申请人:SmithKline Beecham p.l.c.
公开号:US06358974B1
公开(公告)日:2002-03-19
Compounds of formula (I) wherein: R1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-4alkyl, C1-4alkoxy, arylC1-4alkoxy, C1-4alkylthio, C1-4alkoxyC1-4alkyl, C3-6cycloalkylC1-4alkoxy, C1-4alkanoyl, C1-4alkoxycarbonyl, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, C1-4alkylsulfonylC1-4alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-4alkyl, C1-4alkylsulfonamido, C1-4alkylamido, C1-4alkylsulfonamidoC1-4alkyl, C1-4alkylamidoC1-4alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-4alkyl, arylcarboxamidoC1-4alkyl, aroyl, aroylC1-4alkyl, or arylC1-4alkanoyl group; a group R5OCO(CH2)p, R5(CON(R6)(CH2)p, R5R6NCO(CH2)p or R5R6NSO2(CH2)p where each of R5 and R6 independently represents a hydrogen atom or a C1-4alkyl group or R5R6 forms part of a C3-6azacycloalkane or C3-6(2-oxo)azacycloalkane ring and p represents zero or an integer from 1 to 4; or a group Ar3—Z, wherein Ar3 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring and Z representsa bond, O, S, or Ch2; R2 represents a hydrogen atom or a C1-4alkyl group; R3 and R4 each independently represent a C1-4alkyl group, q is 1 or 2; A represents a group of the formula (a), (b), (c), or (d).
式(I)的化合物,其中:R1代表从中选择的取代基:氢或卤原子;羟基、氰基、硝基、三氟甲基、三氟甲氧基、三氟甲磺酰氧基、五氟乙基、C1-4烷基、C1-4烷氧基、芳基C1-4烷氧基、C1-4烷硫基、C1-4烷氧基C1-4烷基、C3-6环烷基C1-4烷氧基、C1-4烷酰基、C1-4烷氧羰基、C1-4烷基磺基、C1-4烷基磺酰氧基、C1-4烷基磺基C1-4烷基、芳基磺基、芳基磺酰氧基、芳基磺基C1-4烷基、C1-4烷基磺胺基、C1-4烷基酰胺基、C1-4烷基磺胺基C1-4烷基、C1-4烷基酰胺基C1-4烷基、芳基磺胺基、芳基羧酰胺基、芳基磺胺基C1-4烷基、芳基羧酰胺基C1-4烷基、芳酰基、芳酰基C1-4烷基或芳基C1-4烷酰基;R5OCO(CH2)p、R5(CON(R6)(CH2)p、R5R6NCO(CH2)p或R5R6NSO2(CH2)p中的一种,其中R5和R6各自独立地代表氢原子或C1-4烷基或R5R6形成C3-6氮杂环烷或C3-6(2-氧代)氮杂环烷环的一部分,p代表零或1到4之间的整数;或Ar3—Z中的一种,其中Ar3代表可选择的取代苯环或可选择的取代的5-或6-成员芳香杂环环,Z代表键,O,S或Ch2;R2代表氢原子或C1-4烷基;R3和R4各自独立地代表C1-4烷基,q为1或2;A代表式(a)、(b)、(c)或(d)的基团。