| 主权项 |
1. A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is H, —NO2, —CN, —OCF3, halogen, or amino; or C1-6aliphatic, C3-7cycloaliphatic, C1-6alkoxy, or C1-4haloalkyl optionally substituted with 0-10 JR groups; R2 is H, —NO2, —CN, —OCF3, halogen, or amino; or C1-6aliphatic, C3-7cycloaliphatic, C1-6alkoxy, or C1-4haloalkyl optionally substituted with 0-10 JR groups; Z1 is C1-6aliphatic or C3-10cycloaliphatic optionally substituted with 0-10 JZ groups; if the bond between Z1 and C is a double bond, then Z1 may also be ═O, ═NR, or ═C(R)2; Z2 is H or halogen; or C1-10haloalkyl, C1-4haloalkoxy, Y, —(Vn)—CN, —(Vn)—NO2, —(Vn)—OH, —(Vn)—(C1-6aliphatic), —(Vn)—(C3-12heterocyclyl), —(Vn)—(C6-10aryl), —(Vn)-(5-10 membered heteroaryl), or —(Vn)—(C3-10cycloaliphatic) optionally substituted with 0-10 JZ groups; or Z1 and Z2, together with the carbon atom to which they are attached, form ring Q; Z3 is H or C1-6alkyl optionally substituted with 0-3 JZ groups; or Z1, Z2, and Z3, together with the carbon atom to which they are attached, form an 6-14 membered saturated, partially saturated, or unsaturated bicyclic ring having 0-3 heteroatoms; if the bond between Z1 and C is a triple bond, then Z2 is absent; if the bond between Z1 and C is a double bond or a triple bond, then Z3 is absent; Q is a 3-8 membered saturated or partially saturated monocyclic ring having 0-3 heteroatoms selected from nitrogen, oxygen, or sulfur, wherein said Q is optionally and independently fused to Q1 or Q2; or to both Q1 and Q2; wherein said Q is optionally substituted with 0-4 JQ groups; Q1 is a 3-8 membered saturated, partially saturated, or unsaturated monocyclic ring having 0-3 heteroatoms selected from nitrogen, oxygen, or sulfur, wherein said Q1 group is optionally substituted with 0-4 JQ groups; Q2 is a 3-8 membered saturated, partially saturated, or unsaturated monocyclic ring having 0-3 heteroatoms selected from nitrogen, oxygen, or sulfur wherein said Q2 group is optionally substituted with 0-4 JQ groups; R is H, optionally substituted C1-6 aliphatic, C3-10 cycloaliphatic, C6-10 aryl, 5-14 membered heteroaryl, or 5-14 membered heterocyclyl; or two R groups, on the same substituent or different substituents, together with the atom(s) to which each R group is bound, form an optionally substituted 3-14 membered saturated, partially unsaturated, or fully unsaturated monocyclic, bicyclic, or tricyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur wherein each R is optionally substituted with 0-10 JR groups; each JQ and JZ substituent on an unsaturated carbon atom is independently selected from hydrogen, —OCF3, C1-6haloalkyl, N(R)2, OR, halogen, Y, —(Vn)—CN, —(Vn)—NO2, —(Vn)—OH, —(Vn)—(C1-6aliphatic), —(C3-10cycloaliphatic)-C(O)R, —(C3-10cycloaliphatic)-(C3-12heterocyclyl); —(Vn)—(C3-12heterocyclyl), —(Vn)—(C6-10aryl), —(Vn)-(5-10 membered heteroaryl), —(Vn)—(C3-10cycloaliphatic); wherein each JQ and JZ is optionally substituted with up to 10 JR groups; each JQ and JZ substituent on a saturated carbon atom is selected from those listed above for an unsaturated carbon and also the following: ═O, ═NN(Ra)2, ═NNHC(O)Ra, ═NNHCO2(C1-4alkyl), ═NNHSO2(C1-4alkyl), and ═NRa wherein each JQ and JZ is optionally substituted with up to 10 JR groups; each JQ and JZ substituent on a nitrogen atom is independently selected from hydrogen, Y, —(Vn)—CN, —(Vn)—NO2, —(Vn)—OH, —(Vn)—(C1-6aliphatic), —(C3-10cycloaliphatic)-C(O)R, —(C3-10cycloaliphatic)-(C3-12heterocyclyl), —(Vn)—(C3-12heterocyclyl), —(Vn)—(C6-10aryl), —(Vn)-(5-10 membered heteroaryl), —(Vn)—(C3-10cycloaliphatic); wherein two JZ groups, on the same substituent or different substituents, together with the atom(s) to which each JZ group is bound, can optionally form an optionally substituted 3-14 membered saturated, partially unsaturated, or fully unsaturated monocyclic, bicyclic, or tricyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; wherein each JQ and JZ is optionally substituted with up to 10 JR groups; JR is selected from halogen, —N(Rb)2, SRb, ORb, oxo, C1-4haloalkoxy, C1-4haloalkyl, L, -(Ln)-(C1-6alkyl), -(Ln)-(C3-12heterocyclyl), -(Ln)-(C6-10aryl), -(Ln)-(5-10 membered heteroaryl), -(Ln)-(C3-10cycloalipahtic), -(Ln)-NO2, -(Ln)-CN, -(Ln)-OH, —CO2Rb, —CORb, —OC(O)Rb, —NC(O)Rb; L is C1-10alkyl wherein up to three methylene units are replaced by —NRb—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NRb—, —C(═N—CN), —NRbCO—, —NRbC(O)O—, —SO2NRb—NRbSO2—, —NRbC(O)NR—, —OC(O)NRb—, —NRbSO2NRb—, —SO—, or —SO2—; V is C1-10aliphatic wherein up to three methylene units are replaced by GV, wherein GV is selected from —NR—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NR—, —C(═N—CN), —NRCO—, —NRC(O)O—, —SO2NR—, —NRSO2—, —NRC(O)NR—, —OC(O)NR—, —NRSO2NR—, —SO—, or —SO2—; Y is C1-10aliphatic, wherein up to three methylene units are replaced by GY wherein GY is selected from —NR—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NR—, —C(═N—CN), —NRCO—, —NRC(O)O—, —SO2NR—, —NRSO2—, —NRC(O)NR—, —OC(O)NR—, —NRSO2NR—, —SO—, or —SO2—; Ra is hydrogen or C1-6 aliphatic group optionally substituted with 0-3 JR groups; Rb is hydrogen or an unsubstituted C1-6 aliphatic group; n is 0 or 1; provided that: when R1 and R2 are H, and Z2 and Z3 are H, then Z1 is not methyl; when R1 is CH3 and R2 is H, then Z1, Z2, and Z3 are not all H; when R1 and R2 are H, and Z2 and Z3 are H, then Z1 is not unsubstituted phenyl, 4-pyridyl, or one of the structures shown below:and
when R1 and R2 are H, Z1 and Z2 taken together are not —C≡C—CH2CH2COOH.
|
