主权项 |
1. A compound of formula I or a pharmaceutically acceptable salt thereof wherein Q is Z is a bond, NH, N(C1-3aliphatic) or C═CH2; R1 is —(C1-2 aliphatic)p-R4 wherein each R1 is optionally substituted with 1-3 occurrences of J; R2 is —(C1-2 aliphatic)d-R5 wherein each R2 is optionally substituted with 1-3 occurrences of J; R3 is halogen, —CN, —NO2 or —(U)m—X, wherein
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;X is H, halogen, CN, NO2, S(O)R, SO2R, C1-4 haloaliphatic, or a group selected from C1-6 aliphatic, a C3-10 cycloaliphatic, C6-10 aryl, 5-10 membered heteroaryl, 5-10 membered heterocyclyl; wherein said group is optionally substituted with 1-4 JX;GU is —NH—, —NR—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NH—, —C(O)NR—, —C(═N—CN)—, —NHCO—, —NRCO—, —NHC(O)O—, —NRC(O)O—, —SO2NH—, —SO2NR—, —NHSO2—, —NRSO2—, —NHC(O)NH—, —NRC(O)NH—, —NHC(O)NR—, —NRC(O)NR, —OC(O)NH—, —OC(O)NR—, —NHSO2NH—, —NRSO2NH—, —NHSO2NR—, —NRSO2NR—, —SO—, or —SO2—; R4 is H, halogen, CN, NH2, NO2, CF3, C1-3 aliphatic, cyclopropyl, NCH3, OCH3, —C(═O)NH2, —C(═O)CH3, —NC(═O)CH3, or OH; R5 is H, halogen, CN, NH2, NO2, CF3, C1-3 aliphatic, cyclopropyl, NCH3, OCH3, —C(═O)NH2, —C(═O)CH3, —NC(═O)CH3, or OH; R is an optionally substituted group selected from C1-6 aliphatic, C3-10 cycloaliphatic, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 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 3-8 membered heterocyclyl; wherein each R group is independently and optionally substituted with 1-4 occurrences of JR; JU, JX, and JR are each 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′, or —NC(O)R′; or two JU, JX, or JR groups, on the same substituent or different substituents, together with the atom(s) to which each JU, JX, and JR group is bound, form a 5-7 membered saturated, unsaturated, or partially saturated ring; JQ is each independently selected from R″, —CH2R″, halogen, —CN, —NO2, —N(R′)R″, —CH2N(R′)R″, —OR″, —CH2OR″, —SR″, —CH2SR″, —COOR″, —NR′COR″, —NR′COCH2R″, —NR′CO(CH2)2R″, —NR′COOR″, —CON(R′)R″, —SO2N(R′)R″, —CONR′(CH2)2N(R′)R″, —CONR(CH2)3N(R′)R″, —CONR′(CH2)4N(R′)R″, —O(CH2)2OR″, O(CH2)3OR″, O(CH2)4OR″, —O(CH2)2N(R′)R″, —O(CH2)3N(R)R″, —O(CH2)4N(R′)R″, —NR′CH(CH2OR8)R″, —NR′CH(CH2CH2OR8)R″, —NR′CH(CH3)R″, NR′CH(CF3)R″, —NR′CH(CH3)C(O)OR″, —NR′CH(CF3)C(O)OR″, —NR′(CH2)R″, —NR′(CH2)2R″, —NR′(CH2)3R″, —NR′(CH2)4R″, —NR′(CH2)N(R′)R″, —NR′(CH2)2N(R′)R″, —NR′(CH2)3N(R′)R″, —NR′(CH2)4N(R)R″, —NR′(CH2)OR″, —NR′(CH2)2OR″, —NR′(CH2)3OR″, —NR′(CH2)4OR″, —NR′CH(CH2CH3)R″, —NR′CH2C(O)N(R′)R″, —NR′CH(CH3)C(O)N(R′)R″, NR′CH(CF3)C(O)N(R)R″, —NR′CH(CH2CH3)C(O)N(R′)R″, —NR′CH(CH(CH3)2)C(O)N(R′)R″, —NR′CH(C(CH3)3)C(O)N(R′)R″, —NR′CH(CH2CH(CH3)2)C(O)N(R′)R″, —NR′CH(CH2OR8)C(O)N(R′)R″ or —NR′CH(CH2CH2N(Me)2)C(O)N(R′)R″; R8 is H or C1-6 alkyl; R′ is 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; R″ is H, or is an optionally substituted group selected from C1-6 aliphatic, C3-10 cycloaliphatic, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 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 3-8 membered heterocyclyl; wherein each optionally substituted R″ group is independently and optionally substituted with 1-6 occurrences of JR; L is a C1-6 aliphatic wherein up to three methylene units are replaced by —NH—, —NR6—, —O—, —S—, —CO2—, —OC(O)—, —C(O)CO—, —C(O)—, —C(O)NH—, —C(O)NR6—, —C(═N—CN), —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 selected from C1-6 aliphatic, C3-10 cycloaliphatic, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocyclyl; or two R6 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; J is halogen, OCH3, OH, NO2, NH2, SCH3, NCH3, CN, unsubstituted C1-2aliphatic; two J's, together with the carbon to which they are attached, form a cyclopropyl ring or C═O; and m, n, d, and p are each independently 0 or 1. |