Contraceptive compositions containing indoline derivatives...

A - Human Necessities – 61 – K

Patent

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A61K 45/06 (2006.01) A61K 31/40 (2006.01) A61K 31/535 (2006.01) A61K 31/56 (2006.01) A61K 31/565 (2006.01) A61K 31/57 (2006.01) A61P 15/18 (2006.01)

Patent

CA 2372595

This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1), wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.

L'invention concerne des thérapies et des traitements cycliques combinés utilisant des composés de dérivés d'indoline substitués qui constituent des antagonistes du récepteur de la progestérone, et sont représentés par la structure générale (1). Dans la formule, R?1¿ et R?2¿ peuvent être des substituants uniques ou condensés de façon à former des noyaux spirocycliques, et sont combinés à des progestatifs et/ou à des oestrogènes. Ces méthodes de traitement peuvent servir de contraception ou pour traiter et/ou prévenir l'aménorrhée secondaire, les saignements anormaux, le léiomyome de l'utérus, l'endométriose, le syndrome des ovaires polycystiques, les carcinomes et adénocarcinomes de l'endomètre, de l'ovaire, du sein, du côlon et de la prostate, ou pour réduire au minimum les saignements du cycle menstruel ou leurs effets secondaires. L'invention comporte des applications supplémentaires telles que la stimulation de l'appétit en vue d'augmenter l'apport d'aliments.

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