申请人:Wyeth
公开号:US06399593B1
公开(公告)日:2002-06-04
This invention concerns cyclic combination therapies using progestational agents and indoline derivatives which are progesterone receptor antagonists of the general structure:
wherein: A, B and D are N or CH, though not all can be CH; R1 and R2 are H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R1 and R2 form a spirocyclic ring; RA is H or optionally substituted alkyl aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH2, alkyl, alkenyl, or CORC; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 membered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception.
这项发明涉及使用孕激素受体拮抗剂和吲哚啉衍生物的循环组合疗法,其一般结构如下:其中:A、B和D为N或CH,但不是所有都可以是CH;R1和R2为H、CORA、NRBCORA,或者是选择性取代的烷基、烯基、炔基、环烷基或芳基;或者R1和R2形成螺环;RA为H或者是选择性取代的烷基芳基、烷氧基或氨基烷基;RB为H、烷基烷基;R3为H、OH、NH2、烷基、烯基或CORC;RC为H、烷基、芳基、烷氧基或氨基烷基;R4为苯或者是5或6元杂环芳环;RF为H、烷基、芳基、烷氧基或氨基烷基;RG为H或烷基;R5为H或烷基;W为O或者是化学键;或其药用盐。这些方法可用于避孕。