申请人:Daiichi Sankyo Company, Limited
公开号:EP2119719A1
公开(公告)日:2009-11-18
The present invention relates to a thiazepine derivative or a pharmacologically acceptable salt thereof having an excellent effect of inhibiting 11β-hydroxysteroid dehydrogenase type 1. A thiazepine derivative or a pharmacologically acceptable salt thereof having general formula (I):
wherein
R1 represents a hydrogen atom, a C1-C6 alkyl group or the like; R2 represents a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 hydroxyalkyl group, or the like; R3 represents a hydrogen atom or a C1-C6 alkyl group; R4 represents a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group a or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group a; Substituent Group a consists of a halogen atom, a C1-C6 alkyl group, a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group b, and so forth; Substituent Group b consists of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, and so forth.
本发明涉及一种噻吩啶衍生物或其药理学上可接受的盐,具有优异的抑制11β-羟基类固醇脱氢酶1型的作用。具有通式(I)的噻吩啶衍生物或其药理学上可接受的盐:
其中
R1代表氢原子、C1-C6烷基或类似物;R2代表C1-C6烷基、C1-C6卤代烷基、C1-C6羟基烷基或类似物;R3代表氢原子或C1-C6烷基;R4代表可能被1至5个独立选择自取代基团a的基团取代的C6-C10芳基,或可能被1至3个独立选择自取代基团a的基团取代的杂环基团;取代基团a由卤原子、C1-C6烷基、可能被1至5个独立选择自取代基团b的基团取代的C6-C10芳基等组成;取代基团b由卤原子、C1-C6烷基、C1-C6卤代烷基等组成。