申请人:The Wellcome Foundation Limited
公开号:US05098929A1
公开(公告)日:1992-03-24
A compound of the formula (I): ##STR1## wherein R is C.sub.2-10 alkyl, alkenyl or alkynyl, each optionally subsituted by or methyl substituted by cyano, C.sub.3-4 cycloalkyl, halo, C.sub.1-4 alkoxy or a group S(O)mR.sup.4 where R.sup.4 is C.sub.1-4 alkyl and m is O, 1 or 2, or R is C.sub.3-10 cycloalkyl, C.sub.4-10 cycloalkenyl or phenyl, each optionally substituted by C.sub.1-4 alkoxy, C.sub.1-3 alkyl, C.sub.2-4 alkynyl, halo, cyano or a group S(O)mR.sup.4 as defined hereinbefore; R.sup.1 is halo, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each optionally substituted by halo, cyano, C.sub.1-4 alkoxy, alkyl carbalkoxy containing up to 6 carbon atoms, a group S(O)mR.sup.4 as defined hereinbefore or alkynyl substituted by tri-C.sub.1-4 alkylsilyl, or R.sup.1 is cyano, spiro-cyclopropyl, gem dimethyl, oxo or methylene optionally substituted by cyano or C.sub.1-3 alkyl optionally substituted by fluorine, or R.sup.1 and R and the carbon atoms to which they are attached form a C.sub.5-7 carbocyclic ring optionally substituted by halo, C.sub.1-3 alkyl or alkoxy or C.sub. 2-3 alkenyl, R.sup.2 is phenyl, C.sub.5-10 cycloalkyl or cycloalkenyl each optionally substituted other than phenyl substituted by C.sub.2-3 alkynyl and R.sup.3 is hydrogen, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each optionally substituted by cyano, C.sub.1-4 alkylthio, C.sub.1-4 alkoxy or halo, or R.sup.3 is cyano, its use in medicine, pharmaceutical compositions containing it and processes for its preparation.
化合物的化学式(I):##STR1## 其中R是C.sub.2-10烷基,烯基或炔基,每个都可以被氰基,C.sub.3-4环烷基,卤素,C.sub.1-4烷氧基或S(O)mR.sup.4基团取代,其中R.sup.4是C.sub.1-4烷基,m为O,1或2,或者R是C.sub.3-10环烷基,C.sub.4-10环烯基或苯基,每个都可以被C.sub.1-4烷氧基,C.sub.1-3烷基,C.sub.2-4炔基,卤素,氰基或如上所定义的S(O)mR.sup.4基团取代; R.sup.1是卤素,C.sub.1-3烷基,C.sub.2-3烯基或炔基,每个都可以被卤素,氰基,C.sub.1-4烷氧基,含有最多6个碳原子的烷基羰基烷氧基,如上所定义的S(O)mR.sup.4基团或炔基取代的三C.sub.1-4烷基硅基,或R.sup.1是氰基,螺环丙基,双甲基,氧代或亚甲基,可选择地被氰基或C.sub.1-3烷基取代,可选择地被氟取代,或R.sup.1和R及其附着的碳原子形成一个C.sub.5-7碳环,可选择地被卤素,C.sub.1-3烷基或烷氧基或C.sub.2-3烯基取代,R.sup.2是苯基,C.sub.5-10环烷基或环烯基,每个都可以选择性地被取代,除苯基外还被C.sub.2-3炔基取代,R.sup.3是氢,C.sub.1-3烷基,C.sub.2-3烯基或炔基,每个都可以选择性地被氰基,C.sub.1-4烷基硫基,C.sub.1-4烷氧基或卤素取代,或R.sup.3是氰基,它在医药中的应用,含有它的制药组合物以及制备它的方法。