申请人:Synthelabo
公开号:US06063810A1
公开(公告)日:2000-05-16
Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.4 taken together form a C.sub.2-6 cycloalkyl or C.sub.3-6 cycloalkenyl ring, e.g., piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures;, as well as pharmaceutically acceptable acid addition salts thereof. The compounds may be used in therapy.
式(I)的化合物,其中A是氢原子或羟基;B是氢原子或C.sub.1-8烷基,C.sub.1-8烯基,C.sub.1-8氟烷基或C.sub.1-8全氟烷基基团;R.sub.1,R.sub.2和R.sub.5中的每一个,它们相同或不同,是氢原子,卤素如氯,溴或氟,C.sub.1-8烷基,C.sub.1-8烯基,C.sub.3-8环烷基,C.sub.3-8环烯基,C.sub.6,C.sub.10或C.sub.14芳基,C.sub.1-6烷氧羰基,C.sub.1-6羟基烷基,C.sub.1-6烷氧基烷基,C.sub.1-6烷氧基,C.sub.1-8氟烷基或C.sub.1-8全氟烷基基团,或R.sub.1和R.sub.2一起形成C.sub.3-8环烷基,C.sub.3-8环烯基或C.sub.6,C.sub.10或C.sub.14芳基环,但不包括R.sub.1和R.sub.2均为氢的化合物;R.sub.3和R.sub.4中的每一个,它们相同或不同,是氢原子或C.sub.1-8烷基,C.sub.1-8烯基,C.sub.3-8环烷基或C.sub.3-8环烯基基团,或R.sub.3和R.sub.4一起形成C.sub.2-6环烷基或C.sub.3-6环烯基环,例如哌啶基,氮杂环丙基或吡咯基;以对映体,非对映异构体或它们的混合物的形式存在,包括外加药用酸盐。这些化合物可用于治疗。