Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
申请人:Bristol-Myers Squibb Company
公开号:US06472414B1
公开(公告)日:2002-10-29
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure
including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;
Rx is H, alkyl, aryl or halogen;
A is
(1) a bond;
(2) —O—; or
(3)
B is:
and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,
are as defined herein.
提供了新型化合物,其为MTP抑制剂,因此对降低血清脂质和治疗动脉粥样硬化及相关疾病有用,具有以下结构,包括其药学上可接受的盐或前药酯,其中q为0、1或2;Rx为H、烷基、芳基或卤素;A为(1)键;(2) —O—;或(3) B为:其中L2、L1、R1、R2、R3、R3′、R3a、R3b、R4、R4′、R5、X如本文所定义。