| 主权项 |
1. A compound having the formula (I) or a stereochemically isomeric form thereof, wherein the bond drawn into the ring indicates that the bond may be attached to any carbon ring atom; R1 is selected from the group consisting of hydrogen; C1-6alkyl; (C1-3alkyloxy)-C1-3alkyl; [(C1-3alkyloxy)-C1-3alkyloxy]C1-3alkyl; C1-3alkyl substituted with one or more independently selected halo substituents; unsubstituted benzyl; benzyl substituted with one or more substituents each independently selected from the group consisting of halo, C1-3alkyl, (C1-3alkyloxy)C1-3alkyl, C1-3alkyloxy, hydroxyC1-3alkyl, cyano, hydroxyl, amino, (C═O)R′, (C═O)OR′, (C═O)NR′R″, mono- or di-(C1-3alkyl)amino, morpholinyl, (C3-7cycloalkyl)C1-3alkyloxy, trifluoromethyl and trifluoromethoxy, wherein R′ and R″ are independently selected from hydrogen and C1-6alkyl; (benzyloxy)C1-3alkyl; unsubstituted C3-7cycloalkyl; C3-7cycloalkyl substituted with one or more independently selected C1-3alkyl substituted with one or more independently selected halo substituents; (C3-7cycloalkyl)C1-3alkyl; 4-(2,3,4,5-tetrahydro-benzo[f][1,4]oxazepine)methyl; Het1; Het1C1-3alkyl; Het2; and Het2C1-3alkyl; R2 is selected from the group consisting of cyano; halo; C1-3alkyl substituted with one or more independently selected halo substituents; C1-3alkyloxy substituted with one or more independently selected halo substituents; C1-3alkyl; C3-7cycloalkyl; and (C3-7cycloalkyl)C1-3alkyl; forms a radical selected from (a), (b), (c), (d) and (e): wherein the bond drawn into (a) indicates that R4 may be attached to any of carbon ring atoms 2 and 3; each R3 is independently selected from the group consisting of hydrogen; unsubstituted C1-6alkyl; C1-6alkyl substituted with one or more substituents independently selected from the group consisting of halo, hydroxy, C1-3alkoxy and trifluoromethyl; unsubstituted C3-7cycloalkyl; C3-7cycloalkyl substituted with one or more substituents independently selected from the group consisting of halo, C1-3alkyl, hydroxy, C1-3alkoxy and trifluoromethyl; C3-7cycloalkylC1-3alkyl; unsubstituted phenyl; phenyl substituted with one or more substituents independently selected from the group consisting of halo, C1-3alkyl, C1-3alkoxy and trifluoromethyl; Het3; and Het3C1-3alkyl; or each R3 is independently selected from a cyclic radical of formula (f) wherein R8 is selected from hydrogen, C1-3alkyl, C1-3alkyloxy and hydroxyC1-3alkyl; q is 1 or 2; X is selected from O, CH2 and CR9(OH), wherein R9 is selected from hydrogen, C1-3alkyl and C3-7cycloalkyl; or X is a cyclic radical of formula (g) wherein r and s are independently selected from 0, 1 and 2, provided that r+s≧2; each R4, R6 and R7 are each independently selected from C1-3alkyl and C1-3alkyl substituted with one or more independently selected halo substituents; each R5 is independently selected from the group consisting of hydrogen, C1-3alkyl, and C1-3alkyl substituted with one or more independently selected halo substituents; n, m and p are each independently selected from 0, 1 and 2; v is 0 or 1; t and u are each independently selected from 1 and 2; W is selected from N and C10; wherein R10 is selected from hydrogen, halo and trifluoromethyl; each Het1 is a saturated heterocyclic radical selected from pyrrolidinyl; piperidinyl; piperazinyl; and morpholinyl; each of which may be optionally substituted with one or more each independently selected from the group consisting of C1-6alkyl; mono-, di- and tri-haloC1-3alkyl; unsubstituted phenyl; and phenyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, trifluoromethyl, and trifluoromethoxy; each Het2 is pyridyl or pyrimidinyl; and each Het3 is a heterocycle selected from the group consisting of tetrahydropyran, pyridyl; and pyrimidinyl; each of them being optionally substituted with one or more substituents each independently selected from the group consisting of halo, C1-3alkyl, C1-3alkoxy and trifluoromethyl; and halo is selected from fluoro, chloro, bromo and iodo; or a pharmaceutically acceptable salt thereof. |
