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CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES

机译:包含环状氨基甲酸酯和酰胺衍生物的避孕药成分

摘要

This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure:where A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. These methods of treatment may be used for contraception.
机译:本发明涉及与孕激素结合使用取代的二氢吲哚衍生物化合物的环状联合疗法和方案,所述的吲哚啉衍生物化合物是具有以下通式的孕激素受体的拮抗剂:其中A和B是选自S,CH或N的独立取代基;前提是当A为S时,B为CH或N;当B为S时,A为CH或N;并且A和B不能同时为CH;当A和B均等于N时,一个N可以任选地被C1-C6烷基取代; R 1和R 2是选自以下的独立取代基:H,C 1至C 6烷基,取代的C 1至C 6烷基,C 2至C 6烯基,取代的C 2至C 6烯基,C 2至C 6炔基,取代的C 2至C 6炔基,C 3至C 8环烷基,取代的C3至C8环烷基,芳基,取代的芳基,杂环,取代的杂环,CORA或NRBCORA;或R 1和R 2稠合形成任选取代的3至8元螺环烷基,烯基或杂环,该杂环含有1-3个选自O,S和N的杂原子;或或其药用盐。这些治疗方法可用于避孕。

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