申请人:Nippon Soda Co., Ltd.
公开号:US05965743A1
公开(公告)日:1999-10-12
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]; ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, n is 0 or 1, X is N-r.sup.1 wherein r.sup.1 is hydrogen or lower alkyl, O, S, SO, SO.sub.2, CH.sub.2, CH(CH.sub.3), CONH or C(r.sup.2).dbd.NO wherein r.sup.2 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; ##STR2## wherein Y is N-r.sup.3 wherein r.sup.3 is hydrogen or lower alkyl, N(r.sup.4)SO.sub.2 wherein r.sup.4 is hydrogen or lower alkyl, O, S, SO, SO.sub.2, CH.sub.2, CH(CH.sub.3), CONH or C(r.sup.5).dbd.NO wherein r.sup.5 is hydrogen or lower alkyl, R.sup.2 is a halogen, a lower alkyl, a lower alkoxy, a cycloalkyl or COOr.sup.6 wherein r.sup.6 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; ##STR3## and X and Y are each independently CH.sub.2 when m is 0, the pharmaceutically-acceptable salts thereof and methods for manufacturing the said compounds and the pharmaceutically-acceptable salts thereof.
本发明提供了新型咪唑衍生物,作为降脂药和动脉硬化的治疗和预防药物,并提供了制造该衍生物的方法。更具体地,本发明涉及以下通式[I]所表示的化合物:
其中,R1为氢或低碳基,n为0或1,X为N-r1,其中r1为氢或低碳基,O,S,SO,SO2,CH2,CH(CH3),CONH或C(r2)=NO,其中r2为氢或低碳基,m为0或1到12的整数,A为甲基或由以下通式表示的基团:
其中,Y为N-r3,其中r3为氢或低碳基,N(r4)SO2,其中r4为氢或低碳基,O,S,SO,SO2,CH2,CH(CH3),CONH或C(r5)=NO,其中r5为氢或低碳基,R2为卤素,低碳基,低碳氧基,环烷基或COOr6,其中r6为氢或低碳基,l为0、1、2或3,但当A为甲基时,m为6到9的整数,或当A为以下通式所表示的基团时,m为0或1到6的整数:
其中,当m为0时,X和Y各自独立地为CH2,其药学上可接受的盐以及制造该化合物及其药学上可接受的盐的方法。