QUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, PREPARATION METHODS AND USES THEREOF
申请人:Shanghai Institute of Pharmaceutical Industry
公开号:EP2284158A1
公开(公告)日:2011-02-16
The present invention discloses a quinoline compound represented by the formula A or pharmaceutically acceptable solvate, optical isomer or polymorph thereof,
wherein X is S or O; M is H, Na+, NH4+ or Ca2+; each of R1, R2 and R3 is independently H, halogen, the group represented by formula D or formula E; R is H, halogen, C1∼C4 alkyl or C1∼C4 alkoxy.
The present invention also discloses its pharmaceutical composition and the preparation method thereof and application in manufacturing a medicament for inhibiting HMG-CoA reductase or for the treatment and prophylaxis of the diseases which can be treated effectively by inhibiting HMG-CoA reductase. The quinloline compound and pharmaceutical composition thereof of the present invention have an excellent lipid reduction effect in vivo and can be applied for treatment of a hyperlipidemia-related disease.
本发明公开了一种由式 A 或其药学上可接受的溶解物、光学异构体或多晶型代表的喹啉化合物、
其中 X 是 S 或 O;M 是 H、Na+、NH4+ 或 Ca2+;R1、R2 和 R3 各自独立地是 H、卤素、式 D 或式 E 所代表的基团;R 是 H、卤素、C1∼C4 烷基或 C1∼C4 烷氧基。
本发明还公开了其药物组合物及其制备方法,以及在制造抑制 HMG-CoA 还原酶的药物或治疗和预防通过抑制 HMG-CoA 还原酶可有效治疗的疾病中的应用。本发明的喹啉化合物及其药物组合物在体内具有良好的降脂效果,可用于治疗高脂血症相关疾病。