Contraceptive compositions containing 3,3-substituted indoline derivatives and uses thereof

摘要: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having general structure (I) wherein: R1, R2 chosen independently from each other H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; optionally alkyl, O(alkyl); aryl; or heteroaryl groups; R1 joined form a ring comprising -CH2(CH2)nCH2- where n = 0-5; -CH2CH2CMe2CH2CH2-; -O(CH2)mCH2- m 1-4; O(CH2)pO- p -CH2CH2OCH2CH2-; -CH2CH2N(H alkyl)CH2CH2-; together comprise double bond CMe2; C(cycloalkyl), O, C(cycloether); R3 is OH, NH2, CORA; alkenyl alkynyl RA H alkoxy, aminoalkyl R?4? halo, CN, aminoalkyl; R5 selected benzene ring; five six membered heterocyclic 4 7-substituted indole benzothiophene; pharmaceutically acceptable salt thereof. These methods treatment may be used for contraception and/or prevention secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas adenocarcinomas endometrium, ovary, breast, colon, prostate, minimization side effects menstrual bleeding. Additional uses include stimulation food intake.