申请人:NIPPON SODA CO., LTD.
公开号:EP0757988A1
公开(公告)日:1997-02-12
The present invention is to provide novel imidazole derivatives effectual as an antihyperlipemic agent and therapeutic and preventive drugs for arteriosclerosis, and to provide methods for manufacturing the said derivatives.
More particularly, the present invention is directed to the compounds represented by the following general formula [I];
wherein R1 is hydrogen or lower alkyl, n is 0 or 1, X is N-r1 wherein r1 is hydrogen or lower alkyl, O, S, SO, SO2, CH2, CH(CH3), CONH or C(r2)=NO wherein r2 is hydrogen or lower alkyl, m is 0 or an integer of from 1 to 12, and A is methyl or a group represented by the following general formula;
wherein Y is N-r3 wherein r3 is hydrogen or lower alkyl, N(r4)SO2 wherein r4 is hydrogen or lower alkyl, O, S, SO, SO2, CH2, CH(CH3), CONH or C(r5)=NO wherein r5 is hydrogen or lower alkyl, R2 is a halogen, a lower alkyl, a lower alkoxy, a cycloalkyl or COOr6 wherein r6 is hydrogen or a lower alkyl, and l is 0, 1, 2 or 3, however, m denotes an integer of from 6 to 9 when A is methyl, or m denotes 0 or an integer of from 1 to 6 when A is a group represented by the following general formula;
and X and Y are each independently CH2 when m is 0, the pharmaceutically-acceptable salts thereof and methods for manufacturing the said compounds and the pharmaceutically-acceptable salts thereof.
本发明旨在提供新型咪唑衍生物,作为抗高血脂药以及治疗和预防动脉硬化的药物,并提供制造上述衍生物的方法。
更具体地说,本发明涉及由以下通式[I]代表的化合物;
其中 R1 是氢或低级烷基,n 是 0 或 1,X 是 N-r1(其中 r1 是氢或低级烷基)、O、S、SO、SO2、CH2、CH(CH3)、CONH 或 C(r2)=NO(其中 r2 是氢或低级烷基),m 是 0 或 1 至 12 的整数,A 是甲基或下式通式所代表的基团;
其中 Y 是 N-r3(其中 r3 是氢或低级烷基)、N(r4)SO2(其中 r4 是氢或低级烷基)、O、S、SO、SO2、CH2、CH(CH3)、CONH 或 C(r5)=NO(其中 r5 是氢或低级烷基)、R2 是卤素、低级烷基、低级烷氧基、环烷基或 CO2、R2是卤素、低级烷基、低级烷氧基、环烷基或 COOr6,其中 r6 是氢或低级烷基,l 是 0、1、2 或 3,但当 A 是甲基时,m 表示 6 至 9 的整数,当 A 是下式通式所代表的基团时,m 表示 0 或 1 至 6 的整数;
当 m 为 0 时,X 和 Y 各自独立地为 CH2、其药学上可接受的盐类以及制造上述化合物及其药学上可接受的盐类的方法。