| 主权项 |
1. A compound of formula I or a pharmaceutically acceptable salt thereof, wherein:
Ring A is a 5-membered monocyclic heteroaryl selected from wherein Ring A is optionally substituted with up to 1-3 occurrences of R8; R1 is H, halogen or C1-4 aliphatic; R2 is H, halogen or C1-4 aliphatic; R5 is H, halogen, CN, NH2, NO2, CF3, C1-4 aliphatic, cyclopropyl, NCH3, OCH3, —C(═O)NH2, —C(═O)CH3, —NC(═O)CH3, or OH; R3 is —(U)m—X; U is a C1-6 aliphatic, wherein up to two methylene units are optionally and independently replaced by GU and wherein U is optionally substituted with 1-4 JU; GU is —NH—, —NR6—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NH—, —C(O)NR6—, —NC(═N—CN)N—, —NHCO—, —NR6CO—, —NHC(O)O—, —NR6C(O)O—, —SO2NH—, —SO2NR6—, —NHSO2—, —NR6SO2—, —NHC(O)NH—, —NR6C(O)NH—, —NHC(O)NR6—, —NR6C(O)NR6, —OC(O)NH—, —OC(O)NR6—, —NHSO2NH—, —NR6SO2NH—, —NHSO2NR6—, —NR6SO2NR6—, —SO—, or —SO2—; R6 is C1-6 aliphatic or a C3-10cycloaliphatic; or two R6 groups, together with the atom to which they are attached, optionally form a 3-7 membered cycloaliphatic or heterocyclyl, wherein said aliphatic, cycloaliphatic or heterocyclyl is optionally substituted with R″, —OR″, —SR″, —NO2, —CF3, —CN, —CO2R″, —COR″, OCOR″, CONHR″, or NHCOR″, wherein R″ is H or an unsubstituted C1-6 aliphatic; m is 0 or 1; X is H, halogen, CN, NO2, S(O)R, SO2R, or a group selected from a C1-6aliphatic, a C3-10 cycloaliphatic, a C6-10 aryl, a 5-10 membered heteroaryl, or a 5-10 membered heterocyclyl, wherein said group is optionally substituted with 1-4 JX; R is an optionally substituted group selected from a C1-6 aliphatic, a C3-10 cycloaliphatic, a C6-10 aryl, a 5-10 membered heteroaryl, or a 5-10 membered heterocyclyl, wherein R is independently and optionally substituted with 1-6 occurrences of JR; each JR is independently selected from halogen, L, -(Ln)-R′, -(Ln)-N(R′)2, -(Ln)-SR′, -(Ln)-OR′, -(Ln)-(C3-10 cycloaliphatic), -(Ln)-(C6-10 aryl), -(Ln)-(5-10 membered heteroaryl), -(Ln)-(5-10 membered heterocyclyl), oxo, C1-4haloalkoxy, C1-4haloalkyl, -(Ln)-NO2, -(Ln)-CN, -(Ln)-OH, -(Ln)-CF3, —CO2R′, —CO2H, —COR′, —COH, —OC(O)R′, —C(O)NHR′, C(O)N(R′)2, —NHC(O)R′, or NR′C(O)R′; or two JR groups, on the same substituent or different substituents, together with the atom(s) to which each JR group is bound, form a 5-7 membered saturated, unsaturated, or partially saturated ring; each JU is independently selected from halogen, L, -(Ln)-R′, -(Ln)-N(R′)2, -(Ln)-SR′, -(Ln)-OR′, -(Ln)-(C3-10 cycloaliphatic), -(Ln)-(C6-10 aryl), -(Ln)-(5-10 membered heteroaryl), -(Ln)-(5-10 membered heterocyclyl), oxo, C1-4haloalkoxy, C1-4haloalkyl, -(Ln)-NO2, -(Ln)-CN, -(Ln)-OH, -(Ln)-CF3, —CO2R′, —CO2H, —COR′, —COH, —OC(O)R′, —C(O)NHR′, C(O)N(R′)2, —NHC(O)R′, or NR′C(O)R′; or two JU groups, on the same substituent or different substituents, together with the atom(s) to which each JU group is bound, form a 5-7 membered saturated, unsaturated, or partially saturated ring; each JX is independently selected from halogen, L, -(Ln)-R′, -(Ln)-N(R′)2, -(Ln)-SR′, -(Ln)-OR′, -(Ln)-(C3-10 cycloaliphatic), -(Ln)-(C6-10 aryl), -(Ln)-(5-10 membered heteroaryl), -(Ln)-(5-10 membered heterocyclyl), oxo, C1-4haloalkoxy, C1-4haloalkyl, -(Ln)-NO2, -(Ln)-CN, -(Ln)-OH, -(Ln)-CF3, —CO2R′, —CO2H, —COR′, —COH, —OC(O)R′, —C(O)NHR′, C(O)N(R′)2, —NHC(O)R′; each L is independently a C1-6 aliphatic wherein up to three methylene units are replaced by —NH—, —NR7—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NH—, —C(O)NR7—, —NC(═N—CN)N, —NHCO—, —NR7CO—, —NHC(O)O—, —NR7C(O)O—, —SO2NH—, —SO2NR7—, —NHSO2—, —NR7SO2—, —NHC(O)NH—, —NR7C(O)NH—, —NHC(O)NR7—, —NR7C(O)NR7, —OC(O)NH—, —OC(O)NR7—, —NHSO2NH—, —NR7SO2NH—, —NHSO2NR7—, —NR7SO2NR7—, —SO—, or —SO2—; each n is independently 0 or 1; each R′ is independently H or C1-6 aliphatic; or two R′ groups, together with the atom to which they are attached, optionally form a 3-6 membered cycloaliphatic or heterocyclyl, wherein said aliphatic, cycloaliphatic or heterocyclyl is optionally substituted with R*, —OR*, —SR*, —NO2, —CF3, —CN, —CO2R*, —COR*, OCOR*, NHCOR*, wherein R* is H or C1-6 aliphatic; R7 is selected from C1-6 aliphatic, C3-10 cycloaliphatic, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocyclyl; or two R7 groups, on the same substituent or different substituents, together with the atom(s) to which each R6 group is bound, form a 3-8 membered heterocyclyl; each R8 is independently —(C1-3 aliphatic)y-R9, wherein R8 is optionally substituted with 1-5 occurrences of JR8; each y is independently 0 or 1; R9 is halogen, CN, NH2, NO2, CF3, C1-4 aliphatic, cyclopropyl, NHR10, N(R10)2, OR10, C(O)OR10, —C(O)NH2, —C(O)R10, —NC(O)R10, or OH; R10 is C1-4 aliphatic; each JR8 is independently selected from halogen, OCH3, OH, NO2, NH2, SCH3, NCH3, CN, or unsubstituted C1-2aliphatic; or two JR8, together with the carbon to which they are attached, form a cyclopropyl ring or C═O. |
