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Title:
PURINE DERIVATIVES HAVING PHOSPHODIESTERASE IV INHIBITION ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2000/059449
Kind Code:
A2
Abstract:
Disclosed are compounds of formula (I), wherein R?3¿, R?6a¿, R?6b¿ and R?8¿ are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need thereof.

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Inventors:
CHASIN MARK (US)
CAVALLA DAVID (GB)
HOFER PETER (CH)
GEHRIG ANDRE (CH)
WINTERGEST PETER (CH)
Application Number:
PCT/US2000/008525
Publication Date:
October 12, 2000
Filing Date:
March 31, 2000
Export Citation:
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Assignee:
EURO CELTIQUE SA (LU)
CHASIN MARK (US)
CAVALLA DAVID (GB)
HOFER PETER (CH)
GEHRIG ANDRE (CH)
WINTERGEST PETER (CH)
International Classes:
A61K31/52; A61P11/06; A61P25/24; A61P25/28; A61P29/00; A61P37/00; A61P37/08; C07D473/18; C07D473/20; C07D473/24; C07D473/34; (IPC1-7): A61K/
Foreign References:
US6066641A2000-05-23
US5939422A1999-08-17
US5744473A1998-04-28
US5994629A1999-11-30
Other References:
FUJI ET AL.: 'Purines. LV.(1) Syntheses and cytokinin activities of some adenine and adenosine derivatives related to 1'-methylzeatin' CHEM. PHARM. BULL. vol. 41, no. 8, August 1993, pages 1362 - 1365, XP002931369
YU ET AL.: 'Structures of cytokinins influence synergistic production of ethylene' PHYTOCHEMISTRY vol. 20, no. 6, 1981, pages 1191 - 1195, XP002931368
See also references of EP 1169321A2
Attorney, Agent or Firm:
Davidson, Clifford M. (Davidson & Kappel LLC 15th floor 1140 Avenue of the Americas New York, NY, US)
Download PDF:
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Claims:
What is claimed is:
1. A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R3, Rua, W'and R'is selected from the group consisting of A and B, wherein A is selected from the group consisting of hydrogen; Ci. alkyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H, =O and benzyloxy; said benzyloxy optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, Cl l0 alkoxy and C312 cycloalkoxy; C210 alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, Cg. cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H and =O; C310cycloalkyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Cl lo) alkyl, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Ci. l0) alkyl, =NOH, =NOCONH2, CO, H and =O; C312 cycloalkyl (C110) alkyl wherein the cycloalkyl portion is optionally substi tuted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, =NOCONH2, CO2H and =O; aryl which is optionally substituted with 13 substituents chosen from the group consisting of C312cycloalkyl,OH,halogen,C110alkoxy,C312cycloalkoxy,NH2,alkyl, Cl alkylamino, C110 dialkylamino, carbamyl, amido, C110 alkylamido, C110 dialkylamido, Ci.
2. 10 acylamino, C110 alkylsulfonylamino, C=NOH, C=NOCONH2, phenyl and benzyl; ar (C14) alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting ofcarboxy, Ci. io alkylcarboxy, halogen, hydroxy, hydroxy (Cl l0) alkoxy, nitro, trihalocarbon, benzyloxy, heterocyclyl, Cl l0 cycloalkyl (C3 l2) alkyloxy, ar (C110) alkyloxy, aryloxy, amino (Cl l0) alkoxy, C110 alkylamino (Cl lo) alkoxy, heteroaryloxy, heteroar (Ci. io) alkyloxy, heterocyclyloxy, C110 alkyl, C312 cycloalkyl, Ci. akloxy and C312 cycloalkoxy ; said alkoxy and cycloalkoxy optionally substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with Cl alkyl; and wherein the alkyl moiety of said ar (Cl 4) alkyl is optionally substituted with OH, halogen, Cl alkoxy or C312 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; heterocyclyl which is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, NH2, C110 alkylamino, C110 dialkylamino, carbamyl, amido, Cl l0 alkylamido, C110acylamino,C110alkylsulfonylamin,C=NOH,dialkylamido, C=NOCONH2, phenyl and benzyl; heterocyclyl (CIC4) alkyl wherein said heterocyclyl moiety is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, alkylamino,C110dialkylamino,carbamyl,amido,C110alkylamido,C110NH2,C110 dialkylamido, Cl. l0 acylamino, C110 alkylsulfonylamino, C=NOH, C=NOCONH2, phenyl and benzyl, and wherein said alkyl moiety is optionally substituted with OH, C110 alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen and halo (Ci. io) alkyl; heteroaryl, which is optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, nitro, CF3, Cl l0 alkoxy, C312 cycloalkoxy and oxo; and heteroaryl (C14) alkyl, wherein the heteroaryl moiety is optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, nitro, trihalocarbon, C110 alkoxy and C312 cycloalkoxy ; and B is selected from the group consisting of Ci. io alkyi which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino; said substituents optionally substituted with 13 substituents chosen from the group consisting of halogen, Ci. io alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy and oxo; said substituted Ci. io alkyi further optionally substituted with 13 substituents chosen from the group consisting of OH, Cl l0 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, COzH, and =O C210 alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkyl which is substituted with 13 substituents chosen from the group consisting of C110 alkyl and C312 cycloalkyl ; said substituted C310 cycloalkyl further optionally substituted with 13 substituents chosen from the group consisting of OH, Ci. in alkoxy, halogen,halo(C110)alkyl,=NOH,=NOCONH2,CO2Hand=O;cycloalkoxy, C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, Cllo akl, C312cycloalkyl, Cllo alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, =NOCONH2, CO2H and =O; C312 cycloalkyl(C110) alkyl wherein the cycloalkyl portion is substituted with 1 3 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, halo (Cl lo) alkyl, and =O; said substituted C312 cycloalkyl(C110)alkyl further optionally substi tuted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, =NOH, =NOCONH2, and CO2H ; aryl which is substituted with 13 substituents chosen from the group consisting of carbamyl, amido, C110 alkylamido, C110 dialkylamido, C110 acylamino and Cl l0 alkylsulfonylamino; said substituted aryl further optionally substituted with 13 substituents chosen from the group consisting of C1_lo alkyl, Cs12 cycloalkyl, OH, halogen, C110 alkoxy, C3 12 cycloalkoxy, NH2, C110 alkylamino, Ci. io dialkylamino, C=NOH, C=NOCONH2, phenyl and benzyl; ar (C14) alkyl wherein the aryl moiety is substituted with 13 substituents chosen from the group consisting of carboxy, C110 alkylcarboxy, hydroxy (C110)alkoxy, nitro, benzyloxy, heterocyclyl, C110 cycloalkyl(C312)alkyloxy, ar (Cl l0) alkyloxy, aryloxy, amino (C1 lo) alkoxy, Cl io alkylamino (Ci. io) alkoxy, heteroaryloxy, heteroar (Ci. io) alkyloxy, heterocyclyloxy, C110 alkoxy andC312 cycloalkoxy ; said alkoxy and cycloalkoxy substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with C110 alkyl and wherein the alkyl moiety of said ar (Cl 4) alkyl is optionally substituted with OH, halogen, Cl l0 alkoxy and C312 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; and said substituted ar (C14)alkyl further optionally substituted with 13 substituents chosen from the group consisting of halogen, hydroxy, trihalocarbon, C312cycloalkyl,C110alkoxyandC312cycloalkoxyalkyl, heterocyclyl which is substituted on the carbons or nitrogens of the ring with 1 3 substituents chosen from the group consisting of carbamyl, C110 acylamino and Cl l0 alkylsulfonylamino; said substituted heterocyclyl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, NH2, C110 alkylamino, C110 dialkylamino, amido, Ci. io alkylamido, Ci. io dialkylamido, C=NOH, C=NOCONH2, phenyl and benzyl; heterocyclyl (ClC4) alkyl wherein said heterocyclyl moiety is substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of Cl 10 acylamino, C110 alkylsulfonylamino, and Ci. io alkyi, said Ci. io alkyi substituted with OH, C 10 alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen or halo (Cl lo) alkyl; said substituted heterocyclyl (ClC4) alkyl further optionally substituted with 13 substituents chosen from the group consisting of Cl l0 alkyl, C312 cycloalkyl, OH, halogen, C110 alkoxy, C312 cycloalkoxy, NH2, C110 alkylamino, C110 dialkylamino, amido, Cl alkylamido and C110 dialkylamido, heteroaryl, which is substituted with oxo ; said substituted heteroaryl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C3 halogen,nitro,CF3,C110alkoxyandC312cycloalkoxy;and12cycloalkyl, heteroaryl (C14) alkyl, wherein the heteroaryl moiety is substituted with nitro; said heteroaryl (Cl 4) alkyl further optionally substituted with 13 substituents chosen from the group consisting alkyl,C312cycloalkyl,halogen,trihalocarbon,C110alkoxyandC312C110 cycloalkoxy; and provided that at least one of R3, R6a, R6b and Rs is B.
3. The compound of claim 1 wherein R3 is A and is ar (Cl 4) alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting of halogen, nitro, C110 alkoxy, C312 cycloalkoxy or CF3, and wherein the alkyl moiety is optionally substituted with 13 substituents chosen from the group consisting of OH, halogen, andC312cycloalkoxy.C110alkoxy.
4. The compound of claim 2 wherein said aralkyl is benzyl.
5. The compound of claim 3 wherein the aryl moiety of said benzyl is substituted with 13 substituents chosen from the group consisting of halogen, nitro, Cl l0 alkoxy, C312 cycloalkoxy and CF3.
6. The compound of claim 4 wherein said benzyl is substituted with cyclopentyloxy and methoxy.
7. The compound of claim 2 wherein R6a is A and is hydrogen.
8. The compound of claims 16 wherein R6b is A and is selected from the group consisting of hydrogen; Cl 8 alkyl which is unbranched or branched and is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H or =0; and C3S cycloalkyl which is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, haloalkyl, =NOH, =NOCONH2,, CO2H or =O.
9. The compound of claims 17 wherein Rs is B and is Cl1. alkyl which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino, said substituents optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy and oxo.
10. A compound of the formula (II): and pharmaceutically acceptable salts thereof, wherein and R6a, selected from the group consisting of A and B, wherein A is selected from the group consisting of hydrogen; C110 alkyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO, H, =O and benzyloxy; said benzyloxy optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, andC312cycloalkoxy;alkoxy C210 alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C312 cycloalkyl, C110 alkoxy, C3 l2 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H and =O ; C310 cycloalkyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, NOCONH2, CO2H and =O; C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (C110)alkyl, =NOH, =NOCONH2, CO2H and =O; Cg. 12 cycloalkyl (Ci. io) alkyl wherein the cycloalkyl portion is optionally substi tuted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, =NOCONH2, C02H and =O; aryl which is optionally substituted with 13 substituents chosen from the group consisting of C312cycloalkyl,OH,halogen,C110alkoxy,C312cycloalkoxy,NH2,alkyl, Cl alkylamino, C110 dialkylamino, carbamyl, amido, C110 alkylamido, C110 dialkylamido, Ci. 10acylamino, C110 alkylsulfonylamino, C=NOH, C=NOCONH2, phenyl and benzyl; ar (Cl 4) alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting of carboxy, Cl l0 alkylcarboxy, halogen, hydroxy, hydroxy (C1 l0) alkoxy, nitro, trihalocarbon, benzyloxy, heterocyclyl, C110 aryloxy,amino(C110)alkoxy,C110alkylamino(C1cycloalkyl(C312)alkyloxy,ar(C110)alkyloxy, heteroar(C110)alkyloxy,heterocyclyloxy,C110alkyl,C312cycloalkyl,10)alkoxy,heteroaryloxy, C110 alkoxy and C312 cycloalkoxy; said alkoxy and cycloalkoxy optionally substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with Ci. io alkyi; and wherein the alkyl moiety of said ar (Cl 4) alkyl is optionally substituted with OH, halogen, C110 alkoxy or C312 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; heterocyclyl which is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, OH, halogen, C110 alkoxy, C312 cycloalkoxy, NH2, C110 alkylamino, C110 dialkylamino, carbamyl, amido, Ci. io alkylamido, C110acylamino,C110alkylsulfonylamino,C=NOH,dialkylamido, C=NOCONH2, phenyl and benzyl; heterocyclyl (ClC4) alkyl wherein said heterocyclyl moiety is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, alkylamino,C110dialkylamino,carbamyl,amido,C110alkylamido,C110NH2,C110 dialkylamido, C110 acylamino, C110 alkylsulfonylamino, C=NOH, C=NOCONH2, phenyl and benzyl, and wherein said alkyl moiety is optionally substituted with OH, Ci. io alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen and halo (Ci. io) alkyl ; heteroaryl, which is optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, nitro, CF3, Ci. io alkoxy, C312 cycloalkoxy and oxo; and heteroaryl (CI4) alkyl, wherein the heteroaryl moiety is optionally substituted with I3 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, nitro, trihalocarbon, C110 alkoxy and C312 cycloalkoxy ; and B is selected from the group consisting of Ci. io alkyi which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino; said substituents optionally substituted with 13 substituents chosen from the group consisting of halogen, Ci. io alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy and oxo; said substituted Ci. io alkyi further optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H, and =O C210 alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, C02H and =O; C310 cycloalkyl which is substituted with 13 substituents chosen from the group consisting of C110 alkyl and C312 cycloalkyl ; said substituted C310 cycloalkyl further optionally substituted with 13 substituents chosen from the group consisting of OH, Cllo alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (C110)alkyl, =NOH, =NOCONH2, CO2H and =O ; C312 cycloalkyl(C110) alkyl wherein the cycloalkyl portion is substituted with 1 3 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, halo (C110)alkyl, and =O; said substituted C312 cycloalkyl(C110)alkyl further optionally substi tuted with 13 substituents chosen from the group consisting of OH, Cl l0 alkoxy, ¬3. 12 cycloalkoxy, =NOH, =NOCONH2, and CO2H ; aryl which is substituted with 13 substituents chosen from the group consisting of carbamyl, amido, C110 alkylamido, C110 dialkylamido, Cl l0 acylamino and Ci. io alkylsulfonylamino; said substituted aryl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, OH, halogen, C110 alkoxy, C3 12 cycloalkoxy, NH2, C110 alkylamino, C110 dialkylamino, C=NOH, C=NOCONH2, phenyl and benzyl; ar (CI4) alkyl wherein the aryl moiety is substituted with 13 substituents chosen from the group consisting of carboxy, C110 alkylcarboxy, hydroxy(C110)alkoxy, nitro, benzyloxy, heterocyclyl, Cl1. cycloalkyl (C312) alkyloxy, ar (C110) alkyloxy, aryloxy, amino (C1 lo) alkoxy, C110 alkylamino (Ci. io) alkoxy, heteroaryloxy, heteroar (Cl l0) alkyloxy, heterocyclyloxy, Cl l0 alkoxy and C312 cycloalkoxy; said alkoxy and cycloalkoxy substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with Ci. io alkyi and wherein the alkyl moiety of said ar (Cl 4) alkyl is optionally substituted with OH, halogen, Ci. io alkoxy and C312 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; and said substituted ar (Cl 4) alkyl further optionally substituted with 13 substituents chosen from the group consisting of halogen, hydroxy, trihalocarbon, C110 alkyl, C312 cycloalkyl, C110 alkoxy and C312 cycloalkoxy heterocyclyl which is substituted on the carbons or nitrogens of the ring with 1 3 substituents chosen from the group consisting ofcarbamyi, Ci. io acylamino and Cl l0 alkylsulfonylamino; said substituted heterocyclyl further optionally substituted with 13 substituents chosen from the group consisting of Cl. 10 akl, OH, halogen, C110 alkoxy, C312 C110alkylamino,C110dialkylamino,amido,C110alkylamido,C110ycloalkoxy,NH2, dialkylamido, C=NOH, C=NOCONH2, phenyl and benzyl; heterocyclyl (ClC4) alkyl wherein said heterocyclyl moiety is substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C, acylamino, Cl l0 alkylsulfonylamino, and Ci. io alkyi, said Ci. io alkyi substituted with OH, C1 10 alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen or halo (Ci. io) alkyl; said substituted heterocyclyl (ClC4) alkyl further optionally substituted with 13 substituents chosen from the group consisting alkyl,C312cycloalkyl,OH,halogen,C110alkoxy,C312cycloalkoxy,C110 NH2, Clo alkylamino, Cl lo dialkylamino, amido, Cl_1o alkylamido and Ci. io dialkylamido, heteroaryl, which is substituted with oxo; said substituted heteroaryl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C3 , halogen, nitro, CF3, C110 alkoxy and C312 cycloalkoxy; and heteroaryl (Ci. alkyl, wherein the heteroaryl moiety is substituted with nitro; said heteroaryl (C11) alkyl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, trihalocarbon, C110 alkoxy and C 312 cycloalkoxy; and provided that at least one of R3, R6a, R6b and R8 is B.
11. The compound of claim 9 wherein R3 is A and is ar (C14) alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting of halogen, nitro, Cl l0 alkoxy, C312 cycloalkoxy or CF3, and wherein the alkyl moiety is optionally substituted with 13 substituents chosen from the group consisting of OH, halogen, Ci. alkoxy and C312 cycloalkoxy.
12. The compound of claim 10 wherein said aralkyl is benzyl.
13. The compound of claim 11 wherein the aryl moiety of said benzyl is substituted with 13 substituents chosen from the group consisting of halogen, nitro, Ci. io alkoxy, C312 cycloalkoxy or CF3.
14. The compound of claim 12 wherein said benzyl is substituted with cyclopentyloxy and methoxy.
15. The compound of claim 9 wherein R6a is A and is hydrogen.
16. The compound of claim 914 wherein R6b is A and is selected from the group consisting of hydrogen; C18 alkyl which is unbranched or branched and is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H or =O; and C38 cycloalkyl which is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, haloalkyl, =NOH, =NOCONH2, CO2H or=O.
17. The compound of claim 915 wherein R8 is B and is Ci. io alkyi which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino, said substituents optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy and oxo;.
18. A compound of the formula (III): and pharmaceutically acceptable salts thereof, wherein R3, R6a, R6b and R8 is selected from the group consisting of A and B, wherein A is selected from the group consisting of hydrogen; C110 alkyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH,NOCONH2, CO2H, =O and benzyloxy; said benzyloxy optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, andC312cycloalkoxy;alkoxy C2 l0 alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (C110) alkyl, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (C1 l0) alkyl, =NOH, =NOCONH2, CO2H and =O; C312 cycloalkyl (C110)alkyl wherein the cycloalkyl portion is optionally substi tuted with 13 substituents chosen from the group consisting of OH, C, _lo alkyl, C3_12 cycloalkyl, Ci. a. lkoxy, Cs12 cycloalkoxy, halogen, halo (Cl. l0) alkyl, =NOH, =NOCONH2, C02H and =O; aryl which is optionally substituted with 13 substituents chosen from the group consisting alkyl,C312cycloalkyl,OH,halogen,C110alkoxy,C312cycloalkoxy,NH2,C110 C110dialkylamino,carbamyl,amido,C110alkylamido,C110dialkylamido,C1C110alkylamino, 10acylamino, C110 alkylsulfonylamino, C=NOH, C=NOCONH2, phenyl and benzyl ; ar (Ci. alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting of carboxy, Cl lo alkylcarboxy, halogen, hydroxy, hydroxy (C110) alkoxy, nitro, trihalocarbon, benzyloxy, heterocyclyl, C110 aryloxy,amino(C110)alkoxy,C110alkylamino(C1ycloalkyl(C312)alkyloxy,ar(C110)alkyloxy, lo) alkoxy, heteroaryloxy, heteroar (C110)alkyloxy, heterocyclyloxy, Cl lo alkyl, C312 cycloalkyl, Ci. io alkoxy and C312 cycloalkoxy ; said alkoxy and cycloalkoxy optionally substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with C110 alkyl ; and wherein the alkyl moiety of said ar (Cl 4) alkyl is optionally substituted with OH, halogen, C110 alkoxy or ¬3. 12 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; heterocyclyl which is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, NH2, Ci. io alkylamino, C110 dialkylamino, carbamyl, amido, Cl l0 alkylamido, C110acylamino,C110alkylsulfonylamino,C=NOH,dialkylamido, C=NOCONH2, phenyl and benzyl; heterocyclyl (ClC4) alkyl wherein said heterocyclyl moiety is optionally substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, OH, halogen, Cl l0 alkoxy, C312 cycloalkoxy, alkylamino,C110dialkylamino,carbamyl,amido,C110alkylamido,C110NH2,C110 dialkylamido, Cl l0 acylamino, Ci. io alkylsulfbnylamino, C=NOH, C=NOCONH2, phenyl and benzyl, and wherein said alkyl moiety is optionally substituted with OH, Cl l0 alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen and halo (Ci. io) alkyl ; heteroaryl, which is optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, nitro, CF3, Cl l0 alkoxy, ¬3. 12 cycloalkoxy and oxo; and heteroaryl (Ci. alkyl, wherein the heteroaryl moiety is optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl halogen, nitro, trihalocarbon, C110 alkoxy and C312 cycloalkoxy ; and B is selected from the group consisting of C1 l0 alkyl which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino; said substituents optionally substituted with 13 substituents chosen from the group consisting of halogen, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy and oxo; said substituted Cl l0 alkyl further optionally substituted with 13 substituents chosen from the group consisting of OH, C312cycloalkoxy,halogen,=NOH,=NOCONH2,CO2H,and=OC110alkoxy, C,lo alkenyl which is unbranched or branched and is optionally substituted with 13 substituents chosen from the group consisting of OH, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkyl which is substituted with 13 substituents chosen from the group consisting of C110 alkyl and C312 cycloalkyl ; said substituted C310 cycloalkyl further optionally substituted with 13 substituents chosen from the group consisting of OH, C1 l0 alkoxy, C312 cycloalkoxy, halogen, halo (C1 l0) alkyl, =NOH, =NOCONH2, CO2H and =O; C310 cycloalkenyl which is optionally substituted with 13 substituents chosen from the group consisting of OH, C110 alkyl, C312 cycloalkyl, C110 alkoxy, C312 cycloalkoxy, halogen, halo (Cl l0) alkyl, =NOH, =NOCONH2, CO2H and =O; C312 cycloalkyl (Cl l0) alkyl wherein the cycloalkyl portion is substituted with 1 3 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, halogen, halo (C110)alkyl, and =O; said substituted C312 cycloalkyl(C110)alkyl further optionally substi tuted with 13 substituents chosen from the group consisting of OH, C110 alkoxy, C312 cycloalkoxy, =NOH, =NOCONH2, and CO2H; aryl which is substituted with 13 substituents chosen from the group consisting ofcarbamyi, amido, Ci. io alkylamido, C110 dialkylamido, C110 acylamino and Cl l0 alkylsulfonylamino; said substituted aryl further optionally substituted with 13 substituents chosen from the group consisting of C110 alkyl, C312 cycloalkyl, OH, halogen, C110 alkoxy, C3 12cycloalkoxy, NH2, C110 alkylamino, Ci. io dialkylamino, C=NOH, C=NOCONH2, phenyl and benzyl ; ar (C14) alkyl wherein the aryl moiety is substituted with 13 substituents chosen from the group consisting of carboxy, C110 alkylcarboxy, hydroxy(C110) alkoxy, nitro, benzyloxy, heterocyclyl, ar(C110)alkyloxy,aryloxy,amino(C1cycloalkyl(C312)alkyloxy, l0) alkoxy, Cl_lo alkylamino (Cl_lo) alkoxy, heteroaryloxy, heteroar (C110)alkyloxy, heterocyclyloxy, C110 alkoxy and C312 cycloalkoxy ; said alkoxy and cycloalkoxy substituted in one position at the alkyl moiety with hydroxy and said heterocyclyl is optionally substituted with Ci. alkyl and wherein the alkyl moiety of said ar (C14) alkyl is optionally substituted with OH, halogen, Ci. io alkoxy and C312 cycloalkoxy said alkoxy and cycloalkoxy being optionally substituted in one position at the alkyl moiety with hydroxy; and said substituted ar (Ci. alkyl further optionally substituted with 13 substituents chosen from the group consisting of halogen, hydroxy, trihalocarbon, C312cycloalkyl,C110alkoxyandC312cycloalkoxyalkyl, heterocyclyl which is substituted on the carbons or nitrogens of the ring with 1 3 substituents chosen from the group consisting of carbamyl, C110 acylamino and Ci. l0 alkylsulfonylamino; said substituted heterocyclyl further optionally substituted with 13 substituents chosen from the group consisting of C1 l0 alkyl, OH, halogen, C110 alkoxy, C312 cycloalkoxy, alkylamino,C110dialkylamino,amido,C110alkylamido,C110C110 dialkylamido, C=NOH, C=NOCONH2, phenyl and benzyl; heterocyclyl (C1C4) alkyl wherein said heterocyclyl moiety is substituted on the carbons or nitrogens of the ring with 13 substituents chosen from the group consisting of C, 10 acylamino, Ci. io alkylsulfbnylamino, and Ci. alkyl, said Cj. io alkyi substituted with OH, C 10 alkoxy, C312 cycloalkoxy, C312 cycloalkyl, halogen or halo (Ci. io) alkyl; said substituted heterocyclyl (C1C4) alkyl further optionally substituted with 13 substituents chosen from the group consisting alkyl,C312cycloalkyl,OH,halogen,C110alkoxy,C312cycloalkoxy,C110 alkylamino,C110dialkylamino,amido,C110alkylamidoandC110dialkylamido,NH2,C110 heteroaryl, which is substituted with oxo; said substituted heteroaryl further optionally substituted with 13 substituents chosen from the group consisting of Cl l0 alkyl, C3 12cycloalkyl, halogen, nitro, CF3, Ci. io alkoxy and C312 cycloalkoxy ; and heteroaryl (Cl4) alkyl, wherein the heteroaryl moiety is substituted with nitro; said heteroaryl (Ci. alkyl further optionally substituted with 13 substituents chosen from the group consisting alkyl,C312cycloalkyl,halogen,trihalocarbon,C110alkoxyandC312C110 cycloalkoxy; and provided that at least one of R3, R6a, R6b and R8 is B.
19. The compound of claim 17 wherein R3 is A and is ar (C14) alkyl wherein the aryl moiety is optionally substituted with 13 substituents chosen from the group consisting of halogen, nitro, Ci. alkoxy, C312 cycloalkoxy or CF3, and wherein the alkyl moiety is optionally substituted with 13 substituents chosen from the group consisting of OH, halogen, andC312cycloalkoxy.C110alkoxy.
20. The compound of claim 18 wherein said aralkyl is benzyl.
21. The compound of claim 19 wherein the aryl moiety of said benzyl is substituted with 13 substituents chosen from the group consisting of halogen, nitro, CI10 AOXY, C312 cycloalkoxy or CF3.
22. The compound of claim 20 wherein said benzyl is substituted with cyclopentyloxy and methoxy.
23. The compound of claim 17 wherein R6a is A and is hydrogen.
24. The compound of claim 1722 wherein R6b is A and is selected from the group consisting of hydrogen; C18 alkyl which is unbranched or branched and is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, =NOH, =NOCONH2, C02H or =O ; and C38 cycloalkyl which is optionally substituted with OH, alkoxy, cycloalkoxy, halogen, haloalkyl, =NOH, =NOCONH2, CO2H or=O.
25. The compound of claim 1723 wherein R8 is B and is Ci. alkyl which is unbranched or branched and is substituted with 13 substituents chosen from the group consisting of benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino, said benzyloxy, methylenedioxybenzyloxy, methylenedioxyphenyl, pyridylmethoxy, thienylmethoxy and alkylamino optionally substituted with 13 substituents chosen from the group consisting of halogen, Cl l0 alkyl, C312 cycloalkyl, C110 alkoxy, Cg. cycloalkoxy and oxo ;.
26. A compound of claim 1 selected from the group consisting of 6amino3 [ (3 cyclopentyloxy4methoxy) benzyl]8 [ ( 1 (2methoxy) benzyloxy1methyl) ethyl]3Hpurine; 6amino3[(3cyclopentyloxy4methoxy) benzyl]8[(1(3methoxy) benzyloxy1 methyl) ethyl]3Hpurine; 6amino3 [ (3,4dimethoxy) benzyl]8[(1(4methyl) benzyloxy1 methyl) ethyl]3Hpurine; 6amino3[(3cyclopenthyloxy4methoxy)benzyl]8[(1(4 chloro) benzyloxy1methyl) ethyl]3Hpurine; 6amino3 [ (3cyclopentyloxy4 methoxy) benzyl]8 [ (1 (2fluoro) benzyloxy1methyl) ethyl]3Hpurine; 6amino3 [ (3 cyclopentyloxy4methoxy) benzyl]8[(1(3fluoro)benzyloxy1methyl) ethyl]3Hpurine; 6 (3fluoro)benzyloxyamino3[3cyclopentyloxy4methoxy)benzyl]8[(1(3 fluoro) benzyloxy1methyl) ethyl]3Hpurine; 6amino3 [ (3cyclopentyloxy4 methoxy) benzyl]8 [ (l (3, 5dimethoxy) benzyloxy1methyl) ethyl]3Hpurine; 6amino3 [ (3 cyclopentyloxy4methoxy) benzyl]8 [ ( 1 (3,4dimethoxy) benzyloxy1methyl) ethyl]3H purine; 6amino3 [ (3cyclopentyloxy4methoxy) benzyl]8 [ (1 (3,4fluoro) benzyloxy1 methyl) ethyl]3Hpurine ; 6amino3 [ (3cyclopentyloxy4methoxy) benzyl]8 [ (3,4 methylenedioxybenzyloxy1methyl) ethyl]3Hpurine; 6amino3 [ (3cyclopentyloxy4 methoxy) benzyl]8 [(2thienylmethoxy1methyl) ethyl]3Hpurine ; 6amino3 [ (3 cyclopentyloxy4methoxy) benzyl]8 [ (3thienylmethoxy1methyl) ethyl]3Hpurine; 6amino 3 [ (3cyclopentyloxy4methoxy) benzyl]8 [ ( 1 (1oxooctyl) amino1methyl) ethyl]3H purine; 6amino3 (3, 4methylenedioxybenzyl)8 [1 (4fluorobenzyloxy)1methylethyl] 3Hpurine; 6amino3 [ (3cyclopentyloxy4methoxy) benzyl]8 [1 (4pyridylmethoxy)1 methylethyl]3Hpurine; 6ethylamino3 (3benzyloxy4methoxybenzyl)8isopropyl3H purine; 3 [ (3benzyloxy4methoxy) benzyl8 [ (1benyloxy1methyl)ethyl]6ethylamino3H purine; 6Amino3(3cyclopentyloxy4methoxybenzyl)8[1(4methoxybenzyloxy)1 methylethyl]3Hpurine; 6Amino3 (3cyclopentyloxy4methoxybenzyl)8 (1 methylethenyl)3Hpurine; 6Amino8benzyloxymethyl3 (3cyclopentyloxy4methoxy benzyl)3Hpurine; 6amino8[(1benzyloxy1methyl)ethyl]3[(3cyclopentyloxy4 methoxy) benzyl]3Hpurine; 6Amino3(3cyclopentyloxy4methoxybenzyl)8[1(4 fluorobenzyloxy)1methylethyl]3Hpurine;[8(1benzyloxy1methyl)ethyl]3[(3 cyclopentyloxy4methoxy) benzyl]6ethylamino3Hpurine; 6ethylamino8benzyloxymethyl 3 (3cyclopentyloxy4methoxybenzyl)3Hpurine; 6ethylamino3 (3, 4 methylenedioxybenzyl)8isopropyl3Hpurine; 3 (3benzyloxy4methoxybenzyl)6 <BR> <BR> <BR> ethylamino8isopropyl3Hpurine; 6Amino3 (3, 4dimethoxybenzyl)8 [l (4<BR> <BR> <BR> <BR> <BR> fluorobenzyloxy)1methylethyl]3Hpurine; 6 (amino8 (1benzyloxy1methylethyl)3 (3,4 dimethoxybenzyl)3Hpurine; 6amino3[(3benzyloxy4methoxy)benzyl]8[(1benzyloxy1 methyl) ethyl]3Hpurine; 6Amino3(3,4dimethyoxybenzyl)8(1methylethenyl)3Hpurine 6amino3 ( (3benzyloxy4methoxy)bezyt)8isopropyI3Hpunne; 3 (3benzyloxy4nitro benzyl)6ethylamino8isopropyl3Hpurine; 3 [ (3cyclopentyloxy4methoxy) benzyl]6 ethylamino8 (lmethylethenyl)3Hpurine and pharmaceutically acceptable salts thereof.
27. A compound selected from the group consisting of 3ethyl6ethylamino8((3 cyclopentyloxy4hydroxy) benzyl)3Hpurine; 3 [3 (3trimethylsilylethoxymethoxy) cyclopentyloxy4methoxy) benzyl)6ethylamino8isopropyl3Hpurine; 6Ethylamino3 [3 <BR> <BR> <BR> <BR> (furan2ylmethoxy)4methoxybenzyl]8isopropyl3Hpurine;; 6Ethylamino3 (3butoxy 4methoxybenzyl)8isopropyl3Hpurine; 6ethylamino2 (3, 4dimethoxybenzyl)8 isopropyl3Hpurine; 6Amino3 (3cyclopentyloxy4methoxybenzyl)3Hpurine; 3 (3 <BR> <BR> <BR> <BR> cyclopentyloxy4methoxybenzyl)6dimethylamino8isopropyl3Hpurine; 3 (3<BR> <BR> <BR> <BR> <BR> cyclopentyloxy4methoxybenzyl)6 (3cyclopentyloxy4methoxybenzylamino)8isopropyl 3Hpurine; 6ethylamino8isopropyl3 (4methoxybenzyl)3Hpurine; 3 (3 ( (3 hydroxy) cyclopentyloxy)4methoxybenzyl)6ethylamino8isopropyl3Hpurine; 3 (3 cyclopentyloxy4methoxybenzyl)6(NbenzoylNethylamino)8isopropyl3Hpurine;3(4 chlorobenzyl)6cyclopropylamino8isopropyl3Hpurine; 6ethylamino8isopropyl3 [ (4 methoxy3 (4hydroxybutoxy)) benzyl]3Hpurine; 6ethylamino3 (4fluorobenzyl)8 isopropyl3Hpurine; 3 [3 (3hydroxy) cyclopentyloxy)]4methoxv) benzyl)6ethylamino8 isopropyl3Hpurine; 6amino3 (3, 4dimethoxybenzyl)gisopropyl3Hpurine; 6Ethylamino 3 [3cyclopentylmethoxy4methoxybenzyl]8isopropyl3Hpurine; 6ethylamino3 (3 hydroxy4methoxybenzyl)8isopropyl3Hpurine; 6Ethylamino3 [3 (2,2 dimethylaminoethoxy4methoxy)]8isopropyl3Hpurine; 3 [ (3cyclopentyloxy4 methoxy) benzyl]8 [ (1methyl1hydroxy) ethyl]6ethylamino3Hpurine ;; 3 (3 cyclopentyloxy4methoxybenzyl)6((2, 2,2trifluoroethyl) amino)8isopropyl3Hpurine; 6 Ethylamino3 [3 (2,2,2)azabicyclooctan3yloxy)4methoxy]8isopropyl3Hpurine; 6 <BR> <BR> <BR> <BR> Ethylamino3 [3 ( 1methylpiperidin4ylmethoxy)4methoxybenzy]8isopropyl3Hpurine;; 6amino8isopropyl3[(4methoxy3([(4hydroxybutoxy))benzyl]3Hpurine;3{2(4 chlorophenyl)ethyl]6ethylamino8isopropyl3Hpurine; 3(4chlorobenzyl)6((1 hydroxy)cyclopentylamino)8isopropyl3Hpurine;3(4chlorobenzyl)6cyclopentylamino8 isopropyl3Hpurine; 6amino3 6 Ethylamino3 [ (exo8methyl8azabicyclo(3,2,1)octan3yloxy)4methoxybenzy]8 isopropyl3Hpurine ;; 3 (4chlorophenyl)6ethylamino8isopropyl3Hpurine; 6ethylamino 3 [ (3hydroxy4methoxy) benzyl]8 [ (lhydroxylmethyl) ethyl] 3Hpurine; 6Ethylamino <BR> <BR> <BR> 3 [ (3pyridin4ylmethoxy) Noxide4methoxy]8isopropyl3Hpurine;3 [3Cyclohexanyl4<BR> <BR> <BR> <BR> <BR> oxy4methoxybenzyl]6ethylamino8isopropyl3Hpurine ; 3 (4chlorobenzyl)2,6 di (ethylamino)8isopropyl3Hpurine; 6amino3(3hydroxy4methoxy)benzyl)8 isopropyl3Hpurine; 6amino3 [3 (4hydroxybutoxy4methoxy) benzyl]8 (1hydroxy1 methylethyl)3Hpurine; 6amino3 (4chlorobenzyl)8isopropyl3Hpurine; 6amino3 cyclopentylmethyl8isopropyl3Hpurine; 8cyclopropyl3ethyl6ethylamino3Hpurine; 6 <BR> <BR> <BR> Ethylamino8isopropyl3 [3 (pyridin4ylmethoxy)4methoxybenzyl]3Hpurine ; 6<BR> <BR> <BR> <BR> <BR> Ethylamino3 (1oxopyridin4ylmethyl)8isopropyl3Hpurine;6amino3 [ (3hydroxy4 methoxy)benzyl)]]8 [ (1hydroxy1methyl) ethyl]3Hpurine, 3 (3COOmethyl4 <BR> <BR> <BR> methoxbenzyl)6ethylamino8isopropyl3Hpurine, 3 (3piperadine4methoxbenzyl)6<BR> <BR> <BR> <BR> <BR> ethylamino8isopropyl3Hpurine,, 3 (3COOH4methoxbenzyl)6ethylamino8isopropyl 3Hpurine, 3 (3pyrrolebenzyl)6ethylamino8isopropyl3Hpurine, 3butyl6pentylamino 8cyclopropyl3Hpurine, 3butyl6cyclopentylamino8cyclopropyl3Hpurine, 3butyl6 dimethylamino8cyclopropyl3Hpurine and pharmaceutically acceptable salts thereof.
28. A method for selectively effecting PDE IV inhibition, compared to PDE III inhibition, in a patient suffering from a disease state selected from the group consisting of asthma, allergies, inflammation, depression, Alzheimer's disease, vascular dementia, multiinfarct demetia, a disease caused by Human Immunodeficiency Virus and disease states associated with abnormally high physiological levels of inflammatory cytokines, said method comprising the administration of a compound of claims 126.
29. A pharmaceutical composition comprising a compound of claims 126 and a pharmaceutically acceptable excipient.
Description:
INTERNATIONALSEARCHREPORTInternationalapplicationNo. PCT/US00/08525 C(Continuation).DOCUMENTSCONSIDEREDTOBERELEVANT Category*Citationofdocument,withindication,whereappropriate, oftherelevantpassagesRelevanttoclaimNo. Y,PUS5,939,422A(CAVALLAETAL)17August1999(17.08. 99), 1,7,9,14,15, see8-cyclopropyland3-cyclohexylmethyl,e.g.,Examples3,7and17, 22,23 A8,Table1,10A 13first,Example15.--- 2-6,10-13,16, 18-21,25--26 YUS5,744,473A(CHASINETAL)28April1998(28.04.98),see9,14,15,17 ,22, Example1(i)andl(ii).23 A 1-7,10-13,18-21, 24-25 X,PUS5,994,629A(BOJSENETAL)30November1999(30.11.99),9,14,15 seespeciesatcolumn26,line65. A1-7,10-13,17-23, 25-26 INTERNATIONALSEARCHREPORTInternationalapplicationNo. PCT/US00/08525 BoxIObservationswherecertainclaimswerefoundunsearchable(Cont inuationofitem1offirstsheet) Thisinternationalreporthasnotbeenestablishedinrespectofcerta inclaimsunderArticle17(2)(a)forthefollowingreasons: a ClaimsNos.: becausetheyrelatetosubjectmatternotrequiredtobesearchedbythi sAuthority,namely: 2. a Claims Nos: becausetheyrelatetopartsoftheinternationalapplicationthatdon otcomplywiththeprescribedrequirementstosuch anextentthatnomeaningfulinternationalsearchcanbecarriedout,s pecifically: 3.nXClaimsNos.:8,16,24,27,28 becausetheyaredependentclaimsandarenotdraftedinaccordancewit hthesecondandthirdsentencesofRule6.4(a). Box11Observationswhereunityofinventionislacking(Continuation ofitem2offirstsheet) ThisInternationalSearchingAuthorityfoundmultipleinventionsin thisinternationalapplication,asfollows: PleaseSeeExtraSheet. 1.nuAsallrequiredadditionalsearchfeesweretimelypaidbytheappl icant,thisinternationalsearchreportcoversallsearchable claims. 2.jAsallsearchableclaimscouldbesearchedwithouteffortjustifyi nganadditionalfee,thisAuthoritydidnotinvitepayment ofanyadditionalfee. 3.aAsonlysomeoftherequiredadditionalsearchfeesweretimelypaid bytheapplicant,thisinternationalsearchreportcovers onlythoseclaimsforwhichfeeswerepaid,specificallyclaimsNos.: 4.Norequiredadditionalsearchfeesweretimelypaidbytheapplicant .Consequently,thisinternationalsearchreportis restrictedtotheinventionfirstmentionedintheclaims;itiscovere dbyclaimsNos.: RemarkonProtestTheadditionalsearchfeeswereaccompaniedbytheap plicant'sprotest. No protestaccompaniedthepaymentofadditionalsearchfees. INTERNATIONALSEARCHREPORTInternationalapplicationNo. PCT/US00/08525 A.CLASSIFICATIONOFSUBJECTMATTER: IPC(7): C07D473/18,473/34,473/22,473/24;A61K31/52,31/522;A61P11/063, 37/08,25/24,31/18,25/28,29/00 BOXII.OBSERVATIONSWHEREUNITYOFINVENTIONWASLACKING ThisISAfoundmultipleinventionsasfollows: GroupI,claims1-7,25 Adenines Group11,claims9-15Guaninesandthioguanines GroupIII,claims17-23Dithiotheophyllines TheinventionslistedasGroups1-111donotrelatetoasingleinventiv econceptunderPCTRule13.1because,under PCTRule13.2,theylookthesameorcorrespondingtechnicalfeaturesf orthefollowingreasons:Eachgrouphasa specialtechnicalfeature(Adenine,Guanine/thioguanineandDithot heophyllinerespectively).Therearenorequired structuralfeaturespresentinallthreegroups.



 
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