. The reaction mixture was then diluted with water (20 mL) and then extracted with EtOAc (5 mL × 3). The combined organics were washed with brine (5 mL × 2), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH4HCO3)- ACN]; B: 10-40%, 9 min) to provide N-ethyl-N-methyl-2-(5-methyl-1H-pyrrolo[2,3- b]pyridin-3-yl)ethan-1-amine (P-31) (30.0 mg, 18%) as an off-white solid. 1 H NMR (400 MHz, CDCl3) δ 9.32 (br s, 1H), 8.13 (d, J = 4.8 Hz, 1H), 7.09 (s, 1H), 6.82 (d, J = 4.9 Hz, 1H), 3.07-3.11 (m, 2H), 2.69-2.73 (m, 2H), 2.71 (s, 3H), 2.57 (q, J = 7.1 Hz, 2H), 2.38 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H). LCMS (ESI+): m/z 218.0 [M+H] + . HPLC Purity (220 nm): 96.7%. Example 25: N,N-dimethyl-2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan -1- amine (P-32): Step 1: 2-chloro-1-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (61) A mixture of 4-fluoro-1H-pyrrolo[2,3-b]pyridine (700 mg, 5.14 mmol) in CH2Cl2 (15 mL) was degassed and purged with N2 three times before adding AlCl3 (3.43 g, 25.7 mmol) at 0 °C under N2. After stirring at 0 °C for 5 min, 2-chloroacetyl chloride (2.90 g, 25.7 mmol) was added at 0 °C and then the mixture was stirred at ambient temperature for 6 h under N2 atmosphere. The reaction was then cooled to 0 °C, quenched with water (20 mL), and adjusted to pH 9 with sat. aq. Na2CO3 before being filtered. The filter cake was washed with EtOAc (30 mL × 4) and the aqueous phase separated, diluted with water (30 mL) and extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to provide crude 2-chloro-1-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3- yl)ethan-1-one (61) (727 mg) as a yellow solid which was used in the next step without purification. Step 2: 3-(2-chloroethyl)-4-fluoro-1H-pyrrolo[2,3-b]pyridine (62) To a solution of 2-chloro-1-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-o ne (700 mg) in TFA (10 mL) was added Et3SiH (2.91 g, 25.0 mmol) and the reaction was stirred at 25 °C for 12 h. The reaction mixture was adjusted to pH 9 with satd. aq. Na2CO3 solution, diluted with H2O (50 mL), and then extracted with EtOAc (75 mL × 3). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was triturated with 1:5 MTBE/Petroleum ether (1/5 v/v, 20 mL) at ambient temperature for 30 min and filtered to afford crude 3-(2-chloroethyl)-4-fluoro-1H-pyrrolo[2,3-b]pyridine (62) (580 mg) as a yellow solid. LCMS (ESI+): m/z 199.1 [M+H] + . Step 3: 2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan -1-amine (P-32) To a solution of crude 3-(2-chloroethyl)-4-fluoro-1H-pyrrolo[2,3-b]pyridine (200 mg) in DMF (5 mL) was added K2CO3 (306 mg, 2.21 mmol) and 2 M dimethylamine in THF (2.01 mL) which was stirred at 50 °C for 12 h in a sealed tube. The reaction mixture was diluted with water (20 mL) and then extracted with EtOAc (20 mL × 5). The combined organics were washed with brine (50 mL), dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH3)-ACN]; B: 18-48%, 10 min) to provide 2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-N,N-dimethylethan -1-amine (P-32) (34.1 mg, 10% over 3 steps) as a yellow solid. 1 H NMR (400 MHz, CDCl3): δ 9.15 (br s, 1H), 8.21 (dd, J = 7.8, 5.5 Hz, 1H), 7.11 (s, 1H), 6.77 (dd, J = 10.3, 5.5 Hz, 1H), 3.02-3.06 (m, 2H), 2.69-2.73 (m, 2H), 2.39 (s, 6H). 19 F NMR (400 MHz, CDCl3): ^ -112.5. LCMS (ESI+): m/z 208.2 [M+H] + . HPLC Purity (220 nm): 96.6%. Example 26: N-ethyl-N-methyl-2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1- amine (P-33): Step 1: N-ethyl-N-methyl-2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)e than-1-amine (P- 33) To a solution of crude 3-(2-chloroethyl)-4-fluoro-1H-pyrrolo[2,3-b]pyridine (200 mg) in DMF (5 mL) was added K2CO3 (306 mg, 2.21 mmol) and ethyl(methyl)amine (238 mg, 4.03 mmol) which was stirred at 50 °C for 12 h in a sealed tube. The reaction mixture was then diluted with water (20 mL) and then extracted with EtOAc (20 mL × 5). The combined organics were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered and filtrate concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge (150*25 mm*5 μm); mobile phase: [water (NH3)-ACN]; B: 20-50%, 10 min) to provide N-ethyl-N-methyl-2-(4-fluoro-1H-pyrrolo[2,3-b]pyridin-3- yl)ethan-1-amine (P-33, 34.1 mg, 9% over 3 steps) as a pink solid. 1 H NMR (400 MHz, CDCl3): δ 9.25 (br s, 1H), 8.21 (dd, J = 7.7, 5.5 Hz, 1H), 7.10 (s, 1H), 6.77 (dd, J = 10.3, 5.5 Hz, 1H), 3.01-3.05 (m, 2H), 2.74-2.77 (m, 2H), 2.59 (q, J = 7.0 Hz, 2H) 2.39 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H). 19 F NMR (400 MHz, CDCl3): δ -112.4. LCMS (ESI+): m/z 222 [M+H] + . HPLC Purity (220 nm): 98.8%. Scheme 8: Compounds of general formula (I) can be synthesised from the appropriately substituted aza-indole following the outlined sequence of steps in Scheme 8 or similar as one skilled in the art may consider. Following a palladium catalysed methoxylation of starting reagent 13, a similar sequence of synthetic transformations as outlined in scheme 8 proved to be a viable method of accessing compounds of general formula I. Friedel-crafts acylation of aza-indole intermediate material 14 provides access to intermediate 15 which can be subjected to chemoselective silane reduction conditions to provide the alkylchloride intermediate 16. Nucleophilic displacement of the alkylchloride with a substituted amine provides compounds of general formula I (exemplified by P-5). One skilled in the art will recognise that utilising differentially substituted amines would allow access to compounds of general formula I claimed herein. Example 27: 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethyletha n-1- amine (P-5):

Step 1: 4-methoxy-1H-pyrrolo[3,2-c]pyridine (14) To a solution of 4-chloro-1H-pyrrolo[3,2-c]pyridine (10.0 g, 65.5 mmol) in toluene (70 mL) was added t-BuONa (18.9 g, 197 mmol), Pd(OAc)2 (1.47 g, 6.55 mmol), t-Bu- Xphos (5.57 g, 13.1 mmol) and MeOH (26.5 mL). The mixture was stirred at 120 °C for 16 h. The mixture was filtered, and the filtrate was concentrated in vacuo. The residue was purified by column chromatography (SiO2, Petroleum ether/EtOAc, v/v, 100:1 to 1:1) to give 4-methoxy-1H-pyrrolo[3,2-c]pyridine (3.80 g, 39%) as light-yellow solid. 1 H NMR (400 MHz, CDCl3): δ 8.59 (s, 1H), 7.86 (d, J = 6.0 Hz, 1H), 7.13 (s, 1H), 6.97 (d, J = 5.6 Hz, 1H), 6.67 (s, 1H), 4.11 (s, 3H). LCMS (ESI+): m/z 149.1 [M+H] + . Step 2: 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (15) To a solution of 4-methoxy-1H-pyrrolo[3,2-c]pyridine (2.50 g, 16.9 mmol) in CH2Cl2 (15 mL) at 0 °C was added AlCl3 (11.2 g, 84.4 mmol) and chloroacetyl chloride (9.53 g, 84.4 mmol) and stirring continued at this temperature for 2 h. The reaction mixture was quenched by addition of H2O (20 mL) at 0 °C, and then adjusted to pH 9 with sat. aq. Na2CO3 solution. The resultant suspension was then filtered, and the filtrate was extracted with EtOAc (80 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na2SO4, and filtered. The filter cake was triturated with THF/EtOAc (100 mL, 1:1., v/v) at 20 °C for 30 min, then filtered. The filtrate was combined with the organic layers and concentrated in vacuo to give 2-chloro-1-(4- methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-one (3.60 g, 95%) as an off-white solid. 1 H NMR (400 MHz, DMSO-d 6 ): δ 8.22 (d, J = 2.8 Hz, 1H), 7.86 (d, J = 5.6 Hz, 1H), 7.12 (d, J = 5.6 Hz, 1H), 5.02 (s, 2H), 3.97 (s, 3H), NH peak unresolved. LCMS (ESI+): m/z 225.0 [M+H] + . Step 3: 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridine (16) To a solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one 15 (4.50 g, 20.0 mmol) in TFA (27 mL) was added Et3SiH (16.3 g, 140 mmol). The mixture was stirred at 20 °C for 16 h. The reaction mixture was adjusted to pH 9 with saturated aqueous Na2CO3 solution and extracted with EtOAc (80 mL × 2). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and concentrated in vacuo to give 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridine (3.70 g, 88%) as a pale red solid. 1 H NMR (400 MHz, DMSO-d6): δ 7.67 (d, J = 6.0 Hz, 1H), 7.16 (d, J = 2.0 Hz, 1H), 6.97 (d, J = 6.0 Hz, 1H), 3.95 (s, 3H), 3.83 (t, J = 7.2 Hz, 2H), 3.19 (t, J = 7.2 Hz, 2H). LCMS (ESI+): m/z 211.1 [M+H] + . Step 4: 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethyletha n-1-amine (P-5) A solution of 3-(2-chloroethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridine (3.00 g, 14.2 mmol) in 2 M Me2NH in THF (92.6 mL, 185 mmol) was treated with NaI 92.13 g, 14.2 mmol) and stirred under reflux for 16 h. Upon completion, the reaction mixture was concentrated in vacuo and the residue was purified by column chromatography (SiO2, Petroleum ether:EtOAc – 90:10 to 0:100) and then preparative HPLC (Column: Phenomenex C18 (80*40 mm*3 µm); mobile phase: [water (NH4HCO3)-ACN]; B: 1-30%, 8 min) to afford 2- (4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethylethan- 1-amine (259 mg, 8%) as a light yellow oil. 1 H-NMR (400 MHz, MeOD-d 4 ) δ 7.63 (d, J = 6.0 Hz, 1H), 7.00 (s, 1H), 6.96 (d, J = 6.0 Hz, 1H), 4.03 (s, 3H), 2.99 - 3.04 (m, 2H), 2.64 - 2.68 (m, 2H), 2.36 (s, 6H). LCMS (ESI+): m/z 220.2 [M+H] + . HPLC Purity (220 nm): 100% Step 5: 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethyletha n-1-amine hydrochloride (P-5·HCl) To an ice-cold solution of 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethyletha n- 1-amine (200 mg, 0.91 mmol) in a mixture of anhydrous Et2O (5 mL) and EtOH (1 mL) was added dropwise 2 M HCl in Et2O over 10 min until the pH of the reaction solution was acidic. The resulting precipitate was collected by filtration and dried overnight in a vacuum desiccator to obtain 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N,N-dimethyletha n-1- amine hydrochloride (80 mg, 34%) which was a white solid. 1 H NMR (400 MHz, D2O): ^ 7.63 (d, J = 6.8 Hz, 1H), 7.40 (s, 1H), 7.36 (d, J = 6.8 Hz, 1H), 4.30 (s, 3H), 3.39 – 3.35 (m, 2H), 3.28 – 3.17 (m, 2H), 2.87 (s, 6H). 13 C NMR (101 MHz, D2O): ^ 155.7, 143.3, 127.1, 127.0, 112.8, 110.4, 104.8, 58.0, 57.6, 42.8, 20.9. HPLC Purity (220 nm): 96.6%. Scheme 9: Compounds of general formula (I) can be synthesised from the appropriately substituted indazole following the outlined sequence of steps in Scheme 9 or similar as one skilled in the art may consider. Following a nucleophilic substitution of alkyl chloride starting reagent 15, a partial reduction of the carbonyl to alcohol provides access to intermediate 64. Further reduction of the alcohol followed by Boc protection for purification simplicity provides intermediate 65 that can be deprotected to provide compounds of general formula (I) (exemplified by P-34). One skilled in the art will recognise that utilising differentially substituted amines would allow access to compounds of general formula I claimed herein. Example 28: N,N-diethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan -1- amine (P-34):

Step 1: 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl) ethan-1-one (63) A solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (500 mg, 2.23 mmol),NaI (500 mg, 3.34 mmol), and Et2NH (0.5 mL, 4.83 mmol). in DMAc (10 mL) was stirred at ambient temperature for 4 h. The reaction was quenched with brine (50 mL) and extracted with CH2Cl2 (30 mL × 3). The combined organic layers were washed with brine (40 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-one (2.00 g) as a yellow oil that was used in the subsequent step without purification. LCMS (ESI+): m/z 262.2 [M+H] + . Step 2: 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl) ethan-1-ol (64) To a solution of crude 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3- yl)ethan-1-one (2.00 g) in MeOH (20 mL) at ambient temperature was added NaBH4 (500 mg, 13.1 mmol) and the mixture was stirred for 1 h. The reaction was quenched with water (100 mL) and extracted with CH2Cl2 (50 mL × 3). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-ol (1.60 g) which was used in the next step without further purification. LCMS (ESI+): m/z 264.3 [M+H] + . Step 3: N,N-diethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan -1-amine (P-34) To a solution of crude 2-(diethylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3- yl)ethan-1-ol (1.60 g) and Et 3 SiH (1.00 mL, 6.26 mmol) in MeCN (8 mL) under N 2 atmosphere at ambient temperature was added BF3·Et2O (1.00 mL, 8.10 mmol). The resulting mixture was stirred overnight. The reaction was quenched with water (50 mL) and the pH of the reaction mixture was adjusted to 9-10 with saturated aqueous NaHCO3 solution, before being extracted with CH2Cl2 (50 mL × 3). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was subjected to preparative thin layer chromatography (SiO2, CH2Cl2:MeOH:NH3(aq.), 80:10:1) to afford crude N,N-diethyl- 2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-amine (350 mg). LCMS (ESI+): m/z 248.3 [M+H] + . Step 4: tert-butyl 3-(2-(diethylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridin e-1- carboxylate (65) To a solution of crude N,N-diethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan -1- amine (200 mg) in CH2Cl2 (5 mL) was added Boc2O (500 mg, 2.29 mmol), DIPEA (0.50 mL, 2.87 mmol), and DMAP (100 mg, 0.82 mmol). The resulting mixture was stirred at room temperature for 1 h. The reaction was quenched with water and extracted with CH2Cl2 (20 mL × 2). The combined organic layers were concentrated, and the residue purified by preparative thin layer chromatography (CH2Cl2:MeOH, 15:1, v/v) to provide tert-butyl 3-(2-(diethylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridin e-1-carboxylate 65 (30 mg) as a white solid. LCMS (ESI+): m/z 348.4 [M+H] + . HPLC Purity (254 nm): 97.6%. Step 5: N,N-diethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan -1-amine hydrochloride (P-34·HCl) To a solution of tert-butyl 3-(2-(diethylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridin e- 1-carboxylate 65 (30 mg, 0.08 mmol) in MeOH (1 mL) was added concentrated aq. HCl (1 mL). After stirring at room temperature for 1 h, the reaction mixture was concentrated under reduced pressure to give N,N-diethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3- yl)ethan-1-amine hydrochloride (20.5 mg, 11%).. 1 H NMR (300 MHz, MeOD-d 4 ): δ 7.79 (d, J = 6.6 Hz, 1H), 7.58 (s, 1H), 7.50 (d, J = 6.6 Hz, 1H), 4.45 (s, 3H), 3.31-3.53 (m, 8H), 1.42 (t, J = 6.9 Hz, 6H). LCMS (ESI+): m/z 248.4 [M+H] + ; HPLC purity (220 nm): 96.4%. Example 29: N,N-dipropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)etha n-1- amine (P-35): Step 1: 2-(dipropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl )ethan-1-one (66) A solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (200 mg, 0.89 mmol), NaI (200 mg, 1.33 mmol), and dipropylamine (297 mg, 2.94 mmol) in DMAc (5 mL) was stirred at ambient temperature for 16 h. The reaction was quenched with brine (50 mL) and extracted with CH2Cl2 (30 mL × 3). The combined organic layers were washed with brine (40 mL), dried over Na 2 SO 4 , filtered, and the filtrate concentrated in vacuo to provide crude 2-(dipropylamino)-1-(4-methoxy-1H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-one (400 mg) as a yellow oil that was used in the subsequent step without purification. Step 2: 2-(dipropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl )ethan-1-ol (67) To a solution of crude 2-(dipropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3- yl)ethan-1-one (400 mg) in MeOH (5 mL) at ambient temperature was added NaBH4 (1.00 g, 26.4 mmol) and the mixture was stirred for 1 h. The reaction was quenched with water (30 mL) and extracted with CH2Cl2 (30 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(dipropylamino)-1-(4-methoxy-1H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-ol (250 mg) which was used in the next step without further purification. LCMS (ESI+): m/z 292.3 [M+H] + . Step 3: N,N-dipropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)etha n-1-amine (P-35) To a stirred solution of crude 2-(dipropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin- 3-yl)ethan-1-ol (250 mg) and Et3SiH (1.00 mL, 6.26 mmol) in MeCN (5 mL) at ambient temperature was added BF3·Et2O (1.00 mL, 8.10 mmol) under N2 and the mixture was stirred overnight The reaction was quenched with water (30 mL) and the pH of the reaction mixture was adjusted to 9-10 with saturated aqueous NaHCO3 solution, before being extracted with CH2Cl2 (30 mL × 2). The combined organic layers were washed with brine (30 mL) before being dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The resulting residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH:NH3(aq.), 80:10:1) to afford N,N-dipropyl-2-(4- methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-amine (40 mg, 26% over 4 steps) which was a white solid. 1 H-NMR (300 MHz, MeOD-d4): δ 7.68 (d, J = 6.0 Hz, 1H), 7.19 (s, 1H), 7.02 (d, J = 6.0 Hz, 1H), 4.06 (s, 3H), 3.41 (m, 2H), 3.19-3.31 (m, 6H), 1.74-1.87 (m, 4H), 1.04 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 276.4 [M+H] + . HPLC Purity (220 nm): 98.3%. Example 30: N,N-diisopropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)e than- 1-amine (P-36): Step 1: 2-chloro-1-(4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1 H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-one (68) To a solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (400 mg, 1.78 mmol) and DIPEA (1.0 mL, 7.33 mmol) in DMAc (15 mL) was added dropwise (2-(chloromethoxy)ethyl)trimethylsilane (473 µL, 2.67 mmol) at ambient temperature under N2 and the mixture was stirred for 4 h. The reaction was quenched with brine (150 mL) and extracted with EtOAc (50 mL × 3). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, the filtrate concentrated, and the residue was triturated with 10% EtOAc in Petroleum ether (50 mL) to afford 2- chloro-1-(4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H- pyrrolo[3,2-c]pyridin-3- yl)ethan-1-one (550 mg, 1.55 mmol) as a white solid. LCMS (ESI+): m/z 355.2 [M+H] + . Step 2: 2-(diisopropylamino)-1-(4-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)-1H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-one (69) A solution of 2-chloro-1-(4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1 H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-one (550 mg, 1.55 mmol), NaI (400 mg, 2.67 mmol), and diisopropylamine (3.00 mL, 21.4 mmol) in DMAc (10 mL) was stirred at ambient temperature for 16 h. The reaction was quenched with brine (50 mL) and extracted with EtOAc (30 mL × 3). The combined organic layers were washed with brine (40 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2- (diisopropylamino)-1-(4-methoxy-1-((2-(trimethylsilyl)ethoxy )methyl)-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-one (800 mg) as a yellow oil that was used in the subsequent step without purification. LCMS (ESI+): m/z 420.4 [M+H] + . Step 3: 2-(diisopropylamino)-1-(4-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)-1H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-ol (70) To a solution of crude 2-(diisopropylamino)-1-(4-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[3,2-c]pyridin-3-yl )ethan-1-one (800 mg) in MeOH (10 mL) at ambient temperature was added NaBH4 (250 mg, 6.61 mmol) and the mixture was stirred for 1 h. The reaction was quenched with water (30 mL) and extracted with EtOAc (50 mL × 2). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(diisopropylamino)-1-(4-methoxy-1-((2-(trimethylsilyl)etho xy)methyl)- 1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-ol (400 mg) which was used in the next step without further purification. LCMS (ESI+): m/z 422.4 [M+H] + . Step 4: 2-(diisopropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3 -yl)ethan-1-ol (71) To a solution of crude 2-(diisopropylamino)-1-(4-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[3,2-c]pyridin-3-yl )ethan-1-ol (400 mg) in MeCN (5 mL) was added BF3.Et2O (1.50 mL, 12.2 mmol) under N2. The reaction was stirred at ambient temperature for 1 h and was then quenched with water (50 mL). The pH of the reaction solution was adjusted to 9-10 with saturated aqueous Na2CO3 solution and then extracted with CH2Cl2 (50 mL × 2). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated. The residue was treated with aqueous ammonium hydroxide (2 mL) in MeOH (5 mL) and stirred at ambient temperature for 16 h. The mixture was concentrated in vacuo and purification was attempted on the residue by preparative thin layer chromatography (CH2Cl2:MeOH:NH3(aq.), 80:10:1), to provide 2- (diisopropylamino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-y l)ethan-1-ol (150 mg) which was used directly in the next step. Step 5: N,N-diisopropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)e than-1-amine (P- 36) To a stirred solution of crude 2-(diisopropylamino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-ol (150 mg) in MeCN (8 mL) was added Et3SiH (0.50 mL, 3.13 mmol) and BF3·Et2O (1.0 mL, 8.10 mmol) and the mixture was stirred at ambient temperature for 4 h. The reaction was quenched with water (50 mL) and the pH was adjusted to 9-10 with saturated aqueous NaHCO3 solution, before being extracted with CH2Cl2 (50 mL × 3). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. N-Boc protection was carried out in the next step to facilitate purification of the title compound from the obtained residue (100 mg). Step 6: tert-butyl 3-(2-(diisopropylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyr idine- 1-carboxylate (72) To a solution of crude N,N-diisopropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)e than- 1-amine (100 mg) in THF (3 mL) was added Et3N (0.20 mL, 1.43 mmol), DMAP (20 mg, 164 µmol), and Boc2O (200 mg, 0.92 mmol) and the mixture was stirred for 1 h at ambient temperature. The reaction was quenched with water (30 mL) and then extracted with EtOAc (20 mL × 3). The combined organic layers were washed with brine (50 mL), dried over Na 2 SO 4 , filtered, and the filtrate concentrated. The residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH, 15:1, v/v) to afford tert-butyl 3-(2- (diisopropylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2-c]pyridine -1-carboxylate (15 mg) which was used in the next step without further purification. LCMS (ESI+): m/z 376.4 (M+H) + . Step 7: N,N-diisopropyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)e than-1-amine (P- 36·HCl) To a solution of tert-butyl 3-(2-(diisopropylamino)ethyl)-4-methoxy-1H-pyrrolo[3,2- c]pyridine-1-carboxylate (15 mg) in MeOH (1 mL) was added concentrated aq. HCl (1 mL) and the mixture was stirred at ambient temperature for 1 h. The reaction was concentrated in vacuo and the residue dried under vacuum to afford N,N-diisopropyl-2- (4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-amine as the hydrochloride salt (12 mg, 2% over 5 steps). 1 H NMR (300 MHz, MeOD-d4): ^ 7.79 (d, J = 6.9 Hz, 1H), 7.61 (s, 1H), 7.50 (d, J = 6.9 Hz, 1H), 4.43 (s, 3H), 3.84 (m, 2H), 3.36 (m, 4H), 1.44-1.50 (m, 12H). LCMS (ESI+): m/z 276.4 [M+H] + . HPLC Purity (220 nm): 99.0%. Example 31: N-ethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N-methyl ethan- 1-amine (P-37): Step 1: 2-(ethyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin -3-yl)ethan-1- one (73) To a solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (500 mg, 2.23 mmol) and NaI (200 mg, 1.33 mmol) in DMAc (5 mL) was added ethyl(methyl)amine (526 mg, 8.90 mmol) and the reaction was stirred at ambient temperature for 3.5 h. The reaction was quenched with brine (50 mL) and then extracted with CH2Cl2 (30 mL × 3). The combined organic layers were washed with brine (40 mL), dried over Na 2 SO 4 , filtered, and the filtrate concentrated in vacuo to provide crude 2-(ethyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin -3- yl)ethan-1-one 73 (2.00 g) as a yellow oil that was used in the subsequent step without purification. LCMS (ESI+): m/z 248.2 [M+H] + . Step 2: 2-(ethyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin -3-yl)ethan-1-ol (74) To a solution of crude 2-(ethyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin -3- yl)ethan-1-one (2.00 g) in MeOH (20 mL) at ambient temperature was added NaBH4 (499 mg, 13.2 mmol) and the mixture was stirred for 1 h. The reaction was quenched with water (30 mL) and extracted with EtOAc (50 mL × 2). The combined organic layers were washed with brine (30 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(ethyl(methyl)amino)-1-(4-methoxy-1H- pyrrolo[3,2-c]pyridin-3-yl)ethan-1-ol (1.50 g) which was used without further purification. LCMS (ESI+): m/z 250.2 [M+H] + . Step 3: N-ethyl-2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-N-methyl ethan-1-amine (P-37) To a stirred solution of crude 2-(ethyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-ol (1.50 g) and Et3SiH (1.00 mL, 8.60 mmol) in MeCN (5 mL) at ambient temperature was added BF3·Et2O (0.70 mL, 5.67 mmol) under N2 and the mixture was stirred overnight. The reaction was quenched with water (50 mL) and the pH was adjusted to 9-10 with saturated aqueous NaHCO3 solution, before being extracted with CH2Cl2 (30 mL × 2). The combined organic layers were washed with brine (30 mL) before being dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The resulting residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH:NH3(aq.), 80:10:1) to afford N-ethyl-2-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)-N-methylethan-1-amine (22 mg, 4% over 3 steps) as a white solid. 1 H NMR (300 MHz, MeOD-d4): δ 7.69 (d, J = 6.0 Hz, 1H), 7.21 (s, 1H), 7.05 (d, J = 6.0 Hz, 1H), 4.09 (s, 3H), 3.50 (m, 2H), 3.23-3.30 (m, 4H), 2.94 (s, 3H), 1.36 (t, J = 7.2 Hz, 3H). LCMS (ESI+): m/z 234.3 [M+H] + ; HPLC Purity (220 nm): 96.1% Example 32: N-(2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethyl)-N- methylpropan-2-amine (P-38): Step 1: 2-(isopropyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyr idin-3-yl)ethan- 1-one (75) A solution of 2-chloro-1-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1- one (200 mg, 0.89 mmol), NaI (170 mg, 1.13 mmol), and methyl(propan-2-yl)amine (300 mg, 4.10 mmol), in DMAc (3 mL) was stirred at ambient temperature for 16 h. The reaction was quenched with brine (50 mL) and then extracted with CH2Cl2 (30 mL × 3). The combined organic layers were washed with brine (40 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(isopropyl(methyl)amino)-1- (4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-one (350 mg) as a yellow oil that was used in the subsequent step without purification. LCMS (ESI+): m/z 262.2 [M+H] + . Step 2: 2-(isopropyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2-c]pyr idin-3-yl)ethan- 1-ol (76) To a solution of crude 2-(isopropyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-one (350 mg) in MeOH (3 mL) at ambient temperature was added NaBH4 (100 mg, 2.64 mmol) and the mixture was stirred for 1 h. The reaction was quenched with water (100 mL) and extracted with CH2Cl2 (50 mL × 2). The combined organic layers were washed with brine (50 mL), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 2-(isopropyl(methyl)amino)-1- (4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethan-1-ol (200 mg) which was used in the next step without further purification. LCMS (ESI+): m/z 264.4 [M+H] + . Step 3: N-(2-(4-methoxy-1H-pyrrolo[3,2-c]pyridin-3-yl)ethyl)-N-methy lpropan-2-amine hydrochloride (P-38·HCl) To a stirred solution of crude 2-(isopropyl(methyl)amino)-1-(4-methoxy-1H-pyrrolo[3,2- c]pyridin-3-yl)ethan-1-ol (200 mg) and Et3SiH (0.50 mL, 3.75 mmol) in MeCN (6 mL) at ambient temperature was added BF 3 ·Et 2 O (0.40 mL, 3.24 mmol) under N 2 and the mixture was stirred overnight. The reaction was quenched with water (50 mL) and the pH of the reaction mixture was adjusted to 9-10 with saturated aqueous NaHCO3 solution, before being extracted with CH2Cl2 (50 mL × 2). The combined organic layers were washed with brine (50 mL) before being dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The resulting residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH:NH3(aq.), 80:10:1) to afford the title compound as the free base which was then dissolved in MeOH (1 mL) and made acidic with methanolic HCl at ambient temperature. The reaction mixture was then concentrated to afford N-(2-(4-methoxy-1H- pyrrolo[3,2-c]pyridin-3-yl)ethyl)-N-methylpropan-2-amine as the hydrochloride salt (25 mg, 11% over 3 steps) which was a white solid. 1 H-NMR (300 MHz, MeOD-d4): δ 7.75- 7.76 (m, 1H), 7.54 (s, 1H), 7.45-7.46 (m, 1H), 4.42 (s, 3H), 3.60-3.76 (m, 1H), 3.30-3.48 (m, 4H), 2.86 (s, 3H), 1.25-1.36 (m, 6H). LCMS (ESI+): m/z 248.3 [M+H] + . HPLC Purity (220 nm): 98.5%. Scheme 10: Compounds of general formula (I) can be synthesised from the appropriately substituted indazole following the outlined sequence of steps in Scheme 10 or similar as one skilled in the art may consider. Addition of SEM protecting group to indazole starting material 17 allows access to intermediate 77 which can be formylated at the 3 position with n-BuLi and DMF to provide intermediate 78. Reaction of intermediate 78 with nitromethane allows access to nitrostyrene intermediate 79 which can be subsequently deprotected at the 1 position with TFA providing intermediate 80. Chemoselective reduction of intermediate 80 with LiAlH4 allows access to intermediate 81. Reductive alkylation and subsequent demethylation provides compounds of general formula (I) (exemplified by P-55 and P-56). One skilled in the art will recognise that utilising different aldehydes during the reductive alkylation step would allow access to alternative compounds of general formula (I) disclosed herein.

Example 36: 2-(1H-indazol-3-yl)-N,N-dimethylethan-1-amine (P-56): Step 1: 4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (77) To a solution of N-cyclohexyl-N-methylcyclohexanamine (17.2 g, 88.0 mmol) in THF (105 mL) was added [2-(chloromethoxy)ethyl]trimethylsilane (13.5 g, 81.0 mmol) and 4-methoxy-1H-indazole (10.0 g, 67.5 mmol). The mixture was stirred at 25 °C for 12 h, at which point the reaction mixture was combined with 0.5 M NaOH (120 mL) and the product was extracted with EtOAc (20 mL × 2). The combined organic layers were washed with H2O (20 mL), then brine (20 mL), and then dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (SiO2, Petroleum ether/EtOAc, v/v, 50/1 to 20/1) to afford 4-methoxy- 1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (12.0 g, 64%) as a yellow oil. 1 H NMR (400 MHz, CDCl3): ^ 8.16 (s, 1H), 7.30-7.33 (m, 1H), 7.20-7.24 (m, 1H), 6.35 (d, J = 7.2 Hz, 1H), 5.70 (s, 2H), 3.95 (s, 3H), 3.60-3.64 (m, 2H), 0.92-0.96 (m, 2H), -0.02 (s, 9H). Step 2: 4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 -carbaldehyde (78) To a solution of 4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (10.0 g, 35.9 mmol) in THF (60 mL), cooled to −65 °C, was added 2.5 M n-BuLi in hexanes (35.9 mL, 89.8 mmol) and DMF (5.25 g, 71.8 mmol). The mixture was stirred at −65 °C for 2 h. The reaction was quenched by dropwise addition of H2O (10 mL) at 0 °C and was then further diluted with H2O (30 mL) before the product was extracted with CH2Cl2 (40 mL × 3). The combined organics were washed with brine (30 mL), dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (SiO2, Petroleum ether/EtOAc, v/v, 50/1 to 5/1) to afford 4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 -carbaldehyde (8.00 g, 73%) as a yellow oil. 1 H NMR (400 MHz, CDCl3): ^ 10.54 (s, 1H), 7.34-7.47 (m, 1H), 7.30-7.32 (m, 1H), 6.65 (d, J = 7.2 Hz, 1H), 6.14 (s, 2H), 4.0 (s, 3H), 3.65-3.69 (m, 2H), 0.91-0.95 (m, 2H), -0.03 (s, 9H). Step 3: (E)-4-methoxy-3-(2-nitrovinyl)-1-((2-(trimethylsilyl)ethoxy) methyl)-1H-indazole (79) To a solution of 4-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 - carbaldehyde (3.00 g, 9.79 mmol) in MeNO2 (6.91 mL, 129 mmol) was added NH4OAc (377 mg, 4.89 mmol) and the mixture was stirred at 100 °C for 2 h. The reaction mixture was cooled to 0 °C and diluted with H2O (20 mL) then extracted with EtOAc (20 mL × 2). The combined organic layers were washed with brine (10 mL), dried over Na2SO4 and concentrated in vacuo. The residue was subjected to column chromatography (Petroleum ether/EtOAc, v/v, 50/1 to 5/1) to yield crude (E)-4-methoxy-3-(2-nitrovinyl)- 1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (7.00 g) as a yellow solid which was used in the subsequent step without purification. Step 4: (E)-4-methoxy-3-(2-nitrovinyl)-1H-indazole (80) Crude (E)-4-methoxy-3-(2-nitrovinyl)-1-((2-(trimethylsilyl)ethoxy) methyl)-1H-indazole (6.00 g) was dissolved in 4 M HCl in MeOH (5 mL) and stirred at 25 °C for 12 h. The reaction mixture was concentrated in vacuo to give (E)-4-methoxy-3-(2-nitrovinyl)-1H- indazole (3.70 g) as a yellow solid. 1 H NMR (400 MHz, CDCl3): ^ 8.44 (d, J = 13.6 Hz, 1H), 8.08 (d, J = 13.6 Hz, 1H), 7.29-31 (m, 1H), 7.05 (d, J = 8.4 Hz, 1H), 6.57 (d, J = 7.6 Hz, 1H), 3.97 (s, 3H). Step 5: 2-(4-methoxy-1H-indazol-3-yl)ethan-1-amine (81) To an ice-cold solution of (E)-4-methoxy-3-(2-nitrovinyl)-1H-indazole (3.70 g, 16.9 mmol) in THF (37 mL) was added LiAlH4 (7.05 g, 186 mmol) portionwise. The mixture was then heated to 50 °C and stirred for 3 h. The mixture was then cooled to 0 °C and quenched by portionwise addition of Na2SO4·10H2O (7.00 g). The mixture was stirred at 20 °C for 10 min and then filtered. The filtrate was concentrated in vacuo to give 2- (4-methoxy-1H-indazol-3-yl)ethan-1-amine (2.60 g) as a brown solid. LCMS (ESI+): m/z 192.2 [M+H] + . Step 6: 2-(4-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine (P-55) To a solution of 2-(4-methoxy-1H-indazol-3-yl)ethan-1-amine (0.30 g, 1.57 mmol) in MeOH (3 mL) was added 37% w/w aqueous formaldehyde (431 mg, 5.31 mmol), AcOH (376 mg, 6.26 mmol) and NaBH3CN (197 mg, 3.13 mmol). The mixture was stirred at 20 °C for 3 h. The reaction mixture was then concentrated in vacuo and the residue was purified by preparative HPLC (column: Waters Xbridge BEH C18 (100*30 mm*10 μm); mobile phase: [water (NH4HCO3)-ACN]; B%: 10-35%, 8 min) to give 2-(4- methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine (20.0 mg, 4% over 2 steps) as a white solid. 1 H NMR (400 MHz, CDCl3): ^ 7.24-7.26 (m, 1H), 6.99 (d, J = 8.4 Hz, 1H), 6.44 (d, J = 7.6 Hz, 1H), 3.96 (s, 1H), 3.28 (t, J = 8.0 Hz, 2H), 2.79 (t, J = 8.0 Hz, 2H), 2.38 (s, 6H). LCMS (ESI+): m/z 220.1 [M+H] + . HPLC Purity (220 nm): 98.5%. Step 7: 3-(2-(dimethylamino)ethyl)-1H-indazol-4-ol (P-56) To a solution of 2-(4-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine (70.0 mg, 0.32 mmol) in CS2 (1 mL) was added AlCl3 (297 mg, 2.23 mmol) and the mixture was stirred at 50 °C for 4 h. The reaction mixture was concentrated in vacuo then quenched with MeOH (30 mL) and concentrated again. The residue was purified by preparative HPLC (column: Phenomenex C18 (75*30 mm*3 µm); mobile phase: [water (NH 4 HCO 3 )-ACN]; B: 1-40%, 8 min) to afford 3-(2-(dimethylamino)ethyl)-1H-indazol-4- ol (9.4 mg, 14%) as a colourless oil. 1 H NMR (400 MHz, D2O): ^ 7.21 (t, J = 8.0 Hz, 1H), 6.79 (d, J = 8.4 Hz, 1H), 6.27 (d, J = 7.6 Hz, 1H), 3.29 - 3.34 (m, 4H), 2.72 (s, 6H). LCMS (ESI+): m/z 206.1 [M+H] + . HPLC Purity (220 nm): 96.0%. Example 37: 2-(1H-indazol-3-yl)-N,N-diethylethan-1-amine (P-43) Step 1: 2-(4-methoxy-1H-indazol-3-yl)-N,N-diethylethan-1-amine (P-42) To a solution of 2-(4-methoxy-1H-indazol-3-yl)ethan-1-amine (200 mg, 1.05 mmol) in MeOH (3 mL) at 0 °C was added a 40% w/w solution of aq. acetaldehyde (287 mg, 2.61 mmol), AcOH (251 mg, 4.18 mmol) and NaBH3CN (131 mg, 2.08 mmol). The mixture was stirred at 20 °C for 3 h. The reaction mixture was then concentrated in vacuo and the residue was purified by preparative HPLC (column: Waters Xbridge Prep OBD C18 (150*40 mm*10 μm); mobile phase: [water (NH4HCO3)-ACN]; B%: 10- 55%, 8 min) to give 2-(4-methoxy-1H-indazol-3-yl)-N,N-diethylethan-1-amine (26 mg, 8% over 2 steps) as a colourless oil. 1 H NMR (400 MHz, CDCl3): ^ 7.25-7.27 (m, 1H), 7.01 (d, J = 8.4 Hz, 1H), 6.45 (d, J = 7.6 Hz, 1H), 3.96 (s, 3H), 3.25-3.29 (m, 2H), 2.74 (q, J = 7.2 Hz, 4H), 2.97-3.01 (m, 2H), 1.15 (t, J = 6.8 Hz, 6H). LCMS (ESI+): m/z 248.1 [M+H] + . Step 2: 3-(2-(diethylamino)ethyl)-1H-indazol-4-ol (P-43) To a solution of 2-(4-methoxy-1H-indazol-3-yl)-N,N-diethylethan-1-amine (78.9 mg, 0.32 mmol) in CS2 (1 mL) was added AlCl3 (297 mg, 2.23 mmol). The mixture was stirred at 50 °C for 4 h at which point the reaction mixture was concentrated in vacuo then quenched with MeOH (30 mL) and concentrated again. The residue was purified by preparative HPLC (column: Phenomenex Luna C18 (75*30 mm*3 μm); mobile phase: [water (formic acid)-ACN]; B: 1-30%, 8 min) to afford 3-(2-(diethylamino)ethyl)- 1H-indazol-4-ol as a formate salt (12.2 mg, 16%) which was a colourless oil. 1 H NMR (400 MHz, MeOD-d4): ^ ).8.55 (br s, 1H), 7.18 (t, J = 7.6 Hz, 1H), 6.93 (d, J = 8.4 Hz, 1H), 6.43 (d, J = 7.6 Hz, 1H), 3.56 - 3.58 (m, 2H), 3.48 - 3.50 (m, 2H), 3.27 - 3.32 (m, 4H), 1.36 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 234.1 [M+H] + . HPLC Purity (220 nm): 95.6%. Example 38: 2-(1H-indazol-3-yl)-N,N-dipropylethan-1-amine (P-45) Step 1: 2-(4-methoxy-1H-indazol-3-yl)-N,N-dipropylethan-1-amine (P-44) To a solution of 2-(4-methoxy-1H-indazol-3-yl)ethan-1-amine (200 mg, 1.05 mmol) and propanal (151 mg, 2.60 mmol) in MeOH (2 mL) at 0 °C was added AcOH (251 mg, 4.18 mmol) and NaBH3CN (164 mg, 2.61 mmol) and the mixture was stirred at 20 °C for 3 h. The reaction mixture was then concentrated in vacuo and the residue was purified by preparative HPLC (column: Phenomenex Luna C18 (75*30 mm*3 μm); mobile phase: [water (formic acid)-ACN]; B: 1-30%, 8 min) to give the formate salt of 2-(4-methoxy-1H-indazol-3-yl)-N,N-dipropylethan-1-amine (20.0 mg, 5% over 2 steps) as a colourless oil. 1 H NMR (400 MHz, CDCl3): ^ 8.62 (s, 1H), 7.26 (t, J = 8.0 Hz, 1H), 7.03 (d, J = 8.4 Hz, 1H), 6.43 (d, J = 7.6 Hz, 1H), 3.94 (s, 3H), 3.34-3.40 (m, 4H), 2.93- 2.97 (m, 4H), 1.72-1.80 (m, 4H), 0.96 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 276.2 [M+H] + . HPLC Purity (220 nm): 96.4%. Step 2: 3-(2-(dipropylamino)ethyl)-1H-indazol-4-ol (P-45) To a solution of 2-(4-methoxy-1H-indazol-3-yl)-N,N-dipropylethan-1-amine (110 mg, 0.40 mmol) in CS 2 (22 mL) was added AlCl 3 (799 mg, 5.99 mmol) and the mixture was stirred at 50 °C under N2 for 2 h. The reaction mixture was concentrated in vacuo and then quenched with MeOH (30 mL) and concentrated again. The residue was purified by preparative HPLC (column: Phenomenex Luna C18 (75*30 mm*3 μm); mobile phase: [water (formic acid)-ACN]; B: 1-30%, 8 min) to afford the formate salt of 3-(2- (dipropylamino)ethyl)-1H-indazol-4-ol (21.3 mg, 20%) which was a white solid. 1 H NMR (400 MHz, CDCl3): ^ 7.23 (t, J = 7.6 Hz, 1H), 6.87 (d, J = 8.4 Hz, 1H), 6.52 (d, J = 7.6 Hz, 1H), 3.22-3.24 (m, 2H), 2.90-2.93 (m, 2H), 2.55-2.59 (m, 4H), 1.51-1.57 (m, 4H), 0.86 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 262.2 [M+H] + . HPLC Purity (220 nm): 97.0%. Example 39: 3-(2-(diisopropylamino)ethyl)-1H-indazol-4-ol (P-47) Step 1: N-isopropyl-N-(2-(4-methoxy-1H-indazol-3-yl)ethyl)propan-2-a mine (P-46) To a solution of 2-(4-methoxy-1H-indazol-3-yl)ethan-1-amine (300 mg, 1.57 mmol) in DCE (2 mL) was added NaBH(OAc)3 (1.20 g, 5.66 mmol) and acetone (227 mg, 3.91 mmol) and the mixture was stirred at 25 °C for 48 h.and the reaction mixture was concentrated in vacuo, then diluted with H2O (15 mL) and extracted with CH2Cl2 (30 mL × 3). The combined organic layers were washed with brine (20 mL), dried over anhydrous Na2SO4 and concentrated in vacuo. The residue was purified by preparative HPLC (column: Phenomenex C18 (75*30 mm*3 μm); mobile phase: [water (formic acid)-ACN]; B: 1-5%, 8 min) to give the formate salt of N-isopropyl-N-(2-(4-methoxy- 1H-indazol-3-yl)ethyl)propan-2-amine (17.6 mg, 3% over 2 steps) which was a white solid. 1 H NMR (400 MHz, CDCl3): ^ 8.70 (s, 1H), 7.24 - 7.26 (m, 1H), 7.30 (d, J = 8.4 Hz, 1H), 6.43 (d, J = 7.6 Hz, 1H), 3.94 (s, 3H), 3.62 - 3.67 (m, 2H), 3.50 - 3.54 (m, 2H), 3.21 - 3.26 (m, 2H), 1.40 (d, J = 6.4 Hz, 12H). LCMS (ESI+): m/z 276.2 [M+H] + . HPLC Purity (220 nm): 96.0%. Step 2: 3-(2-(diisopropylamino)ethyl)-1H-indazol-4-ol (P-47) To a solution of N-isopropyl-N-(2-(4-methoxy-1H-indazol-3-yl)ethyl)propan-2-a mine (50.0 mg, 0.18 mmol) in CS2 (1 mL) was added AlCl3 (169 mg, 1.27 mmol) and the mixture was stirred at 50 °C for 4 h The reaction mixture was concentrated in vacuo and then quenched with MeOH (30 mL) and concentrated again. The residue was purified by preparative HPLC (column: Waters Xbridge Prep OBD C18 (150*40 mm*10 μm); mobile phase: [water (NH4HCO3)-ACN]; B: 10-55%, 8 min) to afford 3-(2- (diisopropylamino)ethyl)-1H-indazol-4-ol (14 mg, 34%) as a brown solid. 1 H NMR (400 MHz, D2O): ^ 7.23-7.27 (m, 1H), 6.89 (d, J = 8.4 Hz, 1H), 6.38 (d, J = 7.6 Hz, 1H), 3.65- 3.72 (m, 2H), 3.42 (s, 4H), 1.26 (d, J = 6.8 Hz, 6H). LCMS (ESI+): m/z 262.2 [M+H] + . HPLC Purity (220 nm): 96.6%. Scheme 13: Compounds of general formula (I) can be synthesised from the appropriately substituted indazole following the outlined sequence of steps in Scheme 13 or similar as one skilled in the art may consider. Under nitrosation conditions, indoles readily convert to indazoles such as intermediate 24, subsequent Henry reaction with nitromethane provides access to nitroalkene 25. Reduction of the nitroalkene gives rise to the alkylamine 26, subsequent reductive alkylation provides compounds of general structure (I), exemplified by P-8. It is not outside the scope of this application that one skilled in the art could protect the amine with a suitable protecting group such as a benzyl or carbamate, subject the protected amine to alkylation with an electrophile followed by subsequent deprotection to give rise to a secondary amine, which then can be subjected to a second alkylation with a different electrophile to give rise to compounds of general structure (I), by which the alkylamine contains alkyl groups that are dissimilar (general structure (I)). Suitable protecting groups are described in Wuts, P. G. M. and Greene, T. W. ‘Greene’s Protective Groups in Organic Synthesis’ (4 th Ed.) 2006, John Wiley & Sons, Inc., Hoboken, new Jersey, USA.

Example 41: 2-(5-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine (P-8) Step 1: 5-methoxy-1H-indazole-3-carbaldehyde (24) To a solution of starting 5-methoxy-1H-indole (4.00 g, 27.1 mmol) in H2O (20 mL) and THF (7 mL) was added NaNO2 (9.38 g, 135 mmol) and 1 M aqueous HCl (135 mL). The mixture was stirred at 25 °C for 12 h. The reaction mixture was extracted with EtOAc (20 mL × 3). The combined organic layers were dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was triturated with CH2Cl2:petroleum ether (v/v 5:1) at 20 °C for 20 min to give 5-methoxy-1H-indazole-3-carbaldehyde (5.70 g) as an off-white solid that was used immediately in the next step. LCMS (ESI+): m/z 177.1 [M+H] + . Step 2: (E)-5-methoxy-3-(2-nitrovinyl)-1H-indazole (25) To a solution of 5-methoxy-1H-indazole-3-carbaldehyde (4.50 g, 25.5 mmol) was added NH4OAc (393 mg, 5.11 mmol) and nitromethane (71 mL). The mixture was stirred at 60 °C for 16 h. The reaction mixture was concentrated in vacuo, the residue was diluted with H2O (20 mL), and then extracted with EtOAc (20 mL × 3). The combined organic layers were dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to give (E)-5-methoxy-3-(2-nitrovinyl)-1H-indazole (4.00 g) as a brown solid which was used immediately in the next step. Step 3: 2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (26) To a suspension of LiAlH4 (2.08 g, 54.7 mmol) in THF (20 mL) was added (E)-5-methoxy- 3-(2-nitrovinyl)-1H-indazole (2.00 g, 9.12 mmol) in THF (10 mL) at 0 °C. The mixture was then stirred at 25 °C for 20 h before being cooled to 0 °C and quenched by dropwise addition H2O (20 mL). The mixture was then extracted with EtOAc (20 mL × 3) and the combined organics washed with brine (1 x 50 mL) before being dried Na2SO4, filtered, and the filtrate concentrated in vacuo to give 2-(5-methoxy-1H-indazol-3-yl)ethan-1- amine (1.40 g, crude) as a white solid that was subjected to alkylation conditions below. LCMS (ESI+): m/z 192.0 [M+H] + . Step 4: 2-(5-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine (P-8) To an ice cold solution of crude 2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (2.00 g) in MeOH (10 mL) was added AcOH (2.51 g, 41.8 mmol) to adjust the pH to 4, followed by the addition of NaBH3CN (1.31 g, 20.9 mmol) and 37% w/w aqueous formaldehyde (2.12 g, 26.1 mmol). The mixture was stirred at 20 °C for 1 h before being concentrated in vacuo and the residue generated was purified by preparative HPLC (column: Phenomenex C1880*40 mm*3 μm; mobile phase: [water (formic acid)-ACN]; B: 5- 35%, 8 min). The collected material was further purified by preparative HPLC (column: Phenomenex Luna C18200*40 mm*10 μm; mobile phase: [water (formic acid)-ACN]; B: 1-20%, 8 min) to give the formate salt of 2-(5-methoxy-1H-indazol-3-yl)-N,N- dimethylethan-1-amine as a white solid (134 mg). 1 H NMR (400 MHz, DMSO-d 6 ): ^ 8.24 (s, 1H), 7.36 (d, J = 8.8 Hz, 1H), 7.14 (d, J = 2.4 Hz, 1H), 6.97 (dd, J = 8.8, 2.4 Hz, 1H), 3.80 (s, 3H), 3.00 – 3.09 (m, 2H), 2.74 - 2.83 (m, 2H), 2.32 (s, 6H). LCMS (ESI+): m/z 220.1 [M+H] + . HPLC Purity (220 nm): 97.9%. Step 4a: 2-(5-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1-amine bis-hydrochloride (P-8·2HCl) To an ice cold (0 °C) solution of 2-(5-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1- amine (100 mg, 0.45 mmol) in anhydrous Et2O (5 mL) and abs. EtOH (1 mL) was added 2 M HCl in Et2O dropwise over 10 min until the pH of the reaction solution was acidic. The resulting precipitate was collected by filtration and dried overnight in a vacuum desiccator to afford 2-(5-methoxy-1H-indazol-3-yl)-N,N-dimethylethan-1- amine as the dihydrochloride salt (78 mg, 59%) which was a white solid. 1 H NMR (400 MHz, DMSO-d6): ^ 10.83 (s, 1H), 7.44 – 7.36 (m, 1H), 7.28 (d, J = 2.0 Hz, 1H), 7.01 (dd, J = 9.0, 2.4 Hz, 1H), 3.81 (s, 3H), 3.55 – 3.28 (m, 4H), 2.84 (d, J = 4.8 Hz, 6H). qNMR Purity (ERETIC): 98.8%. Scheme 14: Compounds of general formula (I) can be synthesised from the appropriately substituted formyl-aza-indole following the outlined sequence of steps in Scheme 14 or similar as one skilled in the art may consider. Addition of SEM protecting group to formyl-aza-indole starting material 24 allows access to intermediate 82. Reaction of intermediate 82 with nitromethane yields intermediate 83 which can be converted to the nitrostyrene 84. Chemoselective reduction with LiAlH4 allows access to the primary amine 85 which permits tertiary amine synthesis using an appropriate aldehyde and reducing agent affording intermediate 86. Final removal of the SEM protecting group provides compounds of general formula (I) (exemplified by P-48). One skilled in the art will recognise that utilising different aldehydes would allow access to compounds of general formula (I) disclosed herein.

Step 1: 5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 -carbaldehyde (82) To a solution of 5-methoxy-1H-indazole-3-carbaldehyde (15.0 g, 85.2 mmol) and DIPEA (17.6 g, 136.2 mmol) in DMF (150 mL) was added (2- (chloromethoxy)ethyl)trimethylsilane (17.0 g, 102.0 mmol) and the mixture was stirred at ambient temperature for 2 h. The reaction mixture was quenched with H2O (300 mL) and then extracted with EtOAc (150 x 3 mL). The combined organics were filtered, dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (EtOAc in Petroleum ether, 2–5% v/v) to provide 5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 -carbaldehyde (11.4 g, 44%) as a yellow solid. 1 H NMR (300 MHz, CDCl3): ^ 1 H NMR (300 MHz, CDCl3) δ 10.23 (s, 1H), 7.65 (d, J = 2.4 Hz, 1H), 7.53 (d, J = 9.3 Hz, 1H), 7.15 (dd, J = 9.1, 2.4 Hz, 1H), 5.78 (s, 2H), 3.90 (s, 3H), 3.56 (t, J = 8.2 Hz, 2H), 0.89 (t, J = 8.2 Hz, 2H), - 0.07 (s, 9H). Step 2: 1-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3-yl)-2- nitroethan-1-ol (83) To a solution of 5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3 - carbaldehyde (8.60 g, 28.1 mmol) and KO t Bu (915 mg, 8.15 mmol) in t BuOH (50 mL) and 1,4-dioxane (50 mL) was added nitromethane (4.98 g, 81.6 mmol) and the mixture was stirred at ambient temperature for 5 h. The reaction was quenched with H2O (200 mL) and then extracted with EtOAc (100 mL × 3). The combined organic layers were washed with brine (150 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo to provide crude 1-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)-2-nitroethan -1-ol (11.4 g) as a yellow oil which was used in the subsequent step without further purification. Step 3: (E)-5-methoxy-3-(2-nitrovinyl)-1-((2-(trimethylsilyl)ethoxy) methyl)-1H-indazole (84) To a solution of crude 1-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3- yl)-2-nitroethan-1-ol (6.69 g) in CH2Cl2 (80 mL) was added N,N-dimethylpyridin-4- amine (100 mg, 0.82 mmol) followed by acetic anhydride (2.22 g, 21.7 mmol) and the mixture was stirred at ambient temperature for 1 h. The reaction was quenched with H2O (200 mL) and then extracted with CH2Cl2 (100 mL × 3). The combined organics were washed with brine (100 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was partially purified by flash chromatography (Petroleum ether/EtOAc, v/v, 50/1 to 20/1) to afford crude (E)-5-methoxy-3-(2- nitrovinyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (4.00 g) as a yellow solid which was used in the subsequent step without further purification. Step 4: 2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3-yl)ethan-1- amine (85) To an ice cold solution of crude (E)-5-methoxy-3-(2-nitrovinyl)-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-indazole (4.00 g) in anhydrous THF (150 mL) was added LiAlH 4 (1.76 g, 46.4 mmol) portionwise and stirring continued at this temperature for 1 h. The reaction was quenched by sequential addition of H2O (1.76 mL), NaOH (1.76 mL, 15% aq. soln.), H2O (5.28 mL) and filtered through a pad of celite. The filtrate was concentrated in vacuo and the residue was partially purified by flash chromatography (MeOH in EtOAc, 0% to 10% v/v) to provide 2-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)ethan-1-amine (1.32 g, 15% over 3 steps) as a yellow oil. 1 H NMR (300 MHz, CDCl3) δ 7.37 (d, J = 9.0 Hz, 2H), 7.06 (dd, J = 9.0, 2.2 Hz, 2H), 6.99 (d, J = 2.3 Hz, 2H), 5.59 (s, 2H), 3.83 (s, 3H), 3.51 (m, 4H), 3.37 (t, J = 6.4 Hz, 2H), 0.81-0.92 (m, 2H), -0.08 (s, 9H). LCMS (ESI+): m/z 322.2 [M+H] + . Step 5: N,N-diethyl-2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl )-1H-indazol-3- yl)ethan-1-amine (86) To a solution of 2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3- yl)ethan-1-amine (150 mg, 0.47 mmol), DIPEA (242 mg, 1.87 mmol) and acetaldehyde (62.0 mg, 1.41 mmol) in CH2Cl2 (10 mL) was added NaBH(OAc)3 (549 mg, 2.59 mmol) in portions which was then stirred at ambient temperature for 16 h. The reaction was quenched with H2O (50 mL) and then extracted with CH2Cl2 (20 mL × 3). The combined organics were washed with brine (20 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was partially purified by preparative thin layer chromatography (CH2Cl2:MeOH, 10:1, v/v) to afford crude N,N-diethyl-2-(5- methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl )ethan-1-amine (137 mg) as a colourless oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 378.3 [M+H] + . Step 6: N,N-diethyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (P-48) To a solution of crude N,N-diethyl-2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl )- 1H-indazol-3-yl)ethan-1-amine (160 mg) in CH2Cl2 (5 mL) was added TFA (10 mL) which was then stirred at ambient temperature for 1 h. The reaction was then quenched with saturated aqueous Na2CO3 solution (30 mL) and then extracted with CH2Cl2 (15 mL × 3). The combined organic layers were washed with brine (20 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was dissolved in MeOH (5 mL) before addition of aqueous NH3 (10 mL) and was then stirred at 50 °C for 1 h. The reaction was concentrated in vacuo and the residue was purified by preparative thin layer chromatography (CH 2 Cl 2 :MeOH, 10:1, v/v) to obtain crude N,N- diethyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (21.0 mg) as a colourless oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 248.3 [M+H] + . Step 7: N,N-diethyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine bis-hydrochloride (P- 48·2HCl) To a solution of crude N,N-diethyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (21 mg) in MeOH (0.5 mL) was added HCl (4 M in Et2O) until the reaction solution was acidic. Stirring was continued at ambient temperature for 30 min. The reaction was concentrated in vacuo and the solid residue was triturated with Et2O to afford N,N-diethyl-2-(5-methoxy- 1H-indazol-3-yl)ethan-1-amine as the dihydrochloride salt (18.4 mg, 12% over 3 steps) which was an off-white solid. 1 H NMR (300 MHz, MeOD-d 4 ): δ 7.44 (d, J = 9.0 Hz, 1H), 7.21 (s, 1H), 7.12 (d, J = 9.0 Hz, 1H), 3.87 (s, 3H), 3.64 (t, J = 7.2 Hz, 2H), 3.33-3.48 (m, 6H), 1.37 (t, J = 7.2 Hz, 6H). LCMS (ESI+): m/z 248.2 [M+H] + . HPLC Purity (254 nm): 97.5%. Example 43: N,N-dipropyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (P-49) Step 1: N-(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-inda zol-3-yl)ethyl)-N- propylpropan-1-amine (87) To a solution of 2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3- yl)ethan-1-amine (150 mg, 0.47 mmol), DIPEA (242 mg, 1.87 mmol) and propanal (68.0 mg, 1.17 mmol) in CH2Cl2 (10 mL) was added NaBH(OAc)3 (594 mg, 2.80 mmol) in portions and the reaction mixture was stirred at ambient temperature for 16 h. The reaction was quenched with H2O (50 mL) and then extracted with CH2Cl2 (20 mL × 3). The combined organic layers were washed with brine (20 mL × 2), dried over Na 2 SO 4 , filtered, and the filtrate concentrated under reduced pressure. The residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH, 20:1, v/v) to afford crude N- (2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazo l-3-yl)ethyl)-N- propylpropan-1-amine (120 mg) as a light yellow oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 406.3 [M+H] + . Step 2: N,N-dipropyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (P-49) To a solution of crude N-(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-inda zol- 3-yl)ethyl)-N-propylpropan-1-amine (120 mg) in CH2Cl2 (5 mL) was added TFA (10 mL) and the reaction mixture was stirred at ambient temperature for 1 h. The reaction mixture was quenched with saturated aqueous Na2CO3 solution (30 mL) and extracted with CH2Cl2 (15 mL × 3). The combined organic layer was washed with brine (20 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The residue obtained was dissolved in MeOH (5 mL) stirred at 50 °C for 1 h after addition of aqueous NH3 solution (10 mL). The mixture was concentrated under reduced pressure and the residue was purified by preparative thin layer chromatography (CH2Cl2:MeOH, 10:1, v/v) to afford crude N,N-dipropyl-2-(5-methoxy- 1H-indazol-3-yl)ethan-1-amine (24.0 mg) as a colourless oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 276.2 [M+H] + . Step 3: N,N-dipropyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine bis-hydrochloride (P-49·2HCl) Crude N,N-dipropyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine (24.0 mg) was dissolved in MeOH (0.5 mL) and then added to solution of 2 M HCl in Et2O (2 mL) at ambient temperature. The mixture was stirred at ambient temperature for 30 min and then concentrated under reduced pressure. The solid residue was washed with Et2O to provide N,N-dipropyl-2-(5-methoxy-1H-indazol-3-yl)ethan-1-amine as the dihydrochloride salt (27.0 mg, 17% over 3 steps) as an off-white solid. 1 H NMR (300 MHz, MeOD-d4): δ 7.42 (d, J = 9.1 Hz, 1H), 7.19 (d, J = 2.2 Hz, 1H), 7.10 (dd, J = 9.0, 2.2 Hz, 1H), 3.85 (s, 3H), 3.64 (t, J = 7.3 Hz, 2H), 3.43 (t, J = 7.4f Hz, 2H), 3.19-3.25 (m, 4H), 1.78 (sext, J = 8.0 Hz, 4H), 1.01 (t, J = 7.3 Hz, 6H). LCMS (ESI+): m/z 276.4 [M+H] + . HPLC Purity (254 nm): 95.4%. Example 45: N-ethyl-2-(5-methoxy-1H-indazol-3-yl)-N-methylethan-1-amine (P- 51): Step 1: tert-butyl (2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazo l-3- yl)ethyl)carbamate (89) To a solution of 2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3- yl)ethan-1-amine (200 mg, 0.62 mmol) and Et3N (126 mg, 1.25 mmol) in THF (20 mL) was added di-tert-butyl dicarbonate (204 mg, 0.94 mmol) and the mixture was stirred at ambient temperature for 2 h. The reaction was quenched with H2O (50 mL) and then extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (30 mL × 2), dried over anhydrous Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The crude product was purified by flash chromatography (SiO2, petroleum ether:EtOAc, v/v, 10:1 to 4:1) to obtain crude tert-butyl (2-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)ethyl)carbama te (197 mg) as a light yellow oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 422.2 [M+H] + . Step 2: tert-butyl ethyl(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-i ndazol-3- yl)ethyl)carbamate (90) To a solution of crude tert-butyl (2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H- indazol-3-yl)ethyl)carbamate (197 mg) dissolved in DMF (8 mL), was added sodium hydride (23.0 mg, 0.96 mmol) at 0 °C. The reaction mixture was stirred at 0 °C for 30 min and then iodoethane (88.0 mg, 0.56 mmol) was added and the mixture was stirred for another 2 h. The reaction mixture was quenched with saturated aq. NH4Cl (20 mL) solution and then extracted with EtOAc (20 mL × 3). The combined organic layers were washed with brine (20 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The crude product was purified by flash chromatography (SiO2, petroleum ether:EtOAc, v/v, 10:1 to 4:1) to provide tert-butyl ethyl(2-(5-methoxy- 1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)ethyl)c arbamate (160 mg) as a light yellow oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 450.4 [M+H] + . Step 3: N-ethyl-2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H -indazol-3-yl)-N- methylethan-1-amine (91) To a solution of crude tert-butyl ethyl(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)- 1H-indazol-3-yl)ethyl)carbamate (160 mg) in THF (10 mL) was added LiAlH4 (41.0 mg, 1.08 mmol) at ambient temperature and the mixture was stirred at 50 °C for 3 h. The reaction was quenched with saturated NH4Cl solution (20 mL) and extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (20 mL), dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The crude product was purified by flash chromatography (SiO2, CH2Cl2:MeOH, v/v, 50:1 to 20:1) to give N-ethyl-2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H -indazol-3-yl)-N- methylethan-1-amine (102 mg) as a light yellow oil which was used in the subsequent step without further purification. LCMS (ESI+): m/z 364.3 [M+H] + . Step 4: N-ethyl-2-(5-methoxy-1H-indazol-3-yl)-N-methylethan-1-amine (P-51) To a solution of crude N-ethyl-2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H - indazol-3-yl)-N-methylethan-1-amine (155 mg, 426 µmol) in THF (6 mL) at 0 °C was added 37% aqeuous HCl (3 mL) and the reaction mixture was stirred at ambient temperature overnight. The reaction was quenched with saturated NaHCO3 (30 mL) and then extracted with EtOAc (20 mL × 3). The combined organics were washed with brine (20 mL × 2), dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The residue was then purified by preparative thin layer chromatography (CH2Cl2:MeOH:NH3(aq.), 100:10:1) to provide N-ethyl-2-(5-methoxy- 1H-indazol-3-yl)-N-methylethan-1-amine (40.6 mg, 28% over 4 steps) as a white solid. 1 H NMR (300 MHz, MeOD-d4): δ 7.35 (d, J = 9.1 Hz, 1H), 7.10 (d, J = 2.0 Hz, 1H), 7.02 (dd, J = 9.0, 2.2 Hz, 1H), 3.83 (s, 3H), 3.10-3.16 (m, 2H), 2.82-2.88 (m, 2H), 2.61 (q, J = 7.3 Hz, 2H), 2.38 (s, 3H), 1.12 (t, J = 7.2 Hz, 3H). LCMS (ESI+): m/z 234.3 [M+H] + . HPLC Purity (254 nm): 99.8%. Example 46: N-(2-(5-methoxy-1H-indazol-3-yl)ethyl)-N-methylpropan-2-amin e (P- 52): Step 1: N-(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-inda zol-3-yl)ethyl)-N- methylpropan-2-amine (92) To a solution of 2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol -3- yl)ethan-1-amine (100 mg, 0.31 mmol), acetone (36.1 mg, 0.62 mmol) and DIPEA (121 mg, 0.94 mmol) in CH2Cl2 (5 mL) was added NaBH(OAc)3 (132 mg, 0.62 mmol) in portions and the mixture was stirred at ambient temperature for 16 h. To this was added formaldehyde (37% w/w aq. solution, 51.4 mg, 0.63 mmol) and NaBH(OAc)3 (132 mg, 0.62 mmol) and the mixture was stirred for another 4 h at ambient temperature. The reaction was quenched with H2O (30 mL) and extracted with CH2Cl2 (15 mL × 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude product was purified by preparative thin layer chromatography (CH2Cl2:MeOH, 10:1, v/v) to afford N-(2-(5-methoxy-1-((2- (trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)ethyl)-N-meth ylpropan-2-amine (105 mg) as a yellow oil which was used in the subsequent step without further purification. Step 2: N-(2-(5-methoxy-1H-indazol-3-yl)ethyl)-N-methylpropan-2-amin e bis- hydrochloride (P-52·2HCl). To a stirred solution of crude N-(2-(5-methoxy-1-((2-(trimethylsilyl)ethoxy)methyl)-1H- indazol-3-yl)ethyl)-N-methylpropan-2-amine (170 mg) in THF (6 mL) was added HCl (37% v/v aq. solution, 1.5 mL) and the reaction mixture was stirred at ambient temperature for 1 h. The reaction was concentrated under reduced pressure and the resulting residue was dissolved in MeOH (5 mL). To this was added aqueous NH3 solution (10 mL) which was then stirred at ambient temperature for 2 h. The mixture was concentrated under reduced pressure and the residue subjected to preparative thin layer chromatography (CH2Cl2:MeOH, 10:1, v/v) to provide crude N-(2-(5- methoxy-1H-indazol-3-yl)ethyl)-N-methylpropan-2-amine (65.0 mg) as a white solid. The impure free base was dissolved in MeOH (1 mL) and added to a solution of 2 M HCl in Et2O (1 mL) which was then stirred at ambient temperature for 30 min. After concentrating the mixture, the residue was purified by preparative HPLC (column: YMC-Pack ODS-A C18 (250*20 mm*5 μm); mobile phase: [water-MeOH]; B: 20-90% 40 min) to afford N-(2-(5-methoxy-1H-indazol-3-yl)ethyl)-N-methylpropan-2-amin e as the dihydrochloride salt (20.0 mg, 20% over 2 steps). 1 H NMR (300 MHz, MeOD-d4): ^ 7.41 (d, J = 6.9 Hz, 1H), 7.21 (s, 1H), 7.07 (d, J = 6.9 Hz, 1H), 3.86 (s, 3H), 3.75 – 3.85 (m, 1H), 3.38 - 3.50 (m, 3H), 2.89 (s, 3H), 1.39 (d, J = 6.3 Hz, 6H). LCMS (ESI+): m/z 248.3 [M+H] + . HPLC Purity (254 nm): 99.9%. Scheme 15: Compounds of general formula (I) can be synthesised from the appropriately substituted hydroxyacetophenone following the outlined sequence of steps in Scheme 15 or similar as one skilled in the art may consider. Conversion of hydroxyacetophenone to 5-hydroxycoumarin by the use of diethylcarbonate followed by subsequent rearrangement provides the appropriate benzo[d]isoxazoles. Standard amidation processes allow for the formation of the required dialkylamide which can be converted to compounds of general structure (I) exemplified by P-9. It is not outside the scope of this application that one skilled in the art could utilise various amines that would give rise to compounds of general structure (I), by which the alkylamine contains alkyl groups that are dissimilar (general structure (I)).

Example 47: 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylethan-1-amine (P- 9): Step 1: 4-hydroxy-6-methoxy-2H-chromen-2-one (28) To a solution of 1-(2-hydroxy-5-methoxyphenyl)ethan-1-one (3.00 g, 18.07 mmol) in toluene (60 mL) was added sodium hydride (60% w/w in mineral oil, 2.89 g, 72.3 mmol) at 0 °C, followed by diethyl carbonate (21.6 g, 182.84 mmol). The reaction mixture was stirred at 110 °C for 16 h. The reaction mixture was quenched with H2O (300 mL), the resulting layers of the biphasic mixture were separated, and the aqueous phase was washed with EtOAc (150 mL × 2). Then the aqueous phase was adjusted pH to 3 with 12 N aqueous HCl and extracted with EtOAc (200 mL × 2). The combined organic layers from the acidified extraction were dried over Na2SO4, filtered and the filtrate concentrated under reduced pressure to provide 4-hydroxy-6-methoxy-2H- chromen-2-one (3.20 g, 92%) as a white solid. 1 H NMR (300 MHz, DMSO-d6): δ 12.52 (br s, 1H), 7.51 - 7.11 (m, 3H), 5.60 (s, 1H), 3.82 (s, 3H). Step 2: 2-(5-methoxybenzo[d]isoxazol-3-yl)acetic acid (29) To a solution of 4-hydroxy-6-methoxy-2H-chromen-2-one (3.56 g, 18.5 mmol) in EtOH (60 mL) was added hydroxylamine hydrochloride (3.87 g, 55.6 mmol) and NaOAc (6.08 g, 74.2 mmol). The reaction was stirred under reflux for 16 h. The reaction mixture was adjusted to pH 4 with 2 M aqueous HCl and the solvent was removed in vacuo. H2O (100 mL) was added to the resulting mixture and then extracted with EtOAc (80 mL × 3). The combined organic layers were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure to provide 2-(5- methoxybenzo[d]isoxazol-3-yl)acetic acid (3.8 g, 99%) as a yellow solid. 1 H NMR (300 MHz, DMSO-d6): δ 12.80 (br s, 1H), 7.63 (d, J = 9.0 Hz, 1H), 7.32 - 7.23 (m, 2H), 4.06 (s, 2H), 3.81 (s, 3H). Step 3: 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylacetamide (30) To a solution of 2-(5-methoxybenzo[d]isoxazol-3-yl)acetic acid (3.66 g, 17.7 mmol) in CH2Cl2 (80 mL) was added CDI (5.73 g, 35.4 mmol). The reaction was stirred at ambient temperature for 2 h and then Me2NH.HCl (2.88 g, 35.4 mmol) was added. The reaction mixture was stirred at ambient temperature for 4 h before saturated aqueous NH4Cl (20 mL) was added. The layers were separated, and the aqueous phase was extracted with EtOAc (20 mL × 3). The combined organics were dried over Na2SO4, filtered, and the filtrate concentrated in vacuo. The resulting residue was purified by flash chromatography (SiO2, 100% EtOAc) to provide 2-(5-methoxybenzo[d]isoxazol- 3-yl)-N,N-dimethylacetamide (1.34 g, 32%) as a white solid. 1 H NMR (300 MHz, CDCl3): δ 7.45 (d, J = 9.0 Hz, 1H), 7.27 – 7.14 (m, 2H), 4.07 (s, 2H), 3.87 (s, 3H), 3.15 (s, 3H), 2.98 (s, 3H). Step 4: 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylethan-1-amine (P-9) To a solution of 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylacetamide ( g, 4.7 mmol) in anhydrous THF (22 mL) was added LiAlH4 (0.36 g, 9.4 mmol) at 0 °C and the reaction was stirred at ambient temperature for 3 h. The resulting mixture was quenched with H2O (0.36 mL), 15% aqueous NaOH solution (0.36 mL) and H2O (1.08 mL), followed by addition of MgSO 4 and EtOAc. The mixture was stirred at ambient temperature for 30 min and filtered through a pad of celite. The filtrate was concentrated and the resulting residue was purified by flash chromatography (SiO2, CH2Cl2/MeOH, v/v, 95/5) to provide 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N- dimethylethan-1-amine (403 mg, 33%) as a yellow oil. 1 H NMR (300 MHz, CDCl3) δ 7.44 (d, J = 9.0 Hz, 1H), 7.15 (dd, J = 9.0, 2.4 Hz, 1H), 7.02 (d, J = 2.4 Hz, 1H), 3.86 (s, 3H), 3.22 – 3.04 (m, 2H), 2.92 – 2.73 (m, 2H), 2.35 (s, 6H). Step 5: 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylethan-1- amine hydrochloride (P-9·HCl) To a solution of 2-(5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylethan-1-amine (150 mg, 0.68 mmol) in Et2O (2 mL) was added HCl/Et2O (3 mL) until the reaction solution pH was acidic. The reaction was stirred at ambient temperature for 3 h and then concentrated in vacuo. The solid residue was washed with Et2O (3 mL × 3) to afford 2- (5-methoxybenzo[d]isoxazol-3-yl)-N,N-dimethylethan-1-amine as the hydrochloride salt (110 mg, 63%) which was a white solid. 1 H NMR (300 MHz, MeOD-d4): δ 7.54 (d, J = 9.0 Hz, 1H), 7.34 – 7.24 (m, 2H), 3.90 (s, 3H), 3.74 (t, J = 7.2 Hz, 2H), 3.52 (t, J = 7.2 Hz, 2H), 3.02 (s, 6H). LCMS (ESI+): m/z 221.2 [M+H]+. HPLC Purity (220 nm): 99.3%. Scheme 16: Compounds of general formula (I) can be synthesised from the appropriately substituted pyrazolopyridine following the outlined sequence of steps in Scheme 16 or similar as one skilled in the art may consider. A similar sequence of synthetic transformations as outlined in Scheme 10 proved to be a viable method of accessing compounds of general formula (I). Formylation of pyrazolopyridine 94 provides access to intermediate 95 which can be further derivatised to the nitrostyrene 96 via a Henry reaction. Reduction allows access to intermediate 97 bearing a primary amine which in the presence of an appropriate aldehyde and reducing agent, can be alkylated to provide compounds of general formula (I) (exemplified by P-54). One skilled in the art will recognise that utilising alternative aldehydes or ketones would allow access to compounds of general formula (I) disclosed herein.

Example 48: 2-(5-methoxypyrazolo[1,5-a]pyridin-3-yl)-N,N-dimethylethan-1 - amine (P-54) Step 1: 5-methoxypyrazolo[1,5-a]pyridine-3-carbaldehyde (95) To a solution of POCl3 (2.79 g, 18.1 mmol) in DMF (7 mL) was added 5- methoxypyrazolo[1,5-a]pyridine (900 mg, 6.07 mmol) in DMF (2 mL) dropwise at 0 °C. The mixture was stirred at 20 °C for 2 h, cooled to 0 °C, and diluted with H2O (10 mL). The pH was adjusted to 7 with 2 M aqueous NaOH and then the product was extracted with CH 2 Cl 2 (10 mL × 3). The combined organic layers were dried over Na 2 SO 4 , filtered, and the filtrate concentrated under reduced pressure to afford crude 5- methoxypyrazolo[1,5-a]pyridine-3-carbaldehyde (850 mg) as a pink solid. LCMS (ESI+): m/z 177.2 [M+H] + . Step 2: (E)-5-methoxy-3-(2-nitrovinyl)pyrazolo[1,5-a]pyridine (96) A mixture of crude 5-methoxypyrazolo[1,5-a]pyridine-3-carbaldehyde (850 mg), nitromethane (17 mL, 317 mmol) and NH4OAc (1.00 g, 13.0 mmol) was degassed and purged with N2 three times. Stirring was continued at 60 °C for 6 h under N2 and then the reaction mixture was filtered and the solid was washed with CH2Cl2 (15 mL). The solid was then dried under reduced pressure to afford (E)-5-methoxy-3-(2- nitrovinyl)pyrazolo[1,5-a]pyridine (840 mg, 57% over 2 steps) as a yellow solid. 1 H NMR (400 MHz, CDCl3): δ 8.38 (d, J = 7.2 Hz, 1H), 8.25 (d, J = 13.6 Hz, 1H), 8.15 (s, 1H), 7.56 (d, J = 13.6 Hz, 1H), 6.91 (s, 1H), 6.69 (d, J = 6.8 Hz, 1H) 3.99 (s, 3H). LCMS (ESI+): m/z 220.2 [M+H] + . Step 3: 2-(5-methoxypyrazolo[1,5-a]pyridin-3-yl)ethan-1-amine (97) To a solution of LiAlH4 (1.61 g, 42.4 mmol) in THF (3 mL) was added (E)-5-methoxy- 3-(2-nitrovinyl)pyrazolo[1,5-a]pyridine (840 mg, 3.83 mmol) in THF (3 mL) dropwise at 0 °C. The mixture was stirred at 20 °C for 1.5 h and then quenched by addition of Na2SO4.10H2O at 0 °C. The mixture was then filtered and washed through with CH2Cl2 (15 mL) and then concentrated under reduced pressure to give 2-(5- methoxypyrazolo[1,5-a]pyridin-3-yl)ethan-1-amine (450 mg, 62%) as a yellow solid. 1 H NMR (400 MHz, CDCl3): δ 8.24 (d, J = 7.6 Hz, 1H), 7.75 (s, 1H), 6.65 (d, J = 2.4 Hz, 1H), 6.42 (dd, J = 7.6, 2.8 Hz, 1H), 3.86 (s, 3H), 3.00 (t, J = 6.8, 2H), 2.83 (t, J = 6.8, 2H). LCMS (ESI+): m/z 192.1 [M+H] + . Step 4: 2-(5-methoxypyrazolo[1,5-a]pyridin-3-yl)-N,N-dimethylethan-1 -amine (P-54) To a solution of 2-(5-methoxypyrazolo[1,5-a]pyridin-3-yl)ethan-1-amine (450 mg, 2.35 mmol) in MeOH (3 mL) and Et3N (1.64 mL, 11.8 mmol) was added 37% w/w formaldehyde (573 mg, 7.06 mmol) dropwise. The mixture was then cooled to 0 °C and NaBH(OAc)3 (2.49 g, 11.8 mmol) was added. The mixture was stirred at 20 °C for 3 h at which point LCMS showed 89% product conversion. The reaction mixture was diluted with H2O (5 mL) and the product extracted with CH2Cl2 (5 mL × 3). The combined organics were washed with brine (10 mL), dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The residue was purified by preparative HPLC (column: Waters Xbridge BEH C18 (150*40 mm*10 μm); mobile phase: [water (NH 4 HCO 3 )-ACN]; B: 1-25% 8 min) to afford 2-(5-methoxypyrazolo[1,5- a]pyridin-3-yl)-N,N-dimethylethan-1-amine (8.94 mg, 2%) as a colourless oil. 1 H NMR (400 MHz, CDCl3): ^ 8.22 (d, J = 7.6 Hz, 1H), 7.73 (s, 1H), 6.63 (d, J = 2.4 Hz, 1H), 6.40 (dd, J = 7.6, 2.8 Hz, 1H), 3.85 (s, 3H), 2.85 - 2.81 (m, 2H), 2.57 - 2.53 (m, 2H), 2.34 (s, 6H). LCMS (ESI+): m/z 220.2 [M+H] + . HPLC Purity (220 nm): 94.4%. Functional assays 5-HT2A, 5-HT2B AND 5-HT2C receptors Activity at 5-HT2A, 5-HT2B and 5-HT2C receptors was determined using a FLIPR Ca2+ flux assay at WuXi AppTec Co. Ltd. (Hong Kong) Discovery Biology Unit according to their standard protocols. Briefly, stably transfected cells expressing the receptor of interest (HEK293 for 5-HT2A and 5-HT2C; CHO-K1 for 5-HT2B) were grown and plated in a 384 well plate and incubated at 37 °C and 5% CO2 overnight. A 250 mM stock solution of probenecid in FLIPR calcium assay buffer (10 mL) was freshly prepared and combined with a fluorescent dye (Fluo-4 Direct) to give a final assay concentration of 2.5 mM. Reference compounds were 4-fold serially diluted and the screening compounds were 3-fold serially diluted in 100% DMSO for 10 points using Agilent Bravo, and 750 nL was added to a 384 well compound plate using Echo along with 30 µL assay buffer. The fluorescent dye was then added to the assay plate along with assay buffer to a final volume of 40 µL. The cell plate was incubated for 50 min at 37 °C and 5% CO2 and placed into the FLIPR Tetra along with the compound plate.10µL of references and compounds were then transferred from the compound plate into the cell plate and the fluorescent signal was read. TABLE 1 Agonist activity of exemplified compounds at selected serotonin (5-HT) receptors in Ca 2+ flux functional assays.

Example 49: In vivo pharmacokinetics experiments The study was conducted using established procedures in accordance with the Australian Code of Practice for the Care and Use of Animals for Scientific Purposes, and the study protocols were reviewed and approved by the Monash Institute of Pharmaceutical Sciences Animal Ethics Committee. The systemic exposure of selected examples was studied in non-fasted male C57BL/6 mice weighing between 18.9 – 25.5 g. Mice had access to food and water ad libitum throughout the pre- and post-dose sampling period. On the day of dosing, the formulation of each compound was prepared by dissolving solid compound in phosphate buffer saline (50 mM) using vortexing, creating colourless solutions (pH 6.4-6.5) for each compound. Compounds were dosed to mice by IP injection (10 mL/kg dose volume via a 27G needle; n=9 mice per compound) and blood samples were collected at 5 and 30 min; 1, 2 and 4 h post-dose (n=3 mice per time point for each compound). A maximum of three blood samples were obtained from each mouse, with plasma samples being taken via submandibular bleed (approximately 120 μL). Once collected, blood samples were centrifuged immediately, supernatant plasma was removed, and stored at −80 °C until analysis by LCMS. In addition, at the 5 and 30 min and 4 h post-dose time points, the whole brain was rapidly removed from the carcass soon after the blood collection. The whole brains were blotted to remove excess blood, placed into pre- weighed polypropylene vials, and weighed. The brains were snap frozen in dry ice and subsequently stored frozen (−80 °C) until analysis. Bioanalytical Method Summary: Concentrations of test compound in plasma and tissue samples were determined using an LCMS/MS method validated for linearity, accuracy, precision, matrix factor and recovery (Table 2). Test compound standard solutions were diluted from a concentrated stock solution (32 mM in H2O) using 50% can in H2O (v/v) and a calibration curve was prepared in a matched matrix to the test samples. Plasma: The plasma calibration curve was prepared by spiking aliquots of blank mouse plasma (25 μL) with test compound standard solutions (5 μL) and internal standard solution (5 μL of diazepam, 5 μg/mL in 50% acetonitrile in water). Test plasma samples (25 μL) were thawed, mixed, and then spiked with internal standard solution (5 μL). Plasma protein precipitation was performed by addition of acetonitrile (3-fold volume ratio) and thorough vortex mixing. Samples were centrifuged (RCF = 9391 x g) for 3 minutes and the supernatant (90 μL) was collected for analysis. Tissue: Pre-weighed tissue samples (brain) were homogenised using a glass rod in buffer containing an EDTA/potassium fluoride solution (0.1 M / 4 mg/mL) as a stabilisation cocktail to minimise the potential for ex vivo degradation (3 mL cocktail/g tissue). The tissue homogenate was briefly centrifuged (RCF = 79 x g) for 10 seconds to separate the foam layer before transferring an aliquot of the tissue homogenate (200 μL) to a fresh Eppendorf tube for sample extraction. Calibration standards were prepared by spiking blank brain homogenate (200 μL) with the solution standards (10 μL) and the internal standard (10 μL). Study samples were similarly prepared, except that acetonitrile (10 μL) was added instead of solution standards to maintain the same volume. Protein precipitation was carried out by the addition of a 3-fold volume of acetonitrile, followed by vortex mixing and centrifugation (RCF = 9391 x g) for 3 min to recover the supernatant for analysis. Replicate analysis: Triplicate analytical replicate (ARs) samples were prepared similarly to the standards for each sample type at three concentrations (50, 500 and 2,000 ng/mL) and repeat injections of these ARs were included throughout the analytical run to assess assay performance. The extraction of the test compound from the standards and ARs were conducted as described above. All test samples were quantified within the calibration range of the assay and the assay performance for ARs were deemed acceptable. The stability of each test compound was confirmed in homogenate during the period of sample processing (15 min; < 15% loss). Table 2: Summary of bioanalytical method for a subset of exemplar compounds The highest abundance product ion with minimum interference with the matrix were selected for quantification. Data acquisition was performed using MassLynx software (V4.2). IS: Internal standard | * Retention time | # Collision-Induced Dissociation Maximal plasma concentrations of compounds P-8, P-5, P-3, and P-1 following IP administration at 10 mg/kg are shown in Table 3. Comprehensive pharmacokinetic data including brain penetration information is displayed in Figure 1 and/or Table 4. Table 3: Exposure parameters for a subset of exemplar compounds: P-8, P-5, P- 3, and P-1 in male C57BL/6 mice following IP administration at 10 mg/kg. Table 4: Individual and mean ± SD (n = 3) plasma and brain concentrations, and brain-to-plasma (B:P) ratios, of a subset of exemplar compounds P-8, P-5, P-3, and P-1 in male C57BL/6 mice following IP administration at 10 mg/kg. ND – Not Detected; <LLQ – Below the analytical lower limit of quantitation Example 50: Biotelemetry and Head-Twitch Response (HTR) experiments Mice (C57BL/6J males) were purchased from the Jackson Laboratory (Bar Harbor, ME, USA) at 5−6 weeks of age and allowed at least 1−2 weeks to acclimate to the NIDA, Intramural Research Program (IRP), animal research facility in Baltimore, MD, USA. The animal facility is fully accredited by the Association for the Assessment and Accreditation of Laboratory Animal Care, and all procedures were approved by the NIDA IRP Animal Care and Use Committee. Mice were initially group housed 3−5 per cage during acclimation and housed in a 12 h light−dark cycle throughout the study, with lights on at 0700 h. Food and water were available ad libitum except during testing. Cohorts of 20−24 mice were used for each test drug. The mice were subjected to experimental testing once every 1−2 weeks for 2−3 months to complete dose−effect curves and antagonist experiments. A minimum of 7 days between treatments was utilized to avoid any tolerance to effects of repeated drug administration. All drug doses represent the weight of the salt dissolved in 0.9% saline vehicle. Mice were tested first in dose−response studies to assess the effects of each compound at doses from 0.03 to 30 mg/kg s.c. and were subsequently tested in antagonist reversal studies utilizing pretreatment with M100907 and WAY100635. All experiments were conducted from 0900 to 1700 local time during the light phase, as sensitivity of rodents to other tryptamine psychedelics is diurnal, with maximal HTR observed in the middle of the light phase. Experiments were run during the light phase also to avoid any potential influence of melatonin receptor activity on HTR as melatonin and related agonists are known to reduce HTR induced by DOI in rats. For each experiment, mice were acclimated to the testing room in their home cage for at least 1 h prior to experimental sessions. Behavioral test sessions were carried out in Tru Scan mouse locomotor arenas equipped with photobeam arrays (Coulbourn Instruments, Holliston, MA, USA), which were modified with cylindrical inserts and transparent floors useful in detecting mouse HTR. Subcutaneous Temperature Transponder Implants. At least 1 week prior to the start of the experiments, mice received s.c. implanted temperature transponders (14 × 2 mm, model IPTT-300, Bio Medic Data Systems, Inc., Seaford, DE, USA) under brief isoflurane anesthesia. Mice were single housed post implant for the remainder of the study to protect the transponder from removal by cage mates. Temperature was determined noninvasively using a handheld receiver that is sensitive to signals emitted from the implanted transponders. Prior to each experiment, mouse body weight and temperature were recorded. Mice were then placed into testing chambers for acclimation. In dose−response studies, after a brief 5 min acclimation, mouse body temperature was recorded for baseline measurement, mice received s.c. injection of test substance or vehicle, and animals were returned to the testing arena for 30 min. During the session, locomotor activity was monitored via photobeam tracking of movements in the horizontal plane to yield distance traveled in centimeter. HTR was monitored by the analysis of GoPro Hero Black 7 video recordings (120 frames per sec and 960p resolution) using a commercially available software package from Clever Sys Inc. (Reston, VA, USA).82 Post-treatment body temperature values were also recorded, and temperature data are represented as change from pretreatment baseline. In antagonist reversal experiments, mice received a s.c. injection of either receptor antagonists or vehicle and were returned to the testing chamber for 30 min. During this period, locomotor activity was monitored to examine the potential effects of antagonist treatment on general behavior or movement. At 30 min after antagonist administration, mice were given test drug or vehicle and returned to the chambers for an additional 30 min of video recording used for analyses. All statistical analyses were conducted using GraphPad Prism 9 (La Jolla, CA, USA). Dose−response data from mouse experiments were analyzed using nonlinear regression, and potency values were determined from the rising phase of the curves for HTR measures. For mouse studies, one-way ANOVA with Dunnett’s post hoc test was used to compare all conditions to vehicle controls (0 or 0,0) in dose−response and antagonist experiments. Time-course drug effects for all parameters in mouse studies are shown for reference. Mean HTR count, distance traveled, and temperature change for each condition were used for statistical comparisons. Alpha was set at 0.05 for all analyses. Results of these experiments for P-4, P-3 and P-1 are shown in Figures 2, 3, 4 and 5. These data show that compounds of the invention are well-tolerated. These data also show that the compounds are not promoting increased head-twitch response, suggesting they are likely not hallucinogenic. Example 51: Tail Suspension Test Experiments Male ICR mice (23 ± 3 g) were purchased from BioLASCO (Taipei, Taiwan) at 4-5 weeks of age and allowed 5-7 days to acclimate to the animal research facility at Pharmacology Discovery Services (Taipei, Taiwan). Mice were housed in groups of 10 in a large cage (47 x 25 x 15 cm) on a 12-hour light cycle (lights on: 0700) and provided ad libitum food and water except during acute restraint stress and tail-suspension testing. Temperature was maintained at 20-24 °C, and all rooms (colony and testing rooms) had similar lighting intensity. All aspects of this work including housing, experimentation, and animal disposal were performed in accordance with the “Guide for the Care and Use of Laboratory Animals: Eighth Edition” (The National Academies Press, Washington, DC, 2011) in a facility accredited by the Association for Assessment and Accreditation of Laboratory Animal Care. All experiments were conducted between 0900 to 1700 local time, during the light phase. Each mouse underwent a single behavioural experiment in which they were randomly allocated to receive a single treatment with vehicle (50mM phosphate buffered saline, pH = 6.5), Ketamine as a positive control (10 mg/kg, diluted in 0.9% saline from 50 mg/ml stock), or one dose of a test drug (n=10 per dose of test drug, n=12 for vehicle, n=12 for ketamine). All drug doses represent the freebase dose in salt form dissolved in vehicle. All solutions were delivered at 5 ml/kg via intraperitoneal injection. Acute Restraint Stress (ARS) Procedure: Mice were moved from the colony room to the procedure room in which ARS was to be performed. Mice received oral gavage of water (10 ml/kg) to avoid dehydration, and then were individually restrained for 5 hours in a clear plastic cylinder (50 mL centrifuge tube with air holes drilled for ventilation), positioned horizontally on a bench with bench towel to absorb urine. This restraint prevented physical movement, without causing pain. Restrainers were washed with veterinary disinfectant between mice. Drug Administration: Immediately after the 5-hour ARS procedure, mice were removed from the restrainers, placed in their home cage, and transported to the room in which Tail Suspension Test was to be conducted. Mice then received intraperitoneal injection with vehicle, ketamine (10 mg/kg), P-3·HCl (3, 10 mg/kg) or P-8·2HCl (3, 10, 30 mg/kg), and were then placed back in their home cage.10 minutes after treatment, animals then underwent the Tail Suspension Test. Tail Suspension Test (TST) Procedure: Mice were individually suspended on the edge of a shelf, 58cm above a tabletop, using adhesive tape placed approximately 1 cm from the tip of the tail, for a total duration of 7 minutes. Using a stopwatch, the experimenters blinded to treatment groups recorded the duration of immobility (defined as hanging passively and motionless) during the 5 minutes spanning from 2-7 minutes. The data from 0-2 minutes was not recorded. Mice undergoing TST were never in view of other mice. Following TST, mice were euthanized via carbon dioxide inhalation. Statistical Analysis: Statistical analyses were conducted using GraphPad Prism 9 (La Jolla, CA, USA), using a priori simple effect comparisons within a one-way ANOVA to compare the test compounds to the Vehicle condition, on time spent immobile (in seconds). The datapoints shown in Figure 6 represent the mean ± the standard error of the mean. Significance was set at α= 0.05. * Signifies p < 0.05; ** p < 0.01. *** p < 0.001. Results of this experiment for compounds P-3 and P-8 are shown in Figure 6. This data indicates the compounds of the invention decrease the immobility time of mice in an Acute Restraing Stressor – Tail Suspension Test mouse model of depression. This indicates that compounds of the invention are likely to be anti-depressant.

Also described herein are the following embodiments 1 to 71: 1. A compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO 2 , N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2- 6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C 1 - 6 alkyl, C 2 - 6 alkenyl, C 2 - 6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X 1 is N, NR 6 , O or S; X 2 is CR 7 , N, O or S; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR 12 )2, C(O)R 12 , CO2R 12 , C(O)N(R 12 )2, S(O)R 12 and SO2R 12 , C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 12 , C(O)N(R 12 )2, OR 12 , N(R 12 )2, NO2, SR 12 and SO 2 R 12 , said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 12 ; each R 12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 , R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X 2 is CR 7 , R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO 2 and NR 14 ; alternatively, when X 1 is NR 6 and X 2 is CR 7 , R 6 and R 7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3- 10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms; and wherein the compound of formula (I) is not one of the following: . 2. The compound of embodiment 1, wherein R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl and C4-14 alkylenecycloalkyl. 3. The compound of embodiment 2, wherein R 1 and R 2 are each independently selected from C1-4 alkyl. 4. The compound of embodiment 3, wherein R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: 5. The compound of embodiment 1, wherein R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is as defined in embodiment 1. 6. The compound of any one of embodiments 1 to 5, wherein R 3 is hydrogen. 7. The compound of embodiment 1, wherein R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is as defined in embodiment 1. 8. The compound of any one of embodiments 1 to 7, wherein R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1- 6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C 6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in embodiment 1. 9. The compound of embodiment 8, wherein R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1- 6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1- 6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined in embodiment 1. 10. The compound of embodiment 9, wherein 1 or 2 of R 7 , R 8 , R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 R 9 , R 10 and R 11 are each hydrogen. 11. The compound of any one of embodiments 1 to 7, wherein R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. 12. The compound of embodiment 11, wherein R 8 and R 9 are combined to form a C5- 8 heterocycloalkyl or C5-10 heteroaryl selected from the following: , wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH 3 ) 2 , C(O)NHCH 3 , OH, NH 2 , N(CH 3 ) 2 , NHCH 3 , NO 2 , SH, SCH 3 , SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. 13. The compound of embodiment 12, wherein R 8 and R 9 are combined to form a C5- 8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. 14. The compound of any one of embodiments 1 to 13, wherein L is C 1-4 alkylene. 15. The compound of embodiment 14, wherein L is methylene. 16. The compound of any one of embodiments 1 to 15, wherein R 6 is selected from hydrogen and C1-6 alkyl. 17. The compound of embodiment 16, wherein R 6 is hydrogen. 18. The compound of any one of embodiments 1 to 17, wherein X 1 is NH or N. 19. The compound of embodiment 18 having the formula (II): wherein R 1 , R 2 , R 3 , R 7 , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 1 to 13; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. 20. The compound of embodiment 19 having the formula (IIa): wherein R 1 , R 2 , R 3 , R 7 , R 9 , R 10 and R 11 are as defined in any one of embodiments 1 to 10. 21. The compound of embodiment 19 having the formula (IIb): ( ) wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 10 and R 11 are as defined in any one of embodiments 1 to 10. 22. The compound of embodiment 19 having the formula (IIc): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 11 are as defined in any one of embodiments 1 to 13. 23. The compound of embodiment 19 having the formula (IId): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 10 are as defined in any one of embodiments 1 to 13. 24. The compound of embodiment 18 having the formula (III): wherein R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 1 to 13. 25. The compound of embodiment 24 having the formula (IIIa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 1 to 13. 26. The compound of embodiment 18 having the formula (IV): wherein X2 is O or S, and R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 1 to 13. 27. The compound of embodiment 26 having the formula (IVa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 1 to 13. 28. The compound of any one of embodiments 1 to 17 wherein X 1 is O. 29. The compound of embodiment 28 having the formula (V): wherein R 1 , R 2 , R 3 , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 1 to 13. 30. The compound of embodiment 29 having the formula (Va): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 1 to 13. 31. The compound of embodiment 1 selected from any one of the following:

or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 32. A medicament comprising a compound of any one of embodiments 1 to 31, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 33. A pharmaceutical composition comprising a compound of any one of embodiments 1 to 31, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, and a pharmaceutically acceptable excipient. 34. A method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R 1 and R 2 are each independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C 3 - 8 cycloalkyl, C 4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4-C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8 heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , said C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C4-C14 alkyleneheterocycloalkyl, C3- C8 heterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; alternatively R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl including 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR 4 , said C3-8 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO 2 R 4 , C(O)N(R 4 ) 2 , OR 4 , N(R 4 ) 2 , NO 2 , SR 4 , SO 2 R 4 , C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-8 alkylamino, C1-8 alkylsulfonyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; R 3 is selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 ; each R 4 is independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl, and C3-7 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 , said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-7 cycloalkyl and C3-7 heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 5 , C(O)N(R 5 )2, OR 5 , N(R 5 )2, NO2, SR 5 and SO2R 5 , said C3-C7 cycloalkyl and C3-7 heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR 5 ; each R 5 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C5-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C 1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; L is selected from C1-4 alkylene, C2-C4 alkenylene and C2-C4 alkynylene; X 1 is N, NR 6 , O or S; X 2 is CR 7 , N, O or S; Z 1 is CR 8 or N; Z 2 is CR 9 or N; Z 3 is CR 10 or N; Z 4 is CR 11 or N; R 6 is selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyleneP(O)(OR 12 )2, C(O)R 12 , CO2R 12 , C(O)N(R 12 )2, S(O)R 12 and SO2R 12 , C3- 6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4- 7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6-9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 12 , C(O)N(R 12 )2, OR 12 , N(R 12 )2, NO2, SR 12 and SO2R 12 , said C3-6 cycloalkyl, C6-9 alkylenecycloalkyl, C3-6 heterocyclyl, C6- 9 alkyleneheterocycloalkyl, C4-7 heterocyclyl, C7-10 alkyneneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being further optionally substituted with a substituent independently selected from (O), C 1-6 alkyl, C 1-6 haloalkyl, C 2 - 6 alkenyl, C 2 - 6 haloalkenyl, C 2 - 6 alkynyl, C 2 - 6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 12 ; each R 12 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R 7 , R 8 , R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C 3-8 cycloalkyl, C 3 - 14 alkylenecycloalkyl, C 3-10 heterocycloalkyl, C 4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; each R 13 is independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl, said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C6-16 alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; alternatively, when X 2 is CR 7 , R 7 and one of R 1 , R 2 , or R 3 are combined with the atoms to which they are attached to form a C5-8 heterocycloalkyl, said C5-8 heterocyclyalkyl being further optionally substituted with one or more substituents selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when X 1 is NR 6 and X 2 is CR 7 , R 6 and R 7 are combined with the atoms to which they are each attached to form a C4-10 heterocycloalkyl or a C5-10 heteroaryl, said C4-10 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C 1-8 alkylsulfonyl, CO 2 R 14 , C(O)N(R 14 ) 2 , OR 14 , N(R 14 ) 2 , NO 2 , SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; alternatively, when Z 1 is CR 8 and Z 2 is CR 9 , or when Z 2 is CR 9 and Z 3 is CR 10 , or when Z 3 is CR 10 and Z 4 is CR 11 , then R 8 and R 9 , or R 9 and R 10 , or R 10 and R 11 are combined with the atoms to which they are each attached to form a C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, or C5-10 heteroaryl, said C4-8 cycloalkyl, C5-8 heterocycloalkyl, C6-12 aryl, and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 14 , C(O)N(R 14 )2, OR 14 , N(R 14 )2, NO2, SR 14 , SO2R 14 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 14 ; each R 14 is independently selected from hydrogen, C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl; said C1-6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3- 10 heterocycloalkyl, C6-12 aryl and C5-10 heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein one or more of X 2 , Z 1 , Z 2 , Z 3 and Z 4 are heteroatoms. 35. The method of embodiment 34, wherein R 1 and R 2 are each independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C 3-8 cycloalkyl and C 4-14 alkylenecycloalkyl. 36. The method of embodiment 35, wherein R 1 and R 2 are each independently selected from C1-4 alkyl. 37. The method of embodiment 36, wherein R 1 and R 2 , together with the nitrogen to which they are attached, form any one of the following: 38. The method of embodiment 34, wherein R 1 and R 2 are combined with the atoms to which they are attached to form C3-6 heterocycloalkyl, said C3-6 heterocycloalkyl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 and SO2R 4 , (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is as defined in embodiment 1. 39. The method of any one of embodiments 34 to 38, wherein R 3 is hydrogen. 40. The method of embodiment 34, wherein R 3 and one of R 1 and R 2 are combined with the atoms to which they are attached to form a C3-8 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 4 , C(O)N(R 4 )2, OR 4 , N(R 4 )2, NO2, SR 4 , SO2R 4 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2 and NR 4 , wherein R 4 is as defined in embodiment 1. 41. The method of any one of embodiments 34 to 40, wherein R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1- 6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)R 13 , C(O)N(R 13 )2, C(O)C(O)N(R 13 )2, OC(O)R 13 , OC(O)OR 13 , OC(O)N(R 13 )2, OS(O)R 13 , OS(O)N(R 13 )2, OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , S(O)N(R 13 )2, SO2R 13 , N(R 13 )2, N(R 13 )C(O)R 13 , N(R 13 )C(O)OR 13 , N(R 13 )C(O)N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2R 13 , C(O)N(R 13 )2, OR 13 , N(R 13 )2, NO2, SR 13 and SO2R 13 , said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR 13 ; wherein R 13 is as defined in embodiment 34. 42. The method of embodiment 41, wherein R 7 , R 8 R 9 , R 10 and R 11 are each independently selected from hydrogen, halogen, CN, OR 13 , N(R 13 )2, SR 13 , C1-6 alkyl, C1- 6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1- 6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, CO2R 13 , C(O)N(R 13 )2, OC(O)R 13 , OSO2R 13 , OP(O)(OR 13 )2, OC1-6alkyleneP(O)(OR 13 )2, S(O)R 13 , SO2R 13 , N(R 13 )2, NO2, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, C4-16 alkyleneheteroaryl, said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-C6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkylamine, C1-6 alkoxy, C1-6 haloalkoxy, C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NO2, NHCH3, SH, SCH3, SO2CH3, and SOCH3, said C3-8 cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16 alkyleneheterocycloalkyl, C6-12 aryl, C7-18 alkylenearyl, C5-10 heteroaryl, and C4-16 alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, NH and NCH3; wherein R 13 is as defined in embodiment 34. 43. The method of any one of embodiments 34 to 42, wherein 1 or 2 of R 7 , R 8 R 9 , R 10 and R 11 when present are each independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl and OR 13 wherein R 13 is selected from C1-6 alkyl and C1-6 haloalkyl, and the other of R 7 , R 8 R 9 , R 10 and R 11 are each hydrogen. 44. The method of any one of embodiments 34 to 42, wherein R 8 and R 9 when present are combined with the atoms to which they are each attached to form a C5-8 heterocycloalkyl or C5-10 heteroaryl, said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, C1-8 alkoxy, C1-8 alkylamino, C1-8 alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C3-6 cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3. 45. The method of embodiment 44, wherein R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: wherein the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached; said C5-8 heterocycloalkyl and C5-10 heteroaryl each being further optionally substituted with a substituent selected from halogen, (O), CN, CO2H, CO2CH3, C(O)NH2, C(O)N(CH 3 ) 2 , C(O)NHCH 3 , OH, NH 2 , N(CH 3 ) 2 , NHCH 3 , NO 2 , SH, SCH 3 , SO2CH3, SOCH3, C1-6 alkyl and C1-6 haloalkyl. 46. The method of embodiment 45, wherein R 8 and R 9 are combined to form a C5-8 heterocycloalkyl or C5-10 heteroaryl selected from the following: where the dashed bond denotes the bond shared with the aromatic ring to which R 8 and R 9 are attached. 47. The method of any one of embodiments 34 to 46, wherein L is C1-4 alkylene. 48. The method of embodiment 47, wherein L is C1 alkylene. 49. The method of embodiment 48, wherein L is methylene. 50. The method of any one of embodiments 34 to 49, wherein R 6 is selected from hydrogen and C1-6 alkyl. 51. The method of embodiment 50, wherein R 6 is hydrogen. 52. The method of any one of embodiments 34 to 51, wherein X 1 is NH or N. 53. The method of embodiment 52 having the formula (II):

wherein R 1 , R 2 , R 3 , R 7 , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 34 to 46; and wherein one or more of Z 1 , Z 2 , Z 3 and Z 4 is N. 54. The method of embodiment 53 having the formula (IIa): wherein R 1 , R 2 , R 3 , R 7 , R 9 , R 10 and R 11 are as defined in any one of embodiments 34 to 43. 55. The method of embodiment 53 having the formula (IIb): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 10 and R 11 are as defined in any one of embodiments 34 to 43. 56. The method of embodiment 53 having the formula (IIc): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 11 are as defined in any one of embodiments 34 to 46. 57. The method of embodiment 53 having the formula (IId): wherein R 1 , R 2 , R 3 , R 7 , R 8 , R 9 and R 10 are as defined in any one of embodiments 34 to 46. 58. The method of embodiment 53 having the formula (III): wherein R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 34 to 46. 59. The method of embodiment 58 having the formula (IIIa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 34 to 46. 60. The method of embodiment 52 having the formula (IV): wherein X2 is O or S, and R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 34 to 46. 61. The method of embodiment 60 having the formula (IVa): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 34 to 46. 62. The method of any one of embodiments 34 to 48 wherein X 1 is O. 63. The method of embodiment 62 having the formula (V): wherein R 1 , R 2 , R 3 , , Z 1 , Z 2 , Z 3 and Z 4 are as defined in any one of embodiments 34 to 46. 64. The method of embodiment 63 having the formula (Va): wherein R 1 , R 2 , R 3 , R 8 , R 9 , R 10 and R 11 are as defined in any one of embodiments 34 to 46. 65. The method of any one of embodiments 34 to 64, wherein the compound of formula (I) is selected from any one of the following:

or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 66. A method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of embodiments 34 to 65, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in combination with another known agent useful for treatment of a disease, disorder or condition by activation of a serotonin receptor. 67. A method of treating a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of embodiments 34 to 65, or a pharmaceutically acceptable salt, solvate, tautomer, N- oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 68. The method of embodiment 67, wherein the mental illness is selected from anxiety disorders; depression; mood disorders; psychotic disorders; impulse control and addiction disorders; drug addiction; obsessive-compulsive disorder (OCD); post- traumatic stress disorder (PTSD); stress response syndromes; dissociative disorders; depersonalization disorder; factitious disorders; sexual and gender disorders; somatic symptom disorders; hallucinations; delusions; psychosis; and combinations thereof. 69. A method for treating a central nervous system (CNS) disease, disorder or condition and/or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of embodiments 34 to 65, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. 70. The method of embodiment 69, wherein the CNS disease, disorder or condition and/or neurological disease, disorder or condition is selected from neurological diseases including neurodevelopmental diseases and neurodegenerative diseases such as Alzheimer’s disease; presenile dementia; senile dementia; vascular dementia; Lewy body dementia; cognitive impairment, Parkinson’s disease and Parkinsonian related disorders such as Parkinson dementia, corticobasal degeneration, and supranuclear palsy; epilepsy; CNS trauma; CNS infections; CNS inflammation; stroke; multiple sclerosis; Huntington’s disease; mitochondrial disorders; Fragile X syndrome; Angelman syndrome; hereditary ataxias; neuro-otological and eye movement disorders; neurodegenerative diseases of the retina amyotrophic lateral sclerosis; tardive dyskinesias; hyperkinetic disorders; attention deficit hyperactivity disorder and attention deficit disorders; restless leg syndrome; Tourette's syndrome; schizophrenia; autism spectrum disorders; tuberous sclerosis; Rett syndrome; cerebral palsy; disorders of the reward system including eating disorders such as anorexia nervosa and bulimia nervosa; binge eating disorder, trichotillomania, dermotillomania, nail biting; migraine; fibromyalgia; and peripheral neuropathy of any etiology, and combinations thereof. 71. A method for increasing neuronal plasticity and/or increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound of formula (I) as defined in any one of embodiments 34 to 65, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in an amount sufficient to increase neuronal plasticity and/or increase dendritic spine density of the neuronal cell.




 
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