首页> 外国专利> ISOMER OF PROSTAGLANDIN-MIMIC COMPOUND HAVING SPECIFIC STERIC CONFIGURATION, AND REMEDY CONTAINING SAID ISOMER AS ACTIVE COMPONENT

ISOMER OF PROSTAGLANDIN-MIMIC COMPOUND HAVING SPECIFIC STERIC CONFIGURATION, AND REMEDY CONTAINING SAID ISOMER AS ACTIVE COMPONENT

机译:具有特定位构型的前列腺素-模拟化合物的异构体,并且包含相同成分的有效成分的补救措施

摘要

PURPOSE:To provide a remedy having strong pharmacological effect (especially hypotensive and blood platelet coagulation inhibiting action, and containing an isomer of a prostaglandin-mimic compound having a specific steric configuration. CONSTITUTION:The objective remedy contains, as an active component, the compound of formula I [A is group of formula II-V (X is cis-vinylene or ethylene; Y is ethylene or trans-vinylene; R1 is H or 1-4C straight- or branched-chain alkyl), etc.; B is group of formula VI-X (R2 is 1-8C straight- or branched- chain alkyl), etc.; n is 0, 1 or 2], its salt, or their cyclodextrin clathrate compound, e.g. 15-[(1S,3R)-3-propylcyclopentyl]-16,17,18,19,20-pentanol-PGF2alpha. It has been found that the SR-isomer, SS-isomer and cis-isomer have stronger pharmacological activity than the other isomers in the PG-mimic compound wherein the 15-position and thereafter are substituted with alkyl-substituted cycloalkyl groups.
机译:目的:提供一种具有强药理作用的药物(特别是降压和抑制血小板凝结作用,并包含具有特定空间构型的前列腺素模拟化合物的异构体)。组成:目标药物包含该化合物作为活性成分式I的化合物[A是式II-V的基团(X是顺式亚乙烯基或亚乙基; Y是亚乙基或反亚乙烯基; R 1是H或1-4C直链或支链烷基),等等。 ; B为式VI-X的基团(R 2为1-8C直链或支链烷基),等等; n为0、1或2],其盐或它们的环糊精包合物,例如15 -[((1S,3R)-3-丙基环戊基] -16,17,18,19,20-戊醇-PGF2α。已发现SR-异构体,SS-异构体和顺式异构体的药理活性高于PG-模拟化合物中的其他异构体,其中15位及之后的位置被烷基取代的环烷基取代。

著录项

  • 公开/公告号YU45985B

    专利类型

  • 公开/公告日1992-12-21

    原文格式PDF

  • 申请/专利权人 ONO PHARMACEUTICALCO. LTD.;

    申请/专利号YU19850001201

  • 发明设计人 IMAKI K.;MIYAKE H.;OKEGAWA T.;

    申请日1985-07-22

  • 分类号C07C177/00;A61K31/40;A61K31/557;C07D207/18;

  • 国家 YU

  • 入库时间 2022-08-22 05:10:21

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