| 主权项 |
1. A compound of Formulae I, II, III, IV, V, VI or VII: or a pharmaceutically acceptable salt, pharmaceutically active metabolite, pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate thereof, wherein, Y is hydrogen, halo, cyano, (C1-C3)alkyl, (C1-C3) hydroxyalkyl, (C1-C5)alkenyl, (C1-C3)haloalkyl, (C1-C3) hydroxyhaloalkyl, (C3-C6)cycloalkyl, (C1-C3)alkoxy or (C1-C3)haloalkoxy; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)hydroxyalkyl or (C1-C6)haloalkyl; X is R2 is (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, aryl or heteroaryl, optionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, hydroxyl, —OR, (C1-C4)hydroxyalkyl, (C1-C4)hydroxyalkoxy, (C1-C4)hydroxyalkoxy(C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)haloalkoxy, —NR2, (R2N)(C1-C4)alkyl-, (C1-C4)alkylthio, (C1-C4)haloalkylthio, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)NR2, —N(R)C(═O)R, —CH2C(═O)R, —CH2C(═O)OR, —CH2OC(═O)R, —CH2C(═O)NR2, —CH2N(R)C(═O)R, —S(═O)2R, —S(═O)2NR2, —N(R)S(═O)2R, -A and —CH2A; R is independently selected for each occurrence from the group consisting of hydrogen, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, (C1-C4)hydroxyalkyl, (C3-C8)cycloalkyl or (C3-C8)heterocycloalkyl; or where a nitrogen is substituted with two R groups they may be taken together with the nitrogen atom to which they are attached to form a 4-, 5-, 6- or 7-membered saturated (C3-C8)heterocycloalkyl which, when so formed, may be optionally substituted with one, two or three substituents independently selected from the group consisting of (C1-C4)alkyl, halo, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)cyanoalkyl, (C1-C4)haloalkyl and ═O; A is independently selected for each occurrence from the group consisting of (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, aryl and heteroaryl, optionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)haloalkoxy, —NR2, (R2N)(C1-C4)alkyl-, (C1-C4)alkylthio, (C1-C4)haloalkylthio, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)NR2, —N(R)C(═O)R, —CH2C(═O)R, —CH2C(═O)OR, —CH2OC(═O)R, —CH2C(═O)NR2, —CH2N(R)C(═O)R, —S(═O)2R, —S(═O)2NR2 and —N(R)S(═O)2R; W isoptionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, (C1-C6)alkyl, (C1-C6)hydroxyalkyl and (C1-C6)haloalkyl;
R3 is (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, aryl, heteroaryl, —C(═O)R4, —C(═O)OR4, —C(═O)N(R5)2 or —S(═O)2R4, optionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)haloalkoxy, —NR2, (R2N)(C1-C4)alkyl-, (C1-C4)alkylthio, (C1-C4)haloalkylthio, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)NR2, —N(R)C(═O)R, —CH2C(═O)R, —CH2C(═O)OR, —CH2OC(═O)R, —CH2C(═O)NR2, —CH2N(R)C(═O)R, —S(═O)2R, —S(═O)2NR2, —N(R)S(═O)2R, -A and —CH2A; R4 is hydrogen, (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, (C3-C8)cycloalkyl(C1-C6)alkyl, (C3-C8)heterocycloalkyl(C1-C6)alkyl, aryl or heteroaryl, optionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)haloalkoxy, —NR2, (R2N)(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)haloalkylthio, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)NR2, —N(R)C(═O)R, —CH2C(═O)R, —CH2C(═O)OR, —CH2OC(═O)R, —CH2C(═O)NR2, —CH2N(R)C(═O)R, —S(═O)2R, —S(═O)2NR2, —N(R)S(═O)2R, -A and —CH2A; and R5 is independently selected for each occurrence from the group consisting of hydrogen, (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, (C3-C8)cycloalkyl(C1-C6)alkyl, (C3-C8)heterocycloalkyl(C1-C6)alkyl, aryl and heteroaryl, optionally substituted with one, two, three, four or five substitutents independently selected for each occurrence from the group consisting of halo, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)cyanoalkyl, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)haloalkoxy, —NR2, (R2N)(C1-C4)alkyl-, (C1-C4)alkylthio, (C1-C4)haloalkylthio, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)NR2, —N(R)C(═O)R, —CH2C(═O)R, —CH2C(═O)OR, —CH2OC(═O)R, —CH2C(═O)NR2, —CH2N(R)C(═O)R, —S(═O)2R, —S(═O)2NR2, —N(R)S(═O)2R, -A and —CH2A; or where a nitrogen is substituted with two R5 groups may be taken together with the nitrogen atom to which they are attached to form a 4-, 5-, 6- or 7-membered saturated C3-8heterocycloalkyl which, when so formed, may be optionally substituted with one, two or three substituents independently selected from the group consisting of (C1-C4)alkyl, halo, hydroxyl, (C1-C4)hydroxyalkyl, (C1-C4)haloalkyl and ═O. |
