Field of the Invention The invention relates to a series of N-heterocyclic compounds and derivatives useful as inhibitors of nitric oxide synthase (NOS) and to methods of therapy for various diseases employing those compounds.

Background of the Invention Nitrogen monoxide (NO) has been implicated in a number of diverse physiological processes, including smooth muscle relaxation, platelet inhibition, nerve transmission, immune regulation and penile erection. Nitric oxide is produced under various conditions by virtually all nucleated mammalian cells. A number of pathologies are ascribed to abnormalities in NO production including stroke, insulin dependent diabetes, septic shock-induced hypotension, rheumatoid arthritis and multiple sclerosis. Nitric oxide is synthesized in biological tissues by an enzyme called nitric oxide synthase (NOS) which uses NADPH and molecular oxygen to oxidize L-arginine to citrulline and nitric oxide.

Nitric oxide synthase (NOS) exists in at least three isoforms, which fall into two primary categories: constitutive and inducible. Two constitutive isoforms, which are calcium and calmodulin dependent, have been identified, and one inducible isoform has been identified.

The constitutive isoforms are (1) a neuronal isoform, NOS-1 or nNOS, which is found in the brain and skeletal muscles and (2) an endothelial isoform, NOS-3 or eNOS, which is expressed in the endothelium of blood vessels, the epithelium of the bronchial tree and in the brain. These constitutive isoforms are not the target of the NOS inhibitors of the present invention.

The inducible isoform (NOS2 or iNOS) is expressed in virtually all nucleated mammalian cells following exposure to inflammatory cytokines or lipopolysaccharide. Its presence in macrophages and lung epithelial cells is particularly noteworthy. The inducible isoform is neither stimulated by calcium nor blocked by calmodulin antagonists. It contains several tightly bound co-factors, including FMN, FAD and tetrahydrobiopterin.

Nitric oxide generated by the inducible form of NOS has been implicated in the pathogenesis of inflammatory diseases. In experimental animals, hypotension induced by lipopolysaccharide or tumor necrosis factor a can be reversed by NOS inhibitors. Conditions

which lead to cytokine-induced hypotension include septic shock, hemodialysis and interleukin therapy in cancer patients. It is expected that an iNOS inhibitor would be effective in treating cytokine-induced hypotension. In addition, recent studies have suggested a role for NO in the pathogenesis of inflammation, and NOS inhibitors would therefore have beneficial effects on inflammatory bowel disease, cerebral ischemia and arthritis. Inhibitors of NOS may also be useful in treating adult respiratory distress syndrome (ARDS) and myocarditis, and they may be useful as adjuvants to short term immunosuppression in transplant therapy.

The diversity and ubiquity of NO function in physiology make the specific therapeutic targeting of NO-related phenomena an important consideration. Since endogenous NO production is the result of the actions of related but distinct isozymes, the differential inhibition of NOS isozymes allows more selective therapy with fewer side effects.

SUMMARY OF THE INVENTION In one aspect, the invention is directed to compounds of formula (I), formula (II) and formula (III): wherein: Ais -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2]2, -N(R1)C(O)R2, -N(R16)C(O)R2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; each X, Y and Z are independently N or C(R19);

each U is N or C(R5), provided that U is N only when X is N and Z and Y are CR IS; V is N(R4), S, O or C(R4)H; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -(C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl,

dialkylaminocarbonyl and -C(=NR18)-NH2; or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -[Co-C8 alkyl]-C(O)ORr6, -[C0-C8 alkyl]-C(H)[C(O)OR16]2, and -[C0-C8 alkyl]-C(O)N(R)R 6; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1)-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)rR22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl;

each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to compounds of formula (IV): wherein: AA is an amino acid; X, Y and Z are independently N or C(R'9); U is N or C(R5), provided that U is N only when X is N and Z and Y are CR 59; Wis N or CH; R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl;

or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -[Co-C8 alkyl]-C(O)ORr6, -[C0-C8 alkyl]-C(H)[C(O)ORr6]2, and -[C0-C8 alkyl]-C(O)N(R)R56; each R9 is independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R19 is hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and t is zero, one or two; as a single isomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to compounds of formula (Va), formula (Vb) or formula (Vc): wherein B is a fused 5-or 6-membered optionally substituted carbocyclyl or heterocyclyl; and wherein: A is -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2 ]2, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; each X and Y are independently N or C(R19);

V is N(R4), S, O or C(R4)H; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -(C2-C8 alkynyl]-R9, -jC2-C8 alkyl]-R° (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR1 8)-NH2;

or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R50, -[C1-C8 alky-R11, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1 )-R23-C(o)oR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl,

halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -S02R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to a compound of formula (Vla), formula (Vlb) or formula (Vlc): wherein B is a fused 5-or 6-membered optionally substituted carbocyclyl or heterocyclyl; and wherein: A is -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2]2, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; each X and Z are independently N or C(R19);

V is N(R4), S, O or C(R4)H; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R5)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)0R2, -N(R1)R21 -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR18)-NH2;

or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R')R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R°, -[C-C8 alkyl]-R5, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1)-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)rR22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl,

halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to compounds of formula (Vlla), formula (Vllb) or formula (Vllc): wherein: A is -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2 ]2, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; each X, Y and Z are independently N or C(R 19); each U is N or C(R5), provided that U is N only when X is N and Z and Y are CR 19;

V is N(R4), S,OorC(R4)H; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[Co-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR18)-NH2;

or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR116, -N(R16)C(O)R16, -[C0-C8 alkyl]-C(O)OR16, -[C0-C8 alkyl]-C(H)[C(O)OR16]2, and -[C0-C8 alkyl]-C(O)N(R1)R16; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryt, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1)-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl;

each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to a compound of formula (VIII): wherein two of X, Y and Z are nitrogen and the third is CH.

In another aspect, the invention is directed to compounds of formula (IXa), formula (IXb) or formula (IXc): wherein: is a solid support;

L is a linker residue; each X, Y and Z are independently N or C(R19);

each U is N or C(R5), provided that U is N only when X is N and Z and Y are CR 19; V is N(R4), S, O or C(R4)H; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R2 is independently chosen from the group consisting of hydrogen, optionally substituted C,-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C 1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[CI-C8 alkyl]-N(R1)R2, -[C -C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C6 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR18)-NH2; or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or

R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -[C0-C8 alkyl]-C(O)OR16, -[C0-C8 alkyl]-C(H)[C(O)OR16]2, and -[C0-C8 alkyl]-C(O)N(R1)R16; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1)-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)fR22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted

aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; as a single stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention is directed to a pharmaceutical composition comprising a compound of formula (I), formula (II) or formula (III) as described above and a pharmaceutically acceptable carrier.

In another aspect, the invention is directed to a process for synthesizing compounds of formula (I), formula (II) and formula (III): wherein: A is -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2]2, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; each X, Y and Z are independently N or C(R19);

each U is N or C(R5), provided that U is N only when X is N and Z and Y are CR19; V is N(R4), S, or O; each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C,-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substututed by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl,

dialkylaminocarbonyl and -C(=NR18)-NH2; or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -[C0-C8 alkyl]-C(O)OR16, -[C0-C8 aIkyI]-C(H)[C(O)OR12, and -[C0-C8 alkyl]-C(O)N(R1)R16; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R, acyl, -C(O)R8, -C(O)-[CI-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(o)-N(R1 )-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl;

each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; comprising the sequential steps of: (a) reacting one equivalent of a compound of formula (XI): where W is N or CH; with about one equivalent of an chloro-substituted compound of formula (XII): where X, Y and Z are independently N or C(R 19); U is N or C(R5), provided that U is N only when Xis N and Z and Y are CR 19, and provided that X, Y and Z can not all be C(R 19) when U is C(R5); R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -tC0-C8 alkyl]-C(O)OR 16, -[C0-C8 alkyl]-C(H)[C(O)OR10]2, and -[C0-C8 alkyl]-C(O)N(R1)R16;

each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl or cycloalkyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; and each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; to produce a compound of formula (XIII): (b) reacting said compound of formula (XIII) with a compound of formula (XIVa), formula (XlVb), or formula (XIVc):

wherein: A is -R1, -OR1, -C(O)N(R1)R2, -P(O)[N(R1)R2]2, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1, -SO2NHC(O)R1, -NHSO2R22, -SO2N(R1)H, -C(O)NHSO2R22, and -CH=NOR1; V is N(R4), S, or O; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two;

is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR18)-NH2; or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, acyl, -C(O)R8, -C(O)-[C1-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryt, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl,

aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1 )-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl; each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; to produce a compound of formula (I), formula (II) or formula (III).

In another aspect, the invention is directed to synthesizing a compound of formula (I), formula (II) and formula (III): wherein: A is -C(O)N(R1a)R2; each X, Y and Z are independently N or C(R 19); each U is N or C(R5), provided that U is N only when X is N and Z and Y are CR 19; V is N(R4), S, O or C(R4)H;

each W is N or CH; Q is chosen from the group consisting of a direct bond, -C(O)-, -O-, -C(=N -R1)-, -S(O)t, and -N(R6)-; m is zero or an integer from 1 to 4; n is zero or an integer from 1 to 3; q is zero or one; r is zero or one, provided that when Q and V are heteroatoms, m, q, and r cannot all be zero; when A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (where t is zero), or -NHSO2R22, n, q, and r cannot all be zero; and when Q is a heteroatom and A is -OR1, -N(R1)C(O)R2, -N(R16)C(O)OR2, -N(R1)R21, -N(R16)C(O)N(R1)R16, -S(O)tR1 (when t is zero) or -NHSO2R22, m and n cannot both be zero; t is zero, one or two; is an optionally substituted N-heterocyclyl; is an optionally substituted carbocyclyl or optionally substituted N-heterocyclyl; Ria is hydrogen; each R1 and R2 are independently chosen from the group consisting of hydrogen, optionally substituted C1-C20 alkyl, optionally substituted cycloalkyl, -[C0-C8 alkyl]-R9, -[C2-C8 alkenyl]-R9, -[C2-C8 alkynyl]-R9, -[C2-C8 alkyl]-R10 (optionally substituted by hydroxy), -[C1-C8]-R11 (optionally substituted by hydroxy), optionally substituted heterocyclyl; or R1 and R2 together with the nitrogen atom to which they are attached is an optionally substituted N-heterocyclyl; R3 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, optionally substituted aryl, haloalkyl, -[C1-C8 alkyl]-C(O)N(R1)R2, -[C1-C8 alkyl]-N(R1)R2, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R10, -[C1-C8 alkyl]-R11, and heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of halo, alkyl, alkoxy and imidazolyl); or when Q is -N(R6)- or a direct bond to R3, R3 may additionally be aminocarbonyl, alkoxycarbonyl, alkylsulfonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl and -C(=NR16)-NH2;

or -Q-R3 taken together represents -C(O)OH, -C(O)N(R1)R2, -C(=NH)-N(R1)R2 or R4 is chosen from the group consisting of hydrogen, alkyl, aryl, aralkyl and cycloalkyl; provided that when A is -R1 or -OR1, R4 cannot be hydrogen, and when V is CH, R4 may additionally be hydroxy; R5 is chosen from the group consisting of hydrogen, halo, alkyl, haloalkyl, optionally substituted aralkyl, optionally substituted aryl, -OR16, -S(O)t-R16, -N(R16)R21, -N(R16)C(O)N(R1)R16, -N(R16)C(O)OR16, -N(R16)C(O)R16, -[C0-C8 alkyl]-C(O)OR16, -[C0-C8 alkyU-C(H)[C(O)OR12, and -[C0-C8 alkyl]-C(O)N(R1)R16; R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8, -[C2-C8 alkyl]-R°, -[C1-C8 alkyl]-R, acyl, -C(O)R8, -C(O)-[CI-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, -C(O)-N(R1)-R23-C(O)OR1; each R8 and R9 are independently chosen from the group consisting of haloalkyl, cycloalkyl (optionally substituted with halo, cyano, alkyl or alkoxy), carbocyclyl (optionally substituted with one or more substituents selected from the group consisting of halo, alkyl and alkoxy), and heterocyclyl (optionally substituted with alkyl, aralkyl or alkoxy); each R10 is independently chosen from the group consisting of halo, alkoxy, optionally substituted aryloxy, optionally substituted aralkoxy, optionally substituted -S(O)t-R22, acylamino, amino, monoalkylamino, dialkylamino, (triphenylmethyl)amino, hydroxy, mercapto, alkylsulfonamido; each R11 is independently chosen from the group consisting of cyano, di(alkoxy)alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl and dialkylaminocarbonyl; each R12, R13, R14, R15, R17, and R20 are independently hydrogen or alkyl;

each R16 is independently hydrogen, alkyl, optionally substituted aryl, optionally subsituted aralkyl or cycloalkyl; R18 is hydrogen, NO2, or toluenesulfonyl; each R19 is independently hydrogen, alkyl (optionally substituted with hydroxy), cyclopropyl, halo or haloalkyl; each R21 is independently hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, -C(O)R22 or -SO2R22; or R21 taken together with R1 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; or R21 taken together with R16 and the nitrogen to which they are attached is an optionally substituted N-heterocyclyl; each R22 is independently alkyl, cycloalkyl, optionally substituted aryl or optionally substituted aralkyl; and R23 is an amino acid residue; comprising photolytically cleaving the compound of formula (IXa), formula (IXb) or formula (IXc): wherein: U, V, W, X, Y, and Z are as defined above; R2, R3, R12, R13, R14, R15, R17, and R20 are as defined above; is a solid support; and L is a linker residue of formula (IX):

wherein the unsatisfied valence on the right of the formula represents the point of attachment to the solid substrate and the unsatisfied valence on the left of the formula represents the point of attachment to the ligand; to form the compound of formula (I), formula (II) and formula (III) as defined above.

In another aspect, the invention is directed to a method of treating a condition resulting from an abnormality in nitric oxide production which comprises administering to a mammal having a condition resulting from an abnormality in nitric oxide production a therapeutically effective amount of a compound of formula (I), formula (II), formula (III), formula (IV), formula (Va), formula (Vb), formula (Vc), formula (Vla), formula (Vlb), formula (Vlc), formula (Vlla), formula (Vllb) or formula (Vllc) as defined above.

Detailed Description of the Invention Definitions As used in this specification and appended claims, unless specified to the contrary, the following terms have the meaning indicated: "Alkyl" refers to a straight or branched hydrocarbon chain radical consisting solely of carbon and hydrogen atoms, containing no unsaturation, having from one to eight carbon atoms, and which is attached to the rest of the molecule by a single bond, e.g., methyl, ethyl, n-propyl, 1-methylethyl (iso-propyl), n-butyl, n-pentyl, 1,1 -dimethylethyl (t-butyl), and the like. Alkyl radicals having more than eight carbon atoms are indicated herein by the notation "[Cx-Cy alkyl]" where x and y indicate the number of carbons present. Alkyl radicals may be optionally substituted by one or more substituents independently selected from the group consisting of haio, hydroxy, alkoxy, carboxy, cyano, carbonyl, alkoxycarbonyl, cyano, amino, monoalkylamino, dialkylamino, nitro, alkylthio, amidino, aryl, heterocyclyl, aryloxy, aralkoxy, acylamino, aminocarbonyl, monoalkylaminocarbonyl, and dialkylaminocarbonyl.

"Alkenyl" refers to a straight or branched chain monovalent or divalent radical consisting solely of carbon and hydrogen, containing at least one double bond and having from one to

eight carbon atoms, e.g., ethenyl, prop-1-enyl, but-1-enyl, pent-1-enyl, penta-1,4-dienyl, and the like.

"Alkynyl" refers to a straight or branched chain monovalent or divalent radical consisting solely of carbon and hydrogen, containing at least one triple bond and having from one to eight carbon atoms, e.g., ethynyl, prop-1-ynyl, but-1-ynyl, pent-1-ynyl, pent-3-ynyl, and the like.

"Alkoxy" refers to a radical of the formula ORa where Ra is an alkyl radical as defined above, e.g., methoxy, ethoxy, propoxy, and the like.

"Alkoxycarbonyl" refers to a radical of the formula -C(O)ORa where Ra is an alkyl radical as defined above, e.g., methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, and the like.

"Alkoxycarbonylalkyl" refers to a radical of the formula -Ra-C(O)ORa where each Ra is independently an alkyl radical as defined above, e.g., 2-(methoxycarbonyl)ethyl, 3-(ethoxycarbonyl)propyl, 4-(n-propoxycarbonyl)butyl, and the like.

"Alkylsulfonylamino" refers to a radical of the formula -N(H)S(O) 2-Ra where Ra is an alkyl radical as defined above, e.g., methylsulfonylamino, ethylsulfonylamino, and the like.

"Alkylsulfonyl" refers to a radical of the formula -S(O) 2-Ra where Ra is an alkyl radical as defined above, e.g., methylsulfonyl, ethylsulfonyl, and the like.

"Alkylthio" refers to a radical of the formula -S-Ra where Ra is an alkyl radical as defined above, e.g., methylthio, ethylthio, n-propylthio, and the like.

"Amidino" refers to a radical of the formula -C(NH)-NH 2.

"Amino" refers to a radical of the formula -NH 2.

"Aminocarbonyl" refers to a radical of the formula -C(O)NH 2.

"Aminosulfonyl" refers to a radical of the formula -S(O) 2NH2.

"Aryl" refers to a phenyl or naphthyl radical. The aryl radical may be optionally substituted by one or more substituents selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, nitro, cyano, cycloalkyl, hydroxyalkyl, alkoxyalkyl, phenoxyalkyl, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonyamino, amino, monoalkylamino, dialkylamino, monophenylamino, monophenylalkylamino, sulfonylamino, akylsulfonylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, monophenylaminoalkyl, monophenylalkylaminoalkyl, acyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, and dialkylaminocarbonylalkyl, as defined herein.

"Aralkyl" refers to a radical of the formula -RaRb where R9 is an alkyl radical as defined above and Rb is an aryl radical as defined above, e.g., benzyl, and the like. The aryl radical may be optionally substituted as described above.

"Aryloxy" refers to a radical of the formula -ORb where Rb is an aryl radical as defined above, e.g., phenoxy and naphthoxy, and the like. The aryl radical may be optionally substituted as described above.

"Aryloxycarbonyl" refers to a radical of the formula -C(O)OR b where Rb is an aryl radical as defined above, e.g., phenoxycarbonyl.

"Aralkoxy" refers to a radical of the formula -OR where Roc is an aralkyl radical as defined above, e.g., benzyloxy, and the like. The aralkyl radical may be optionally substituted as described above.

"Aralkoxycarbonyl" refers to a radical of the formula -C(O)OR where Roc is an aralkyl radical as defined above, e.g., benzyloxycarbonyl, and the like. The aralkyl radical may be optionally substituted as described above.

"Arylaminocarbonyl" refers to a radical of the formula -C(O)N(R b)H where Rb is an aryl radical as defined above, e.g., phenylaminocarbonyl, and the like. The aryl radical may be optionally substituted as described above.

"Arylaminosulfonyl" refers to a radical of the formula -S(O) 2N(Rb)H where Rb is an aryl radical as defined above, e.g., phenylaminosulfonyl, and the like. The aryl radical may be optionally substituted as described above.

"Arylsulfonyl" refers to a radical of the formula -S(O) 2-Rb where Rb is an aryl radical as defined above, e.g., phenylsulfonyl, and the like. The aryl radical may be optionally substituted as described above.

"Arylsulfonylaminocarbonyl" refers to a radical of the formula -C(O)N(H)S(O) 2Rb where Rb is an aryl radical as defined above, e.g., phenylsulfonylaminocarbonyl, and the like. The aryl radical may be optionally substituted as described above.

"Acyl" refers to a radical of the formula -C(O )~Ra and -C(O)Rb where Ra is an alkyl radical as defined above and Rb is an aryl radical as defined above, e.g., acetyl, propionyl, benzoyl, and the like.

"Acylamino" refers to a radical of the formula -N(H)-C(O)-Ra and -N(H)-C(O)-Rb where Ra is an alkyl radical as defined above and Rb is an aryl radical as defined above, e.g., acetylamino, benzoylamino and the like.

"Alkylene" refers to straight or branched chain divalent radical consisting solely of carbon and hydrogen, containing no unsaturation and having from one to eight carbon atoms,

e.g., methylene, ethylene, propylene, n-butylene, and the like. The alkylene radical may be optionally substituted by one or more substituents selected from the group consisting of alkyl, hydroxy, -N(R16)R21 or -C(O)N(R1)R16 where R1, R16 and R21 are as defined above in the Summary of the Invention.

"Amino acid" refers to a divalent radical of the formula -N(R 1)-R23-C(of where R1 is as described above in the Summary of the Invention for R1 and R23 is an amino acid residue.

"Amino acid residue" refers to the alkylene chain between the nitrogen atom and the carboxy group, which is substituted by the various "side chains" of the known amino acids. For example, amino acid residues of a-amino acids include the a-carbon (to which the carboxy group and the nitrogen atom is attached) and the side chain. For example, the amino acid residue of alanine is -C(CH3)-; the amino acid residue of serine is -C(CH2OH)-, and so forth.

The term "amino acid" is therefore intended to include a-amino acids, amino acids, y-amino acids, and so forth, and all optical isomers thereof. Examples of such amino acids include alanine, asparagine, N-P-trityl-asparagine, aspartic acid, aspartic acid- Ft-butyl ester, arginine, N6-Mtr-arginine, cysteine, S-trityl-cysteine, glutamic acid, glutamic acid- y-t-butyl ester, glutamine, N-y-trityl-glutamine, glycine, histidine, ltm-trityl-histidine, isoleucine, leucine, lysine, Ne-Boc-lysine, methionine, phenylalanine, proline, serine, O-t-butyl-serine, threonine, tryptophan, Nin-Boc-tryptophan, tyrosine, valine, sarcosine, L-alanine, chloro-L-alanine, 2- aminoisobutyric acid, 2-(methylamino)isobutyric acid, D,L-3-aminoisobutyric acid, aminoisobutyric acid, (S)-(+)-2-aminoisobutyric acid, D-leucine, L-leucine, D-norvaline, L- norvaline, L-2-amino-4-pentenoic acid, D-isoleucine, L-isoleucine, D-norleucine, 2,3- diaminopropionic acid, L-norleucine, D,L-2-aminocaprylic acid, palanine, D,L-3-aminobutyric acid, 4-aminobutyric acid, 4-(methylamino)butyric acid, 5-aminovaleric acid, 5-aminocaproic acid, 7-aminoheptanoic acid, 8-aminocaprylic acid, 11-aminodecanoic acid, 12- aminododecanoic acid, carboxymethoxylamine, D-serine, D-homoserine, L-homoserine, D- allothreonine, L-allothreonine, D-threonine, L-threonine, D, LA-amino-3-hydroxybutyric acid, D- ,L-3-hydroxynorvaline, (3S,4S)-(-)-statine, 5-hydroxy-D,L-lysine, 1-amino-1- cyclopropanecarboxylic acid, l-amino-l -cyclopentanecarboxylic acid, 1-amino-1- cyclohexanecarboxylic acid, 5-amino-1 ,3-cyclohexadiene-1-carboxylic acid, 2-amino-2- norbornanecarboxylic acid, (S)-(-)-2-azetidinecarboxylic acid, cis4-hydroxy-D-proline, cis-4- hydroxy-L-proline, frans-4-hydroxy-L-proline, 3,4-dehydro-D,L-proline, 3,4-dehydro-L-proline, D- pipecolinic acid, L-pipecolinic acid, nipecotic acid, isonipecotic acid, mimosine, 2,3- diaminopropionic acid, D,L-2,4-diaminobutyric acid, (S)-(+)-diaminobutyric acid, D-ornithine, L- ornithine, 2-methylornithine, N-e-methyl-L-lysine, N-methyl-D-aspartic acid, D,L-2-

methylglutamic acid, D,L-2-aminoadipic acid, D-2-aminoadipic acid, L-2-aminoadipic acid, (+/-)- 3-aminoadipic acid, D-cysteine, D-penicillamine, L-penicillamine, D,L-homocysteine, S-methyl-L- cysteine, L-methionine, D-ethionine, L-ethionine, S-carboxymethyl-L-cysteine, (S)-(+)-2- phenylglycine, (R)-(-)-2-phenylglycine, N-phenylglycine, N-(4-hydroxyphenyl)glycine, D- phenylalanine, thienylalanine, (S)-(-)indoline-2-carboxylic acid, a-methyl,D,L-phenylalanine, P- methyl-D,L-phenylalanine, D-homophenylalanine, L-homophenylalanine, D,L-2- fluorophenylglycine, D,L-2-fluorophenylalanine, D,L-3-fluorophenylalanine, D,L4- fluorophenylalanine, D,L4-chlorophenylalanine, L-4-chlorophenylalanine, 4-bromo-D, L- phenylalanine, 4-iodo-D-phenylalanine, 3,3',5-triiodo- L-thyronine, (+)-3,3',5-triiodo- L-thyronine, D-thyronine, L-thyronine, D,L-m-tyrosine, D4-hydroxyphenylglycine, D-tyrosine, L-tyrosine, O-methyl-L-tyrosine, 3-fluoro-D,L-tyrosine, 3-iodo-L-tyrosine, 3-nitro-L-tyrosine, 3,5-diiodo-L- tyrosine, D,L-dopa, L-dopa, 2,4,5-trihydroxyphenyl-D,L-alanine, 3-amino-L-tyrosine, 4-amino-D- phenylalanine, 4-amino-L-phenylalanine, 4-amino-D, L-phenylalanine, 4-nitro-L-phenylalanine, 4-nitro-D,L-phenylalanine, 3,5-dinitro-L-tyrosine, D, L-a-methyityrosine, L-a-methyltyrosine, (-)-3-(3,4-dihydroxyphenyl)-2-methyl-L-alanine, D,L-threo-3-phenylserine, trans4- (aminomethyl)cyclohexane carboxylic acid, 4-(aminomethyl)benzoic acid, D ,L-3-aminobutyric acid, 3-aminocyclohexane carboxylic acid, cis-2-amino-1-cyclohexane carboxylic acid, y-amino- >(p-chlorophenyl)butyric acid (Baclofen), D,L-3-aminophenylpropionic acid, 3-amino-3-(4- chlorophenyl)propionic acid, 3-amino-3-(2-nitrophenyl)propionic acid, and 3-amino4,4,4- trifluorobutyric acid.

"Carbocyclyl" refers to a stable 3- to 15-membered ring radical consisting solely of carbon and hydrogen atoms. For purposes of this invention, the carbocyclyl radical may be a monocyclic, bicyclic or tricyclic ring system, and may include fused or bridged ring systems, and the ring system may be partially or fully saturated or aromatic, and the carbon atoms in the ring system may be optionally oxidized. Examples of such carbocyclyl radicals include, but are not limited to, cycloalkyl radicals (as defined herein), norbornane, norbornene, adamantyl, bicyclo[2.2.2]octane, phenyl, naphthalenyl, indanyl, indenyl, azulenyl, fluorenyl, anthracenyl, and the like. The carbocyclyl ring may be substiuted by R6 as described above in the Summary of the Invention, or by one or more substituents selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, nitro, cyano, cycloalkyl, hydroxyalkyl, alkoxyalkyl, phenoxyalkyl, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonyamino, amino, monoalkylamino, dialkylamino, monophenylamino, monophenylalkylamino, sulfonylamino, akylsulfonylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, monophenylaminoalkyl,

monophenylalkylaminoalkyl, acyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, and dialkylaminocarbonylalkyl, as defined herein.

"Cycloalkyl" refers to a stable 3- to lO-membered monocyclic or bicyclic radical which is saturated, and which consist solely of carbon and hydrogen atoms, e.g., cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, decalinyl and the like. Unless otherwise stated specifically in the specification, the term "cycloalkyl" is meant to include cycloalkyl radicals which are optionally substituted by one or more substituents independently selected from the group consisting of alkyl, halo, hydroxy, amino, cyano, nitro, alkoxy, carboxy and alkoxycarbonyl.

"Carboxy" refers to the radical of the formula -C(O)OH.

"Carboxyalkyl" refers to a radical of the formula -Ra-C(O)OH where Ra is an alkyl radical as defined above, e.g., carboxymethyl, 2-carboxyethyl, 3-carboxypropyl, and the like.

"Di(alkoxy)alkyl" refers to a radical of the formula -Ra(-ORa)2 where each Ra is independently an alkyl radical as defined above and where the ORa groups may be attached to any carbon in the Ra group, e.g., 3,3-dimethoxypropyl, 2,3-dimethoxypropyl, and the like.

"Dialkylamino" refers to a radical of the formula -N(Ra)Ra where each Ra is independently an alkyl radical as defined above, e.g., dimethylamino, diethylamino, (methyl)(ethyl)amino, and the like.

"Dialkylaminocarbonyl" refers to a radical of the formula -C(O)N(Ra)Ra where each Ra is independently an alkyl radical as defined above, e.g., dimethylaminocarbonyl, methylethylaminocarbonyl, diethylaminocarbonyl, dipropylaminocarbonyl, ethylpropylaminocarbonyl, and the like.

"Dialkylaminosulfonyl" refers to a radical of the formula -S(O) 2N(Ra)Ra where each Ra is independently an alkyl radical as defined above, e.g., dimethylaminosulfonyl, methylethylaminosulfonyl, diethylaminosulfonyi, dipropylaminsulfonyl, ethylpropylaminosulfonyl, and the like.

"Halo" refers to bromo, chloro, iodo or fluoro.

"Haloalkyl" refers to an alkyl radical, as defined above, that is substituted by one or more halo radicals, as defined above, e.g., trifluoromethyl, difluoromethyl, trichloromethyl, 2,2,2-trifluoroethyl, 1 -fluoromethyl-2-fluoroethyl, 3-bromo-2-fluoropropyl, 1-bromomethyl-2-bromoethyl, and the like.

"Haloalkoxy" refers to a radical of the formula -ORd where Rd is an haloalkyl radical as defined above, e.g., trifluoromethoxy, difluoromethoxy, trichloromethoxy, 2,2,2-trifluoroethoxy,

1 -fluoromethyl-2-fluoroethoxy, 3-bromo-2-fluoropropoxy, 1 -bromomethyl-2-bromoethoxy, and the like.

"Heterocyclyl" refers to a stable 3- to 15-membered ring radical which consists of carbon atoms and from one to five heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur. For purposes of this invention, the heterocyclyl radical may be a monocyclic, bicyclic or tricyclic ring system, which may include fused or bridged ring systems; and the nitrogen, carbon or sulfur atoms in the heterocyclyl radical may be optionally oxidized; the nitrogen atom may be optionally quaternized; and the heterocyclyl radical may be partially or fully saturated or aromatic. The heterocyclyl radical may be attached to the main structure at any heteroatom or carbon atom which results in the creation of a stable compound. Examples of such heterocyclyl radicals include, but are not limited to, azepinyl, azetidinyl, acridinyl, benzimidazolyl, benzodioxolyl, benzodioxanyl, benzothiazolyl, benzoxazolyl, benzopyranyl, benzofuranyl, benzothienyl, carbazolyl, cinnolinyl, decahydroisoquinolyl, dioxolanyl, furyl, isothiazolyl, quinuclidinyl, imidazolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, indolyl, isoindolyl, indolinyl, isoindolinyl, indolizinyl, isoxazolyl, isoxazolidinyl, morpholinyl, naphthyridinyl, oxadiazolyl, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, 2-oxoazepinyl, oxazolyl, oxazolidinyl, perhydroazepinyl, piperidinyl, piperazinyl, 4-piperidonyl, phenazinyl, phenothiazinyl, phenoxazinyl, phthalazinyl, pteridinyl, purinyl, pyrrolyl, pyrrolidinyl, pyrazolyl, pyrazolidinyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, quinazolinyl, quinoxalinyl, quinolinyl, quinuclidinyl, isoquinolinyl, thiazolyl, thiazolidinyl, thiadiazolyl, triazolyl, tetrazolyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydroisoq uinolyl, thienyl, thiomorpholinyl, thiomorpholinyl sulfoxide, and thiomorpholinyl sulfone. The heterocyclyl radical may be optionally substituted by R6 as defined above in the Summary of the Invention or may be optionally substituted by one or more substituents selected from the group consisting of hydroxy, mercapto, halo, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, phenylalkenyl, alkoxy, phenoxy, phenylalkoxy, haloalkyl, haloalkoxy, formyl, nitro, cyano, amidino, cycloalkyl, hydroxyalkyl, alkoxyalkyl, phenoxyalkyl, phenylalkoxyalkyl, amidino, ureido, alkoxycarbonyamino, amino, monoalkylamino, dialkylamino, monophenylamino, monophenylalkylamino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, monophenylaminoalkyl, monophenylalkylaminoalkyl, alkylcarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, and imidazolyl, as defined herein.

"Linker residue" refers to any component capable of being selectively cleaved to release the residue of the compound of the invention from the solid support. See, e.g., Greene and Wuts, Protective Groups in Organic Synthesis, 2nd ed., Wiley (1991). Specific linker residues and cleavage reagents for them are depicted in Table 7 below.

"Monoalkylamino" refers to a radical of the formula -N(H)Ra where Ra is an alkyl radical as defined above, e.g., methylamino, ethylamino, propylamino, and the like.

"Monoalkylaminocarbonyl" refers to a radical of the formula -C(O)N(H)Ra where Ra is an alkyl radical as defined above, e.g., methylaminocarbonyl, ethylaminocarbonyl, propylaminocarbonyl, and the like.

"Monoalkylaminosulfonyl" refers to a radical of the formula -S(O)2N(H)Ra where Ra is an alkyl radical as defined above, e.g., methylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, and the like.

"N-heterocyclyl" refers to a heterocyclyl radical as defined above which contains at least one nitrogen atom and which is attached to the main structure through the nitrogen atom. The N-heterocyclyl radical may contain up to three additional hetero atoms. Examples include piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, azetidinyl, indolyl, pyrrolyl, imidazolyl, tetrahydroisoquinolyl, perhydroazepinyl, tetrazolyl, triazolyl, oxazinyl, and the like, and may be optionally substituted as described above for heterocyclyl radicals. In addition to being optionally substituted by the substituents listed above for a heterocyclyl radical, the N-heterocyclyl radical may also be optionally substituted by R6 as defined above in the Summary of the Invention.

"Phenylalkyl" refers to an alkyl radical as defined above substituted by a phenyi radical, e.g., benzyl, and the like.

"Optional" or "optionally" means that the subsequently described event of circumstances may or may not occur, and that the description includes instances where said event or circumstance occurs and instances in which it does not. For example, "optionally substituted aryl" means that the aryl radical may or may not be substituted and that the description includes both substituted aryl radicals and aryl radicals having no substitution. The term "-[C2-C8 alkyl]-R10 (optionally substituted by hydroxy)" means that the alkyl has the optional substitution. The same goes for the term "-[C1-C8 alkyi]-R (optionally substituted by hydroxy)". The term "optionally substituted -S(O)tR22" means that the R22 substituents all have the optional substitution.

"Phenylalkenyl" refers to an alkenyl radical as defined above substituted by a phenyl radical.

The term "pharmaceutically acceptable salt" refers to salts prepared from

pharmaceutically acceptable non-toxic acids or bases including inorganic acids and bases and organic acids and bases. When the compounds of the present invention are basic, salts may be prepared from pharmaceutically acceptable non-toxic acids including inorganic and organic acids. Suitable pharmaceutically acceptable acid addition salts for the compounds of the present invention include acetic, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric acid, p-toluenesulfonic, and the like. When the compounds contain an acidic side chain, suitable pharmaceutically acceptable base addition salts for the compounds of the present invention include metallic salts made from aluminum, calcium, lithium, magnesium, potassium, sodium and zinc or organic salts made from lysine, N,N'-dibenzylethylenediamine, chloroprocaine, choline, diethanolamine, ethylenediamine, meglumine (N-methylglucamine) and procaine.

"Solid support" refers to the material upon which synthesis of the compounds of the invention may be performed, and may be also referred to herein as beads or resins. The term "solid support" is intended to include beads, pellets, disks, fibers, gels, or particles such as celluslose beads, pore-glass beads, silica gels, polysteyrene beads optionally cross-linked with divinylbenzene and optionally grafted with polyethylene glycol and optionally functionalized with amino, hydroxy, carboxy, or halo groups, grafted co-poly beads, poly-acrylamide beads, latex beads, dimethylacrylamide beads optionally cross-linked with N,N'-bis-acryloyl ethylene diamine, glass particles coated with hydrophobic polymer, etc., i.e., material having a rigid or semi-rigid surface; and soluble supports such as low motecular weight non-cross-linked polystyrene.

"Therapeutically effective amount" refers to that amount of a compound of the invention which, when administered to a human in need thereof, is sufficient to effect treatment, as defined below, for conditions resulting from an abnormality in nitric oxide production. The amount of a compound of the invention which constitutes a "therapeutically effective amount" will vary depending on the compound, the condition and its severity, and the age of the human to be treated, but can be determined routinely by one of ordinary skill in the art having regard to his own knowledge and to this disclosure.

"Treating" or "treatment" as used herein covers the treatment of a condition in a human, which condition results from an abnormality in nitric oxide production, and includes: (i) preventing the condition from occurring in a human, in particular, when such human is predisposed to the condition but has not yet been diagnosed as having it;

(ii) inhibiting the condition, i.e., arresting its development; or (iii) relieving the condition, i.e., causing regression of the condition.

The yield of each of the reactions described herein is expressed as a percentage of the theoretical yield.

Most of the compounds described herein contain one or more asymmetric centers and may thus give rise to enantiomers, diastereomers, and other stereoisomeric forms that may be defined, in terms of absolute stereochemistry, as ( R)- or (S)- or, as (D)- or (L)- for amino acids.

The present invention is meant to include all such possible isomers, as well as, their racemic and optically pure forms. Optically active ( R)- and (S)-, or (D)- and (L)- isomers may be prepared using chiral synthons or chiral reagents, or resolved using conventional techniques.

When the compounds described herein contain olefinic double bonds or other centers of geometric asymmetry, and unless specified otherwise, it is intended that the compounds include both E and Z geometric isomers. Likewise, all tautomeric forms are also intended to be included.

The nomenclature used herein is a modified form of the l.U.P.A.C. nomenclature system wherein the compounds of the invention are named herein as amide derivatives. For example, the following compound of the invention: is named herein as 2-[[6-chloro-2-(1 H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-[(4- methoxyphenyl)methyl]pentanediamide. Unless otherwise indicated, compound names are intended to include any single stereoisomer, enantiomer, racemate or mixtures thereof.

Utilitv of the Compounds of the Invention: Nitric oxide generated by the inducible form of nitric oxide synthase (i-NOS) has been implicated in the pathogenesis of numerous inflammatory and autoimmune diseases and also in diseases which are generally not regarded as inflammatory, but nevertheless may involve

cytokines which locally up-regulate i-NOS. The compounds of the invention, alone or in combination with other pharmaceutical agents, are therefore useful in treating mammals, preferably humans, having a condition resulting from an abnormality in nitric oxide production.

Such conditions include, but are not limited to, the following: Multiple sclerosis (Parkinson, J.F. et al., J. Mol. Med. (1997), Vol. 75, pp. 1 74-186); stroke or cerebral ischemia (ladecola, C. et al., J. Neurosci. (1997), Vol. 17, pp. 9157-9164); Alzheimer's disease (Smith, M.A. petal, J. Neunsci. (1997), Vol. 17, pp.2653-2657; Wallace, M.N. et al., Exp. Neurol. (1997), Vol. 144, pp. 266-272); HIV dementia (Adamson D.C. et al., Science (1996), Vol. 274, pp. 1917-1921); Parkinson's disease (Hunot, S. et al., Neuroscience (1996), Vol. 72, pp. 355-363); meningitis (Koedel, U. et al., Ann. Neurol. (1995), Vol. 37, pp.

313-323); dilated cardiomyopathy and congestive heart failure (Satoh M et awl., J. Am. Coll.

Cardiol. (1997), Vol. 29, pp. 716-724); atheroscierosis (Wilcox, J.N. etna/., Arterioscler. Thromb.

Vasc. Biol. (1997), Vol. 17, pp. 2479-2488); restenosis or graft stenosis, septic shock and hypotension (Petros, A. et al., Cardiovasc. Res. (1994), Vol. 28, pp. 34-39); hemorrhagic shock (Thiemermann, C. et al., Proc. Natl. Acad. Sci. (1993), Vol. 90, pp. 267-271); asthma (Barnes, P.J., Ann. Med. (1995), Vol. 27, pp. 389-393; Flak, T.A. et awl., Am. J. Respir. Crit. Care Med.

(1996), Vol. 154, pp. S202-S206); adult respiratory distress syndrome, smoke or particulate- mediated lung injury (Ischiropoulos, H. etc!., Am. J. Respir. Crit. Care Med. (1994), Vol. 150, pp. 337-341; Van Dyke, K., Agents Actions (1994), Vol. 41, pp. 4449); pathogen-mediated pneumonias (Adler, H. etc!., J. Exp. Med. (1997), Vol. 185, pp. 1533-1540); trauma of various etiologies (Thomae, K.R. et al., Surgery (1996), Vol. 119, pp. 61-66); rheumatoid arthritis and osteoarthritis (Grabowski, P.S. etal., Br. J. Rheumatol. (1997), Vol. 36, pp. 651-655); glomerulonephritis (Weinberg, J.B. etna/., J. Exp. Med. (1994), Vol. 179, pp. 651-660); systemic lupus erythematosus (Belmont, H.M. et al., Arthritis Rheum. (1997), Vol. 40, pp. 1810-1816); inflammatory bowel diseases such as ulcerative colitis and Crohn's disease (Godkin, A.J. et al., Eur. J. Clin. Invest (1996), Vol. 26, pp. 867-872; Singer, l.l. etal., Gastroenterology (1996), Vol.

111, pp. 871-885); insulin dependent diabetes mellitus (McDaniel, M.L., et al., Proc. Soc. Exp.

Biol. Med. (1996), Vol. 211, pp. 24-32); diabetic neuropathy or nephropathy (Sugimoto, K. and Yagihashi, S., Microvasc. Res. (1997), Vol. 53, pp. 105-112; Amore, A. et al., Kidney Int.

(1997), Vol. 51, pp. 27-35); acute and chronic organ transplant rejection (Worrall, N.K. et al., Transplantation (1997), Vol. 63, pp. 1095-1101); transplant vasculopathies (Russell, M.E. et al., (1995), Vol. 92, pp. 457464); graft-versus-host disease (Kichian, K. et al., J. Immunol. (1996), Vol. 157, pp. 2851-2856); psoriasis and other inflammatory skin diseases (Bruch-Gerharz, D. et

al., J. Exp. Med. (1996), Vol. 184, pp. 2007-2012); and cancer (Thomsen, L.L. etna/., Cancer Res. (1997), Voi. 57, pp. 3300-3304).

The compounds of the current invention may also be useful for the management of male and female reproductive functions when used alone or combined with other drugs commonly used for these indications. Examples, without implied limitation, include: inhibition of fertilization, endometrial receptivity and implantation (alone or in combination with a progesterone antagonist); post-coital contraception (alone or in combination with a progesterone antagonist); induction of abortion (in combination with an antiprogestin and in further combination with a prostaglandin); control and management of labor and delivery; treatment of cervical incompetence (alone or in combination with progesterone or a progestin); treatment of endometriosis (alone or in combination with other drugs, including LHRH- agonists/antagonists, antiprogestins orprogestins by either sequential application or by concomitant administration). See, for example, the following references: Chwalisz, K. et awl., J.

Soc. Gynecol. Invest. (1997), Vol. 4, No. 1 (Supplement), page 104a, which discusses the inhibition of fertilization, endometrial receptivity and implantation, or post-coital contraception, alone or in combination with a progesterone antagonist; Chwalisz, K. et al., Prenat. Neonat Med. (1996), Vol. 1, pp. 292-329, which discusses the induction of abortion, in combination with an antiprogestin and in further combination with a prostaglandin, and the control and management of labor and delivery; and Chwalisz, K. et al., Hum. Reprod. (1997), vol. 12, pp.

101-109, which discusses the treatment of cervial incompetence, alone or in combination with progesterone or a progestin.

Those skilled in the art will also recognize that the compounds of the present invention include 1-substituted imidazoles. This class of compounds has previously been described as mechanism-based, heme-binding inhibitors of the cytochrome P450 family of enzymes (Maurice, M. et al., FASEB J. (1992), Vol. 6, pp. 752-8) in addition to nitric oxide synthesis (Chabin, R.NM. et al., Biochemistry (1996), Vol.35, pp.9567-9575). The compounds of the present invention may thus be useful as inhibitors of selected cytochrome P450 family members of therapeutic interest including, but not limited to, P450 enzymes involved in steroid and retinoid biosynthesis (Masamura et al., Breast Cancer Res. Treat. (1995), Vol. 33, pp.

19-26; Swart, P. et awl., J. Clin. Endocrinol. Metab., Vol. 77, pp. 98-102; Docks, P. et al., Br. J.

Dermatol. (1995), Vol. 133, pp. 426-32) and cholesterol biosynthesis (Burton, P.M. et awl., Biochem. Pharmacol. (1995), Vol. 50, pp. 529-544; and Swinney, D.C. et al., Biochemistry (1994), Vol. 33, pp. 47024713). Imidazole-based compounds may also have antifungal activity (Aoyama, Y. etna/., Biochem. Pharmacol. (1992), Vol. 44, pp. 1701-1705). The P450 inhibitory

activity of the compounds of the present invention can be assessed using appropriate assay systems specific for the P450 isoform of interest. Such assays are included in the references cited above. One additional example of mammalian cytochrome P450 isoform that may be inhibited by the compounds of the present invention is cytochrome P450 3A4 which can be assayed in a manner similar to the method described in Yamazaki et al., Carcinogenesis (1995), Vol. 16, pp. 2167-2170.

Testing of the Compounds of the Invention Nitric oxide synthases are complex enzymes that catalyze the conversion of L-arginine to nitric oxide (NO) and citrulline. Catalysis proceeds through two successive oxidations of the guanidinium group of L-arginine.

A cell-based nitric oxide synthase assay employing the measurement of nitric oxide oxidation product, nitrite, in the conditioned medium of cultured cells was employed for the evaluation of the compounds of the invention. The murine monocytic cell lines RAW 264.7 and J774 are well documented as capable of producing >10 pM nitrite in response to immunostimulation: Induction of iNOS in RAW 264.7 Mouse Monocvtes RAW 264.7 murine macrophage cells were obtained from American Type Culture Collection (Rockville, Maryland) and were maintained in RPMI 1640 containing 10% fetal bovine serum (FBS), 5000 units/mL of penicillin and streptomycin, and 2mM glutamine (maintenance medium). NOS activity was measured by a fluorescent assay of the nitric oxide oxidation product, nitrite, (Diamani et al., Talanta (1986), Vol. 33, pp. 649-652). Induction of iNOS (inducible nitric oxide synthase) is stimulated by treatment of the cells with lipopolysaccharide and y-interferon. The method of the assay is described below.

Cells are harvested, diluted to 500,000 cells/mL with maintenance medium, and seeded into 96-well plates at 100 CLl/well. The plates are incubated overnight at 37"C, under a 5% CO 2 atmosphere. The medium is then replaced with 90 lli of BME medium containing 10% FBS, 100 units/mL of penicillin, 100 lli streptomycin, 2 mM glutamine, 100 units/mL of interferon- y and 2 llg/mL of lipopoly-saccharide. N-guanidino-methyl-L-arginine is added to four wells (negative control) at a final concentration of 200 ,uM using 10 I of 2 mM stock solution in 100 mM Hepes, pH 7.3 + 0.1% DMSO and four wells receive only the 100 mM Hepes/0.1 % DMSO buffer (positive control). Compounds for evaluation are dissolved at 10-fold the desired final concentration in Hepes/DMSO and 10 µL of these solutions is transferred to the 96-well plate. The plates are incubated for 17 hrs at 37"C, under a 5% CO 2 atmosphere. Nitrite

accumulated in the culture medium is determined as follows: add 15 'LL of 2,3-diaminbnaphthalene (10 ,ug/mL in 0.75 M HCI) to each well and incubate for 10 minutes at room temperature. Add 15 Xul of 1 N NaOH and measure the fluorescence emission at 405 nm, using an excitation wavelength of 365 nm. Enzyme activity in experimental wells is normalized to percent control using the positive and negative control values. The signal to noise ratio is >10 for the assay.

The compounds of the invention, when tested in this assay, demonstrated the ability to inhibit nitric oxide production.

Various in vivo assays may be employed to determine the efficacy of the compounds of the invention in treating a condition resulting from an abnormality in nitric oxide production, such as arthritis. The following is a description of such an assay utilizing rats: Effects of Comoounds of the Invention on Adiuvant-lnduced Arthritis in Rats Male Lewis rats were injected intradermally (proximal quarter of the tail) with 0.1 mL of Mycobacterium butyricum in Incomplete Freund's Adjuvant (10 mg/mL). Either vehicle (acidified saline, 1 mUkg) or a compound of the invention (3, 10, or 30 mg/kg) were administered subcutaneously (b.i.d.), starting on the day following adjuvant immunization, and continued until the end of the experiment (N= 10 rats per treatment group). Clinical scores (see below) were measured in all limbs 3 times per week throughout the study. Rats were euthanized 34-35 days after immunization. At the time of euthanasia, a radiologic evaluation (see below) of the hind paws was performed, a blood sample was collected for clinical blood chemistry and drug levels (high dose group only; 6 or 12 hours post final dose), a section of liver was obtained for measurement of potential toxicity, and the hind limbs were preserved for histopathological determination.

Clinical scoring - each limb was graded according to the following scale: 0 no signs of inflammation 1 moderate redness, first indication of swelling, joint flexible 2 moderate redness, moderate swelling, joint flexible 3 redness, significant swelling and distortion of the paw, joint beginning to fuse 4 redness, gross swelling and distortion of the paw, joint completely fused

Radiological scoring - each hind limb was graded on a scale of 0-3 for each of the following parameters: soft tissue swelling cartilage loss erosion heterotropic ossification The compounds of the invention, when tested in this assay, demonstrated the ability to treat the arthritis present in the rats.

Those skilled in the art will also recognize that numerous assays for the activity of the NOS isoforms (iNOS, nNOS and eNOS) exist which can be used to evaluate the biological activity of the compounds of the current invention. These include assays for native NOS isoforms in tissues studied ex vivo (Mitchell et al., Br. J. Pharmacol. (1991), Vol. 104, pp. 289- 291; Szabo et al., Br. J. Pharmacol. (1993), Vol. 108, pp. 786-792; Joly et al., Br. J. Pharmacol.

(1995), Vol. 115, pup.491497) as well as primary cell cultures and cell lines (Forstermann etc!., Eur. J. Pharmacol. (1992), Vol. 225, pp. 161-165; Radmoski etal., Cardiovasc. Res. (1993), Vol. 27, pp. 1380-1382; Wang etal., J. Pharmacol. Exp. Ther. (1994), Vol. 268, pp.552-557).

Those skilled in the art will also recognize that recombinant NOS enzymes can be expressed in heterologous cells by either transient transfection (Karlsen et al., Diabetes, (1995), Vol. 44, pp.

753-758), stable transfection (McMillan et al., Proc. Natl. Acad. Sci. (1992), Vol.89, pp. 11141- 11145; Sessa etna!., J. Biol. Chem. (1995), Vol. 270, pp. 17641-17644) or via the use of lytic virus transfection (Busconi & Michel, Mol. Pharmacol. (1995), Vol. 47, pp. 655-659; List etal., Biochem. J. (1996), Vol. 315, pp. 57-63) using NOS cDNAs. Heterologous expression can be achieved in mammalian cells (McMillan petal., Proc. Natl. Acad. Sci. (1992), Vol. 89, pp. 11141- 11145), insect cells (Busconi & Michel, Mol. Pharmacol. (1995), Vol. 47, pp. 655-659; List etc!., Biochem. J. (1996), Vol. 315, pp. 57-63), yeast (Sari et al., Biochemistry (1996), Vol. 35, pp.

7204-7213) or bacteria (Roman et al., Proc. Natl. Acad. Sci. (1995), Vol. 92, pp. 8428-8432; Martasek et al., Biochem. Biophys. Res. Commun. (1996), Vol. 219, pp. 359-365). Any of these heterologous expression systems can be used to establish iNOS, nNOS and eNOS assay systems to evaluate the biological activity of the compounds of the present invention.

Administration of the Compounds of the Invention Any suitable route of administration may be employed for providing a patient with an effective dosage of compounds of the invention. For example, oral, rectal, parenteral (subcutaneous, intramuscular, intravenous), transdermal, and like forms of administration may

be employed. Dosage forms include tablets, troches, dispersions, suspensions, solutions, capsules, patches, and the like.

The pharmaceutical compositions of the present invention comprise the compounds of the invention as the active ingredient, and may also contain a pharmaceutically acceptable carrier, and optionally, other therapeutic ingredients. Carriers such as starches, sugars, and microcrystalline cellulose, diluents, granulating agents, lubricants, binders, disintegrating agents, and the like are suitable in the case of oral solid preparations (such as powders, capsules, and tablets), and oral solid preparations are preferred over the oral liquid preparations. Methods for their preparation are well known in the art.

Because of their ease of administration, tablets and capsules represent the most advantageous oral dosage unit forms, in which case solid pharmaceutical carriers are employed. If desired, tablets may be coated by standard aqueous or nonaqueous techniques.

In addition to the common dosage forms set out above, the compounds of the present invention may also be administered by controlled or sustained release means and delivery devices.

Pharmaceutical compositions of the present invention suitable for oral administration may be presented as discrete units such as capsules, cachets, or tablets, each containing a predetermined amount of the active ingredient, as a powder or granules, or as a solution or a suspension in an aqueous liquid, a non-aqueous liquid, an oil-in-water emulsion, or a water-in- oil liquid emulsion. Such compositions may be prepared by any of the methods of pharmacy, but all methods include the step of bringing into association the active ingredient with the carrier which constitutes one or more necessary ingredients. In general, the compositions are prepared by uniformly and intimately admixing the active ingredient with liquid carriers or finely divided solid carriers or both, and then, if necessary, shaping the product into the desired presentation.

Preferred Embodiments: In the various aspects of the invention, certain embodiments are preferred. A preferred group of compounds of formula (I), formula (II) and formula (III) are those compounds of formula (I) having the formula (la), formula (Ib) or formula (Ic): A preferred subgroup of this group of compounds are those compounds wherein A is -OR1, -C(O)N(R1)R2, -N(R16)C(O)N(R1)R16, -NR1C(O)R2 or -N(R1)R21; V is N(R4); and W is CH.

A preferred class of compounds of this subgroup are those compounds wherein A is

-C(O)N(R1)R2; q, rand n are zero; R1 is hydrogen; R2 is lower alkyl or -(C1-C8]-R9; R4 is hydrogen or lower alkyl; and R5 is hydrogen, halo, alkyl, or alkoxy.

A preferred subclass of compounds of this class of compounds are those compounds wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan-6-yl, 1,3-benzodioxol-5-yl, chlorophenyl, carboxyphenyl, dimethoxyphenyl, 2-thienyl or morpholinyl.

Another preferred subgroup of compounds of this group of compounds are those compounds where A is -C(O)N(R1)R2; mis zero; Q is a direct bond to R3; and R3 is hydrogen.

A preferred compound of this subgroup is N-[(1 ,3-benzodioxol-5-yl)ethyl]-2-[[2-(1 H- imidazol-1 -yl)-6-methylpyrimidin-4-yl](methyl)amino]acetamide.

Another preferred group of compounds of formula (I), formula (II) and formula (III) are those compounds of formula (II) having the formula (Ila), formula (llb) or formula (IIc): A preferred subgroup of compounds of this group of compounds are those compounds wherein the N-heterocyclyl is selected from the group consisting of piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, azetidinyl, indolyl, pyrrolyl, imidazolyl, tetrahydroisoquinolyl, and perhydroazepinyl.

A preferred class of compounds of this subgroup of compounds are those compounds wherein the N-heterocyclyl is piperazinyl substituted by R6, i.e., the compound of formula (lid), formula (lle) or formula (elf):

A preferred subclass of compounds of this class of compounds are those compounds where A is -OR1, -C(O)N(R1)R2, -N(R16)C(O)N(R1)R16, -NR1C(O)R2 or -N(R1)R21; W is CH; and R6 is chosen from the group consisting of hydrogen, alkyl, cycloalkyl, -[C1-C8 alkyl]-R8,

-[C2-C8 alkyl]-R50, -[C1-C8 alkyl]-R, acyl, -C(O)R8, -C(O)-[CI-C8 alkyl]-R8, alkoxycarbonyl, optionally substituted aryloxycarbonyl, optionally substituted aralkoxycarbonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heterocyclyl, alkoxycarbonylalkyl, carboxyalkyl, optionally substituted arylsulfonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, optionally substituted arylaminocarbonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, arylsulfonylaminocarbonyl, optionally substituted N-heterocyclyl, -C(=NH)-N(CN)R1, -C(O)-R23-N(R1)R2, -C(O)-R23-N(R1)C(O)-R23-N(R1)R2, and -C(O)-N(R1)-R23-C(O)OR1.

Of this subclass of compounds, preferred compounds are those compounds wherein A is -C(O)N(R1)R2; R1 is hydrogen; R2 is lower alkyl, -[C1-C8 alkyl]-R9, or -[C1-C8)-R10; R6 is hydrogen, acetyl, t-butoxycarbonyl, 4-methoxyphenylaminocarbonyl, 4-methoxyphenyl- methyl, methoxycarbonyl, methyl or benzyl; R5 is hydrogen, halo, alkyl, or alkoxy; and n is 0 or 1. Of this group of preferred compounds, more preferred compounds are those compounds wherein R2 is -CH2-R9 or -[C1-C8]-R10; R9 is aryl or substituted aryl; and R10 is methylthio. Of this group of more preferred compounds, most preferred compounds are those compounds wherein R2 is -CH2-R9; R6 is hydrogen, acetyl or t-butoxycarbonyl; and R9 is phenyl, tolyl, anisyl, 1 ,4-benzodioxan-6-yl, 1 ,3-benzodioxol-5-yl , methylthiophenyl, chlorophenyl, carboxyphenyl, dimethoxyphenyl, or 2-thienyl. Of this group of most preferred compounds, preferred compounds are those compounds wherein R5 is chloro, R6 is acetyl and R9 is p-tolyl, or those compounds wherein R5 is chloro, R6 is hydrogen and R9 is p-tolyl, or those compounds wherein R5 is chloro, R6 is hydrogen and R9 is 1 ,4-benzodioxan-6-yl or 1 ,3-benzodioxol-5-yl, or those compounds wherein R5 is chloro, R6 is t-butoxycarbonyl and R9 is 1 ,4-benzodioxan-6-yl or 1 ,3-benzodioxol-5-yl.

Preferred compounds of this subgroup of compounds may be selected fro m the following list: N-[(l ,3-benzodioxol-5-yl)ethy1]4-[2-( H-imidazol-l -yl)-6-methylpyrimidin-4-yl]-l -(2- methyl -oxopropyl)piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-4- (methoxycarbonyl)piperazine-2-acetamide; N-[(l ,4-benzodioxan-6-yl)methyl]-l -[2-(1 H-triazol-1 -yl)pyrimidin-4-yl]-4- [(dimethylethoxy)carbonyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-[2-(1H-imidazol-1-yl)-6-m ethoxypyrimidin-4-yl]-1- (methoxycarbonyl)piperazine-2-acetamide; 1-(acetyl)-N-[(1,3-benzodioxol-5-yl)methyl]-4-[6-chloro-2-(1 H-imidazol-1-yl)pyrimidin-4- yl]piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-methoxy-3-chlorophenyl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; and 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(pyridin-3-yl)meth yl]-4-(tetrahydro-3- furanoyl)piperazine-2-carboxamide.

Another preferred class of compounds of this subgroup of compounds are those compounds wherein the N-heterocyclyl is piperidinyl, i.e., the compound of formula (IIg), formula (llh) or formula (Ili):

A preferred subclass of compounds of this class of compounds are those compounds wherein A is -OR1, -C(O)N(R1)R2, -N(R16)C(O)N(R1)R16, -NR1C(O)R2 or -N(R1)R21; and W is CH.

Preferred compounds of this subclass of compounds are those compounds wherein A is -C(O)N(R1)R2; R1 is hydrogen; R2 is lower alkyl or -[C1-C8 alkyl]-R9; R5 is hydrogen, halo, alkyl, or alkoxy; and n is zero or one. More preferred compounds of these preferred compounds are

those compounds where R2 is lower alkyl or -CH2-R9 and R9 is 4-methoxyphenyl, 1 ,4-benzodioxan-6-yl, 1 ,3-benzodioxol-5-yI or 3,4-dimethoxyphenyl.

Preferred compounds of this subgroup of compounds may be selected from the following list: N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)pyrimidin4-yl]piperidine-2- ethanamine; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]piperidine-2 acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(m orpholin-4-yl)ethyl]piperidine- 2-acetamide; 1 -[2-( 'H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-(1 -methylhexyl)piperidine-2-acetamide; N-[(4-chlorophenyl)methyl]-1 -[2 ,6-bis(1 H-imidazol-1 -yl)pyrimidin-4-yl]piperidine-2- acetamide; 1 -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(4-methoxyphenyl)ethyl] piperidine-2- acetamide; and N-[(1,3-benzodioxol-5-yl)methyl]-4-[2-(1H-imidazol-1-yl)-6-m ethoxypyrimidin-4- yl]piperidine-2-acetamide.

Another preferred class of compounds of this subgroup of compounds are those compounds wherein the N-heterocyclyl is pyrrolidinyl, i.e., the compound of formula (IIj), formula (Ilk) or formula (llm): A preferred subclass of compounds of this class of compounds are those compounds wherein A is -OR1, -C(O)N(R1)R2, -N(R16)C(O)N(R1)R16, -NR1C(O)R2 or -N(R1)R21; and W is CH.

Preferred compounds of this subclass of compounds are those compounds wherein A is -C(O)N(R1)R2; R1 is hydrogen; R2 is lower alkyl or -[C1-C8 alkyl]-R9; R5 is hydrogen, halo, alkyl, or alkoxy; and n is zero or one. More preferred compounds of the preferred compounds are those compounds having the R-configuration at C-2 of the pyrrolidinyl ring.

Preferred compounds of this subgroup of compounds may be selected from the following list: N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4-yl]pyrrolidine- 2-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-et hylpyrimidin-4-yl]pyrrolidine-2- carboxamide; N-[(3,4-dimethoxyphenyl)methyl]-1 -[2-( IH-imidazol-1 -yl)pyrimidin-4-yl]pyrrolidine-2- acetamide; N-[(4-methoxyphenyl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-methylpyrimidin4-yl]pyrrolidine-2 carboxamide; and N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-e thylpyrimidin-4-yl]pyrrolidine- 2-acetamide.

Additional preferred compounds of the group of compounds as defined above may be selected from the following list: 4-[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(l ,3-benzodioxol-5-yl)ethyl]morpholine-2- carboxamide; 4-[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxyphenyl)ethyl]- thiomorpholine-2-acetamide; N-[(1,3-dioxolan-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyrimid in-4-yl]perhydroazepine-2- acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]azetidine- 2-carboxamide; and 4-[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(l ,4-benzodioxan-6-yl)ethyl]morpholine-2- carboxamide.

Another preferred group of compounds of formula (I), formula (II) and formula (III) are those compounds of formula (III) having the formula (Illa), formula (Illb) or formula (IIIc): A preferred subgroup of compounds of this group of compounds are those compounds wherein is optionally substituted phenyl or optionally substituted naphthyl.

Another preferred group of compounds of formula (I), formula (II) or formula (III) are those compounds wherein each X, Y or Z is C(R 19), and each U is C(R5).

Another preferred group of compounds of formula (I), formula (II) or formula (III) are those compounds wherein each X, Y or Z is N, and each U is C(R5).

Another preferred group of compounds of formula (I), formula (II) or formula (III) are

those compounds wherein each X is N, each Z or Y is C(R 19), and each U is N.

Another preferred group of compounds of formula (I), formula (II) or formula (III) are those compounds wherein in each formula, one of X, Y, and Z is N and the others are C(R 19), and U is C(R5).

A preferred group of compounds of formula (IV) are those compounds of formula (IVa), formula (IVb) or formula (IVc): A preferred subgroup of compounds of this group of compounds are those compo unds wherein said amino acid is an a-aminoacid of the L configuration at the carbon a to the acid.

Another preferred subgroup of compounds of this group of compounds are those compounds wherein said amino acid is an a-aminoacid of the D configuration at the carbon a to

the acid.

Another preferred subgroup of compounds of this group of compounds are those compounds wherein R1 is hydrogen; R2 is lower alkyl or -[C1-C8 alkyl]-R9; and R5 is hydrogen, halo, alkyl, or alkoxy.

A preferred class of compounds of this subgroup of compounds are those compounds wherein R9 is phenyl, tolyl, anisyl, 1,4-benzodioxan6-yl , 1 ,3-benzodioxol-5-yl , chlorophenyl, carboxyphenyl, 2-thienyl, dimethoxyphenyl or morpholinyl.

A preferred group of compounds of formula (Va), formula (Vb) or formula (Vc) are those compounds wherein each X and each Y is N; each W is CH; and B is a fused optionally substituted heterocyclyl.

A preferred subgroup of compounds of this group of compounds are those compounds having the formula (Vba): where A is -OR1, -C(O)N(R1)R2, -N(R16)C(O)N(R1 )R16, -NR1 C(O)R2 or )R21; and is an N-heterocyclyl selected from group consisting of piperidinyl, piperazinyl, pyrrolidinyl or morpholinyl.

A preferred compound of this subgroup of compounds is N-[(1,3-benzodioxol-5- yl)methyl]-1 -[2-( 1 H-imidazol-1 -yl)purin-6-yl]piperidine-2-acetamide.

Of the compounds of formula (Vlla), formula (Vllb) or formula (Vllc), a preferred compound is N-[(1,3-benzodioxol-5-yl)methyl]-1-[6-chloro-2-(pyridin-3-yl )pyrimidin-4- yl]piperidine-2-acetamide.

Of the compounds of formula (VIII), preferred are 4,6-dichloro-2-(1 H-imidazol-1 - yl)pyrimidine and 2,4-dichloro-6-(1 H-imidazol-I -yl)pyrimidine.

Of the linker residues used in this invention, most preferred is the photolytically cleavable linkage of the formula (X):

wherein the unsatisfied valence on the right of the formula represents the point of attachment to the solid substrate and the unsatisfied valence on the left of the formula represents the point of attachment to the ligand.

Preparation of the Compounds of the Invention The compounds of the invention may be synthesized by two general approaches, one of which (solid phase) could be thought of as a variant of the other (solution phase). The solution phase generic synthesis is shown in the following Reaction Scheme 1 which, for illustration purposes only, illustrates the synthesis of a compound of formula (I) where A is -C(O)N(R1)R2.

It is understood that other compounds of the invention may be prepared in a similar manner. In the following Reaction Scheme 1, PG is a suitable protecting group; m, n, q, r, Q, U, W, X, Y and Z are as described above in the Summary of the Invention; V is N(R 4), S or O (where R4is as described in the Summary of the Invention); and R 5, R2, R3, R12, R13, R14, R15, R17, and R20 are as described above in the Summary of the Invention: Reaction Scheme 1

In general, the compounds of formula (I) are prepared by first adding one equivalent of a compound of formula (Xl) in one portion to a solution of one equivalent of a compound of formula (XII) having at least two substituents displaceable by a nucleophile and 1.1 equivalents of a trialkyl amine base (such as triethylamine) in a polar, nonprotic solvent such as THF or methylene chloride to provide the compound of formula (XIII). Upon completion of the reaction, the mixture is purified by conventional methods.

The compounds of formula (XlVcc) are synthesized by methods well known in the amino acid and peptide synthetic art from the appropriate compound of formula (XIVaa), wherein PG is a standard protecting group for the V subsituent. Compounds of formula (XIVaa) are commercially availabie, usually in protected form, or are readily synthesized by procedures well-known in the art. Preferred protecting groups are Boc t-butoxycarbonyl) and Fmoc (fluorenylmethoxy-carbonyl), although others, such as CBZ (benzyloxycarbonyl), and Troc (trichloroethoxycarbonyl), could be used for particular circumstances. Side chain functionalities may be protected, as is well known in the peptide art, by Trt (triphenylmethyl), tBu (t-butyl), Acm (acetamidomethyl) etc. The protected compounds of formula (XIVaa) are reacted with the appropriate amine to produce the compounds of formula (XlVbb) and deprotected to produce the compound of formula (XlVcc), once again by methods well known in the peptide art.

One equivalent of the compound of formula (XIVcc) is added to a solution of one equivalent of the compound of formula (XIII) and one equivalent of base in a polar, aprotic solvent such as THF. The reaction is heated to a temperature at which the reaction proceeds cleanly to completion in less than 16 hours. Upon completion of the reaction, the compound of formula (I) is purified and characterized by conventional methods.

Compounds of formula (I) having the so-called "reverse amide", i.e., where A is -N(R1)C(O)R2 can be made from the appropriate acid of formula (XIVaa) by Hofmann rearrangement of the acid to an amine, followed by acylation with an appropriate acid under the conditions described above. In many cases, the desired diamine can be obtained commercially.

The compounds of formula (I) in which A is a urea may be prepared by reacting a compound of formula (I) where A is -N(R1)R21 (where R1 is hydrogen and R21 is hydrogen, alkyl, aryl or aralkyl) with an isocyanate. Similarly, the compounds of formula (I) in which A is a carbamate may be prepared by reacting a compound of formula (I) (where A is -N(R 1)R21 where R1 is hydrogen and R21 is hydrogen, alkyl, aryl or aralkyl) with an alkyl chloroformate or by Curtius rearrangement of the carboxylic acid azide of the compound of formula (XIVaa) in the presence of the appropriate alcohol.

A specific embodiment of the generic synthesis of a compound of the invention is shown below in Reaction Scheme 2 as applied to a 6-chloro-2-(1-imidazolyl)-4-pyrimidinamine that incorporates the residue of D- -thienylalanine piperonylamide: Reaction Scheme 2

One equivalent of isobutyl chloroformate is added to a solution of N-Boc-D-> thienylalanine and one equivalent of a base such as N-methyl morpholine in THF. After two minutes, one equivalent of piperonylamine is added and the mixture allowed to warm to room temperature. After thirty minutes, the reaction mixture is passed through a bed of Celite and all volatiles are removed under reduced pressure to yield N-Boc-D-P-thienylalanine piperonylamide.

The N-Boc-D-Pthienylalanine piperonylamide in methanol is treated with acetyl chloride.

After 45 minutes, all volatiles are removed under reduced pressure to yield D->thienylalanine piperonylamide hydrochloride.

One equivalent of imidazole is added in one portion to a solution of one equivalent of trichloropyrimidine and 1.5 equivs of triethylamine in THF. After reaction is complete, the reaction mixture is poured into saturated, aqueous ammonium chloride and extracted three times with ethyl acetate. The combined organic layers are washed with brine and dried. The reaction mixture is filtered and all volatiles removed under reduced pressure. The product 2-imidazolyl4,6-dichloropyrimidine (the compound of formula (Vllla)) is isolated by flash chromatography (20% ethyl acetate in hexane) as an off-white solid.

Two equivalents of D->thienylalanine piperonylamide hydrochloride are added to a solution of one equivalent of 2-imidazolyl-4,6-dichloropyrimidine (the compound of formula (Vllla)) and three equivalents of Hunig's base (diisopropylethylamine) in THF. After reaction is complete, all volatiles are removed and the product (the compound of formula (laa)) is isolated.

A specific example of the synthesis as applied to sarcosine piperonylamide hydrochloride is provided: Isobutyl chloroformate (226 'LL, 1.73 mmol) was added to a solution of N-Boc sarcosine (1.73 mmol) and N-methylmorpholine (192 'LL, 1.73 mmol) in THF. After two minutes, piperonylamine (216 mL, 1.73 mmol) was added and the mixture allowed to warm to room temperature. After thirty minutes, the reaction mixture was passed through a bed of Celite and all volatiles were removed under reduced pressure to yield N-Boc sarcosine piperonyl amide (531 mg, 95%) as a white solid. 1H NMR: (CDC13) 6 2.41 (s,3H), 3.28 (s,2H), 4.39 (d,2H), 5.95 (s,2H), 6.80 (m,3H), 7.43 (bs,lH), 9.04 (bs,lH).

N-Boc sarcosine piperonylamide (500 mg, 1.54 mmol) in methanol (10 mL) was treated with acetyl chloride (1 mL). After 45 minutes, all volatiles were removed under reduced pressure to yield sarcosine piperonyl amide hydrochloride (395 mg, quant.) as a sticky solid.

Imidazole (9.5 g, 140 mmol) was added in one portion to a solution of trichloropyrimidine (24.7 g, 135 mmol) and triethylamine (30 mL, 216 mmol) in THF (500 mL). After 16 hrs, the

reaction mixture was poured into saturated, aqueous ammonium chloride and extracted three times with ethyl acetate. The combined organic layers were washed with brine and dried over MgSO4. The reaction mixture was filtered and all volatiles were removed under reduced pressure. 2-lmidazolyl4,6-dichloropyrimidine (the compound of formula (Vllla)) (9.61 g, 33%) was isolated by flash chromatography (20% ethyl acetate in hexane) as an off-white solid.

H NMR: (CDCI3) 6 7.13 (s,lH), 7.25 (s,lH), 7.76 (s,lH), 8.50 (s, 1H).

Sarcosine piperonyl amide hydrochloride (50 mg, 0.19 mmol) was added to a solution of 2-imidazolyl4,6-dichloropyrimidine (Vllla) (20 mg, 0.093 mmol) and Hunig's base (50 ijL, 0.29 mmol) in THF (1 mL). After 16 hrs, all volatiles were removed and the product was isolated as a waxy solid (29 mg, 78%). 1H NMR (CDCI3) ô 3.2 (s,3H), 4.25 (s,2H), 4.38(s,2H), 5.88 (s,2H), 6.30 (bs,lH), 6.42 (bs,2H), 6.65 (m,3H), 7.05 (s,lH), 8.40 (s,lH).

Another specific example of the synthesis of a compound of (Xlc) is provided: Boc-pyrrolidine (3.0 g, 17.5 mmol) was dissolved in ether (35 ml) and tetramethylethylenediamine (TMEDA) (2.03 g, 17.5 mmol), cooled to -78 "C and s-butyllithium (1.3 M, 13.5 mL, 18 mmol) was added. After stirring for 1 hour, allyl bromide was added in ether (5 mL). After warming to room temperature, the reaction was quenched with water and the organic layer was separated. The organic layer was washed with 1 M solution of NaH 2PO4 and water, then dried over MgSO4. The solvent was removed in vacuo and the residue was purified by chromatography on silica gel (hexanes/ethyl acetate (9:1) to give the olefin (0.50 g, 14%, 1H NMR (CDCI3) 6 5.65-5.85 (m, 1H), 5.00-5.20 (m, 2H), 3.70-3.90 (m, 1H). 3.20-3.45 (m, 2H). 2.35-2.60 (M, 1 H). 2.00-2.20 (m, 1H), 1.60-2.00 (m, 4H), 1.45 (s, 9H)). The olefin (500 mg, 2.37 mmol), 5-bromo-1 ,3-benzodioxolane (476 mg, 2.37 mmol), triethylamine (478 mg, 4.74 mmol), tri-o-tolylphosphine (96 mg. 0.31 mmol) and Pd(OAc)2 (26 mg, 0.12 mmol) was dissolved in CH3CN and refluxed overnight under argon. An additional 1 equivalent (476 mg) of the bromide and Pd(OAC)2 (52 mg, 0.24 mmol) was added and refluxing continued for 4.5 hours. The reaction was filtered and the solvent was evaporated. The residue was taken up in ether and washed successively with water, 1 M NaH 2PO4, water, and brine. After drying, the solvent was removed and the product was purified by chromatography (silica gel. hexane:ethyl acetate, 4:1) to yield 152 mg (19%) of the Boc-protected [(1 ,3-benzodiox-5-yl)prop-2- enyl]pyrrolidine (1H NMR (CDCI3) 86.90 (s, 1H), 6.70-6.80 (m, 2H), 6.35 (d, 1H). 3.80-3.95 (m, 1 H), 3.25-3.50 (m. 2H), 2.45-2.70 (m, 1 H), 2.20-2.35 (M, 1 H), 1.70-2.00 (M, 4H), 1.45 (s, 9H)).

The Boc group was removed under standard conditions.

Another specific embodiment of the generic syntheis as applied to a compound of the invention follows:

To butyl alchohol (3 ml) was added 2-fluoro-4-chloropurine (41 mg, 0.24 mmol), N-[(1,3-benzodioxol-5-yl)methyl]piperidine-2-acetamide (66 mg, 0.24 mmol), and Hünig's's base (diisopropylethylamine) (0.042 mL, 0.24 mmol). After stirring at 90 "C for 6 hours, the reaction was diluted with ethyl acetate. The organic material was washed with saturated NH 4CI and brine, dried (MgSO4), and the solvent was removed in vacuo. Chromatography of the residue (CH2C12/MeOH, 10/1) gave 42 mg of the fluoropurine. The fluoropurine (18.9 mg, 0.046 mmol) was dissolved in DMSO and reacted with TMS-imidazole (0.10 g, 0.66 mmol) and CsF (61 mg, 0.40 mmol). After stirring at 130 " C for 72 hours, the reaction was diluted with ethyl acetate and washed with saturated NH4CI and brine. The organic layer was dried (MgSO4), the solvent removed in vacuo, and the residue chromatographed (CH2C12/MeOH, 19/1) to give 12 mg of N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)purin-6-yl]piperidine-2-acetamide, Another specific example of the synthesis is provided: To THF (10 mL) was added cyanuric chloride (158 mg, 0.85 mmol), N-[(1,3- benzodioxol-5-yl)methyl]piperidine-2-acetamide (47 mg, 0.17 mmol), and imidazole (58 mg, 0.85 mmol). After stirring for 12 hours, the reaction was diluted with ethyl acetate. The organic material was washed with saturated NH4CI and brine, dried (MgSO4), and the solvent was removed in vacuo. Chromatography of the residue (hexanes/ethyl acetate, 4/1) gave 60 mg of the dichlorotriazine. The dichlorotriazine (20 mg, 0.047 mmol) was dissolved in THF and reacted with TMS-imidazole (0.009 mL, 0.06 mmol) and CsF (11 mg, 0.07 mmol) at 0 "C . After warming to room temperature and stirring for 4 hours, the reaction was diluted with ethyl acetate and washed with saturated NH4CI, water, and brine. The organic layer was dried (MgSO4), the solvent removed in vacuo, and the residue chromatographed (ethyl acetate/hexanes/MeOH, 4/4/1) to give 6.5 mg of N-[(l ,3-benzodioxol-5-yl)methyl]-l -[3-chloro-5- (1H-imidazol-l -yl)triazin-2-yl]piperidine-2-acetamide.

Another specific example of the synthesis is provided: To a solution of indole-5-carboxylic acid (0.50 g, 3.1 mmol) in MeOH (25 mL) was added trimethylsilyldiazomethane until no gas evolution was observed. The solution was concentrated, dissolved in CH2C12, and washed with saturated NaHCO3 and brine. The organic layer was dried (MgSO4) and the solvent was removed in vacuo to give 0.54 g of the ester (1H NMR (CDCI3) 5 3.95 (s, 3H), 6.63 (s, 1H), 7.25 (m, lH), 7.40 (d, 1H), 7.95 (d, 1H), 8.25-8.4 (br s, 1H), 8.45 (s, lah)). The ester (100 mg, 0.58 mmol) was dissolved in DMF (10 mL) and 4-chloro-2-imidazol-1-ylpyrimidine (113 mg, 0.63 mmol) was added. After heating at 60 "C for 18 hours, the solvent was removed in vacuo, the residue was dissolved in CH2C12, and washed with saturated NaHCO3 and brine. The organic layer was dried (MgSO4), the solvent was

removed in vacuo and the residue was chromatographed (CH2C12/MeOH, 19/1) to give 68 mg (37%) of the pyrimidine (1H NMR (CDCI3) 83.95 (s, 3H), 6.90 (s, 1H), 7.25 (m, 2H), 7.80 (m, 1H), 7.95 (s, 1H), 8.10 (d, 1H), 8.4 (s, 1H), 8.50 (d, 1H), 8.70 (m, 2H)). The pyrimidine was dissolved in THF/water (1/1) and LiOH (6 mg, 0.21 mmol) was added. After heating at 60 °C for 3 hours, the solvent was removed in vacuo and acidified with methanolic HCI. The solvent was removed in vacuo, dissolved in DMF and treated with HATU (42 mg, 0.11 mmol), DIEA (37 mg, 0.21 mmol), and piperonylamine (26 mL, 0.21 mmol). After stirring for 18 hours, the solvent was removed in vacuo, the residue was dissolved in CH2CI2, and washed with saturated NaHCO3 and brine. The organic layer was dried (MgSO4), the solvent was removed in vacuo, and the residue was chromatographed (CH2CI2/MeOH, 19/1) to give 2 mg (4%) of N-[(1,3- benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyrimidin-4- yl]indole-6-carboxamide; 1H NMR (CDCI3) 8 3.75 (s, 2H), 5.95 (s, 2H), 6.80-6.90 (m,2H), 7.05-7.15 (m, 2H), 7.25 (m, 2H), 7.75- 7.85 (m, 2H), 8.00 (s, 2H), 8.50-8.60 (m, 2H), 8.70-8.80 (m, 1 H); MS: (439.2 M+H) +.

Another specific embodiment of the generic synthesis as applied to a compound of the invention is N-[(l ,3-benzodioxol-5-yl)ethyl]-l -[2-(1 H-imidazol-1-yl)pyrimidin-4-yl]pyrrole-2- carboxamide [MS: (403.2 M+H)'], which was prepared in a similar manner described above for <BR> <BR> N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)pyrimidin4-yl]indole-6-carboxamide.

The following Reaction Scheme 3 depicts a method of preparing the compounds of the invention where U is CR5 (where R5 is hydrogen) and X, Y and Z are CR19 (where R19 is hydrogen): Reaction Scheme 3

The above synthesis may be carried out as follows: To benzene (20 mL) was added 1-(3-aminophenyl)imidazole (755 mg, 4.7 mmol), 7-chloro-3-oxoheptanoic acid ethyl ester (982 mg, 4.7 mmol), Na2HPO4 (667 mg, 4.7 mmol), 12 (60 mg, 0.23 mmol), and 4A molecular sieves (500 mg). After refluxing for 6 hours, more 12 (60 mg) was added. After stirring for 16 hours, the reaction was filtered, the solvent was removed in vacuo, and the residues chromatographed (CH2C12/MeOH, 98/2) to give 120 mg (8%) of 1-[3-(1 H-imidazol-1- yl)phenyl]piperidine-2-acrylic acid ethyl ester (1H NMR (CDCI3) 6 7.85 (s, 1 H), 7.05-7.50 (m, 6H), 4.80 (s, 1H), 4.15 (q, 2H), 3.45 (t, 2H), 2.4 (t, 2H0, 1.5-1.8 (m, 6H, 1.30 (t, 3H)). This ester (120 mg, 0.38 mmol) was dissolved in MeOH (20 mL) and reacted with 10% Pd/C (60 mg) and 1 atm of H2. After reacting for 60 hours, the reaction was filtered, the solvent removed in vacuo, and the residue chromatographed (ethyl acetate/hexanes, 1/1) to give 24 mg of 1-[3- (1 H-imidazol-1 -yl)phenyl]piperidine-2-acetic acid ethyl ester (compound of formula (XV)). This ester (24 mg, 0.076 mmol) was dissolved in 5% methanolic NaOH. After stirring for 16 hours, the reaction was acidified with methanolic HCI, the solvent removed in vacuo, and the residue dissolved in DMF. Piperonyiamine (1 eq), Hunig's base (2 eq) and HATU (1 eq) were added.

After reaction completion the reaction mixture was partitioned with water and ethyl acetate. The organic layer was separated, washed with water, and dried. The solvent was removed in vacuo and the residue was chromatographed (ethyl acetate/MeOH, 98/2) to give 6 mg of the compound of formula (Ibb), N-[(1 ,3-benzodioxol-5-yl)methylj-1 -[3-(1 H-imidazol-1 - yl)phenyl]piperidine-2-acetamide: 1H NMR (CDCI3) 87.80 (s, 1H), 7.10-7.30 (m, 4H), 6.50- 6.70 (m, 5H), 5.90 (s, 2H), 4.20-4.35 (m, 2H), 3.85 (br s, 1 H), 3.50 (t, 2H), 2.95 (d, 1 H), 2.35- 2.55 (m, 2H), 1.4-1.9 (m, 6H); MS: (419 M+H) +.

The following Reaction Scheme 4 depicts a method of preparing compounds of the invention where A is -OR1: Reaction Scheme 4

The above synthesis may be carried out as follows: To DMF (100 ml) was added 4-chloro-2-imidazol-1-ylpyrimidine (0.50 9, 2.77 mmol), 2-piperidineethanol (0.359 g, 2.77 mmol), and Hünig's base (0.536 g, 4.15 mmol). After heating at 80 °C for 5 hours, the solvent was removed in vacuo and the residue was chromatographed (CH2Cl2/MeOH, 19/1) to give 349 mg (46 % ) of 1-[(1 H-imidazol-1-yl)pyrimidin-4-yl]piperidine-2-ethanol (the compound of formula (XVI)), (1H NMR (CDCI3) 58.54 (s, 2H), 8.11 (d, lH), 7.82 (t, lH), 7.11 (d, 1H), 6.44 (d, lH), 3.60 (m, 2H), 3.03 (m, 1H), 1.77 (m); MS: 274 (M+H) +). To a solution of 1-[(1 H- imidazol-1-yl)pyrimidin-4-yl]piperidine-2-ethanol (25 mg, 0.092 mmol) dissolved in DMF (5 ml) was added NaH (60% dispersion in oil, 5.5 mg, 0.14 mmol) followed by piperonyl chloride (17 mg, 0.10 mmol) and t-butyl ammonium chloride. After stirring for 16 hours at 80 " C, the solvent was removed in vacuo and the residue was partitioned with saturated NH4Cl and CH2Cl2. The organic layer was separated, dried (MgSO4), the solvent removed in vacuo, and the residue chromatographed (CH2CI2/MeOH, 19/1) to give 13 mg (35%) of 4-[2-[[(1,3-benzodioxol-5- yl)methoxy]ethyl]piperidin-1-yl]-2-(1 H-imidazol-l -yl)pyrimidine (the compound of formula (Icc)); 1H NMR (CDCl3) 8 8.52 (s, 1H), 8.05 (d, 1H), 7.80 (s, 1H), 7.09 (s, 1H), 6.73 (m,3H), 6.45 (d, 1H), 5.93 (s, 2H), 4.30 (s, 2H), 3.45 (m, 2H), 2.95 (m, 1H), 1.55 (m); MS: 408.7 (M+H) +.

Compounds of formula (XVI) may be used to prepare other compounds of the invention as depicted below in Reaction Scheme 5 where Rab is hydrogen or -CH3, Ms is mesyl and Ac is acetyl: Reaction Scheme 5

The above synthesis may be carried out as follows: To a solution of 1-[(1 H-imidazol-1- yl)pyrimidin-4-yl]piperidine-2-ethanol (the compound of formula (XVI)) (236 mg, 0.86 mmol) and methanesulfonyl chloride (99 mg, 0.87 mmol) dissolved in CH2Cl2 (20 mL) was added TEA (87.5 mg, 0.87 mmol). After stirring for 16 hours at 0 °C, methanesulfonyl chloride (99 mg, 0.87 mmol) and TEA (87.5 mg, 0.87 mmol) were added and the solution was warmed to ambient temperature. After stirring for 1 hour, the solution was washed with saturated NH 4CI and brine, dried (MgSO4), and the solvent removed in vacuo to give 276 mg (91%) of the compound of formula (XVII) (1H NMR (CDCl3) 58.72 (s, 1H), 8.15 (d, 1H), 7.89 (s, 1H), 7.18 (s, 1H), 6.46 (d, 1H), 4.24 (m, 3H), 2.95 (s, 3H), 2.18 (m, 6H), 1.76 (m). MS: 352.5 (M+H) +). A solution of the compound of formula (XVII) (100 mg, 028 mmol) and a compound of formula (XVIII) (429 mg, 2.84 mmol) dissolved in CH2Cl2 (7.5 ml) was stirred for 16 hours, and then DMF (7.5 ml) was added. After stirring for 2 hours, the solvent was removed in vacuo and the residue was partitioned with saturated NH4CI and CH2C12. The organic layer was separated, washed with brine, dried (MgSO4), the solvent removed in vacuo, and the residue chromatographed (CH2CI2/MeOH, 19/1) to give 6.6 mg (21%) of N-[(1 ,3-benzodioxol-5- yl)methyl]-1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]piperidine- 2-ethanamine (the compound of formula (lee)): 1H NMR (CDCl3) 5 8.50 (s, 1H), 8.08 (d, 1H), 7.77 (s, 1H), 7.08 (s, 1H), 6.66 (m, 3H), 6.43 (d, 1 H), 5.91 (s, 2H), 3.60 (d, 2H), 3.00 (m, 1H), 2.57 (m, 2H), 2.02 (m, 1 H), 1.65 (m).

MS: 407.8 (M+H)+.

To THF (3 mL) was added N-[(1 ,3-benzodioxol-5-yl)methyl]-1-[2-(1 H-imidazol-1- yl)pyrimidin-4-yl]piperidine-2-ethanamine (8 mg, 0.03 mmol), Hünig's base (8 mg, 0.06 mmol), and acetic anhydride (4 mg, 0.04 mmol). After stirring for 16 hours, the solvent was removed in vacuo and the residue was chromatographed (CH2Cl2/MeOH. 19/1) to give 8 mg (60%) of N-acetyl-N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol- 1-yl)pyrimidin-4-yl]piperidine-2- ethanamine (the compound of formula (lgg)): 1H NMR (CDC13) 58.48 (s, 1H), 8.08 (d, 1H), 7.76 (s, 1 H), 7.09 (s, 1H), 6.66 (m, 3H), 6.33 (m, 1H), 5.94 (s, lH), 5.91 (s, 1 H), 4.43 (m,3H), 3.40 (m, 2H), 2.11 (d, 3H), 1.14(m); MS: 450.0 (M+H) +.

Alternatively, to THF (3 mL) was added N-[(1 ,3-benzodioxol-5-yl)methyl]-1-[2-(1 H- imidazol-l -yl)pyrimidin4-yi]piperidine-2-ethanamin (8 mg, 0.03 mmol), Hunig's base (8 mg, 0.06 mmol), and methanesulfonyl chloride (4.5 mg, 0.04 mmol). After stirring for 16 hours, the solvent was removed in vacuo and the residue was chromatographed (CH2Cl2/MeOH. 19/1) to give 7 mg (51%) of N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N- (methylsulfonyl)piperidine-2-ethanamine (the compound of formula (Iff)); 1H NMR (CDCl3) 5 8.10 (s 1H), 7.78 (d, 1H), 7.13 (s, 1H), 6.82 (s, 1H), 6.72 (s, 2H), 6.30 (d, 1H), 5.94 (s, 2H),

4.23 (m, 3H), 3.20 (m, 2H), 2.80 (s, 3H), 1.14 (m); MS: 485.7 (M+H) +.

To DMF (5 ml) was added the compound of formula (XVII) (50 mg, 0.14 mmol), Hunig's base (28 mg, 0.21 mmol), and N-methylpiperonylamine (28 mg, 0.17 mmol). After stirring at 80°C for 16 hours, the solvent was removed in vacuo and the residue was partitioned with saturated NH4CI and CH2Cl2. The organic layer was separated, washed with brine, dried (MgSO4), the solvent removed in vacuo, and the residue was partitioned with ethyl acetate and water. The organic layer was separated, washed with brine, dried (MgSO 4), the solvent was removed in vacuo, and the residue was chromatographed (ethyl acetate/MeOH, 19/1) to give 7 mg (12%) of N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)pyrimidin-4-yl]-N- methylpiperidine-2-ethanamine (the compound of formula (Idd)); 'H NMR (CDCI3) 5 8.53 (s, lH), 8.07 (d, 1H), 7.80 (s, 1H), 7.10 (s, lH), 6.78 (s, 1H), 6.69 (m, 2H), 6.43 (d, 1H), 5.92 (s, 2H), 3.40 (m, 2H), 2.97 (m, lH), 1.80 (m); MS: 422.0 (M+H) +.

Reaction Scheme 6 depicts another method of preparing compounds of the invention where V is C(R4)H: Reaction Scheme 6

The above synthesis may be carried out as follows: To a solution of LDA (1.28 g, 12 mmol) in THF (30 mL) at -78°C was added 2,4-dichloro-6-methylpyrimidine (1.96 g, 12 mmol) in THF (15 mL). After stirring for 15 minutes, 3,3-dimethylallyl bromide (1.79 g, 12 mmol) in THF (5 mL) was added dropwise. After the reaction warmed to ambient temperature, water and ethyl acetate was added. The organic layer was separated, the solvent was removed in vacuo, and the residue was chromatographed (ethyl acetate/hexane, 1/19) to give 2.06 g (74%) of 2,4-dichloro-6-(4-methyl-3-pentenyl)pyrimidine (1H NMR (CDCI3) 87.15 (s, 1H), 5.10 (t, 1H), 2.80 (t, 2H), 2.45 (m, 2H), 1.70 (s, 3H), 1.55 (s, 3H)). To a solution of NalO4 (17 g, 81 mmol) and KMnO4 (251 mg, 1.59 mmol) in water was added K 2CO3 (1.29 g, 9.38 mmol) and 2,4-dichloro-6-(4-methyl-3-pentenyl)pyrimidine (2.06 g, 8.9 mmol) in t-butanol.

After stirring for 16 hours, the reaction was acidified to pH 3 and extracted with ethyl acetate.

The organic layer was extracted with aqueous NaHCO3. The aqueous layer was acidified to pH 3 and extracted with ethyl acetate. The organic layer was dried and the solvent removed in vacuo to give 980 mg of 3-(2,4-dichloropyrimidin-6-yl)propionic acid (the compound of formula (XIX)), 1H NMR (CDCI3) 8 7.30 (s, 1H), 3.05 (t, 2H), 2.90 (t, 2H). The acid was coupled to piperonylamine under standard conditions with isobutyl chloroformate and N-methylmorpholine to give the compound of formula (XX). Imidazole was added under standard conditions (1 -trimethylsilylimidazole and CsF in DMF at 60 "C) to give N-[(1 ,3-benzodioxol-5-yI)ethyl]-6- chloro-2-( 1 H-imidazol-1 -yl)pyrimidine-4-propionamide (the compound of formula (Ihh)); MS: 386 (M+H) .

The solid phase generic synthesis may be conceptualized as the generic synthesis of Reaction Scheme 1 in which R1 has been replaced by a cleavable attachment to a derivatized polymer resin. At the end of the synthetic scheme, the resin is cleaved and R 1 becomes hydrogen. The solid phase synthetic scheme is illustrated in Reaction Scheme 7 as applied to the specific example, as before, of a piperonylamide, but in this case the amino acid is piperazine-2-acetic acid: Reaction Scheme 7 Reaction Scheme 7 continued Boc N NO2 O (XXV) Lys N H Fmoc O deprotect Boc CI N NO2 0 NN gN (Vlllb) ½ I + XLYS-NH < H <N (XXVI) OJ I oc NO2 0N N I $ NN (IXaa) HsN jiaN) /eavage ¼/N N NN$ K AN (lii) ¼/N

In the solid phase synthesis, the group which is to become R 1 is attached to the resin through a cleavable linkage, such as the 2-nitrobenzyl residue, which can be photolytically cleaved. In the example shown, the piperonylamine (see above) has been protected with Boc and reacted with 4-(bromomethyl)-3-nitrobenzoic acid to produce the Boc-protected compound of formula (XXI), which is then attached to a free amine of the lysine-derivatized, amino- functionalized synthetic support. In this case, a polyethyleneglycol-grafted crossliked polystyrene, 1% DVB crosslinked polystyrene or crosslinked polydimethylacrylamide is suspended in a polar aprotic solvent such as methylene chloride, DMF or THF. An excess of the suitably protected linker-synthon is added to the suspended support followed by a coupling reagent such as diisopropylcarbodiimide (DIC), dicyclohexylcarbodiimide (DCC), bis(2-oxo-3- oxazolidinyl)phosphinic chloride (BOP), or 0-(7-azabenzotriazol-1 -yl)-1 ,1 ,3,3- tetramethyluronium-hexafluorophosphate (HATU) and optionally an acylation catalyst such as dimethylaminopyridine (DMAP) or hydroxybenzotriazole (HOBT). The mixture is agitated at ambient temperature for 1 to 24 hours or until the reaction is complete as judged by a ninhydrin test. The resin is washed with an appropriate solvent or solvents multiple times to remove excess reagents and by-products to give the resin-compound of formula (XXI I).

The resin-compound of formula (XXII) is deprotected to liberate the compo und of formula (XXIII), which is then suspended in a polar aprotic solvent such as methylene chloride or DMF. An excess of an appropriately protected compound of formula (XXIV) is added followed by a coupling agent such as HATU, BOP or DIC with the optional addition of an acylation catalyst such as DMAP or HOBT. Alternatively an excess of an activated form of the compound of formula (XXIV), such as the symmetrical anhydride or acyl fluoride may be added to the resin. The mixture is shaken for 1 to 24 hours at ambient temperature and then washed multiple times with an appropriate solvent or solvents to remove excess reagents and by- products to give the resin-compound of formula (XXV).

Resin-compound of formula (XXV) is deprotected to liberate the compound of formula (XXVI), which is then suspended in a polar aprotic solvent such as DMF or THF. An excess of the appropriate compound of formula (Vlllb) is added followed by an excess of a base such as triethylamine or diisopropylethylamine. The mixture is agitated and heated to 50-100"C for 1 to 24 hours, then cooled and washed multiple times with an appropriate solvent to remove excess reagents and by products to give resin-compound of formula (IXaa). The resin-compound of formula (IXaa) is optionally treated to liberate protected functionality incorporated as part of a synthon to produce the compound of formula (lii).

For those compounds in which the substitution pattern of the piperazine is reversed

(e.g., examples 95-102 below), the procedure of the preceding paragraph may be slightly modified. Resin-compound of formula (XXV) is deprotected with piperidine to liberate an amine and then dissolved or suspended in an inert solvent, such as methylene dichloride. An excess of an appropriately protected acid that will furnish R6 is added followed by a coupling agent such as HATU, BOP or DIC with the optional addition of an acylation catalyst such as DMAP or HOBT. Alternatively an excess of an activated form of the acid, such as the symmetrical anhydride or acyl fluoride may be added to the resin. The mixture is shaken for 1 to 24 hours at ambient temperature and then washed multiple times with an appropriate solvent or solvents to remove excess reagents. The product is suspended in a polar aprotic solvent, such as DMF or THF. An excess of the appropriate compound of formula (Vlllb) is added followed by an excess of a base such as triethylamine or diisopropylethyl-amine. The mixture is agitated and heated to 50-100"C for 1 to 24 hours, then cooled and washed multiple times with an appropriate solvent to remove excess reagents and by products to give resin compounds analogous to the resin-compound of formula (IXaa), but having the pyrimidine attached to the piperazineacetic acid at the 4-position.

This resin compound analogus to the resin-compound of formula (IXaa) is then suspended in a protic solvent such as methanol or acetonitrile-water and stirred and photolyzed to cleave the product from the resin. Filtration, and evaporation of the filtrate gives the crude product, which is then purified and characterized by standard techniques.

In a specific example, 1.57 g of an amino-functionalized TentaGel resin (0.80 mmole) was suspended in 20 mL of methylene chloride and treated with 1.05 g of linker acid (2.4 mmole), 0.50 mL of DIC (3.2 mmole), and 20 mg of DMAP (0.16 mmole). The mixture was shaken at room temperature for 20 hours and then washed with methylene chloride ten times to give a resin-compound of formula (XXI I). The resin-compound of formula (XXII) was treated with 50% trifluoroacetic acid (TFA) in methylene chloride at room temperature for 2 hours and then washed with methylene chloride ten times, 15% triethylamine in methylene chloride for 10 minutes, and again methylene chloride for 5 times. The deprotected resin-compound of formula (XXIII) was then suspended in 12 mL of methylene chloride and treated with 1.444 g of the compound of of formula (XXIV) (3.2 mmole), 1.216 g of HATU (3.2 mmole), and 1.3 mL of diisopropylethylamine (7.2 mmole). The mixture was shaken for 16 hours at ambient temperature and then washed 5 times to give resin-compound of formula (XXV). The Fmoc was removed by treatment with 30% piperidine in DMF and 777 mg of the resulting resin-bound compound of formula (XXVI) (0.35 mmole) was then reacted with 320 mg of 2-imidazolyl- chloropyrimidine (the compound of formula (Vlllb)), in the presence of 0.61 mL of

diisopropylethylamine (3.5 mmole) in 12 mL of DMF at 80"C for 15 hours and then cooled to room temperature and washed with DMF and methylene chloride to give the resin-compound of formula (IXaa). The final product was cleaved from the resin by photolysis in methanol (MeOH) for 17 hours to give 54.6 mg of product, a compound of formula (lii) (31%). The crude product was purified by flash chromatography (eluted with 4:4:1 ethyl acetate:hexanes:MeOH). The Boc-protected amine product was treated with 3 mL of 30% TFA-methylene chloride for 1 hour and was dried in vacuo to give quantitative amount of product.

The piperazineacetic acid compound of formula (XXIV) employed in the synthesis above and many others in this application was synthesized as follows: Twelve milliliters (50 mmol) of N,N'-dibenzylethylene-diamine, 14 mL (100 mmol) of Et3N and 250 mL toluene were combined at 0°C, and 7 mL (50 mmol) of methyl 4-bromocrotonate (7 mL, 50 mmol) was added. The reaction was slowly warmed to room temperature, stirred for 24 hours, filtered, concentrated in vacuo to a residue and treated with 10% aqueous HCI (300 mL). The mixture was filtered again and the filtrate washed with ethyl acetate (2x100 mL). The filtrate was made basic with K 2C03 and extracted with ethyl acetate (3x150 mL). The combined extracts were washed with brine, dried over MgSO4 and concentrated in vacuo to give 13.7 g of methyl 1 ,4-dibenzylpiperazine-2- acetate. 1H NMR (CDCI3) 6 2.28-2.50 (m,4H), 2.5-2.75 (m,4H), 3.1 (bs, 1H), 3.42 (d,2H), 3.52 (d,lH), 3.6 (s,3H), 3.75 (d,lH), 7.15-7.35 (m,lH).

The 13.7 g (40 mmol) of methyl 1 ,4-dibenzylpiperazine-2-acetate, 150 mL of MeOH, 50 mL of 1 N HCI (aqueous) and 3 g of 10% Pd/C were combined and hydrogenated with H 2 (50 psi) for 24 hours. The reaction was filtered, the filtrate was concentrated in vacuo to remove most of the MeOH, and the residue was made basic with K 2CO3 to pH = 9-10, and 9.8 g (40 mmol) of BOC-ON was added slowly at 0° C. The reaction was stirred at 0° for 1 hour, allowed to warm up to room temperature, stirred for 2 hours, and extracted with ethyl acetate (2x200 mL). The combined extracts were treated with 50 mL of 10% HCI (aqueous).

The aqueous layer was washed with ethyl acetate, basified with K 2C03 and extracted three times with ethyl acetate. The combined organic layers were washed with brine, dried over MgSO4 and concentrated in vacuo to give 7.89 g of methyl 4-Boc-piperazine-2-acetate; H NMR (CDCl3) a 1.4 (s,9H), 2.31 (dd,lH), 2.37 (dd, 1H), 2.55 (b, 1H), 2.69-3.02 (m,4H), 3.75 (s,3H), 3.88 (b,2H).

A portion (5.2 g; 20 mmol) of the methyl 4-Boc-piperazine-2-acetate product from the previous step was combined with 60 mL of THF and 60 mL of 1 N NaOH (aqueous) and stirred at room temperature for 6 hours to saponify the methyl ester. The reaction was cooled to 0°C, adjusted to pH 9-10 with 10% HCl(aqueous), and 5.2 g (20 mmol) of FMOC-CI was added.

The reaction was stirred at room temperature for 6 hours, (adding 1 N NaOH (aqueous) to maintain pH = 9-10) 1 hour, then acidified with 10% HCI to pH = 1. The reaction was extracted twice, the combined organic layers were washed with brine, dried over MgSO 4 and concentrated in vacuo to give 8.56 g of the desired 4-Boc-1 -Fmoc-piperazine-2-acetic acid (the compound of formula (XXIV)); 1H NMR (CDC13) 1.4 (s,9H), 2.5-3.0 (m,5H), 3.9-4.2 (m,6H), 4.5 (m,lH), 7-25 (t,4H), 7.32 (t,4H), 7.48 (d,4H), 7.75 (d,4H).

In the cases in which 4-Boc-1 -Fmoc-piperazine-2-acetic acid (the compound of formula (XXIV)) was replaced by 4-Boc-1-Fmoc-piperazine-2-carboxylic acid, the starting material was prepared by dissolving 5.25 g (25.85 mmol) of 2-piperazine carboxylic acid-2HCI in 160 mL of 1:1 dioxane/H20, and adjusting the pH to 11 with 50% NaOH (aq.). A solution of 7.21 g (29.28 mmol) of BOC-ON in 40 mL of dioxane was slowly added (in portions) while maintaining the pH at 11 with 50% NaOH (aq.) during the addition. The reaction was stirred at room temperature for 5 hours, then cooled to 0°C and adjusted to pH 9.5 with 50% NaOH (aq.). A solution of 7.34 g (28.37 mmol) of FMOC-CI in 40 mL of dioxane was slowly added (in portions) , maintaining a pH of 9.5 during the addition with 50% NaOH (aq.). The mixture was warmed to room temperature, stirred for 20 hours, washed with ethyl ether (3x150 mL), adjusted to pH = 2-3 with 6N HCI (aq.), and extracted with toluene (3x150 mL). The combined extracts were dried over Na2SO4, concentrated in vacuo to a volume of 150 mL and chilled at -20" C overnight.

The resulting solids were filtered off, washed with hexane and dried in vacuo to give 5.4 g of the desired 4-Boc-1 -Fmoc-piperazine-2-carboxylic acid.

Alternatively, 4-Boc-morpholine-3-carboxylic acid, which can be substituted for the compound of formula (XXIV) in Reaction Scheme 7 above to prepare other compounds of the invention, can be prepared in the following manner: To a solution of 4-phenylmethylmorpholin- 5-one-3-carboxylic acid methyl ester (5.1 g. 20.5 mmol) in 100 mL of THF was added borane/DMS (1 OM, 2.6 mL) slowly while cooling at 0 "C. The solution was allowed to warm to ambient temperature and stirred for 18 hours. Water (100 mL) was then added and the mixture extracted with ethyl acetate. The organic layers were dried over MgSO 4 and concentrated.

The resulting oil was purified on a silica gel column eluted with 3:7 ethyl:hexanes to yield the morpholine (3.0 g, 64%). The morpholine (3.0 g. 12.75 mmol) was dissolved in 50 mL MeOH and 10% Pd/C (10 mg) was added. The mixture was stirred at ambient temperature under a H 2 atmosphere for 16 hours. The mixture was then filtered through celite and concentrated. The resulting oil was dissolved in CH2Cl2 (25 mL) and di-t-butyldicarbonate (2.8 g, 12.75 mmol) was added. After stirring for 4 hours, the mixture was concentrated and taken up in CH 2CI2 and washed with water, saturated NaHCO3, and brine. The organic layer was dried over MgSO4 and

concentrated to yield 2.8 g (89%) of the ester. The ester was dissolved in MeOH (30 mL) and NaOH (1.4 g, 35 mmol) was added. After stirring for 4 hours at reflux, the solution was concentrated, acidified with 1 N HCI and extracted with CH 2cm2. The organic layer was dried (MgSO4) and concentrated to yield 4-Boc-morpholine-3-carboxylic acid as a white solid (2.4 g, 90 %). 1H NMR (CDC13)61.40 (m, 9H). 3.20-350(m. 2H), 3.70(m, 2H), 3.90 (m, 1H). 4.30-4.65 (m, 2H).

1-Boc-perhydroazepine-2-acetic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: N-Boc- perhydroazepine (1.06 g, 6.16 mmol) in ether is treated with TMEDA (715 mg, 6.16 mmol) followed by sec-butyliithium (1.3 M. 4.74 ml, 6.16 mmol) at -78 "C. The reaction was slowly warmed to A00C, stirred for 1 hour, cooled to -78 "C and treated with a solution of 3,3- dimethylallyl bromide (918 mg. 6.16 mmol) in ether. After warming to room temperature and quenching with water, the organic layer is washed with water, 1 M NaH 2P04, water, and brine.

After drying (MgSO4), the solvent is removed and the product is purified by chromatography (silica gel, hexane:ethyl acetate 95:5), to yield the olefin (300 mg, 21%, 1H NMR (CDCI3) 85.05-5.20 (m, lH), 3.55-3.80 (m, 2H), 2.60-2.75 (m, lH). 1.90-2.20 (M, 3H), 1.10-1.80 (m, 22H). To a solution of NalO4 (2.17 g, 10.2 mmol) and KMnO4 (32 mg, 0.2 mmol) in 45 mL of water was added K2C03 (162 mg, 1.18 mmol) and the olefin (300 mg, 1.12 mmol) dissolved in t-butanol (11 ml). After stirring for three days, the reaction was acidified to pH 3 and extracted with ethyl acetate. The organic layer was washed with water and brine, dried (MgSO 4), and the solvent was removed in vacuo to give 1-Boc-perhydroazepine-2-acetic acid (250 mg, 87%): 1H NMR (CDCI3) ô 4.20-4.45 (m, lH), 3.55-3.80 (m, lH), 2.00-2.80 (m, 4H), 1.10-1.80 (m, 16H).

4-Boc-morpholine-3-acetic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7, and can be prepared in the following manner from 4-benzylmorpholine-3-acetic acid ethyl ester (Brown, G. R; Foubister. A. J.; Stribling. D. J.

Chem. Soc. Perkin Trans. 1 (1987), p. 547). After hydrogenolysis (Pd(OH)2, H2) of the benzyl group, the N-Boc derivative is prepared by treatment with di- t-butyldicarbonate and the ethyl ester is hydrolyzed by aqueous base to provide 4-Boc-morpholine-3-acetic acid.

1 -Boc-pyrrolidine-2-propionic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: Boc-pyrrolidine (5.0 g, 29.2 mmol) was dissolved in ether (35 ml) and TMEDA (3.0 g, 20 mmol), cooled to -78°C and s-butyllithium (1.3 M, 17 ml, 22 mmol) was added. After stirring for 1 hour, allyl bromide (5.1 mL, 57 mmol) was added. After warming to room temperature, the reaction was quenched with water and the organic layer was separated. The organic layer was dried

(MgSO4) and the solvent was removed in vacuo to give the olefin (2.9 g, 47%, 1H NMR (CDC13) a 5.65-5.85 (m. 1H), 5,.00-5.20 (m, 2H), 3.70-3.90 (m 1H). 3.20-3.45 (m, 2H). 2.35-2.60 (M, 1 H). 2.00-2.20 (m, 1 H), 1.60-2.00 (m, 4H), 1.45 (s, 9H)). To the olefin (1.0 g, 4.7 mmol) in THF (20 mL) at 0 "C was added borane/THF. After warming to room temperature and stirring for 1 hour, H202 (30%, 14 mL) and 3N NaOH (3.2 mL) were added. The reaction was partitioned with ethyl acetate and separated. The organic layer was dried and concentrated in vacuo. The residue was added to NalO4 (1.2 g, 5.4 mmol) and Ru04 (10 mg, 0.08 mmol) in water (100 mL) and acetone (10 mL). After stirring for 1 hour, the reaction was concentrated and extracted with CH2CI2. The organic layer was extracted with 1 N NaOH. The aqueous layer was washed with CH2CI2, made acidic with 1 N HCI, and extracted with CH 2Cl2. The organic layer was dried (MgSO4) and concentrated to give 0.14 g (26%) of 1-Boc-pyrrolidine-2-propionic acid: 1H NMR (CDCI3) 8 1.40 (m, 9H), 1.60-2.00 (m, 6H), 2.20 (m, 2H). 2.40 (m, 2H), 3.30 (m. 2H), 3.90 (m, lH).

4-Boc-thiomorpholine-3-carboxylic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: To THF was added cysteine ethyl ester hydrochloride (1.15 g, 6.18 mmol), triethylamine (4.17 mL, 30 mmol) and dibromoethane (2.51 mL, 6.2 mmol). After stirring for 1 hour and refluxing for 16 hours, the solids were removed by filtration. The solvent was removed in vacuo and the residue was chromatographed on silica to give thiomorpholinecarboxylic acid ethyl ester (0.94 g, 87%). The ester (15.3 g, 95 mmol) was dissolved in dioxane/water (1/1) and di- t- butyldicarbonate (24 g, 110 mmol) and LiOH were added. After stirring for 3 hours, the solvent was removed in vacuo and the pH was adjusted to 3 with KHSO 3 and extracted with ethyl acetate. The organic layer was separated, washed with brine, dried (MgSO 4), and the solvent was removed in vacuo to give 17.4 9 (78%) 4-Boc-thiomorpholine-3-carboxylic acid: 1H NMR (CDCI3) ô 1.45 (m, 9H), 2.45 (m, lH), 2.71 (m, lH). 2.93 (m, lH), 3.10 (m. lH), 3.29 (m, 1H), 4.11 (m, lH), 4.19 (m, 1H), 5.20 (m, lH).

4-Boc-thiomorpholine-3-acetic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: To THF (50 mL) was added methyl bromocrotonate (1.0 mL, 8.6 mmol), Hünig's base (1.5 mL, 8.6 mmol), and N-Boc-2-aminoethanethiol (1.5 g, 8.6 mmol). After stirring for 3 hours, the reaction was poured into saturated NH4CI and extracted with ethyl acetate. The organic layer was washed with brine, dried (MgSO4), and the solvent was removed in vacuo. Chromatography (hexane/ethyl acetate, 6/1) gave N-Boc-2-aminoethanethiocrotonic acid methyl ester. The ester was dissolved in CH2C12 (80 mL) and TFA (20 mL) was added. After stirring for 1 hour, the solvent

was removed in vacuo. The residue was added to a solution of toluene and TEA (2.5 ml). After stirring for 16 hours, the solvent was removed in vacuo and the residue was chromatographed to give the thiomorpholine. The ester (18.0 g, 95 mmol) was dissolved in dioxane/water (1/1) and di-t-butyldicarbonate (19.6 g, 90 mmol) and LiOH were added. After stirring for 12 hours, the solvent was removed in vacuo and the pH was adjusted to 3 with KHSO 3 and extracted with ethyl acetate. The organic layer was separated, washed with brine, dried (MgSO 4), and the solvent was removed in vacuo to give 20.3 g (86%) 4-Boc-thiomorpholine-3-acetic acid: 1H NMR (CDCI3) 1.45 (m, 9H), 2.45 (m, 1 H), 2.51 (m, 1 H). 2.68 (m, 1 H), 2.82 (m, 1 H), 3.05 (m.

4H), 4.24 (s, 1H), 4.93 (s, 1H).

4-Boc-thiomorpholine-2-acetic acid can also be substituted for the compound of formula (XXIV) in Reaction Scheme 7 and can be prepared in the following manner: To THF (100 mL) was added diethyl fumarate (3.27 mL, 820 mmol), DBU (7.22 mL, 50 mmol), and aminoethanethiol hydrochloride (2.26 g, 20 mmol). After refluxing for 16 hours, the reaction was poured into saturated NaHCO3, and extracted with ethyl acetate. The organic layer was washed with brine, dried (MgSO4), and the solvent was removed in vacuo. Chromatography (ethyl acetate) gave thiomorpholinone (2.61 g, 70%). The ester was dissolved in THF (50 mL) and borane/DMS (3 mL, 30 mmol) was added. After stirring for 16 hours, ethanol was added to quench the reaction. HCI gas was bubbled into the reaction and the mixture was refluxed for 2 hours. The solvent was removed in vacuo and the residue was suspended in 0.5 M NaOH and CH2CI2. The organic layer was separated, dried (Na2SO4), and the solvent was removed in vacuo. Chromatography on silica (MeOH/ethyl acetate) afforded starting material (0.71 g, 29%) and the thiomorpholine (1.26 g, 56%). The ester (3.0 g, 11.4 mmol) was dissolved in dioxane/water (1/1) and di-t-butyldicarbonate (2.29 g, 10.5 mmol) and LiOH were added. After stirring for 12 hours, the solvent was removed in vacuo and the pH was adjusted to 3 with KHSO4 and partitioned with ethyl acetate. The organic layer was separated, washed with brine, dried (MgSO4), and the solvent was removed in vacuo to give 2.20 g (81%) 4-Boc- thiomorpholine-2-acetic acid: 1H NMR (CDCI3) 8 1.44 (m, 9H), 2.59 (m, 4H), 3.17 (m, lH). 3.2- 4.0 (m, 4H).

Reaction Scheme 7 depicts a synthesis in which a preformed, protected compound of formula (XXI) is coupled to the resin and deprotected to allow reaction with the protected compound of formula (XXIV). It will be apparent to the artisan that the sequence of this reaction series could be altered to provide the same deprotected piperonylamino-methyl benzoyl resin. An example of such a sequence follows. This example also illustrates how one would reverse the substitution pattern in the piperazineacetic acid ring.

4-Bromomethyl-3-nitrobenzoic acid (819 mg, 3.15 mmol) and HOBt (426 mg, 3.15 mmol) were taken up in 15 mL of DMF, DIC (795 mg, 6.30 mmol) was added and the contents were stirred for 30 min at ambient temperature. The mixture was then added to the resin and shaken overnight. The resin was filtered, washed and dried as before. The resin showed negative ninhydrin stain. The resin was taken in 15 mL of THF containing piperonyl amine (1.51 g, 10 mmol), and shaken over the weekend. The resin was filtered, washed and dried (1.507 g). N'-Fmoc-N4-Boc-piperazine-2-acetic acid (978 mg, 2.1 mmol), HATU (798 mg, 2.1 mmol) and DIEA (542 mg, 4.2 mmol) were mixed in 15 mL of DMF; and then added to the resin. After shaking for 24 hours, the resin was filtered, washed and dried as usual; the resin weighed 1.693 g. The resin was taken in 15 mL of 30% v/v piperidine in DMF, and shaken for 2 hours to cleave the Fmoc protecting group. After filtration, the resin was subjected to the usual wash and dry cycle; the resin weighed 1.588 g. The resin, acetic anhydride (591 mg, 5.8 mmol) and DIEA (748 mg, 5.8 mmol) were taken in 15 mL of meth ylene chloride and shaken overnight to acetylate at N1. After filtration, the resin was washed with methylene chloride and dried in a vacuum desiccator for 5 hours. The resin was shaken with 15 mL of 1:1 TFA:methylene chloride for 1 hour to cleave the tBoc protecting group at N4. After filtration, the resin was washed with methylene chloride (5x15 mL), followed by 20% triethyl amine in methylene chloride (5x15 mL) and then again with methylene chloride (5x15 mL). After drying, the resin weighed 1.294 g. 669 Mg of the resin from the previous step, DIEA (116 mg., 0.9 mmol) and 4-chloro-2-(1-imidazolyl)-6-isopropylpyrimidine (200 mg, 0.9 mmol) were taken up in 6 mL of DMF and heated to 80"C for 24 hours. After filtration the resin was washed (DMF, methanol and methylene chloride) and dried. A portion (377 mg) of the resin from the previous step was suspended in methanol and photolyzed at 50"C for 6 hours. The solution was filtered, the solvent was removed and the residue was purified by chromatography (silica, methylene chloride:methanol, 95.5), yield 14 mg. 1H NMR and MS were consistent with the proposed structure.

The following compounds, shown in Table 1 through Table 7 are representative of the compounds of the inventions and were synthesized by the foregoing methods. All exhibited iNOS inhibitory activity at concentrations less than 25 FM.

TABLE 1 Ex. # R2 R5 R0 N 1 -CH2R9 R6 H H N \CH3 isNY CH3 2 -CH2R9 R6 CI Ac ½ f Na CH3 )NY CH3 3 -CH2R9 R6 6 H Boc ½ fN\ $NY CH3 Vex.# R2 A R9 . ' ., . o ,., 0 ~~ 4 -CH2R9 R6 | Cl 6 Boc N I;N)L CH3 5 -CH2R9 R6 F Boc ½ S -CH CH3 6 -CH2R9 R6 CI H n N $NY 7 j -CH2R9 R6 | tRN6i CI tCH3 H IsNY CH3 8 -CH2R9 R6 CI H N Ex. # RZ (J) 1 R6 9 R9 . ... " 9 -CH2R9 R6 Cl H ½ N N CI 10 -(CH2)rR9 R6 CI H g sNY 11 -CH3 R6 Cl H IsNY 12 -(CH2)3-R9 R6 CI H ½ N I;NY 13 -CH3 ½ CI Ex.# R2 R6 - R9 I - 9 29 | -CH R6 | H | < H ½ N $NY R6 H H 30 -CH2R9 sNY ¼OCH3 34 -CH2R9 R6 | Cl H 1 N (INY 35 -(CH2)2-R9 R6 CI H 36 -CH2R9 R6 Cl H N $NY iBe # # () f R6 R9 N 52 -CH2R9 -C R6 < try H < H 58 -CH2R9 R6 j CI Boc N $NY CI 59 -CH3 R6 Cl Boc sNY 60 -CH2R9 R6 CI Boc 1 coy $NY 76 -(CH2)rR9 R6 CI -C(O)CH2OCH3 O N A r\ R2 (T) Rs f R9 I - 77 -(CH2)rR9 -(CH2 2or9 | R6 H -C(O)O(CH2)3CH3 ¼) sNY 78 -(CH2)rR9 R16 iPr °<O O O> f sNY 79 71 (C Rffl -(CH2)rR9 R6 H I 80 -(CH2)2-R9 R6 CI Boc OCH3 IsNY OCH3 81 -(CH2)rR9 R6 CH3 Boc OCH3 I ½ N N 7 - r - | t Rl R3 - R9 82 -(CH2 2-R9 R6 Cl Ac < OCH3 ½ N N 83 -(CH2 2-R9 R16 Rs | CI -C(O)CH2CH(CH3)2 OCH3 IsNY OCH3 84 -(CH2 2-R9 R6 CNR6i | CI H | 4 OCH3 ½ N NI 85 -(CH2 2-Rg R6 | CH3 H | < OCH3 sNY OCH3 86 -(CH2)rR9 CI R AN (;;) R2 f ~~. I - 87 -(CH2)rR9 R6 )/ Cl -C(O)CH2CH(CH3)2 OCH3 I 1$ N' 88 -(CH2)rR9 R6 CH3 Ac \C OCH3 I I) sNY OCH3 89 (CH2)rR9 -(CH2 2or9 P con f | CH3 -C(O)CH2CH(CH3)2 \ OCH3 ';NY OCH3 90 -CH2R9 R6 | CNRS | CI -C(O)OCH3 i < I I) sNY 91 -CH2R9 gSoC3 C O 0 R6 Cl ocHa I 0 N M¼N. (NY H 0 Ex# f Re a F? gN 92 -CH2R9 R6 b CI ½OCH3 It rNA <~O N 95 -CH2R9 R6 iPr -C(O)OCH3 ½ 0 (NY 96 -CH2R9 R6 CH3 -C(0)OCH3 N Ex.# F? AN R R 97 -CH2R9 R6 Cl -C(O)OCH3 XL XC 98 -CH2R9 R6 H -C(O)OCH3 ) (NY 99 -CH2R9 R6 CI -C(O)OCH3 t CH X (NY 100 -CH2R9 R6 H -C(O)OCH3 \0- (NY 101 -CH2R9 R6 CF3 Ac ½ 0 N Ex. # ç AN Re Re R9 I - 102 j -CH2R9 R6 iPr Ac C O (NY 103 -CH2R9 R6 CH3 -C(O)OC(CH3)3 N Io (NY 104 -CH2R9 R6 iPr -C(O)OC(CH3)3 (NY 105 -CH2R9 R6 b CF3 Ac N (NY 106 -CH2R9 R6 iPr Ac ½ coy N (NY Rr RB A Re R9 N ... . 107 -CH2R9 R6 Et Ac N I (NY 0 108 -CH2R9 °sg CI \> 109 -CH2R9 °sg CH3 N 110 -CH2R9 °sg iPr N I 111 -CH2R9 S CI 0 112 -CH2R9 S CH3 Ex, # 1R2 R5 5 Rg R9 N 113 -CH2R9 (:Y iPr 114 -(CH2)rR9 S CI N 115 -(CH2)2-R9 S CH3 N 116 -(CH2)2-R9 S iPr N 117 -CH2R9 s Cl 118 -CH2R9 sg CH3 \> Ex. # R5 (^) RS lR6 R9 AN : 119 -CH2R9 .S iPr 120 -(CH2)2-R9 S CI N 0 121 -(CH2)2-R9 sug CH3 \< 122 -(CH2)2-R9 .S Pr ALl; TABLE 2 Ex. # R2 - Q) R5 R9 R9 19 -CH2-R9 HO, Cl N H 42 -(CH2)rR9 ( Cl OCH3 OCH3 H 123 -(CH2)rR9 R6 Cl -C(O)CH2CH(CH3)2 ½ OCH3 N (NY r Ex.# 1t2 (;) F? f 1 R9 N 124 -(CH2)rR9 R6 CI Boc OCH3 I I OCH3 N 125 -(CH2)2-RS R6 CJ H .OCH3 1 126 -(CH2)rRS 6 CI AC ½ OCH3 N (NY OCH3 127 -(CH2)rR9 R6 CI Ac <OC (NY 128 -(CH2)rR9 o CI H Ex. # R2 fl (m F? R9 N lll 129 -(CH2)2-R9 Ko Pr 130 -(CH2)rR9 0 CI N 131 -(CH2)2-R9 o iPr N 132 -(CH2)2 R9 O CI ½ OCH3 N OCH3 133 -(CH2)2-R9 0 iPr 134 -(CH2)rR9 (:Y Ci Ex.# R2 czars Re R9 135 -(CH2)2-R9 °st Pr \> 136 -CH2- 9 H3CN, CH3 0 0 it 137 -CHrR9 H3C 0 N iPr ¼;) H3C iii 138 -CHrR9 H3C)m CI it 139 -CH2-R9 CH3 \< H 140 -CH2-RS Et \< H tt~~ - ll ll lll Ex.# R2 AN M R. R9 N 141 -CHrR9 iPr \< H 142 -CH2-R9 CI O H 143 -(CH2)rR9 \ CH3 \< H 144 -(CH2)2-R9 Et AL) H 145 -(CH2)rR9 iPr \> I H 146 -(CH2)2-R9 Cl AL) H TABLE 3 Amino Acids (AA) Derived Compounds of the Invention Ex. R2 R4 R5 QwR3 R9 (from m n p AA (from om R2) 14 -CH2R9 H CI -SCH3 \+ 2 0 O D-Met ~ ~ 15 -CH2R9 H CI -SCH3 < 2 0 0 D-Met oc 16 -(CH2)2R9 H CI < OCH3 1 0 0 [D] OCH3 17 -(CH2)3CH3 H CI 1 ° ° [D] s ~ ~ ~ 18 -CH2R9 H CI H > 0 2 2 Acp 20 -(CH2)2R9 H Cl H orsrOCH3 O 0 O Gly ocH3 21 -CH2R9 H CI -OH < > 1 0 O D,L- Io Ser EL # R2 e R4 49 s10 m n p AA (fro-in R2) 22 -CH2R9 CH3 Cl H \+ 0 0 O Sar 23 -CH2R9 H CI -CONH2 \+ 2 0 o L-Gln 24 -(CH2)2R9 H CI H OCH3 1 0 0 D,L- uOCH3 Ala 25 -CH2R9 H CI -CONH2 w 2 0 0 D-Gln L-Arg 26 -CH2R9 H CI NHyjNO2 XCC°> 3 3 ° 0 (NO2) NH2 O 27 -(CH2)2R9 H CI -CONH2 orsrOCH3 2 0 o D-Gln 28 -CH2R9 H Cl -NH2 O 3 0 0 D,L- uo> Orn o 31 -(CH2)3R9 H H /7 / \ 1 0 O [D] h O m/ 32 -CH2R9 H H -CONH2 o 2 0 o L-Gln 37 -CH2R9 H CI -SCH3 orsrOCH3 2 0 0 D-Met 38 -CH3 H CI -SCH3 i 2 0 0 D-Met 10 39 -(CH2)3R H Cl -StBu -SCH3 1 0 0 L-Cys 40 -(CH2)3R9 H CI -StBU phenyl 1 0 0 D-Cys 41 -CH2R9 H CI hM A° 1 ° ° [D] tsS Wo> ~ ~ Ex 2 M e wg (Rf n R2) p n P MAA n - (from) ., 43 -CH2R9 H CI -CONH2 4;OCH3 2 0 O D-Gln OCH3 44 -CH2R9 H CI -CONH2 orOCH3 2 0 O L-Gln 45 -CH2R9 H CI NNO2 3 0 0 L-Arg -NH/ \0ocy, (N03 NH2 48 -(CH2)3CH3 H Cl -NH2 3 0 0 D,L- Orn 49 -(CH2)2R1° H CI -COOH -COOH 1 0 O D,L- Asp 50 -(CH2)3R9 H CI phenyl -S(O)2CH3 1 0 0 D,L- Phe 51 -CH2R9 CH3 Cl H N 0 0 0 Sar CH3 CI H O 0 53 -CH2R9 H H -OH Co> 1 0 0 D,L- Ser 54 -CH2R9 H H N- NO2 O 3 0 O L-Arg (NO2) NH2 56 -(CH2)2R9 H CI 03 OCHs 1 0 O [L] 57 -CH2R9 H Cl 03 <2> 1 0 O [L] 61 -(CH2)2R9 CH3 CI H oO O 0 O Sar Ex. Rz Rs . RorR10 m n p AA # . tfrom 2) I36 (frwn R2) P AA 62 -(CH2)2R9 H CI H OCH3 1 0 O D-Ala OCH3 64 -(CH2)3R9 H Cl (3 OCH3 1 0 O [D] dOCH3 65 -(CH2)4R9 H Cl O #;;:; 1 0 O [D] OCH3 66 -(CH2)2R9 H H (3 y;s:1; 1 0 O [D] S OCH3 ~ ~ 67 -(CH2)3R9 H H (3 sctoCH3 1 0 O [D] I YI 3 OCHS 68 -CH2R9 H CI -SCH3 \+ 2 0 O L-Met 69 -CH2R9 H CI -NHTrt o 2 0 O NY- trityl L- pd trityl L- Gln 70 -CH2R9 H CI -NHTrt o 2 0 0 NY- trityl D- o Gln TABLE 4 Amino Acids (AA) Derived Compounds of the Invention Ex. R2 R4 R5 CR3 R9orR10 m n p AA (from R2) 71 -(CH2)2R9 H CI H OCH3 1 0 0 D-Ala OCH3 72 -(CH2)3R9 H CI t y;OcH3 1 0 O O [D] OCH3 73 -(CH2)4R9 H CI \CtocH, 1 O o [D] OCH3 74 -CH2R9 CH3 Cl H tl 0 0 O Sar TABLE 5 Amino Acids (AA) Derived Compounds of the Invention Ex.# R2 R4 R5 O-R3 R9 or R10 (from m n p AA 2 R) 75 -(CH2)2R9 H Cl H ¼ocH3 1 0 O D-Ala ocH3 63 -(CH2)2R9 H H H OCH3 1 0 O D-Ala oc TABLE 6 Physical Data for Compounds of the Invention Ex. # Formula FABMS Definitive 1H NMR (ppm) 1 C21H24N7O 392 9.6(1H), 8.3 (1H), 8.2(1H), 6.9-7.5 (6H), 2.2 (3H) 2 C23H26ClN7O 468 8.5 (1H), 7.6-7.8 (1H), 6.9-7.2 (6H), 2.3 (3H), 2.1 (3H) 3 C26H32N7O3 492 8.5 (1H), 8.2 (1H), 7.8 (1H), 7.0-7.2 (5H), 6.6 (1H), 2.3 (3H), 1.5 (9H) 4 C26H32CIN703 526 8.5 (1H), 7.8 (1H), 7.0-7.2 (6H), 2.3 (3H), 1.5 (9H) 5 C26H32FN703 510 8.5 (1H), 7.8 (1H), 7.0-7.2 (6H), 2.3 (3H), 1.5 (9H) 6 C21H22ClN7O3 456 ND 7 C21H24CIN70 ND 9.6 (1 H), 8.3 (1 H), 8.2(1 H), 6.9-7.5 (6H) 9 C20H21C12N70 446 9.6 (1H), 8.1 (1H), 7.4 (1H), 7.0 (4H), 6.9 (1H) 11 Cr4H8CIN7O 336 9.7 (1 H), 8.2 (1 H), 7.5 (1 H), 6.9 (1 H), 2.6 (3H) 14 C20H21ClN6O3S 461 2.0 (SCH3) 16 C23H23ClN603S ND 2.65 (m, 2H), 3.36 (m, 2H), 3.55 (m, 2H), 3.79 (s, 3H), 3.80 (m, 2H), 3.83 (s, 3H), 4.77(m, 1H), 6:30 (s, 1H), 6.32(bs, 1H), 6.55-6.95(m, 5H), 7.08 (s, 1H), 7.18(d, 1H), 7.78 (s, 1H), 8.45 (s, 1H). 18 C21H23CIN603 443 8.4 (1H), 7.8 (1H), 7.2 (1H), 7.0 (1H), 6.7 (2H), 5.9 (1H) 4.2 (2H), 2.2 (2H) 22 C18H17ClN6O3 ND 3.2 (s,3H), 4.25 (s,2H), 4.38 (s, 2H), 5.88(s, 2H), 6.30 (brs, 1 H), 6.42(bs, 2H), 6.65(m, 3H), 7.05(s, 1 H), 8.40(s, 1 H). 56 C24H25ClN6O3S ND 8.5 (1H), 7.8 (1H), 7.2 (1H), 7.1 (1H), 3.9 (6H) 57 C22H19ClN6O3S ND 8.5 (1H), 7.8 (1H), 7.2 (1H), 7.1 (1H), 4.3 (2H) 58 C25H29Cl2N7O3 546 8.5 (1H), 7.8 (1H), 7.2-7.4 (5H), 6.6 (1H), 1,4 (9H) 59 C19H26ClN7O3 436 8.5 (1H), 7.8 (1H), 7.1 (1H), 6.6 (2H), 1.5 (9H) 60 C26H30CIN705 556 8.5 (1H), 7.8 (1H), 7.1 (1H), 6.7 (4H), 5.9 (2H), 1.5 (9H) 61 C19H20N6O3 ND 3.22(s, 3H), 4.24(bs, 2H), 4.32(d, 2H), 5.92(s, 2H), 6.30(bs, 1H), 6.47(d, 1H), 6.65(m,3H), 7.04 (s, 1H), 7.68(s, 1H), 7.95(d, 1H), 8.41(s, 1H). Ex. # Formula FABMS Definitive 1H NMR (ppm) 62 C2oH23clN6o3 ND 1.48(d, 3H), 2.78(m, 2H), 3.58(2H, m), 3.80(6H, s), 4.60(1 H, m), 5.9-6.25(3H, m), 6.55-6.8(3H, m), 7.12(1H, s), 7.78(1H, s), 8.44(1H, s). 63 C20H24N603 ND 1 .40(d, 3H) 64 C24H25CIN603S ND 1.75(m, 2H), 2.50(m, 2H), 3.2-3.5(m, 4H), 3.82(s, 6H), 4.78(m, 1H), 6.21(m,1H), 6.36(m, 2H), 6.60-6.95(m, 5H), 7.10(s, 1H), 7.21(d, 1H), 7.80(s, 1H), 8.53(s, 1H). 65 C25H27C1N603S ND 1 .47(m, 4H), 2.52(m, 2H), 3.2-3.45(m, 4H), 3.83(s, 6H), 4.78(m, 1H), 6.08(m, 1H), 6.17(m, 2H), 6.64(m, 2H), 6.77(m, 3H), 7.13(s,1H), 7.19(d, 1H), 7.80(s, 1H), 8.51(s, 1H). 66 C23H24N603S ND 3.35-3.6(m), 3.83(s, 6H), 4.62(m, 1H), 5.75(m, 1H), 6.18(m, 1H), 6.50-6.95(m, 7H), 7.17(s, 1H), 7.19(s, 1H), 7.57(s, , 1H), 8.27(s, 1H). 67 C24H26N603S ND 1.70(m, 2H), 2.48(m, 2H), 3.1-3.5(m, 4H), 3.82(s, 6H), 4.77(s, 1 H), 5.90(d, 1 H), 6.03(m, 1 H), 6.29(d, 1H), 6.60(m, 1 H), 6.61(s, 1 H), 6.75-6.95(m, 3H), 7.12(s, 1H), 7.20(d, 1H), 7.82(s, 1H), 8.14(d, 1H), 8.57(s, 1H). 68 C20H21CIN603S 461 2.0 (SCH3) 69 C38H34ClN7O4 700 8.4 (1H), 7.6 (1H), 6.8-7.5 (16H), 6.5 (3H), 5.8- 5.9 (3H) 70 C39H34ClN7O4 700 8.4 (1H), 7.6 (1H), 6.8-7.5 (16H), 6.5 (3H), 5.8- 5.9 (3H) 71 C20H23ClN6O3 ND 1.43(d, 3H), 2.79(m, 2H), 3.57(m, 2H), 3.80(s, 3H), 3.82(s, 3H), 4.60(m, 1H), 5.95-6.20(m, 3H), 6.60-6.80(m, 3H), 7.18(s, 1H), 7.51(s, 1H), 8.28(s, 1H). 72 C24H25ClN6O3S ND 1.75(m, 2H), 2.50(m, 2H), 3,2-3,5(4H), 3.82(s, 6H), 4.78(m, 1 H), 5.85(m, 1 H), 6.10-6.25(m, 2H), 6.6-7.0(m, 3H), 6.8-7.0(m, 2H), 7.57(s, 1 H), 8.38(s, 1 H). 73 C25H27CIN603S ND 1.47(m, 4H), 2.52(m, 2H), 3.2-3.45(m, 4H), 3.83 (s, 6H), 4.78(m, 1 H), 5.80(m, 1 H), 6.22(m, 2H), 6.63-6.95(m, 5H), 7.20(m, 2H), 7.50(s, 1H), 8.33(m, 1H). 74 C18H17ClN6O3 ND 3.22(s, 3H), 4.24(s, 2H), 4.37(d, 2H), 5.96(s, 2H), 6.29(s, 1H), 6.76(s, 2H), 7.17(s, 1H), 7.56(s, 1H), 8.37(s, 1H). Ex. # Formula - FABMS Definitive 1H NMR (ppm) 75 C20H23CIN603 ND 1.43(d, 3H), 2.80(m, 2H), 3.57(m, 2H), 3.80(s, 3H), 3.82(s, 3H), 4.60(m, 1 H), 6.20(m, 1 H), 6.4- 6.5(m, 2H), 6.60-6.80(m, 3H), ,7.18(s, 1H), 7.51(s, 1 H), 8.28(s, , 1H). 76 C25H28ClN705 542 8.5(1H), 7.8(1H), 7.1(1H), 6.4-6.8 (3H), 5.9(2H), 3.4(3H) 77 C27H33N705 536 8.5(1 H), 8.2(1 H), 7.8(1 H), 7.1 (1 H), 5.9(2H) 78 C30H37N705 576 8.5(1H), 7.8(1H), 7.1(1H), 6.4(3H), 5.9(2H), 1.3(6H) 79 C29H36N804 561 8.5(1H), 8.2(1H), 7.8(1H), 7.1(1H), 5.9(2H) 80 C28H36CIN705 586 8.5(1H), 7.8(1H), 6.7-6.8(4H), 3.8(6H), 1.5(9H) 81 C29H39N705 566 8.5 (1H), 7.8(1 H), 7.1(1H), 6.6-6.8(4H), 3.8(6H), 2.4(3H), 1 .4(9H) 82 C25H30CIN704 528 8.5(1H), 7.8(1H), 7.1(1H), 6.6-6.8(4H), 3.8(6H), 2.2(3H) 83 C28H36CIN704 570 ND 84 C23H28ClN7O3 486 9.5(1H), 8.0(1H), 3.9(6H) 85 C24H31N7O3 466 9.6(1H), 8.1(1H), 2.4(3H) 86 C25H30CIN704 528 8.5(1 H), 7.8(1 H), 7.1(1 H), 3.9(6H), 2.2(3H) 87 C28H36CIN704 570 8.5(1H), 7.8(1 H), 7.1(1H), 3.9(6H), 1.0(6H) 88 C26H33N74 508 8.5(1H), 7.8(1H), 7.1(1H), 3.9(6H), 2.4(3H), 2.2(3H) 89 C29H39N704 550 8.5(1H), 7.8(1H), 7.1(1 H), 3.9(6H), 2.4(3H), 1.0(6H) 90 C23H24CIN705 514 8.5(1H0, 7.8(1H), 7.1(1H), 6.4-6.8(4H), 5.9(2H), 3.7(3H) 91 C2gH29CIN805 605 8.4(1 H), 7.6(1H), 7.2(1H), 6.9(1H), , 6.5-6.8(5H), 5.8(2H), 3.7(3H) 92 C29H30CIN7)4 576 8.4(1 H), 7.7 (1 H), 7.0(1 H), 5.8(2H), 3.7(3H) 93 C23H37ClN805S 563 8.5(1H), 7.8(1H), 7.5(3H), 7.1(1H), 5.9(2H), 2.8(6H) 94 C28H25CI2N1103 634 8.5(1H), 8.3(1H), 7.8(1H), 7.5(1H), 7.0(2H), 6.6-6.8(3H), 6.4(2H), 5.9(2H) 95 C26H31N7O5 522 8.6(1H), 7.8(1 H), 7.1(1H), 6.6-6.8(2-3H), 5.9(2H), 3.7(3H), 1.2(6H) Ex. # Formula FABMS Definitive 1H NMR (ppm) 96 C26H31N7O5 494 8.6(1H), 7.8(1H), 7.1(1H), 5.9(2H), 3.7(3H), 2.4(3H) 97 C23H24CIN705 514 8.5(1H), 7.8(1H), 5.9(2H), 3.8(3H) 98 C23H25N705 480 8.6(1H), 8.2(1H), 7.8(1H), 5.9(2H), 3.7(3H) 99 C22H23Cl2N7O3 504 8.4(1H), 7.7(1H), 7.0-7.3(6H), 3.7(3H) 100 C22H24C1N03 470 8.5(1H), 8.1(1 H), 7.8(1H), 7.1-7.3(6H), 3.8(3H) 101 C24H24F3N704 532 8.4(1H), 7.6(1H), 7.2(1H), 5.9(2H), 2.3(3H) 102 C26H31N7O4 506 8.5(1H), 7.8(1H), 7.1(1H0, 5.9(2H), 2.3(3H) 1.3(6H) 103 C27H33N705 536 8.45(1H), 7.85(1H), 7.1(1H), 5.9(2H), 2.4(3H), 1.4(9H) 104 C29H37N705 564 8.35(1H), 7.7(1H), 7.1(1H), 5.9(2H), 1.4(9H), 1.25(6H) 105 C24H24F3N704 532 8.4(1H), 7.6(1H), 7.1(1H), 5.9(2H), 2.2(3H) 106 C26H31N7O4 506 8.5(1H), 7.8(1H), 7.05(1H), 5.9(2H), 1.25(6H) 107 C25H29N704 492 | 8.5(1H), 7.8(1H), 5.9(2H), 2.65(2H), 1.3(3H) 108 C21H21ClN6O4 457 8.5(1H), 7.8(1H), 7.1(1H), 6.8(3H), 6.4(1H), 5.9(2H), 4.4(2H) 109 C22H24N604 8.5(1H), 7.8(1H), 7.1(1H), 6.8(3H), 6.2(1H), 5.9(2H), 4.4(2H), 2.4(3H) 110 C24H28N604 465 8.5(1H), 7.8(1H), 7.1(1H), 6.8(3H), 6.2(1H), 5.9(2H), 4.4(2H), 1.2(6H) 111 C21H21ClN6O3S 473.3 8.48(s, 1H), 7.76(s, 1H), 7.10(s, 1H), 6.60(m, 3H), 5.88(m, 3H), 4.32(m, 2H), 2.6-3.1(m, 6H) 112 C22H24N6O3S 453.3 8.45(s, 1H), 7.79(s, 1H), 7.07(s, 1H), 6.60(m, 3H), 6.40(bs, 1H), 6.10(m, 1H), 5.90(s, 2H), 4.30(d, 2H), 2.5-3.1(m, 6H), 3.40(s, 3H). 113 C24H28N603S 8.5(s, 1H), 7.8(s, 1H), 7.03(s, 1H), 6.60(m, 3H), 6.37(bs, 1H), 6.10(bs, 1H), 5.83(s, 2H), 4.28(m 2H), 2.45-3.1(7H), 1.24(d, 6H). 114 C22H23ClN5O3S 487.3 8.40(s, 1H), 7.68(s, 1H), 7.03(s, 1H), 6.76(s, 1H), 6.70(s, 2H), 6.53(bs, 1H), 6.45(bs, 1H), 5.93(s, 2H), 4.40(m, 4H), 3.6(m, 2H), 3.35(m, 2H), 3.00(m, 2H), 2.6-2.9(m, 4H). Ex. # Formula FABMS Definitive 1H NMR (ppm) 115 C23H26N6O3S 467.5 8.44(s, 1H), 7.7(s, 1H), 7.05(s, 1H), 6.77(s, 1H), 6.77(s,1 H), 6.71(s, H),6.50(bs,1 H), 6.28(s,1 H), 5.95(s,1 H), 5.92(s,2H), 4.40(m,4H), 3.58(m,2H), 3.30(m, 2H), 2.6-3.05(m, 6H), 2.40(s, 3H). 116 C25H30N6O3S 495.4 8.45(s, 1H), 7.77(s, 1H), 7.06(s, 1H), 6.86(s, 1 H), 6.70(s, 2H), 6.55(bs, lH), 6.28(s, 1 H), 5.90(s, 2H), 4.41(d, 2H), 3.58(m, 2H), 3.38(m, 2H), 2.6-3.0(m, 7H), 1.25(d, 6H). 117 C21H21ClN6O3S 473.4 8.41(s, 1H), 7.78(s, 1H), 7.03(s, 1H), 6.75(m, 2H), 6.43(s, 1H), 6.30(bs, 1H), 4.2-4.5(bs, 4H), 3.76(m, 2H), 3.4(m, 1 H), 2.4-2.8(m; 4H). 118 C22H24N603S 453.4 8.58 (1H), 7.82(s, 1H), 7.10(s, 1H), 6.6-6.8(m, 4H), 6.30(s, 1 H), 5.92(m, 2H), 6.76(m, 1 H), 4.25-4.45(m, 4H), 3.76(m, 3H), 3.4(m, 1 H), 2.4- 2.8(7H), 2.4(s, 3H). 119 C24H28N6O3S 481.4 8.47(s, 1H), 7.82(s, 1H), 7.08(s, 1H), 6.71(m, 2H), 6.30(s, 1H), 6.03(m, 1H), 5.90(s, 2H), 4.224.44(m, 4H), 3.75(m, 2H), 3.4(m, 1 H). 120 C22H23ClN603S 487.4 8.42(s, 1 H), 7.77(s, 1 H), 7.03(s, 1 H), 6.6- 6.75(m, 3H), 6.42(s, 1H), 6.02(bs, 1H), 5.90(s, 2H), 3.30-3.9(m, 6H), 2.75(m,4H), 2.40(m, 2H). 121 C23H26N6O3S 467.5 8.57(s, 1H), 7.81(s, 1H), 7.10(s, 1H), 6.57- 6.75(m, 3H), 6.30(s, 1H), 5.95(s, 2H), 5.47(m, 1 H), 4.37(m, 4H), 3.25-3.8(m, 5H), 2.77(m, 4H), 2.40(s, 3H). 122 C23H30N603S 495.5 8.55(s, lH), 7.82(s, 1H), 7.08(s, 1H), 6.58- 6.76(m, 3H), 6.30(s, 1 H), 5.90(s, 2H), 5.60(m, 1 H), 4.37(m, 2H), 3.28-3.8(m, 5H), 2.6-2.9(m, 5H), 2.40(m, 2H), 1 .23(d, 6H). 123 C27H34CIN704 556 ND 124 C27H34ClN7O5 572 8.4(1H), 7.7(1H), 7.1(1 H), 6.4(1H), 6.5-6.8(3H), 3.9(6H), 1.5(9H) 125 C22H26CIN703 472 9.0(1H), 7.9(1H), 7.2(1H), 6.4-6.8(4H) 126 C24H28CIN704 514 | 8.4(1H), 7.7(1 H), 7.1(1H), 6.4-6.8(4H), 2.1(3H) 127 C4H28CIN704 514 8.5(1 H), 7.8(1 H), 7.1(1H), 6.4-6.8(4H), 3.8(6H) 128 - C22H25ClN6O4 473.13 8.5(1H), 7.7(1H), 7.1(1H), 6.4(1H), 3.8(6H) 129 C25H32N604 481.26 8.5(1H), 7.8(1 H), 7.1(1H), 6.2(1 H), 1.3(6H) 130 C21H21ClN6O4 457.17 8.4(1 H), 7.7(1H), 7.1(1 H), 6.4(1H), 5.9(1H) Ex. # Formula FABMS Definitive 1H NMR (ppm) 131 C24H28N604 465 8.5(1H), 7.8(1H), 7.1(1H), 6.2(1H), 5.9(2H), 1 .2(6H) 132 C22H25ClN6O4 473.13 8.5(1H), 7.8(1H), 7.1(1H), 6.5(1H), 3.8(6H) 133 C25H32N604 480.63 8.5(1H), 7.8(1H), 7.1(1H), 6.3(1H), 3.9(6H), 1.2(6H) 134 C21H21CIN604 457.17 8.5(1H), 7.8(1 H), 7.1(1 H), 6.5(1H), 5.9(2H) 135 C24H28N604 465 8.6(1H), 7.8(1H), 7.1(1H), 6.3(1H), 5.9(2H), 1.2(6H) 136 C23H25N704 464 8.4(1H), 7.6(1 H), 6.95(1H), 5.9(2H), 2.35(3H), 2.0(3H) 137 C25H29N704 492 8.4(1H), 7.6(1H), 6.95(1H), 5.9(2H), 2.0(3H), 1.25(6H) 138 C22H22ClN7O4 484 8.4(1H), 7.6(1H), 7.0(1H), 5.9(2H), 2.0(3H) 139 C2H22N603 407 8.4(1H), 7.7(1H), 7.05(1H), 5.9(2H) 140 C22H24N6O3 421 8.4(1H), 7.7(1H), 7.05(1H), 5.9(2H), 2.6(2H), 1.3(3H) 141 C23H26N603 435 8.4(1H), 7.7(1H), 7.05(1H), 5.9(2H), 1.3(6H) 142 C20H19ClN6O3 427 8.4(1H), 7.6(1 H), 6.6(2H), 5.9(2H) 143 C22H24N603 421 8.45(1H), 7.7(1H), 7.05(1H), 5.9(2H) 144 C23H26N6O3 435 8.45(1H), 7.7(1 H), 7.05(1H), 5.9(2H), 2.65(2H), 1.3(3H) 145 C24H28N603 449 8.45(1H), 7.7(1H), 7.05(1H), 5.9(2H), 1.3(6H) 146 C21H21ClN603 441 8.45(1H), 7.7(1H), 7.05(1H), 5.9(2H) TABLE 7 Linker Groups (L) thnker Group (-L-) Cleavage Reagent N02 Light NOB 0, Light %OB o 0 R°\ B Ce(NH4)2(NO3)6 1 Li, Mg, or BuLi J, Br H30' OMe 1> 1) O2 or Br2, MeOH 2) H30+ CH=CH(CH2)2- 03, OsO4/lO4-, or KMnO4

Uker Group (} Cleavage l111:eagent tCH=CHCH2 03, OsO4/lOi, or KMnO4 -CH2CH=C 03, OSOIO4, or KMnO4 $ CH=CHCH2B (Ph3)PRhCI (H) -SCH2B- Hg+Z Zn or Mg OH Oxidation, e.g., Pb(OAc)4 or H5106 r'R" is H or alkyl; "B" is O or NH; X is an electron withdrawing group such as Br, CI, or I; and is the point of attachment to -C(O)-.j The following compounds were made according to the methods disclosed herein: 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]piperazine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenyl)me thyl]piperazine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]piperazine-2- acetamide; 2-[[2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-3-hydroxy-N-[( 1,3-benzodioxol-5- yl)methyl]propanamide; 2-[[2-(1 H-imidazol-l -yl)pyrimidin-4-yl]amino]-N-[(l ,3-benzodioxol-5- yl)methyl]pentanediamide; 2-[[2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-5-[[amino(nitr oimino)methyl]amino]- N-[(1 ,3-benzodioxol-5-yI)methyl]pentanamide; 2-[[2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-3-(thiophene-2 -yl)-N-[3-(morpholin-

4-yl)propyl]propanamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]piperazine 2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]piperazine 2-acetamide; N-[(4-chlorophenyl)methyl]-1 -[2 ,6-bis(1 H-imidazol-1 -yl)pyrimidin-4-yl]piperidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-[2-(1H-imidazol-1-yl)-6-m ethoxypyrimidin-4-yl]-1- (methoxycarbonyl)piperazine-2-acetamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)pyrimidin4-yl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yi)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]piperidine-2- acetamide; 1 -t6-chloro-2-( 1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-methoxyphenyl)methyl]piperazine- 2-acetamide; 1 -[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[phenylmethyl]piperazine-2-acetamide; <BR> <BR> <BR> 1-[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(3,4- <BR> <BR> <BR> <BR> <BR> dimethoxyphenyl)ethyl]piperazine-2-acetamide; <BR> <BR> <BR> <BR> 1 -[6-chloro-2-(1 H-imidazol-1-yl)pyrimidin4-yl]-N-[3-phenylpropyl]piperazine- 2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-phenyle thyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(thiophen e-2-yl)methyl]piperazine- 2-acetamide; 1 -[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-(methyl)piperazine-2-acetamide; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-3-(me thylthio)- N-[( 1 ,3-benzodioxol-5-yl)methyl]butanamide; 2-[[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin-4-yl]amino]4-(methylthio)- <BR> <BR> <BR> N-[(4-methoxyphenyl)methyl]butanamide; <BR> <BR> <BR> <BR> <BR> 2-t[6-chloro-2-(1 H-imidazol-1-yl)pyrimidin4-yl]amino]4-(methylthio)- N-[2-(3,4-dimethoxyphenyl)ethyl]butanamide; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-4-(me thylthio)-N- (methyl)butanamide;

2-[[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]amino]-3-[( 1,1 -dimethylethyl)thio]- N-[3-(methylthio)propyl]propanamide; 2-[[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]amino]-3-[(1,1 -dimethylethyl)thio]- N-[3-(phenyl)propyl]propanamide; α-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-[2 -(3,4-dimethoxyphenyl)ethyl]- 2-thiophenepropanamide; α-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-(b utyl)-2- thiophenepropanamide; α-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-[( 1,3-benzodioxol-5-yl)methyl]- 2-thiophenepropanamide; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-3-[(1 ,1-dimethylethyl)thio]- N-[2-(3,4-dimethoxyphenyl)ethyl]propanamide; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-[2- (3,4- dimethoxyphenyl)ethyl]acetamide; 2-[[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin-4-yl]amino]- N-[2-(3,4- dimethoxyphenyl)ethyl]propanamide; 2-[[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin9-yl]amino]-N-[2-(3,4- dimethoxyphenyl)ethyl]pentanediamide; 2-[[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin-4-yl]amino]- N-[(4- methoxyphenyl)methyl]pentanediamide; N-[(1,3-benzodioxol-5-yl)methyl]-2-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4- yl]amino]pentanediamide; N-[(1,3-benzodloxol-5-yl)methyl]-2-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4-yl]amino]- 5-[[amino(nitroimino)methyl]amino]pentanamide; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-[(4 -methoxyphenyl)methyl]-5- [[imino(amino)methyl]amino]pentanamide; <BR> <BR> <BR> <BR> 1-[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin-4-yl]-N-[2-(3,4- <BR> <BR> <BR> <BR> <BR> <BR> dimethoxyphenyl)ethylipyrrolidine-2-carboxamide; 2-[[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]amino]-N-[(4-methoxyphenyl)methyl]-5- [[imino(nitroamino)methyl]amino]pentanamide; N-[(1,3-benzodioxol-5-yl)methyl]-2-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4-yl]amino]- 5-[[amino(imino)methyl]amino]pentanamide; 1 -[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-4-hydroxy-N- [4-(hydroxyCarbonyl)phenyl]methyl]pyrrolidine-2-carboxamide;

N-[(1,3-benzodioxol-5-yl)methyl]-2-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4-yl]amino]- 3-hydroxypropanamide; 6-amino[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]- N-[2-(3,4- <BR> <BR> <BR> <BR> dimethoxyphenyl)ethyl]hexanamide; <BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> α-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]amino]-N-(3 - (methylsulfonyl)propyl]benzene-propanamide; N-[(1,3-benzodioxol-5-yl)methyl]-2-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4- yl](methyl)amino]acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-6-[[6-chloro-2-(1H-imidazol -1-yl)pyrimidin-4- yl]amino]hexanamide; 5-amino-N-[(1,3-benzodioxol-5-yl)methyl]-2-[[6-chloro-2-(1H- imidazol-1-yl)pyrimidin-4- yl]amino]pentanamide; 5-amino-N-butyl-2-[[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin-4-yl]amino]pentanamide; 4-[3-hydroxy-3-oxopropyl)amino]-3-[[6-chloro-2-(1H-imidazol- 1-yl)pyrimidin-4-yl]amino]- 4-oxobutanoic acid; 2-[[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl](methyl)amin o]-N-[(pyridin-4- yl)methyl]acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-methylpipe ridine-2-carboxamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-á-[[6-(1H-imidazol-1-yl)py rimidin-4-yl]amino]-2- thiophenepropanamide; N-[(1 ,3-benzodioxol-5-yl)methyl]-2-[[6-(1 H-imidazol-1 -yl)pyrimidin-4-yl]amino]-4- methylpentanamide; N-[( 1 ,3-benzodioxol-5-yl)methyl]-2-[[6-(1 H-imidazol-l -yl)pyrimidin-4- yl]amino]pentanediamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[[6-( 1 H-imidazol-l -yl)pyri mid in-4-yl]amino]4- methylpentanamide; N-[(1 ,3-benzodioxol-5-yl)methyl]-2-[[6-(1 H-imidazol-1 -yl)pyrimidin-4-yl]amino]-3- hydroxypropanamide; N-[(l ,3-benzodioxol-5-yl)methyl]-8-[[6-(l H-imidazol-l -yl)pyrimidin4- yl]amino]benzenepropanamide; 5-[[amino(imino)methyl]amino]-6-(1H-imidazol-1-yl)pyrimidin- 4-yl]-N- (phenylmethyl)pentanamide; N-[(1,3-benzodioxol-5-yl)methyl]-1,4-bis[6-chloro-2-(1H-imid azol-1-yl)pyrimidin- 4-yl]piperazine-2-acetamide;

N-[(l ,3-benzodioxol-5-yl)methyl]-l -[6-chloro-2-(l H-imidazol-l -yl)pyrimidin9-yl]- 4-[[(phenyl)amino]carbonyl]piperazine-2-acetamide; <BR> <BR> <BR> <BR> N-[(1,3-benzodioxol-5-yl)methyl]-1-[6-chloro-2-(1 H-imidazol-l -yl)pyrimid in4-yl]- <BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> 4-[(methoxy)carbonyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[6-chloro-2-(1 H-imidazol- 1 -yl)pyrimidin-4-yl]- 4-[(4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-(acetyl)-N-[(1,3-benzodioxol-5-yl)methyl]4-[6-chloro-2-(1 H-imidazol-1-yl)pyrimidin- 4-yl]piperazine-2-acetamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-1- methylpiperazine-2-acetamide; 4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-1- methyipiperazine-2-acetamide; N-[(3-chloro-4-methoxyphenyl)methyl]-4-[2-(1H-imidazol-1-yl) -6-methylpyrimidin-4-yl]-1- methylpiperazine-2-acetamide; 4-[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[(3-chloro4-methoxyphenyl)methyl]-1 - methylpiperazine-2-acetamide; 4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4,5-tr imethoxyphenyl)methyl]-1- methylpiperazine-2-acetamide; N-[2-(1 ,4-benzodioxan-6-yl)ethyl]-4-[2-(1 H-imidazol-l -yl)pyrimidin4-yl]-l - methylpiperazine-2-acetamide; 1-butyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[( furan-2-yl)methyl]piperazine-2- carboxamide; N-[( 1 ,4-benzodioxan-6-yl)methyl]-1 -butyl-4-[6-chloro-2-( 1 H-imidazol-1 -yl)pyrimidin-4- yl]piperazine-2-acetamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-butyl-4-[6-chloro-2-(1H- imidazol-1-yl)pyrimidin-4- yl]piperazine-2-acetamide; N-[(2,3-d i methoxyphenyl)methyl]-1 -buty14-[2-(1 H-imidazol-l -yl)pyrimid in4- yl]piperazine-2-acetamide; 4-[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-chlorophenyl)methyl]-1 -[(4- methyoxyphenyl)methyl]lpiperazine-2-acetamide; 4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-1-[(4- methyoxyphenyl )ethyl]lpiperazine-2-acetamide;

4-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-carboxamide; 4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-acetamide; 4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-acetamide; 4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-acetamide; 4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-acetamide; 4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(indan-5- yl)methyl]-1-[(4- methyoxyphenyl)methyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(2,3-dichlorophenyl)meth yl]-4-[2-(1H-imidazol-1- yl)pyrimidin4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(3,4-dichlorophenyl)meth yl]-4-[2-(1H-imidazol-1-yl)- 6-methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[( 1 ,3-benzodioxol-5-yI)methyl]-1 -[(3,4-dichlorophenyl)methyl]4-[2-( 1 H-imidazol-1 - yl)pyrimidin-4-yl]piperazine-2-carboxamide; <BR> <BR> <BR> 4-[6-methyl-2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-12-(1 ,3-benzodioxol-5-yl)ethyl]-l -[(3,4- <BR> <BR> <BR> <BR> <BR> <BR> dichlorophenyl)methyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(1,3-benzodioxol-5-yl)me thyl]-4-[2-(1H-imidazol-1- <BR> <BR> <BR> yl)pyrimidin-4-yl] piperazine-2-acetamide; <BR> <BR> <BR> <BR> <BR> N-[(l ,3-benzodioxol-5-yl)methyll-l -[(1 ,3-benzodioxol-5-yl)methy1]4-[2-(1 H-imidazol-1- <BR> <BR> <BR> <BR> <BR> yl)-6-methylpyrimidin-4-yl]piperazine-2-carboxamide; <BR> <BR> <BR> <BR> <BR> <BR> N-[(1 ,3-benzodioxol-5-yI)methyll-1 -[(1 ,3-benzodioxol-5-yl)methyl]A-[6-chlorn-2-( 1 H- imidazol-1-yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -[(1 ,3-benzodioxol-5-yl)methyl]4-[6-(l H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(1,3-benzodioxol-5-yl)m ethyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxan-6-yl)ethyl]-1-[(1,3-benzodioxol-5-yl)m ethyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acatamide; N-[(4-methoxyphenyl)methyl]-1-[(1,3-benzodioxol-5-yl)methyl] -4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-carboxamide;

N-[(4-methoxyphenyl)methyl]-1-[(1,3-benzodioxol-5-yl)methyl] -4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1-[(1,3-benzodioxol-5-yl)methyl] -4-[2-(1H-imidazol-1-yl)-6- (iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-methoxyphenyl)ethyl]-1-[(1,3-benzodioxol-5-yl)methyl ]-4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[[2-(phenyl)cyclopropyl]amino]-1-[(1,3-benzodioxol-5-yl)me thyl]-4-[6-chloro-2-(1H- imidazol-1-yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[(4-ethoxyphenyl)methyl]-1-[(1,3-benzodioxan-6-yl)methyl]- 4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(1,3-benzodioxan-6-yl)me thyl]-4-[2-(1H-imidazol-1- yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(1,3-benzodioxan-6-yl)me thyl]-4-[2-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl[-1-[(1,3-benzodioxan-6-yl)me thyl]-4-[6-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(1,3-benzodioxan-6-yl)m ethyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(1,3-benzodioxan-6-yl)m ethyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[(4-methoxyphenyl)methyl]-1-[(1,3-benzodioxan-6-yl)methyl] -4-[2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(3,4-dimethoxyphenyl)methyl]-1-[(1,3-benzodioxan-6-yl)met hyl]-4-[2-(1H-imidazol-1- yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(3,4-dimethoxyphenyl)methyl]-1-[(1,3-benzodioxan-6-yl)met hyl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(pyridin-3-yl)methyl]-4 -[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[(pyridin-3-yl)methyl]-4- [2-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-[(pyridin-3-yl)methyl]-4 -[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1-[(pyridin-3-yl)methyl]-4-[2-(1 H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide;

N-[(3,4-dimethoxyphenyl)methyl]-l -[(pyridin-3-yl)methy1]4-12-(1 H-imidazol-1 -yl)-6-(iso- propyl)pyrimidin-4-yi]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-1-[(3-fluoro-4-methoxypheny l)methyl]-4-[2-(1H- imidazol-1 -yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[3-(3,4-dimethoxyphenyl)propyl]-l -[(3-fluoro4-methoxyphenyl)methyl]4-[2-(l H- imidazol-1 -yl)-6-(iso-propyl)pyrimidin4-yl]piperazine-2-acetamide; N-[(4-ethoxyphenyl)methyl]-1-[(3-fluoro-4-methoxyphenyl)meth yl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-methylphenoxy)ethyl]-1-[(3-fluoro-4-methoxyphenyl)me thyl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(4-methylphenyl)methyl]-1-[(3-fluoro-4-methoxyphenyl)meth yl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(4-chlorophenyl)methyl]-1-[(3-fluoro-4-methoxyphenyl)meth yl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(4-chlorophenyl)methyl]-1-[(3-fluoro-4-methoxyphenyl)meth yl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -[(3-fluoro-4-methoxyphenyl)methyl]4-[2-( H- imidazol-1-yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide ; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(3-fluoro-4-methoxyphen yl)methyl]-4-[2-(1H- imidazol-1-yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide ; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(3-fluoro-4-methoxyphen yl)methyl]-1-[2-(1H- imidazol-1-yl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1 ,4-benzod ioxan6-yl)ethyl]-l -[(3-fluoro-4-methoxyphenyl )methy1]4-[2-(? H- imidazol-1-yl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-methoxyphenyl)ethyl]-1-[(3-fluoro-4-methoxyphenyl)me thyl]-4-[2-(1H-imidazol-1- yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(3,4-d i methoxyphenyl)ethyl]-1 -acetyl-4-[2-(1 H-imidazol-l -yl )-6-(iso-propyl)pyri mid in- 4-yl]piperazine-2-acetamide; N-[(4-ethoxyphenyl)methyl]-1-acetyl-4-[2-(1H-imidazol-1-yl)- 6-(iso-propyl)pyrimidin-4- yl]piperazine-2-carboxamide; N-[2-(4-methyl p he noxy)ethyl]-l -acetyl-4-[2-( 1 H-imidazol-1 -yl)-6-chloropyrimidin-4- yl]piperazine-2-acetamide; N-[2-(3-ch loro-4-methoxyphenyl )ethyl]-l -acety14-12-(1 H-imidazol-1-yl)-6- chloroylpyrimidin-4-yl]piperazine-2-carboxamide;

N-[(1,3-benzodioxol-5-yl)methyl]-1-acetyl-4-[2-(1H-imidazol- 1-yl)-6-methylpyrimidin-4- yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1-acetyl-4-[2-(1H-imidazol-1-yl) -6-methylpyrimidin-4- yl]piperazine-2-carboxamide; N-[(4-methoxyphenyl)methyl]-1-acetyl-4-[2-(1H-imidazol-1-yl) -6-chloropyrimidin-4- yl]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-1-(3-methyl-1-oxobutyl)-4-[ 2-(1H-imidazol-1-yl)-6-(iso- propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-1-(3-methyl-1-oxobutyl)-4-[ 2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(3-chloro-4-methoxyphenyl)ethyl]-1-(3-methyl-1-oxobutyl )-4-[2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(3-chloro-4-methoxyphenyl)ethyl]-1-(3-methyl-1-oxobutyl )-4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-(3-methyl-1-oxobutyl)-4-[ 2-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-(3-methyl-1-oxobutyl)-4-[ 2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(3-methyl-1-oxobutyl)-4- [2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-(3-methyl-1-oxobutyl)-4-[ 2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-(3-methyl-1-oxobutyl)-4- [2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-(3-methyl-1-oxobutyl)-4- [2-(1H-imidazol-1-yl)-6- (trifluoromethyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(2,6-dimethoxyphenyl)methyl]-1-(3-methyl-1-oxobutyl)-4-[2 -(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-1-(methoxyacetyl)-4-[2-(1H- imidazol-1-yl)-6-(iso- propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(methoxyacetyl)-4-[2-(1H -imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(methoxyacetyl)-4-[2-(1H -imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide;

N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(methoxyacetyl)-4-[2-(1H -imidazol-1-yl)-6- (trifluoromethyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(3,4-dimethylphenyl)methyl]-1-(methoxyacetyl)-4-[6-(1H-im idazol-1-yl)-6- (trifluoromethyl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-(methoxyacetyl)-4-[2-(1H- imidazol-1-yl)-6-(iso- propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-(methoxyacetyl)-4-[2-(1H- imidazol-1-yl)-6-(iso- propyl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-(methoxyacetyl)-4-[2-(1H -imidazol-1-yl)-6- (trifluoromethyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1-(methoxyacetyl)-4-[2-(1H-imida zol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-1-[(tetrahydrofuran-2-yl)ca rbonyl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[(4-methylphenyl)methyl]-1-[(tetrahydrofuran-2-yl)carbonyl ]-4-[2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-chlorophenyl)ethyl]-1-[(tetrahydrofuran-2-yl)carbony l]-4-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[(3-chloro-4-methoxyphenyl)methyl]-1-[(tetrahydrofuran-2-y l)carbonyl]-4-[2-(1H- imidazol-1-yl)-6-chloropyrimidin-4-yl]piperazine-2-carboxami de; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(tetrahydrofuran-2-yl)ca rbonyl]-4-[2-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(tetrahydrofuran-2-yl)ca rbonyl]-4-[6-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(tetrahydrofuran-2-yl)c arbonyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(tetrahydrofuran-2-yl)c arbonyl]-4-[2-(1H-imidazol-1- yl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(tetrahydrofuran-2-yl)c arbonyl]-4-[2-(1H-imidazol-1- yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide; N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-[(tetrahydrofuran-2-yl)c arbonyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[(tetrahydrofuran-2-yl)ca rbonyl]-4-[2-(1H-imidazol-1- yl)-6-(iso-propyl)pyrimidin-4-yl]piperazine-2-acetamide;

N-[(l ,4-benzodioxan-6-yl)methyl]-l -[(tetrahydrofuran-2-yl)carbonyl]4-[2-(l H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[(tetrahydrofuran-2-yl)ca rbonyl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(1,4-benzodioxan-6-yl)ethyl]-1-[(tetrahydrofuran-2-yl)c arbonyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[(4-methoxyphenyl)methyl]-l -[(tetrahydrofuran-2-yl)carbonyl]4-[2-(l H-imidazol-I -yl)- 6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-methoxyphenyl)ethyl]-1-[(tetrahydrofuran-2-yl)carbon yl]-4-[2-(1H-imidazol-1-yl)- 6-chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(3-methoxyphenyl)ethyl]-1-[(tetrahydrofuran-2-yl)carbon yl]-4-[2-(1H-imidazol-1-yl)- 6-chloropyrimidin-4-yl]piperazine-2-carboxamide; <BR> <BR> <BR> <BR> N-[(l ,4-benzodioxan-2-yl)methyl]-l -[(tetrahydrofuran-2-yl)carbonyl]-4-[2-( 1 H-imidazol-I - <BR> <BR> <BR> <BR> <BR> <BR> <BR> yl)-6-(iso-propyl)pyrimidin4-yl]piperazine-2-carboxamide; <BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> N-[(3,4-dimethoxyphenyl)methyl]-l -[(tetrahydrofuran-2-yl)carbonyl]-4-12-( H-imidazol-1- <BR> <BR> <BR> <BR> <BR> <BR> <BR> yl)-6-(iso-propyl)pyrimidin4-yl]piperazine-2-acetamide; N-[(3,5-dimethoxyphenyl)methyl]-1-[(tetrahydrofuran-2-yl)car bonyl]-4-[2-(1H-imidazol-1- yl)-6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(4-ethoxyphenyl)methyl]-1-[(2-hydroxy-2-oxoethoxy)acetyl] -4-[2-(1H-imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[(3-chloro-4-methoxyphenyl)methyl]-1-[(2-hydroxy-2-oxoetho xy)acetyl]-4-[2-(1H- imidazol-1-yl)-6-chloropyrimidin-4-yl]piperazine-2-carboxami de; N-[(1,3-benzodioxol-5-yl)methyl]-1-[(2-hydroxy-2-oxoethoxy)a cetyl]-4-[2-(1H-imidazol-1- yl)-6-methylpyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-l -(phenoxyacetyl)-4-[2-(1 H-imidazol-I -yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[3-(3,4-dimethoxyphenyl)propyl]-1-(phenoxyacetyl)-4-[2-(1H -imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(4-methylphenyl)methyl]-1-(phenoxyacetyl)-4-[2-(1H-imidaz ol-1-yl)-6-methylpyrimidin- 4-yl]piperazine-2-acetamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -(phenoxyacetyl)-4-[2-(1 H-imidazol-I -yl)pyrimidin-4- yl]piperazine-2-carboxamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -(phenoxyacetyl)4-[6-(1 H-imidazol-I -yl)pyrimidin-4- yl]piperazine-2-acetamide;

N-[2-(1,3-benzodioxol-5-yl)ethyl]-1-(phenoxyacetyl)-4-[2-(1H -imidazol-1-yl)pyrimidin-4- yl]piperazine-2-acetamide; N-[2-(1 ,3-benzodioxol-5-yl)ethyl]-l -(phenoxyacetyl)4-[2-(1 H-imidazol-I -yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-(phenoxyacetyl)-4-[2-(1H- imidazol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-acetamide; N-12-(1 ,4-benzodioxan-6-yl)ethyl]-l -(phenoxyacetyl)4-[2-(1 H-imidazol-l -yl)pyrimidin4- yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-l -(phenoxyacetyl)4-[2-(1 H-imidazol-I -yl)pyrimidin-4- yl]piperazine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1-(phenoxyacetyl)-4-[2-(1H-imida zol-1-yl)-6- chloropyrimidin-4-yl]piperazine-2-carboxamide; N-[2-(4-methoxyphenyl)ethyl]-1-(phenoxyacetyl)-4-[2-(1H-imid azol-1-yl)-6- methylpyrimidin-4-yl]piperazine-2-acetamide; N-[2-(4-methoxyphenyl)ethyl]-1-(phenoxyacetyl)-4-[2-(1H-imid azol-1-yl)pyrimidin-4- yl]piperazine-2-acetamide; N-[2-(3,4-dimethoxyphenyl)ethyl]-l -[(4-methoxyphenyl)carbonyl]4-[2-(l H-imidazol-I -yl)- 6-chloropyrimidin-4-yl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-(6-fluoropyridin-2-yl)-1- [2-(1H-imidazol-1-yl)pyrimidin- 4-yl]piperazine-2-acetamide; 1-(acetyl)-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4- methylsu Ifonylp henyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylsulfonylp henyl)methyl]piperidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-[[2-(ethoxycarbonyl)methy l]-1-[2-(1H-imidazol-1- yl)pyrimidin4-yl]piperazine-2-acetamide; 4-[amino(imino)methyl]-N-[(1,3-benzodioxol-5-yl)methyl]-1-[2 -(1H-imidazol-1- yl)pyrimidin4-yl]piperazine-2-acetamide; 1-methyisulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[2-(1,4-benzodioxan- 6-yl)ethyl]piperazine-2-acetamide; 1-methylsuflonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2 -(1,4-benzodioxan-6- yl)ethyl]piperazine-2-acetamide; 1-methylsulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide;

1 -methylsulfonyl4-[6-iso-propyl-2-(l H-imidazol-l -yl)pyrimidin4-yl]-N-[(3,4- dimethoxyphenyl]methyl]piperazine-2-acetamide; 1-(n-octyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(n-octyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(3-chloro-4- <BR> <BR> <BR> <BR> methoxyphenyl)methyl]piperazine-2-acetamide; <BR> <BR> <BR> <BR> <BR> <BR> <BR> 1 -(n-octyl)su lfony14-[6-(1 H-imidazol-l -yl)pyrimid in4-yl]- N-[(l ,3-benzod ioxol-5- yl)methyl]piperazine-2-acetamide; 1 -(n-octyl)sulfonyl4-[6-methyl-2-(l H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(1 ,3-benzodioxol- 5-yl)ethyl]piperazine-2-acetamide; 1-(n-octyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(n-octyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(3- methoxyphenyl)methyl]piperazine-2-acetamide; 1-(n-octyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(4- fluorophenyl)sulfonylipiperazine-2-acetamide; 1-(4-methylphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[(pyridin-3- yl)methyl]piperazine-2-carboxamide; 1-(4-methylphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-methylphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methylipiperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-carboxamide;

1-(4-methoxyphenyl)sulfonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[(2- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(4-fluorophenyl)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-fluorophenyl)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin- 4-yl]-N-[2-(1,4-benzodioxan- 6-yl)ethyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(4- methylphenyl)methyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[2-(3-chloro-4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[6-methyl-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[(1,3-benzodioxol-5- yl)methyl]piperazine-2-carboxamide; 1-(dimethylamino)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[(1,4-benzodioxan-6- yl)methyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[6-trifluoromethyl-2-(1H-imidazo l-1-yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[6-iso-propyl-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide;

1-(dimethylamino)sulfonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1 -(dimethylamino)sulfonyl4-[6-methyl-2-(l H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(dimethylamino)sulfonyl-4-[6-iso-propyl-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1-(n-propyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1-(n-propyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(4- chlorophenyl)ethyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(3-chloro- 4-methoxyphenyl)methylipiperazine-2-acetamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(3-chloro- 4-methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-iso-propyl-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(1,3- benzodioxol-5-yi)methyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1 -(n-propyl)aminocarbonyl4-[6-chloro-2-(l H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(n-propyl)aminocarbonyl-4-[6-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[2-(1,3-benzodioxol- 5-yl)ethyl]piperazine-2-carboxamide; 1 -(n-propyl)aminocarbonyl-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4 -yl]-N-[2-(1,4-benzodioxan- 6-yl)ethyl]piperazine-2-carboxamide; 1-(n-propyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)py rimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide;

1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(4- ethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(3-chloro-4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(3- chloro-4-methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3-bnzodioxol- 5-yl)ethyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-trifluoromethyl-2-(1H-imida zol-1-yl)pyrimidin-4-yl]-N-[- (1,4-benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-2-yl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-2-yl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(2,3- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(cyclohexyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(2,3- dimethoxyphenyl)methyl]piperazine-2-carboxamide;

1-(phenylsulfonyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2- (3,4-dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4- ethoxyphenyl)methyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyrim idin-4-yl]-N-[(4- ethoxyphenyl)methylipiperazine-2-acetamide; 1-(phenylsuflonyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4- methylphenyl)methyl]piperazine-2-acetamide; 1-(phenylsufonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1- yl)pyrimidin-4-yl]-N-[2-(3- chloro-4-methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(phenylsufonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1- yl)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2- <BR> <BR> <BR> (1 ,4-benzodioxan-6-yl)ethyl]piperazine-2-acetamide; <BR> <BR> <BR> <BR> <BR> 1 -(phenylsulfonyl)aminocarbonyl-4-12-(l H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(1 ,4- <BR> <BR> <BR> <BR> benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-(phenylsulfonyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(2,5- dimethoxyphenyl)methylipiperazine-2-acetamide; 1-[2-(thien-2-yl)ethyl]-4-[2-(1H-imidazol-1-yl)pyrimidin-4-y l]-N-[(1,3-benzodioxol-5- yl)methyl]piperazine-2-carboxamide; 1-[2-(thien-2-yl)ethyl]-4-[6-methyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1 -[2-(thien-2-yl)ethyl]-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide;

1-[2-(thien-2-yl)ethyl]-4-[6-chloro-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-[2-(thien-2-yl)ethyl]-4-[6-chloro-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(2,3- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1 -[2-(thien-2-yl)ethyl]-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N- [(cyclopropyl)methyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)aminocarbonyl-4-[6-chloro-2-(1H-imidazol- 1-yl)pyrimidin-4-yl]-N-[(4- chlorophenyl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[2-(2,4- dimethoxyphenyl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)aminocarbonyl-4-[6-methyl-2-(1H-imidazol- 1-yl)pyrimidin-4-yl]-N- [(1 ,3-benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1 -(4-methoxyphenyl)aminocarbonyl4-[2-(l H-imidazol-1 -yl)pyrimidin4-yl]-N-[(1 ,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)aminocarbonyl4-[6-chloro-2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N- [(1,4-benzodioxan-6-yl)methyl]piperazine-2-carboxamide; <BR> <BR> <BR> 1-(4-methoxyphenyl)aminocarbonyl4-[6-methyl-2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[2- <BR> <BR> <BR> <BR> <BR> (1 ,4-benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-(3,4-dichlorophenyl)aminocarbonyl-4-[6-methyl-2-(1H-imidaz ol-1-yl)pyrimidin-4-yl]-N- [2-(3,4-dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(3,4-dichlorophenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethylipiperazine-2-acetamide; 1-(3,4-dichlorophenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(3,4-dichlorophenyl)aminocarbonyl-4-[6-chloro-2-(1H-imidaz ol-1-yl)pyrimidin-4-yl]-N- [(4-methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(3,4-dichlorophenyl)aminocarbonyl-4-[2-(1H-imidazol-1-yl)p yrimidin-4-yl]-N-[(3,5- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(methoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide;

1-(methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethylipiperazine-2-carboxamide; 1-(methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(3-chloro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-(methoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[2-(3-chloro-4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1 -(methoxy)carbonyl-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1 -(methoxy)carbonyl4-[2-( 1 H-imidazol-l -yl)pyrimidin-4-yl]-N-[2-( 1,4-benzodioxan-6- yl)ethyl]piperazine-2-carboxamide; 1-(methoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N -[2-(1,4-benzodioxan-6- yl)ethyl]piperazine-2-acetamide; 1-(methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-carboxamide; 1 -(methoxy)carbonyl-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin4-yU-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N- [(cyclopropyl)methyl]piperazine-2-carboxamide; 1-(iso-propoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-carboxamide; 1-(iso-propoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(4- methylphenyl)methyl]piperazine-2-carboxamide; 1-(iso-propoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1 -(iso-propoxy)carbonyl4-[2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[( 1,3-benzodioxol-5- yl)methyl]piperazine-2-acetamide; 1-(iso-propoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-carboxamide; 1-(iso-propoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(iso-propoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide;

1-(iso-propoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N- (cyclopropyl)piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]- N-[(1,3-benzodioxol-5- yl)methyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[(1,3-benzodioxol- 5-yl)methyl]piperazine-2-acetamide; 1 -(n-butoxy)carbonyl4-[2-( 1 H-imidazol-1 -yl)pyri midin4-yl]-N-[2-(l ,3-benzod ioxol-5 yl)ethyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1-yl)pyr imidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1-(n-butoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol -1-yl)pyrimidin-4-yl]-N-[3- (,4-dimethoxyphenyl)propyl]piperazine-2-carboxamide; 1 -(2-methoxy)ethoxy)carbonyl-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2- (1,3-benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol -1-yl)pyrimidin-4-yl]-N- [(1,4-benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-(1H-imidazol-1-yl)pyrimid in-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(2-(methoxy)ethoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-y l)pyrimidin-4-yl]-N-[2-(3- methoxyphenyl)ethylipiperazine-2-carboxamide; 1-(1-methylpropoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-acetamide;

1-(1-methylpropoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-(1-methylpropoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-(1-methylpropoxy)carbonyl)-4-[6-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,3-benzodioxol- 5-yl)methyl]piperazine-2-carboxamide; 1-(1-methylpropoxy)carbonyl)-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-(1-methylpropoxy)carbonyl)-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(1-methylpropoxy)carbonyl)-4-[6-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,4-benzodioxan- 6-yl)methyl]piperazine-2-carboxamide; 1-(1-methylpropoxy)carbonyl)-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1-(1-methylpropoxy)carbonyl)-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(1-methylpropoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1 -(phenoxy)carbonyl-4-[6-iso-propyl-2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(phenoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(phenoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1 -(phenoxy)carbonyl4-[6-( 1 H-imidazol-l -yl)pyrimidin4-yl]-N-[(1 ,3-benzodioxol-5- yl)methyl]piperazine-2-carboxamide; 1-(phenoxy)carbonyl)-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]- N-[(furan-2- yl)methyl]piperazine-2-acetamide; 1-(phenoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(phenoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1 -(phenoxy)carbonyl4-C2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[2-(1 ,4-benzodioxan-6- yl)ethyl]piperazine-2-carboxamide;

1 -(phenoxy)carbonyl4-[6-chloro-2-(l H-imidazol-l -yl)pyrimidin4-yl]-N-[(4- <BR> <BR> <BR> <BR> methoxyphenyl)methyl]piperazine-2-carboxamide; 1-(phenoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1-yl)pyri midin-4-yl]-N-[(3,4- dimethoxyphenyl)methylipiperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1 -(4-methoxyphenoxy)carbonyl-4-[2-( 1 H-imidazol- 1 -yl)pyrimidinA-yl]-N-[2-( I ,4- benzodioxan-6-yl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(2,4- dimethoxyphenyl)methylipiperazine-2-carboxamide; 1-(4-methoxyphenoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methylphenoxy)ethyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[(1,3-benzodioxol- 5-yl)methyl]piperazine-2-carboxamide; 1 -((phenyl)methoxy)carbonyl-4-[6-iso-propyl-2-(1 H-imidazol-1 -yl)pyrimidinA-yI]-N-(( 1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-((phenyl)methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; I -((phenyl)methoxy)carbonyl-4-[6-methyl-2-( 1 H-imidazol-l -yl)pyrimidin-4-yl]-N-[2-(1 ,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide;

1-((phenyl)methoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-((phenyl)methoxy)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-acetamide; 1-((phenyl)methoxy)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-((phenyl)methoxy)carbonyl-4-[6-iso-propyl-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)carbonyl-4-[6-(1H-imidazol-1-yl)pyrimidin -4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-(4-methoxyphenyl)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-(4-methoxyphenyl)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl) pyrimidin-4-yl]-N-[(1,4- benzodioxan-2-yl)methyl]piperazine-2-carboxamide; 1-(pyridin-3-yl)carbonyl-4-[6-methyl-2-(1H-imidazol-1-yl)pyr imidin-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-(pyridin-3-yl)carbonyl-4-[6-chloro-2-(1H-imidazol-1-yl)pyr imidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-(pyridin-3-yl)carbonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4- yl]-N-[2-(1,3-benzodioxol-5- yl)ethyl]piperazine-2-acetamide;

1 -(pyrid i n-3-yl )carbonyl4-[6-iso-propyl-2-( 1 H-imidazol-1- -yl)pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1 -(pyridin-3-yl)carbonyl-4-[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1 -(pyridin-3-yl)carbonyl4-[6-chloro-2-(l H-imidazol- 1 -yl)pyrimidin-4-yl]-N-2-(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 1 -(pyridin-3-yl)carbonyl-4-[6-chloro-2-(1 H-imidazol- I -yl)pyrimidin4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(3-chloro-4- methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[6-methyl-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[6-iso-propyl-2-(1H-imidazol- 1-yl)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1 -I2-(4-methoxyp henyl)ethyl]9-[6- iso-propyl-2-( 1 H-imidazol-1 -yl)pyrimidin4-yl]-N-[( 1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(1,4-benzodioxan- 6-yl)methyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[6-methyl-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[6-chloro-2-(1H-imidazol-1-yl )pyrimidin-4-yl]-N-[2-(4- methoxyphenyl)ethyl]piperazine-2-carboxamide; 1-[2-(4-methoxyphenyl)ethyl]-4-[2-(1H-imidazol-1-yl)pyrimidi n-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-[(3,4-dichlorophenyl)methyl]carbonyl-4-[6-iso-propyl-2-(1H -imidazol-1-yl)pyrimidin-4- yl]-N-[2-(3,4-dimethoxyphenyl)ethyl]piperazine-2-acetamide; 1-[(3,4-dichlorophenyl)methyl]carbonyl-4-[6-chloro-2-(1H-imi dazol-1-yl)pyrimidin-4-yl]-N- [(4-methylphenyl)methyl]piperazine-2-carboxamide; 1-[(3,4-dichlorophenyl)methyl]carbonyl-4-[6-methyl-2-(1H-imi dazol-1-yl)pyrimidin-4-yl]-N- [2-(1,3-benzodioxol-5-yl)ethyl]piperazine-2-acetamide;

1-[(3,4-dichlorophenyl)methyl]carbonyl-4-[6-chloro-2-(1H-imi dazol-1-yl)pyrimidin-4-yl]-N- <BR> <BR> <BR> [(3,4, 5-trimethoxyp henyl)methyl]pi perazine-2-carboxamide ; <BR> <BR> <BR> <BR> <BR> 1-[(3,4-dichlorophenyl)methyl]carbonyl4-[6-chloro-2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]-N- [(3,4-dimethoxyphenyl)methyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl4-[6-chloro-2-(1 H-imidazol-l-yl)pyrimidin-4-yl]- N-[2-(3,4-dimethoxyphenyl)ethyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-iso-propyl-2-( 1H-imidazol-1-yl)pyrimidin-4- yl]-N-[3-(3,4-dimethoxyphenyl)propyl]piperazine-2-carboxamid e; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-iso-propyl-2-( 1H-imidazol-1-yl)pyrimidin-4- yl]-N-[3-(3,4-dimethoxyphenyl)propyl]piperazine-2-acetamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-iso-propyl-2-( 1H-imidazol-1-yl)pyrimidin-4- yl]-N-[(1,3-benzodioxol-5-yl)methyl]piperazine-2-carboxamide ; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(1,3- benzodioxol-5-yl)ethyl]piperazine-2-carboxamide; 1-[(1 ,3-benzodioxol-5-yl)methyl]carbonyl4-[2- H-imidazol-l -yl)pyrimidin4-yl]-N-[(1 ,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-methyl-2-(1H-i midazol-1-yl)pyrimidin-4-yl]- N-[(4-methoxyphenyl)methyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-iso-propyl-2-( 1H-imidazol-1-yl)pyrimidin-4- yl]-N-[(4-methoxyphenyl)methyl]piperazine-2-carboxamide; <BR> <BR> <BR> 1 -[(1 ,3-benzod ioxol-5-yl)methyl]carbonyl-4-[6-( 1 H-imidazol-l -yl)pyrimid in4-yl]- N-[(4- <BR> <BR> <BR> <BR> methoxyphenyl)methyl]piperazine-2-carboxamide; 1-[(1,3-benzodioxol-5-yl)methyl]carbonyl-4-[6-chloro-2-(1H-i midazol-1-yl)pyrimidin-4-yl]- N-(2-phenylcyclopropyl)piperazine-2-carboxamide; 1-methylsulfonyl-4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2 -(1,3-benzodioxol-5- yl)ethyl]piperazine-2-carboxamide; N-[(3,4-dimethoxyphenyl)methyl]-1-[2-(1H-imidazol-1-yl)pyrim idin-4-yl]pyrrolidine-2- carboxamide;

N-[(3,4-dimethoxyphenyl)methyl]-1 -[2-( IH-imidazol-I -yl)pyrimidin4-yl] pyrrolidine-2- acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-1 -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]pyrrolidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]pyrrolidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrim idin-4-yl]pyrrolidine-2- carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]pyrrolidine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-e thylpyrimidin-4-yl]pyrrolidine- 2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-( methylethyl)pyrimidin-4- yl]pyrrolidine-2-acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-et hylpyrimidin-4-yl]pyrrolidine-2- carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4-yl]pyrrolidine- 2-carboxamide; N-[(3-chloro-4-methoxyphenyl)methyl]-1-[2-(1H-imidazol-1-yl) pyrimidin-4-yl]pyrrolidine-2- acetamide; N-[(3-chloro4-methoxyphenyl)ethyl]-1 -[2-(1H-imidazol-1 -yl)-6-ethylpyrimidin-4- yl]pyrroiidine-2-carboxamide; N-[(4-methoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-methylp yrimidin-4-yl]pyrrolidine-2- carboxamide; N-[(3,4-dihydroxyphenyl)ethyl]-1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]pyrrolidine- 2-carboxamide; N-octyl-1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]pyrro lidine-2-carboxamide; N-(phenylpropyl)-1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4 -yl]pyrrolidine-2- carboxamide; N-[(pyridin-3-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-methylpyri midin-4-yl]pyrrolidine-2- carboxamide; N-[(morpholin-4-yl)ethyl]-1-(2-(1H-imidazol-1-yl)-6-methylpy rimidin-4-yl]pyrrolidine-2- carboxamide;

N-[(2-methoxypyridin-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4- yl]piperidine-2-carboxamide; N-[(2-methylpyridin-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]piperidine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)pyri midin-4-yl]aminolacetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- <BR> <BR> <BR> yl](methyl)amino]acetamide; <BR> <BR> <BR> <BR> <BR> 2-[[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4-yl](methyl)amino]-N-octylacetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl](phenylmethyl)amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-( methylethyl)pyrimidin-4- yl]amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4-yl][(1,3- benzodioxol-5-yl)methyl]amino]acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-2-[[2-( ?H-imidazol-l -yl)-6-methylpyrimidin4- yl](methyl)amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl][(morpholin4-yl)ethyl]amino]acetamide; <BR> <BR> <BR> N-[(1 ,3-benzodioxol-5-yl)ethyl]-2-[[2-( IH-imidazol-1 -yl)pyrimidin4- <BR> <BR> <BR> <BR> <BR> yl](methyl)amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl](methylethyl)amino]acetamide; N-[(1,3-benzodioxol-5-oxy)ethyl]-2-[[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4- yl](methyl)amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[4-(1H-imidazol-1-yl)-6-( methylethyl)pyrimidin-2- yl]amino]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[[4-(1H-imidazol-1-yl)-6-m ethylpyrimidin-2- yl]amino]acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-3-[[2-[1H-imidazol-1-yl)-6- methylpyrimidin-4- yl]amino]propionamide; N-[(4-trifluoromethylphenyl)methyl]-3-[[2-(1H-imidazol-1-yl) -6-methylpyrimidin-4- yl]amino]propionamide;

N-[(1,3-benzodioxol-5-yl)ethyl]-3-[[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]amino]propionamide; N-[(1,3-benzodioxol-5-oxy)ethyl]-2-(1H-imidazol-1-yl)pyrimid inpyrimidine-4-amine; N-[(1,3-benzodioxol-5-yl)ethyl]-4-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4-yl]-1-(2- methyl -oxopropyl)piperazine-2-acetamide; N-[(4-methoxyphenyl)ethyl]-4-[2-(1H-imidazol-1-yl)-6-methylp yrimidin-4-yl]-1-(2-methyl- 1 -oxopropyl)piperazine-2-acetamide; N-[(4-nitrophenyl)methyl]-1-[2-(1H-imidazol-1-yl)-6-methylpy rimidin-4-yl]piperidine-2- acetamide; N-[[4-(acetylamino)phenyl]methyl]-1-[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4- yl]piperidine-2-acetamide; N-[[4-(methylsulfonylamino)phenyl]methyl]-1-[2-(1H-imidazol- 1-yl)-6-methylpyrimidin-4- yl]piperidine-2-acetamide; N-[(2,3-dihydrobenzofuran-5-yl)methyl]-1-[2-(1H-imidazol-1-y l)-6-methylpyrimidin-4- yl]piperidine-2-acetamide; N-[(indan-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-methylpyrim idin-4-yl]piperidine-2- acetamide; N-[(3-chloro-4-methoxyphenyl)methyl]-1-[2-(1H-imidazol-1-yl) pyrimidin-4-yl]piperidine-2- acetamide; N-[(l ,3-benzod ioxol-5-yl)methyl]- 1 -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]4-(1 - oxopropyl)piperazine-2-acetamide; N-[(4-methoxyphenyl)aminocarbonyl]-1-[2-(1H-imidazol-1-yl)py rimidin-4-yl]piperidine-2- methaneamine; N-[(1,3-benzodioxol-5-yl)methylcarbonyl-1-[2-(1H-imidazol-1- yl)pyrimidin-4- yl]piperidine-2-methaneamine; N-[(4-methoxyphenoxy)carbonyl]-1 -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]piperidine-2- methaneamine; N-[(4-methoxyphenyl)methylcarbonyl]-1 -[2-( IH-imidazol-I -yl)pyrimidin4-yljpiperidine-2- methaneamine; N-[(1,3-benzodioxol-5-yl)carbonyl]-1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4- yl]piperidine-2-ethaneamine; 2,4-bis( 1H-imidazol-1 -yl)-6-methylpyrimidine; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-5-m ethylpyrimidin-4-yl]-4- (phenylmethyl)piperazine-3-acetamide;

N-[(3,4-dimethoxyphenyl)ethyl]-6-[2-(1H-imidazol-1-yl)pyrimi din-4-yl]-N-methyl-5,6,7,8,- tetrahydropyrido[5,6-c]pyrimidine-4-amine; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5-yl)methyl]- 4-methylthiobutanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5-yl)ethyl]-4- methylthiobutanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(4 -methoxyphenyl)methyl]-4- methylsulfonylbutanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5-yl)ethyl]-4- (butylthio)butanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(c yclopropyl)methyl]-3-[(3,4- dimethylphenyl)methylthio]propanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(2 ,5-dimethoxyphenyl)methyl]- 3-methyl-3-[(phenylmethyl)thio]butanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(4 -chlorophenyl)methyl]-3- thiophenepropanamide; 5-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5- yl)methyl]pentanamide; 5-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,4-benzodioxan-6- yl)ethyl]pentanamide; 7-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-(2- phnenylcyclopropyl)heptanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-[(3-c hloro-4- methoxyphenyl)ethyl]acetamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5- yl)ethyl]acetamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,4-benzodioxan-6- yl)ethyl]acetamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(4 - methoxyphenyl)ethyl]acetamide; 4-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(1 ,3-benzodioxol-5- yl)ethyl]butanamide; 2-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]amino]-N-[(4 -chlorophenyl)ethyl]pyridine- 3-propanamide;

2-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6- yl)ethyl]isoquinoline-3-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4- methoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]piperidine-2- acetamide; 1 -l[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-[(1,4-benzodioxan-6- yl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,4- dimethoxyphenyl)methylipiperidine-2-acetamide;

1 -[2-( lH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]piperidine-2- acetamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yl)ethyl]thiomorpholine-2-acetamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4- methoxyphenyl)ethyl]thiomorpholine-2-acetamide; 4-[(dimethylethoxy)carbonyl]- 1 -[2-(1H-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-[(3- chloro4-methoxyphenyl)methyl]piperazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]-1-[2-(1H-imidazol-1-yl)-6-methy lpyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]-1-[2-(1H-imidazol-1-yl)-6-methy lpyrimidin-4-yl]-N-[(1,3- benzodioxol-5-yl)ethyl]piperazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]-1-[2-(1H-imidazol-1-yl)-6-methy lpyrimidin-4-yl]-N-[(1,4- benzod ioxan-6-yl)methyl]pi perazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]-1-[2-(1H-imidazol-1-yl)-6-methy lpyrimidin-4-yl]-N-[(1,4- benzodioxan-6-yl)ethyl]piperazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]- 1 -t2-( IH-imidazol-1 -yl)6-methyl pyri midin4-yl]-N-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 4-[(dimethylethoxy)carbonyl]- 1 -[2-(1H-imidazol-1 -yl)6-methyl pyrimid in4-yl]- N-[(3,4- dimethoxyphenyl)methyl]piperazine-2-acetamide; I -[2-( IH-imidazol- 1 -yl)-6-methylpyrimidin4-yl]-N-[(1,3-benzodioxol-5- yl)methyl]piperidine-3-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]piperidine- 3-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6- yl)methyl]piperidine-3-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]piperidine-3- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperidine-3-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4- methoxyphenyl)methyl]piperidine-3-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yl)methyl]piperidine-3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]piperidine- 3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6- yl)methyl]piperidine-3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]piperidine- 3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]piperidine-3- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]piperidine-3- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,4- dimethoxyphenyl)methyl]piperidine-3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperidine-3-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6- yl)ethyl]pyrrolidine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]pyrrolidine-2- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]pyrrolidine-2- carboxamide; 1-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl](methyl)amin o]-N-[(1,3-benzodioxol-5- yl)ethyl]acetamide; 1-[[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl](methyl)amin o]-N-[(1,4-benzodioxan-6- yl)ethyl]acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)ethyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- methylpiperazine-2-acetamide;

1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-[(4-chlorophenyl)methyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- methylpiperazine-2-acetamide; 1 -[2-( lH-imidazol-I -yl)pyrimidin4-yl]-N-[(3-chloro4-methoxyphenyl)ethyl]-4- methylpiperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- methylpiperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dime thoxyphenyl)ethyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- methylpiperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- methylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-methoxyphenyl)m ethyl]-4-methylpiperazine- 2-carboxamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)ethyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ [4-(2- methoxyethoxy)phenyl))methyl]-4-methylpiperazine-2-carboxami de; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4- methylpiperazine-2-acetamide;

1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclopropyl)methy l]-4-methylpiperazine-2- acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(indan-5- yl)methyl]-4- methylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(3-c hloro-4- methoxyphenyl )methyl]-4-butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(1,3 -benzodioxol-5-yl)methyl)-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- butylpiperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-butylpiperazine-2- acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[1,4-benzodioxan-6- yl)ethyl]-4-butylpiperazine-2- acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4- butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- butylpiperazine-2-acetamide;

1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-[(4-methoxyphenyl)methyl]-4- butylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4-butylpiperazine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4- butylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- [(4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- [(4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1 -[6-chloro-2-( ? H-imidazol-l -yl)pyrimidin4-yl]-N-[( 1 ,4-benzod ioxan-6-yl)methyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-[(4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1 -[6-chloro-2-( 1H-imidazol-l -yl)pyrimidin-4-yl]-N-[( 1 ,4-benzod ioxan-6-yl)ethyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(4- methoxyphenyl)methylipiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-( 2-phenylcyclopropyl)-4-[(4- methoxyphenyl)methyl]piperazine-2-acetamide;

1 -[2-( 1H-imidazol-1 -yl )-6-methyl pyri midin4-yl]-N-[(3,4-d imethoxyphenyl )methyl]-4-[(4- <BR> <BR> <BR> <BR> methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-[(3,4- dichlorphenyl)methylipiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1 -[6-chloro-2-( lH-imidazol-I -yl)pyrimidinA-yl]-N-[( I ,4-benzodioxan-6-yl)methyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-[(3,4- dichlorphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro xyphenyl)methyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(-[(1,3-benzodioxo l-5-yl)methyl-4-[(1,3- benzod ioxol-5-yl)methyl]pi perazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(-[(1,3-b enzodioxol-5-yl)methyl]-4- [(1,3-benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(-[(1,3-benzodioxo l-5-yl)ethyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; I -[2-( lH-imidazol-1 -yI)pyrimidin4-yl]-N-[( I ,4-benzodioxan-6-yI)methyl]-4-[( 1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4-[(1,3- benzodioxol-5-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methylphenyl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)ethyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,5-dime thoxyphenyl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,-benzo dioxan-6-yl)methyl]-4-[(14- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4-[(1,4-benzodioxan- 6-yl)methyl]piperazine-2-acetamide: 1-[2-(1H-imidazol-1-yl)6-methylpyrimidin-4-yl]-N-[(3-methoxy phenyl)ethyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thiophenyl)ethy l]-4-[(1,4-benzodioxan-6- yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3,5-dimethoxyphenyl)methyl]- 4-[(1,4-benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1-adaman tyl)methyl]-4-[(1,4- benzodioxan-6-yl)methyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(5-indanyl)methyl] -4-[(1,4-benzodioxan-6- yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)propyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4-[(pyridin-3- yl)methyl]plperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4-[(pyridin-3- yl)methyl]plperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4-[(pyridin-3- yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-[(pyridin-3- yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(pyridin- 3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-[(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4-[(pyridin-3- yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- [(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(pyridin- 3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(pyridin- 3-yl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-[(pyridin- 3-yl)methyl]piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-[(pyridin-3- yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,6-dimethoxyphenyl)methyl]- 4-[(pyridin-3-yl)methyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-[(pyridin-3-yl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclopropyl)methy l]-4-[(pyridin-3- yl)methyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(3- fluoro-4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(3- fluoro4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-[(3-fluoro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(3- fluoro4-methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(3-fluoro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)e thyl]-4-[(3-fluoro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-[(3-fluoro- 4-methoxyphenyl)methyl]piperazine-2-acetamide: 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4-[(3-fluoro-4- methoxyphenyl)methylipiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1-adamantyl)methy l]-4-[(3-fluoro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclopro pyl)methyl]-4-[(3-fluoro-4- methoxyphenyl)methyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imdiazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- acetylpiperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methylphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenyl)me thyl]-4-acetylpiperazine-2- acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxy-3- chlorophenyl)methyl]-4-acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxy-3-chlor ophenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3,5-dimethoxyphenyl) ethyl]-4- acetylpiperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-7l)pyrimidin-4-yl]-N-[(3,4,5-tr imethoxyphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- acetylpiperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-acetylpiperazine 2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl )methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4-acetylpiperazine-2 acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 -methoxyphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin4-yl]-N-[(3-methoxyphenyl)ethyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-difl uoroxyphenyl)ethyl]-4- acetylpiperazine-2-acetamide; I -[6-chloro-2-( lH-imidazol- I -yl)pyrimidin-4-yl]-N-[( I ,4-benzodioxan-2-yl)methyl]-4- acetylpiperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-phenylc yclopropyl)-4- acetylpiperazine-2-acetamide; 1 -[6-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )methyl]-4- acetylpiperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- acetylpiperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-(cyclopropyl)4-acetylpiperazine-2- acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(indan-5- yl)methyl]-4-acetylpiperazine- 2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-(3-methyl- 1 -oxobutyl)piperazine-2-acetamide; 1 -(6-chlorn-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(4-methylphenyl)methyl]-4-(3-methyl-1 - oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; I -[6-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)ethyl]-4-(3-methyl-1 - oxobutyl)piperazine-2-acetamide; 1 -[6-chloro-2-( lH-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-chlorophenyl)ethyl]-4-(3-methyl-1 - oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- (3-methyl-1-oxobutyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1 -[6-ch loro-2-( ? H-imidazol-l -yl)pyri midin-4-yl]-N-[(4-methoxy-3-chlorophenyl )ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)-methyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- (3-methyl-1-oxobutyl)piperazine-2-carboxamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5-yl)ethyl]-4-(3-met hyl-1 - oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5-yl)ethyl]-4-(3-met hyl-1- - oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide;

1 -[6-chloro-2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)methyl]-4-(3-methyl- 1 -oxobutyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxyphenyl)methyl]-4-( 3- methyl -oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-(3-methyl- 1 -oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; 1 -[6-chloro-2-( 1H-i midazol-l -yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)ethyl]-4-(3-methyl-1 - oxobutyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thieny l)ethyl]-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[[4-(2-methoxyethox y)phenyl]ethyl]-4-(3-methyl- 1 -oxobutyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)ethyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-phenylcyclopropy l)4-(3-methyl-1- oxobutyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-(3- methyl -oxobutyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(indan-2-yl)-4-(3-m ethyl-1-oxobutyl)piperazine-2- carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(indan-5-y l)-4-(3-methyl-1- oxobutyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- (2-methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-91H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-(methylethyl)pyrimidin4-yl]-N-[(4-ethoxyphenyl)ethyl] -4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)ethyl]-4-(2-methoxy-1- oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)ethyl]-4-(2-methoxy- 1 oxoethyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-(2-methoxy- 1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-(2-methoxy- 1 -oxoethyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(4-chlorophenyl)methyl]-4-(2 -methoxy- 1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- (2-methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4-(2- methoxy-1-oxoethyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[( 1 ,3-benzodioxol-5-yl)methyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-(2- methoxy-1-oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- (2-methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-(2-methoxy-1- oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-(2- methoxy-1-oxoethyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[( ,3-benzodioxol-5-yl)ethyl]-4- (2-methoxy-1-oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-(2-methoxy-1- oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-(2- methoxy-1-oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-(2- methoxy-1 -oxoethyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4-(2 methoxy-1-oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-(2- methoxy-1-oxoethyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-methylpyrimidin4-ylj-N-[(4-methoxyphenyl)ethylj-4-(% methoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(2-methoxy-1-oxoethyl)piperazine-2-acetamide; 1 -[6-chloro-2-( lH-imidazol-1 -yl)pyrimidin-4-yl]-N-(indan-5-yl)-4-(2-methoxy-1 - oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)propyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4-ethoxyphenyl)ethyl ]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)ethyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)ethyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenyl)me thyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methylphenyl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -chlorophenyl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide;

1 -[6-chloro-2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(4-methoxy-3-chlorophenyl)ethyi]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1 -[2-( lH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxy-3-chlorophenyl)et hyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-(tetrahydro-3 furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thylphenyl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(pyridin-3-yl)meth yl]-4-(tetrahydro-3- furanoyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imdiazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidiazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-metho xyphenyl)ethyl]-4-(tetrahydro- 3-furanoyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-difluoropheny l)ethyl]-4-(tetrahydro-3- furanoyl)piperazine-2-carboxamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(2,5-dimethoxyphenyl )methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )methyl]-4- (tetrahydro-3-furanoyl)piperazine-2-acetamide;

1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dimethoxyphen yl)methyl]-4-(tetrahydro-3- furanoyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )ethyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1 -[6-chloro-2-( lH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )butyl]-4-(2- carboxymethoxy-1 -oxoethyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyri midi n-4-yl]-N-[(3-chioro-4-methoxyphenyi )methyl]4- (2-carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-(2- carboxymethoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1 -!6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)ethyl]-4-(2- carboxymethoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)ethyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,4-dimethoxyphen yl)methyl]-4-(2- carboxymethoxy-1 -oxoethyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,6-dimethoxyphenyl)methyl]- 4-(2-carboxymethoxy-1 -oxoethyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,6-dimethoxyphen yl)methyl]-4-(2- carboxymethoxy-1-oxoethyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- (2-phenoxy-1 -oxoethyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl )propyl]-4-(2- phenoxy-1-oxoethyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-(2- phenoxy-1-oxoethyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-(2- phenoxy-l -oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3,4-dimethylphenyl)methyl]-4 (2-phenoxy-1-oxoethyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-(2- phenoxy-l -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-(2- phenoxy-1 -oxoethyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl)propyl]-4-(pyrid in-3- ylcarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)butyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -ethoxyphenyl)methyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1 -[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-t(4-methoxy-3-chlorophenyl)methylj-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)ethyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,5-dime thylphenyl)methyl]-4-(pyridin 3-ylcarbonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)ethyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-(pyridin- 3-ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4- (pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1 -(2-( IH-imidazol- I -yI)-6-methylpyrimidin-4-yl]-N-j(4-methoxyphenyl)ethyl]-4-(p yridin-3- ylcarbonyi)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-methox yphenyl)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thieny l)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thienyl)ethyl]- 4-(pyridin-3- ylcarbonyl)piperazine-2-carboxamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-difluoropheny l)ethyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(pyridin-3-ylcarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(5-indany l)methyl]-4-(pyridin-3- ylcarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- [2-(4-methoxyp henyl)-l -oxoethyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -chlorophenyl)methyl]-4-[2-(4- methoxyphenyl)-1 -oxoethyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4 [2-(4-methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- [2-(4-methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxy-3-chlor ophenyl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dimethoxyphen yl)ethyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (1,3-benzodioxol-5-yl)ethyl]-4- [2-(4-methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thylphenyl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethylpheny l)methyl]-4-[2-(4- methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethylphenyl)ethyl]-4-[2- (4-methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3-pyridinyl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-[2-(4-methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4-[2- (4-methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 -methoxyphenyl)ethyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thienyl)ethyl]- 4-[2-(4-methoxyphenyl)-1- oxoethyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1-methylpyrrol-2- yl)ethyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-carboxamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-[2-(4- methoxyphenyl)-1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3,4-dimethoxyphenyl)methyl]- 4-[2-(4-methoxyphenyl)-1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[2- (1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[2- (1 ,3-benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1 -[6-chloro-2-(1H-imidazol-1 -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4- methoxyphenyl)methyl]-4-[2-(1 ,3-benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenoxy)e thyl]-4-[2-(1,3-benzodioxol- 5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-4-[2-(1,3-benzodioxol- 5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-[2-(1,3- benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4-[2-(1,3- benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)ethyl]-4-[2- (1 ,3-benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,5-dimethoxyphenyl)ethyl]-4- [2-( 1, 3-benzodioxol-5-yl) 1 -oxoethyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[2- (1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[2- (1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1 -[6-( lH-imidazol- I -yl)pyrimidin4-yl]-N-[(3,4-dimethylphenyl)ethyl]-4-j2-( I ,3- benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[2- (1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide;

I -[2-( IH-imidazol-I -yl)pyrimidinA-yl]-N-[(I ,4-benzodioxan-6-yl)ethyl]-4-[2-(I ,3- benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3-methoxyphenyl)ethyl]-4-[2- (1 ,3-benzodioxol-5-yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)ethyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 -thienyl)ethyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)methyl]-4-[2- (1 ,3-benzod ioxol-5-yl)l -oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-[2-(1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide ; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-[2- (1,3-benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(2-indanyl )-4-[2-(1,3-benzodioxol-5- yl)1 -oxoethyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(5-indany l)methyl]-4-[2-(1,3- benzodioxol-5-yl)1-oxoethyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(5-indany l)methyl]-4-[2-(1,3- benzodioxol-5-yl)1 -oxoethyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox y-3-chlorophenyl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol- 5-yl)ethyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)e thyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2-methox yphenyl)ethyl]-4- (methylsulfonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(methylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- (methylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (octylsu Ifonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-methoxyphenyl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1 -t6-chloro-2-( IH-imidazol- 1 -yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)ethyl]-4- (octylsulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4 (octylsulfonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin4-yl]-N-[(3,4-dimethoxyphenyl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (4-chlorophenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)pyrimid in4-yl]-N-[(l ,3-benzodioxol-5-yl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(dimethylaminosulfonyl)piperazine-2-carboxamide; 1 -[2-( lH-imidazol-I -yl)pyri midin4-yl]-N-[(l ,4-benzod ioxan-6-yl )methyl]4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (dimethylaminosuifonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(3-methoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,6-dime thoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; I -[6-chloro-2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1 -[2-( I H-imidazol- 1 -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl) methyl]- 4-(dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,5-dime thoxyphenyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-adaman tyl)methyl]-4- (dimethylaminosulfonyl)piperazine-2-carboxamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,3-dimethoxyphen yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -!6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)propyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)butyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxyphenyl)me thyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -ethoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (4-methylphenoxy)ethyl]-4- (propylaminocarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-[(4-methylphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenyl)et hyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-(methyiethyl)pyrimidin4-yl]-N-[(4-methylphenyl)methyl ]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide;

1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3-chloro-4-methoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)6-methyi pyrimidi n4-yl]-N-[(l ,3-benzodioxol-5-yl )ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thylphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(propylaminocarbonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-methoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[2-( I H-imidazol-I -yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)e thyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-methox yphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-methox yphenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thieny l)ethyl]-4 (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thienyl)ethyl]- 4- (propylaminocarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-difl uorophenyl)ethyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-2-yl)methyl]- 4-(propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4 (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dime thoxyphenyl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dimethoxyphen yl)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-( cyclopropyl)-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-indanyl)-4-(prop ylaminocarbonyl)piperazine- 2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(5-indany l)methyl]-4- (propylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxyphenyl)me thyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-(cyclohexylaminocarbonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1 -[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-methox yphenyl)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thieny l)ethyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-difl uorophenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(2,5-dimethoxyphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,5-dimethoxyphenyl)methyl]- 4-(cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-indanyl )-4- (cyclohexylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (phenylsulfonylaminocarbonyl)piperazine-2-acetamide;

1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(l ,3-benzodioxol-5-yl)methyl]-4- (phenylsulfonylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (phenyisulfonylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (phenylsulfonylaminocarbonyl)piperazine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-trifluoromethyl pyrimidin4-yl]-N-[(2,3-dimethoxyphenyl)methyl]- 4-(phenylaminocarbonyl)piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)propyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-ethoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-chloro phenyl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (3-chloro-4- methoxyphenyl)ethyl]-4-(phenylaminocarbonyl)piperazine-2-car boxamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)ethyl]-4 (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -methoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1 -[2-( I H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; I -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(3-methoxyphenyl)ethyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-thienyl)ethyl]- 4- (phenylaminocarbonyl)piperazine-2-acetamide; I-[6-chloro-2-( IH-imidazol-l -yl)pyrimidin-4-yl]-N-[(3,4-difluorophenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[3,4-dimet hoxyphenyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(phenylaminocarbonyl)piperazine-2-acetamide;

1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclopropyl)methy l]-4- (phenylaminocarbonyl)piperazine-2-carboxamide; 1 -[6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(5-indanyl)methyl]-4- (phenylaminocarbonyl)piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,3-dimethoxyphen yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,3-dimethoxyphenyl)ethyl]-4- [(4-methOxyphenyl)aminocarbonyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxyphenyl)me thyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1 -[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(4-methylphenoxy)ethyl]4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methylphenoxy)e thyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (4-methylphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- [(4-methOxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1 -t6-chloro-2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-[(3-chloro4-methoxyphenyl)ethyl]-4- [(4-methOxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dimethoxyphen yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-carboxamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- [(4-methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thylphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethylpheny l)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-furyl)methyl]-4 -[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-[(4-methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1 -(6-chloro-2-( IH-imidazol- I -yl)pyrimidin4-yl]-N-{(3-methoxyphenyl)ethyl]-4-{(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1 -[2-( IH-imidazol- 1 -yl)pyrimidin4-yl]-N-[(3-methoxyphenyl)ethyl]4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-2-yl)ethyl]-4- [(4-methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,3-dime thoxyphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyi]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1 -[6-chloro-2-( 1H-imidazol-l -yl)pyrimidin-4-yl]-N-[(3 ,4-d i methoxyphenyl)meth yl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclopro pyl)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-indanyl )-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(5-indany l)methyl]-4-[(4- methoxyphenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; I-[6-chloro-2-( ?H-imidazol-l -yl)pyrimidinA-yl]-N-[(3,4-dimethoxyphenyl)prnpyl]A-[(3,4- dichlorophenyl)aminocarbonyl[piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)butyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4 -ethoxyphenyl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenoxy)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chlorophenyl)me thyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro-4-methox yphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4dimet hylphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-methox yphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,5-dimethoxyphenyl)methyl]- 4-[(3,4-dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,5-dime thoxyphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl)-N-[(3,4-dimethoxyphen yl)methyl]-4-[(3,4- dichlorophenyl)aminocarbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxphenyl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-ethoxy phenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methyl phenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]]-N-[(1,3-ben zodioxol-5-yl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1 -[2-( IH-imidazol-I -yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(4-methOxyphenyl)meth yl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidzol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxy phenyl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methox yphenyl)ethyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-2-yl)methyl]-4- (methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)methyl]- 4-(methoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4- (methylethoxycarbonyl)piperazine-2-acetamide; I -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]-N-[(4-methoxyphenyl)methyl]4- (methylethoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- (butoxycarbonyl)piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- (butoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4- (butoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxphenyl)me thyl]-4- (butoxycarbonyl)piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-difluorophenyl)methyl]-4- (butoxycarbonyl)piperazine-2-carboxamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-chloro phenyl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro -4-methoxyphenyl)methyl]-4- [(2-methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,3-benzodioxol-5-yl)methyl]-4- [(2-methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N[(1,4-benzodioxan-6- yl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)ethyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-([(4-metho xyphenyl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dime thoxyphenyl)methyl]-4-[(2- methoxyethoxy)carbonyl]piperazine-2-acetamide;

1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl)-N-[(4-chloro phenyl)methyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benz odioxol-5-yl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)methyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(1 ,4-benzodioxan-6-yl)methyl]- 4-[(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl)methyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-thienyl)ethyl]- 4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dime thoxyphenyl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4-dimethoxyphenyl)ethyl]-4- [(phenylmethoxy)carbonyl]piperazine-2-acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]-4-[(1- methylpropoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]-4-[(1- methylpropoxy)carbonyl]piperazine-2-acetamide; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]-4-[(1- methylpropoxy)carbonyl]piperazine-2-acetamide; 1 -[6-chloro-2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3-chloro-4-methoxyphenyl)methyl]-4- [(4-methoxyphenoxy)carbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(3 ,4,5- trimethOxyphenyl)methyl]-4-[(4-methoxyphenoxy)carbonyl]piper azine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-trifluoromethylpyrimidin-4-yl]-N-[ (1,4-benzodioxan-6-yl)methyl]- 4-[(4-methoxyphenoxy)carbonyl]piperazine-2-carboxamide; 1 -[2-( IH-imidazol-1 -yl)pyri mid i n4-yl]-N-[(l ,4-benzod ioxan-6-yl)methyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6-yl]ethyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-acetamide; 1-[6-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-methoxyphenyl)m ethyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1-methyl pyrrol-2-yl)ethyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-(methylethyl)pyrimidin-4-yl]-N-[(2 ,4-dimethoxyphenyl)methyl]- 4-[(4-methoxyphenoxy)carbonyl]piperazine-2-carboxamide; I -[6-chloro-2-( IH-imidazol-I -yl )pyrimidin-4-yl]-N-[(2,6-dimethoxyphenyl)methyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-carboxamide; 1 -[2-( IH-imidazol- I -yl)-6-methyl pyrimidinA-yl]-N-((3,4-dimethoxyphenyl)methyl]-4-[(4- methoxyphenoxy)carbonyl]piperazine-2-carboxamide; I -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]-N-[1 -(phenylmethyl)piperidin4- yl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-cyanocy clohexyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(2,2- dimethoxyethyl)piperidine-2- acetamide; I -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]-N-tridecylpiperidine-2-ace tamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-hydroxy-4-methyl thiobutyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N,N-[bi s(2-cyanoethyl)piperidine-2 acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N,N-[bis(2-c yanomethyl)]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(4,4- diethoxybutyl)piperidine-2- acetamide; 1 -(4-fluorophenyl)-4-[1 -[2-( IH-imidazol-I -yl)pyrimidin-4-yl]piperidine-2-acetyl]piperazine; 1-[(1,3-benzodioxol-5-yl)methyl]-4-[1-[2-(1H-imidazol-1-yl)p yrimidin-4-yl]piperidine-2- acetyl]piperazine; 1 -(phenylmethyl)-4-[1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]piperidine-2-acetyl]piperazine; 4-[1-[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]piperidine-2-acetyl]piperazine-1 -carboxylic acid, ethyl ester; 1 -(4-chlorophenyl)-4-[1 -[2-( IH-imidazol-1 -yl)pyrimidin-4-yl]piperidine-2-acetyl]-4- hydroxypiperidine; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,3-dihy drobenzofuran-5- yl)methyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(indan-5- yl)methyl)piperidine-2- acetamide; 1 -[2-( IH-imidazol-I -yl)-6-methylpyrimidinA-yl]- N-[(cyclohexyl)methyl]piperidine-2- acetamide; I -[2-( IH-imidazol-I -yl)pyrimidin-4-yl]-N-(l ,2,3,4-tetrahydronaphthalen-l -yl)piperidine-2- acetamide; 1 -(2-( IH-imidazol- I -yl)pyrimidin-4-yl]-N-[(naphthalen- 1 -yl)methyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(1,3 -benzodioxol-5- yl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(4- chlorophenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(2-et hylhexyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-ethylhexyl)piper idine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(2-ethylhe xyl)piperidine-2-acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(m orpholin-4-yl)ethyl]piperidine- 2-acetamide; I -[2-( lH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-(l -methylhexyl)piperidine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]-N-(1 -methylhexyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1-methylhexyl)pipe ridine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-methylphenyl)me thyl]piperidine-2-acetamide; 1 -[2-( I H-imidazol- 1 -yl )-6-methylethylpyrimid i n-4-yl]- N-[(4- methoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(cycl ooctyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-ethyl-3 -hydroxy-1- hydroxyethylpropyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[3-(m orpholin-4- yl)propyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(1-me thyl-3- phenylpropyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1-methyl-3-phenylp ropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-methyl- 3-phenylpropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(1-me thylheptyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1-methylheptyl)pip eridine-2-acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-(l -methylheptyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-fluorophenyl)me thyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-fluoro phenyl)methyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]- N-[(4- methylphenyl)methyl]piperidine-2-acetamide; 1 -[2-( IH-imidazol- I -yl)pyrimidin-4-yI]-N-( I -phenylethyl)piperidine-2-acetamide;

1 -[2-(1H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-phenylmethylpiperidine-2-acet amide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(3,4 - dichlorophenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(2-phenylethyl)pipe ridine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(2-phenyle thyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[3-(p yrrolidinon-1- yl)propyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1,5-dimethylhexyl) piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1,5-dimet hylhexyl)piperidine-2- acetamide; 1-[2-1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(1,5-d imethylhexyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2-fluorophenyl)me thyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2-fluoro phenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(3,4 - dimethoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(2-chlo rophenyl)ethyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol- 1 -yl)pyrimidin-4-yl]-N-[(furan-2-yl)methyl]piperidine-2-aceta mide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(furan-2- yl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(fur an-2-yl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(pyr idin-2-yl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(pyridin-2-yl)meth yl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(pyridin- 2-yl)methyl]piperidine-2- acetamide; 1 -[2-( 1H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(3- trifluoromethylphenyl)methyl]piperidine-2-acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3-trifluoromethyl phenyl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(2-phenylp ropyl)plperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(2-phenylp ropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(2-meth oxyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-pyrimidin-4-yl]-N-[2-(2-methoxypheny l)ethyl]piperidine-2- acetamide; I -[2-( I H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-(2-hydrox methylthiobutyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(2-hy droxy-4- methylthiobutyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,4-dich lorophenyl)methyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(3- methylphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-pyrimidin-4-yl]-N-[(3-methylphenyl)m ethyl]piperidine-2-acetamide; 1 -(2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(3-methylphenyl)methyl]piper idine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(3 - methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-methoxyphenyl )ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(3-meth oxyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-methoxyphenyl )ethyl]pyrrolidine-2- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(3 ,4- dimethoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3,4-dimethoxyph enyl)ethyl]piperidine-2- acetamide;

1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(3,4- dimethoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3,4-dimethoxyph enyl)ethyl]pyrrolidine-2- carboxamide; I -[2-( lH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]- N-(phenylbutyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-pyrimidin-4-yl]-N-(phenylbutyl)piper idine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1-hydroxymethylpen tyl)piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-hydroxy methylpentyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(3,5 - dimethoxyphenyl )methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,5-dimethoxyphen yl)methyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3,5- dimethoxyphenyl)methyl]piperidine-2-acetamide; 1 -[2-( lH-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]- N-[2-(4- ethoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-ethoxyphenyl) ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-etho xyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-ethoxyphenyl) ethyl]pyrrolidine-2- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(4 - bromophenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-bromophenyl)e thyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-brom ophenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-bromophenyl)e thyl]pyrrolidine-2- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-penty lpiperidine-2-acetamide; I -[2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-pentylpiperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-pentylpipe ridine-2-acetamide;

1 -[2-(1H-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]- N-[3-(1H-imidazol-1 - yl)propyl]piperidine-2-acetamide; 1 -[2-( IH-imidazol-I -yl)-6-methylpyrimidin-4-yl]- N-[3-( 1H-imidazol-l -yl)propyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-chloro phenyl)methyl]piperidine-2- acetamide; 1 -[2-( I H-imidazol- I -yl)pyrimidin-4-yl]-N-[(3-chlorophenyl)methyl]piperidine-2-a cetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(2,4-dich lorophenyl)methyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(2,4-dichloropheny l)methyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[2-(1 -phenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[1-(phenyl)ethyl]pi peridine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(3-fluo rophenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(3 -ethoxy-4- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-ethoxy-4-meth oxyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(3-etho xy-4- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-ethoxy-4-meth oxyphenyl)ethyl]pyrrolidine- 2-carboxamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-chlorophenyl) ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-chlo rophenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(5-hydroxy pentyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-butylpiperidine-2-a cetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]- N-[(4- fluorophenyl)(methyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-fluorophenyl)(m ethyl)methyl]piperidine-2- acetamide;

I -[2-( IH-imidazol-1 -yl)pyrimidin-4-yl]-N-[2-(2,5-dimethoxyphenyl)ethyl]piperidi ne-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(2,5- dimethoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(2,5-dimethoxyph enyl)ethyl]pyrrolidine-2- carboxamide; 1 -[2-(1H-imidazol-1 -yl)-6-methylethyl pyrimid i n-4-yl]- N-[2-(4-ethoxy-3- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-ethoxy-3-meth oxyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-etho xy-3- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-ethoxy-3-meth oxyphenyl)ethyl]pyrrolidine- 2-carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[2-(4 - methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-methoxyphenyl )ethyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[2-(4-methoxyphenyl)ethyl]pip eridine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-methoxyphenyl )ethyl]pyrrolidine-2- carboxamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[3- (methylethoxy)propyl]piperidine-2-acetamide; 1 -[2-( IH-imidazol- I -yl)-6-methylethylpyrimidin4-yl]-N-hexylpiperidine-2-acetami de; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-hexylpiperidine-2-a cetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-hexylpiper idine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(cyclohexen-1-yl )ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(cycloh exen-1-yl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(3-fluoro -5- trifluoromethylphenyl)methyl]piperidine-2-acetamide;

1 -[2-(1H-imidazol-1 -yl)pyrimidin-4-yl]-N-[(3-fluoro-5- trifluoromethylphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-pyrimidin-4-yl]-N-[2-(4-methylphenyl )ethyl]piperidine-2 acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-meth ylphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(3-et hoxypropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(3-ethoxyp ropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-hepty lpiperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-heptylpiperidine-2- acetamide; I -t2-( lH-imidazol- 1 -yl)-6-methyspyrimidin-4-yl]-N-heptylpiperidine-2-acetamide; 1 -[2-( I H-imidazol-1 -yl)-6-methylpyrimidin4-yl]-N-(3-methoxypropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(1-cyclohexylethyl) piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-cyclohe xylethyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(4- trifluoromethoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1 H-imid azol-l-yl)-6-methyl pyrimidin-4-yl]- N-[(4- trifluoromethoxyphenyl)methyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(4-flurophenyl)e thyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(4-flur ophenyl)ethyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol-I -yl)-6-methylethylpyri mid i n-4-yl]- N-[2-(3-bromo4- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-bromo-4-metho xyphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(3-brom o-4- methoxyphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[2-(3-bromo-4-metho xyphenyl)ethyl]pyrrolidine- 2-carboxamide;

1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-(3-ph enylpropyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-(3-phenylpropyl)pip eridine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(3-phenylp ropyl)piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin4-yl]-N-octylpiperidine-2-acetami de; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-octylpiper idine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(1-hydroxy -3-methylbutyl)piperidine-2- acetamide; 1 -!2-( IH-imidazol-I -yl)-6-methylethylpyrimidin-4-yl]-N-[1 -(4- methylphenyl)ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[1-(4-methylphenyl) ethyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[1-(4-meth ylphenyl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(4,4-dieth oxybutyl)piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(4- trifluoromethylphenyl)methyl]piperidine-2-acetarmide; 1-[2-(1H-imidazol-1-yl)-pyrimidin-4-yl]-N-[(4-trifluoromethy lphenyl)methyl]piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(4- trifluoromethylphenyl)methyl]piperidine-2-acetamide; 1 -[2-(1H-imidazol-1 -yl)-6-methylethylpyrimidin-4-yl]-N-(3-butoxypropyl)piperid ine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-(3-butoxyp ropyl)piperidine-2- acetamide; 1 -[2-( IH-imidazol-1 -yl)-6-methylethylpyrimidin4-yl]- N-[2-(thiophen-2-yl)ethyl]piperidine- 2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[2-(thioph en-2-yl)ethyl]piperidine-2- acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[3-(p yrrolidin-1- yl)propyl]piperidine-2-acetamide; 1-[2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]-N-[(cyc lohexyl)methyl]piperidine-2- acetamide;

1-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(cyclohexyl)methyl ]piperidine-2-acetamide; 4-[[1 -[2-( IH-imidazol-1 -yl)pyrimidin4-yl]piperidine-2-acetyl]amino]piperidine-1 -carboxylic acid, ethyl ester; 4-[[1-(2-(1H-imidazol-1-yl)-6-methylethylpyrimidin-4-yl]pipe ridine-2- acetyl]amino]piperidine-1-carboxylic acid, ethyl ester; 4-[[1 -[2-( IH-imidazol-I -yl)-6-methylpyrimidin-4-yl]piperidine-2-acetyl]amino]piperi dine-1 - carboxylic acid, ethyl ester; 1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-fluoro phenyl)methyl]piperidine-2 acetamide; N-[(l ,3-benzodioxol-5-yl)methyl]-l -[3-(1 H-imidazol-l -yl)phenyl]piperidine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[3-chloro-5-(1H-imidazol- 1-yl)triazin-1-yl]piperidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1 -[2-(1 H-imidazol-1 -yl)purin-6-yl]piperidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1 -[6-(1 H-imidazol- 1 -yl)pyrazin-2-yl]piperidine-2- acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-6-chloro-2-(1H-imidazol-1-yl )pyrimidine-4-propionamide; N-[(1,3-benzodioxol-5-yl)methyl]-2-(1H-imidazol-1-yl)pyrimid ine-4-propionamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-(1H-imidazol-1-yl)pyrimidi ne-4-propionamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[2-(1H-imidazol-1-yl)pyrim idin-4-oxy]acetamide; N-[(1,3-benzodioxol-5-yl)ethyl]-2-[2-(1H-imidazol-1-yl)pyrim idin-4-thio]acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]piperidine-2- ethanamine; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N- methylpiperidine-2-ethanamine; N-acetyl-N-[(l ,3-benzodioxol-5-yl)methyl]-l -[2-(1 H-imidazol-l -yl)pyrimidin4- yl]piperidine-2-ethanamine; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-N- (methylsulfonyl)piperidine-2-ethanamine; 4-[2-[[( I ,3-benzodioxol-5-yl)methoxy] ethyl]piperidin-1 -yl]-2-(1 H-imidazol-I -yl)pyrimidine; 4-[2-[[4-(methoxy)phenoxy]propyl]pyrrolidin-1 -yl]-2-(1 H-imidazol-1 -yl)pyrimidine; 4-[2-[[4-(methoxy)phenoxy]propyl]pyrrolidin-1-yl]-2-(1H-imid azol-1-yl)-6- methylpyrimidine; 4-[2-[(1 ,3-benzodioxol-5-yl)propyl]pyrrolidin-1 -yl]-2-(1 H-imidazol-1 -yl)pyrimidine;

4-[2-[(1,3-benzodioxol-5-yl)prop-2-enyl]pyrrolidin-1-yl]-2-( 1H-imidazol-1-yl)pyrimidine; 4-chloro-2-(1H-imidazol-1-yl)-6-(perhydroazepin-1-yl)pyrimid ine; 1-[6-chloro-2-(1H-imidazol-1-yl)pyrimidin-4-yl]piperidine-2- ethanol; 4-chloro-2-(1 H-imidazol-1 -yl)-6-(piperidin-1 -yl)pyrimidine; 4-chloro-2-(1H-imidazol-1-yl)-6-(2-ethylpiperidin-1-yl)pyrim idine; 4-fluoro-2-(1H-imidazol-1-yl)-6-[[(3,4-dimethoxyphenyl)ethyl ]amino]pyrimidine; 4-fluoro-2-(1 H-imidazol-1 -yl)-6-[[(phenyl)ethyl]amino]pyrimidine; N-[(1,4-benzodioxan-6-yl)methyl]-1-[2-(1H-triazol-1-yl)pyrim idin-4-yl]-4- [(dimethylethoxy)carbonyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[6-(morpholin-4-yl)-2-(1H -imidazol-1-yl)pyrimidin-4- yl]piperidine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-[2-(1H-imidazol-1-yl)-6-m ethoxypyrimidin-4- yl]piperidine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-4-[6-[bis(ethoxycarbonyl)me thyl]-2-(1H-imidazol-1- y)lpyrimidin-4-yl]-1-[(methoxy)carbonyl]piperazine-2-acetami de; N-[(1,3-benzodioxol-5-yl)methyl]-4-[6-(aminocarbonyl)-2-(1H- imidazol-1-y)lpyrimidin-4- yl]-1-[(methoxy)carbonyl]piperazine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-3-[2-(1H-imidazol-1-yl)pyri midin-4-yl]-4- methoxybenzamide; 4-chloro-2-(1 H-imidazol-1 -yl)-6-[(2-methoxyphenyl)amino]pyrimidine N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]indole-6- carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrim idin-4-yl]pyrrole-2- carboxamide; N-[(3,4-dimthoxyphenyl)ethyl]-2-[2-(1H-imidazol-1-yl)pyrimid in-4-yl]-1,2,3,4- tetrahydroisoquinoline-3-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]pyrrolidine-2- propionamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4-yl]pyrrolidine- 2-propionamide; N-[(3,4-dimethoxphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrimid in-4-yl]pyrrolidine-3- carboxamide; N-[(3 ,4-dimethoxyphenyl )ethyl]-l -[2-(1 H-imidazol-l -yl)-6-methyl pyrimidin4- yl]pyrrolidine-3-carboxamide;

N-[(3,4-dimethoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrimi din-4-yl]pyrrolidine-3- acetamide; N-E(3,4-dimethoxyphenyl)ethyl]-l -[2-(1 H-imidazol-l -yl)-6-methylpyrimidin4- yl]pyrrolidine-3-acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-eth ylpyrimidin-4-yl]pyrrolidine- 3-acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-met hylpyrimidin-4-yl]azetidine- 2-carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)ethyl]morpholine-2- carboxamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yl)ethyl]morpholine-2-carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,4-benzodioxan-6 -yl)ethyl]morpholine-2- carboxamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,4-benz odioxan-6- yl)ethyl]morpholine-2-carboxamide; 4-[2-(1 H-imidazol-l -yl)pyrimidin4-yl]-N-[(4-methoxyphenyl)ethyl]morpholine-2- carboxamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(4-methox yphenyl)ethyl]morpholine-2- carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(3,4-dimethoxyphen yl)ethyl]morpholine-2- carboxamide; 4-[2-(1 H-imidazol-1 -yl)-6-methylpyrimidin-4-yl]-N-[(3,4- dimethoxyphenyl)ethyl]morpholine-2-carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(4-methoxyphenyl)m ethyl]morpholine-2- carboxamide; 4-[2-(1 H-imidazol-l -yl)-6-methylpyrimidin-4-yl]-N-[(4-methoxyphenyl)methyl]morp holine- 2-carboxamide; 4-[2-(1H-imidazol-1-yl)pyrimidin-4-yl]-N-[(1,3-benzodioxol-5 -yl)methyl]morpholine-2- acetamide; 4-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]-N-[(1,3-benz odioxol-5- yl)methyl]morpholine-2-acetamide; N-[(l ,3-benzodioxol-5-yl)methyll-4-[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]morpholine-3- carboxamide;

N-[(1,3-benzodioxol-5-yl)methyl]-4-[2-(1H-imidazol-1-yl)-6-( methylethyl)pyrimidin-4- yl]morpholine-3-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-4-[6-ethyl-2-(1H-imidazol-1- yl)pyrimidin-4-yl]morpholine- 3-carboxamide; N-[(l ,3benzod ioxol-5-yl)ethyl]-4-[2-( 1 H-imidazol-1 -yl)pyrimidin-4-yl]morpholine-3- carboxamide; N-[(4-methoxyphenyl)methyl]-4-[2-(1H-imidazol-1-yl)-6-methyl pyrimidin-4-yl]morpholine- 3-carboxamide; N-[(4-chlorophenyl)methyl]-4-[2-(1H-imidazol-1-yl)-6-methylp yrimidin-4-yl]morpholine-3- carboxamide; N-[(3,4-dichlorophenyl)methyl]-4-[2-(1H-imidazol-1-yl)-6-met hylpyrmidin-4- yl]morpholine-3-carboxamide; N-[(4-methylphenyl)methyl]-4-[2-(1H-imidazol-1-yl)-6-methylp yrimidin-4-yl]morpholine-3- carboxamide; N-[(3,4-dimethylphenyl)methyl]-4-[2-(1H-imidazol-1-yl)-6-met hylpyrimidin-4- yl]morpholine-3-carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-2-[[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4- yljamino]acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-2-[[2-(1H-imidazol-1-yl)-6- methylpyrimidin-4- yl]amino]acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]perhydroazepine- 2-carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-1 -[2-(1 H-imidazol-1 -yl)-6-methylpyrimidin-4- yl]perhydroazepine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-( methylethyl)pyrimidin-4- yl]perhydroazepine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]perhydroazepine- 2-carboxamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]perhydroazepine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrim idin-4-yl]perhydroazepine-2- carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4- yl]perhydroazepine-2-carboxamide;

N-[(1,3-benzodioxol-5-yl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-ethylpyrimidin4- yl]perhydroazepine-2-carboxamide; N-[(1,3-benzodioxol-5-yl)ethyl]-1-[6-chloro-2-(1H-imidazol-1 -yl)pyrimidin-4- yl]perhydroazepine-2-carboxamide; N-[(1,4-benzodioxan-6-yl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]perhydroazepine-2- carboxamide; N-[(1 ,4-benzodioxan-6-yl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-methylpyrimidinA- yl]perhydroazepine-2-carboxamide; N-[(3,4-dimethoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)pyrimi din-4-yl]perhydroazepine-2- carboxamide; N-[(3,4-dimethoxyphenyl)ethyl]-1 -[2-( 1 H-imidazol-1 -yl)-6-methylpyrimidin4- yl]perhydroazepine-2-carboxamide; N-[(3,4-dimethoxyphenyl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-ethylpyrimidin4- yl]perhydroazepine-2-carboxamide; N-[(3,4-dimethoxyphenyl)methyl]-1-[2-(1H-imidazol-1-yl)-6-(m ethylethyl)pyrimidin-4- yl]perhydroazepine-2-carboxamide; N-[(3,4-dimethoxyphenyl)ethyl]-1-[6-chloro-2-(1H-imidazol-1- yl)pyrimidin-4- yl]perhydroazepine-2-carboxamide N-[(1,3-benzodioxol-5-yl)methyl]-1-[2-(1H-imidazol-1-yl)pyri midin-4-yl]perhydroazepine- 2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1 -[2-(1 H-imidazol-1 -yl)-6-methylpyrimidin4- yl]perhydroazepine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1 -[2-(1 H-imidazol-1 -yl)-6-ethylpyrimidin4- yl]perhydroazepine-2-acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-1 -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]perhydroazepine- 2-acetamide; N-[(1,4-benzodioxan-6-yl)methyl]-1-[2-(1H-imidazol-1-yl)-6-m ethylpyrimidin-4- yl]perhydroazepine-2-acetamide; N-[(3,4-dimethoxyphenyl)methyl]-1-[2-(1H-imidazol-1-yl)-6-me thylpyrimidin-4- yl]perhydroazepine-2-acetamide; N-[(3,4-dimethoxyphenyl)methyl]-1 -[2-(1 H-imidazol-1 -yl)-6-(methylethyl)pyrimidin-4- yl]perhydroazepine-2-acetamide; N-[(3,4-dimethoxyphenyl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-met hylpyrimidin-4- yl]perhydroazepine-2-acetamide;

N-[(3,4-dimethoxyphenyl)ethyl]-1 -[2-(1 H-imidazol-1 -yl)-6-(methylethyl)pyrimidin4- yl]perhydroazepine-2-acetamide; N-[(4-methoxyphenyl)methyl]-1 -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]perhydroazepine-2- acetamide; N-[(4-methoxyphenyl)methyl]-1 -[2-(1 H-imidazol- 1 -yl)-6-methylpyrimidin4- yl]perhydroazepine-2-acetamide; N-[(1,3-benzodioxol-5-yl)methyl]-1-[6-chloro-2-(pyridin-3-yl )pyrimidin-4-yl]piperidine-2 acetamide; N-[(l ,3-dioxolan-5-yl)methyl]-l -[2-(1 H-imidazol-1 -yl)pyrimidin-4-yl]perhydroazepine-2- acetamide; N-[(4-trifluoromethoxyphenyl)methyl]-l -[2-(1 H-imidazol-1 -yl)pyrimidin4- yl]perhydroazepine-2-acetamide; and N-[(4-trifl uoromethoxyphen yl)methyl]-l -[2-( I H-imidazol-1 -yl)-6-methyl pyrimidin-4- yl]perhyd roazepi ne-2-acetamide.

While the present invention has been described with reference to the specific embodiments thereof, it should be understood by those skilled in the art that various changes may be made and equivalents may be substituted without departing from the true spirit and scope of the invention. In addition, many modifications may be made to adapt a particular situation, material, composition of matter, process, process step or steps, to the objective, spirit and scope of the present invention. All such modifications are intended to be within the scope of the claims appended hereto.