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17-branched alkynyl- and 20-oxopregna-derivatives of vitamin D, their preparation and their pharmaceutical compositions

机译:维生素D的17支链炔基和20-氧杂环戊烷衍生物,其制备方法和药物组合物

摘要

The 1-hydroxypregcarceropyrrole derivatives of formula (I) and their corresponding 5,6-trans adducts exhibit anti-progesterone activity and are useful as anti-neoplastic, antifibrotic, antiproliferative, immunosuppressive and / or anti-inflammatory agents . Wherein R 1 is a hydroxyl group or a lower alkoxy group and R 2 is an optionally hydroxylated or lower alkoxylated lower alkynyl or R 1 is -C (R A ) (R B ) CH 3 wherein R A is optionally hydroxylated or lower alkoxylated lower alkynyl group and R B is a hydroxyl group or a lower alkoxy group, or R a and R B represents an a-oxo together, R 2 is hydrogen, hydroxyl or lower alkoxy, And R 3 and R 4 are each a hydrogen atom.
机译:式(I)的1-羟基precarcarceropyrrole衍生物及其相应的5,6-反式加合物表现出抗孕酮活性,并且可用作抗肿瘤剂,抗纤维化剂,抗增殖剂,免疫抑制剂和/或抗炎剂。其中R 1 是羟基或低级烷氧基,R 2 是任选地羟基化或低级烷氧基化的低级炔基,或R 1 为- C(R A )(R B )CH 3其中, R A 可选地为羟基化或低级烷氧基化的低级炔基基,R B 为羟基或低级烷氧基,或R a 和R B 一起表示α-氧代,R < Sup> 2 是氢,羟基或低级烷氧基,R 3 和R 4 分别是氢原子。

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