首页> 外国专利> New derivatives of amino - 16 - 18, 19, 20 - trinor - prostaglandin and their addition salts, acids, for their preparation and medicinal products containing them,

New derivatives of amino - 16 - 18, 19, 20 - trinor - prostaglandin and their addition salts, acids, for their preparation and medicinal products containing them,

机译:氨基的新衍生物-16-18、19、20-trinor-前列腺素及其加成盐,酸,用于制备以及含有它们的药用产品,

摘要

The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9 alpha ,11 alpha ,15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-17-phenyl-5-cis,13-tra ns-18,19,20-trinor-prostadienoic acid derivative of general formula XII-wherein C-15 and C-16 may have either S or R configuration, W is as defined above, and Y stands for a lower alkyl group-in an optional sequence with the limitation that in those compounds of general formula I where W is as defined above and Y stands for a lower alkyl group, solely the p-nitrobenzyloxycarbonyl group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt. The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied in cattle raising for estrus and birth synchronization, furthermore in the veterinary praxis for the treatment of sterility, chronic endometritis and pyometry.
机译:本发明涉及通式I的新的16-氨基-18,19,20-trinor-前列腺素衍生物,在C-17具有取代或未取代的苯基,其中C-15和C-16可以具有S或R式中,Y代表氢原子或低级烷基,W代表氢原子,卤原子,羟基,低级烷基或烷氧基及其酸加成盐。这些化合物可以通过除去9α,11α,15-三羟基-16-对硝基苄氧基羰基酰胺基17-苯基-5-顺,13-tra ns-18的酯基和对硝基苄氧基羰基保护基来制备。通式XII的19,20-trinor-炔诺酮酸衍生物-其中C-15和C-16可具有S或R构型,W如上定义,Y代表低级烷基-局限性在于在其中W如上定义且Y代表低级烷基的那些通式I的化合物中,仅去除了对硝基苄氧基羰基,并且通式I的所得产物任选地被有机或无机转化。酸成盐。本发明的新的前列腺素衍生物具有有价值的治疗特性,可用于牛的发情和出生同步,此外还可用于兽医,以治疗不育症,慢性子宫内膜炎和脓毒症。

著录项

  • 公开/公告号FR2495611B1

    专利类型

  • 公开/公告日1983-12-09

    原文格式PDF

  • 申请/专利权人 GYOGYSZERKUTATO INTEZET;

    申请/专利号FR19810022904

  • 发明设计人

    申请日1981-12-08

  • 分类号C07C177/00;A61K31/557;

  • 国家 FR

  • 入库时间 2022-08-22 08:45:45

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