公开(公告)号：US5219874A

公开(公告)日：1993-06-15

申请号：US763304

申请日：1991-09-20

申请人： Alan W. Faull ,  Keith Russell ,  Williams J. Watkins

发明人： Alan W. Faull ,  Keith Russell ,  Williams J. Watkins

IPC分类号： A61K31/415 ,  A61K31/425 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D263/26 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04

CPC分类号： C07D403/04 ,  C07D263/26 ,  C07D417/04

摘要： The invention concerns novel 1,3-dioxane alkenoic acid derivatives of the formula I ##STR1## wherein: n is the integer 1 or 2;Y is methyleneoxy, vinylene or ethylene;A.sup.1 is (1-6C)alkylene;R.sup.1 is a group of the formula R.sup.2.A.sup.2 --, in which:R.sup.2 is phenyl unsubstituted or bearing up to three substituents which are independently selected from (1-6C)alkyl, (1-6C)alkoxy, (2-6C)alkanoyl, (1-6C)alkylthio, (1-6C)alkylsulphonyl, halogeno, trifluoromethyl, nitro and cyano;A.sup.2 is a direct bond to R.sup.2 or a group of the formula --W--C(R.sup.4)(R.sup.5)-- wherein W is oxygen, methylene or a direct bond to R.sup.2, and R.sup.4 and R.sup.5 are independently (1-4C)alkyl;Q is a heterocyclyl group selected from thiazol-5-yl and imidazol-5-yl, the latter being unsubstituted or bearing a (1-12C)alkyl group at the 1-position of the imidazole ring; andR.sup.3 is hydroxy, a physiologically acceptable alcohol residue, or (1-4C)alkanesulphonamido;or a pharmaceutically acceptable salt thereof. The compounds are thromboxane A.sub.2 antagonists and inhibitors of thromboxane A.sub.2 synthase.

摘要翻译： 本发明涉及式I的新型1,3-二恶烷烯酸衍生物，其中：n是整数1或2; Y是亚甲氧基，亚乙烯基或亚乙基; A1为（1-6C）亚烷基; R1是式R2.A2-的基团，其中：R2是未取代的或最多带有三个独立地选自（1-6C）烷基，（1-6C）烷氧基，（2-6C）烷酰基的取代基的苯基 ，（1-6C）烷硫基，（1-6C）烷基磺酰基，卤代，三氟甲基，硝基和氰基; A2是与R2或式-W-C（R4）（R5） - 的基团的直接键合，其中W是氧，亚甲基或与R2的直接键合，R4和R5独立地是（1-4C）烷基; Q是选自噻唑-5-基和咪唑-5-基的杂环基，后者是未取代的或在咪唑环的1位带有（1-12C）烷基; 和R3是羟基，生理上可接受的醇残基或（1-4C）烷基磺酰胺基; 或其药学上可接受的盐。 化合物是凝血恶烷A2拮抗剂和血栓烷A2合酶抑制剂。