3,5-Dihydroxy-6,8-nonadienoic acids and derivatives as hypocholesterolemic agents
申请人:PFIZER INC.
公开号:EP0312269A2
公开(公告)日:1989-04-19
A compound for use in lowering blood cholesterol having the relative stereochemical formula:-
wherein R is hydrogen, (C₁-C₃)alkyl, phenyl, benzyl or a conventional radical forming an ester group which is hydrolyzable under physiological conditions;
R¹ and R², when taken separately, and R₃ are each independently hydrogen, (C₁-C₃)alkyl, benzyl, naphthyl, phenyl or phenyl mono or disubstituted with the same or different substituents selected from the group consisting of F, Cl, Br, I, (C₁-C₃)alkyl, CF₃, (C₁-C₃)alkoxy, benzyl and phenyl; with the proviso that at least one of R¹ and R² is other than hydrogen or (C₁-C₃)alkyl; and
R¹ and R², when taken together, are combined with the double bonded carbon atom which they are attached to form a diradical ylidene group of the formula
wherein n is 0 or 1 and Y is oxygen, OCH₂, sulfur, SCH₂, methylene or ethylene; or
a pharmaceutically acceptable cationic salt thereof when R is hydrogen.
一种用于降低血液胆固醇的化合物,其相对立体化学式为
其中 R 是氢、(C₁-C₃)烷基、苯基、苄基或形成在生理条件下可水解的酯基的常规基团;
R¹和 R² 分别独立地为氢、(C₁-C₃)烷基、苄基、萘基、苯基或苯基单胞、苯基或被选自 F、Cl、Br、I、(C₁-C₃)烷基、CF₃、(C₁-C₃)烷氧基、苄基和苯基的相同或不同取代基单取代或二取代的苯基;但 R¹ 和 R² 中至少有一个不是氢或 (C₁-C₃)烷基;以及
当 R¹ 和 R² 结合在一起时,与它们所连接的双键碳原子结合形成式中的二叉亚 乙基
其中 n 为 0 或 1,Y 为氧、OCH₂、硫、SCH₂、亚甲基或亚乙基;或
当 R 为氢时,其药学上可接受的阳离子盐。