申请人:G.D. Searle & Co.
公开号:EP0195379A2
公开(公告)日:1986-09-24
The present invention describes allenic prostacyclin derivatives of the formula:
wherein:
n is 0, 1, 2
R1 is hydrogen or lower alkyl;
R2 is hydrogen, lower alkyl, cycloalkyl, hetereoalkyl, halogen, aryl, alkylthio, arylthio, alkylsulfinyl, arylsulfinyl or trifluoromethyl;
R3 is a lower alkyl, a cycloalkyl, a cycloheteroalkyl, a lower alkyl having one or more fluorines or containing 1 or 2 unsaturated bonds;
carbon 15 may be in the R or the S configuration, or a mixture of R and S.
These compounds are useful for the treatment of platelet dysfunction, atherosclerosis, allergic disorders, gastric ulcers, hypertension and tumor cell metastasis. Also disclosed is the process for preparing them and the appropriate intermediates.
本发明描述了式中的异烯前列环素衍生物:
其中
n 是 0、1、2
R1 是氢或低级烷基
R2 是氢、低级烷基、环烷基、正烷基、卤素、芳基、烷硫基、芳硫基、烷基亚磺酰基、芳基亚磺酰基或三氟甲基;
R3 是低级烷基、环烷基、环杂烷基、具有一个或多个氟的低级烷基或含有 1 或 2 个不饱和键的低级烷基;
碳 15 可以是 R 或 S 构型,也可以是 R 和 S 的混合物。
这些化合物可用于治疗血小板功能障碍、动脉粥样硬化、过敏性疾病、胃溃疡、高血压和肿瘤细胞转移。同时公开的还有制备它们的工艺和适当的中间体。