EP 1173211 A1 20020123 - CONTRACEPTIVE COMPOSITIONS CONTAINING 3,3-SUBSTITUTED INDOLINE DERIVATIVES AND USES THEREOF
Title (en)
CONTRACEPTIVE COMPOSITIONS CONTAINING 3,3-SUBSTITUTED INDOLINE DERIVATIVES AND USES THEREOF
Title (de)
EMPFÄNGNISVERHÜTENDE ZUSAMMENSETZUNGEN, WELCHE 3,3-SUBSTITUIERTE INDOLINE DERIVATEN ENTHALTEN
Title (fr)
COMPOSITIONS CONTRACEPTIVES RENFERMANT DES DERIVES D'INDOLINE 3,3-SUBSTITUES, ET UTILISATIONS CORRESPONDANTES
Publication
Application
Priority
- US 0011748 W 20000501
- US 18305799 P 19990504
- US 55263100 A 20000419
Abstract (en)
[origin: CA2372591A1] This invention relates to cyclic combination therapies and regimens utilizin g substituted indoline derivative compounds that are antagonists of the progesterone receptor having general structure (I) wherein: R1, and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to form a ring comprising -CH2(CH2)nCH2- where n = 0-5; -CH2CH2CMe2CH2CH2-; -O(CH2)mCH2- where m = 1-4; O(CH2)pO- where p = 1-4; -CH2CH2OCH2CH2-; -CH2CH2N(H or alkyl)CH2CH2-; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl groups; RA = H or optionally substituted alky l, alkoxy, or aminoalkyl groups; R4 = H, halo, CN, NH2, or optionally substitut ed alkyl, alkoxy, or aminoalkyl; R5 is selected from optionally substituted benzene ring; a five or six membered heterocyclic ring; a 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt thereof. 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 an d adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses o f the invention include stimulation of food intake.
IPC 1-7
IPC 8 full level
A61K 31/567 (2006.01); A61K 31/403 (2006.01); A61K 31/404 (2006.01); A61K 31/565 (2006.01); A61K 31/57 (2006.01); A61K 45/06 (2006.01); A61P 5/24 (2006.01); A61P 15/18 (2006.01); C07D 209/08 (2006.01); C07D 209/86 (2006.01)
CPC (source: EP)
A61K 31/57 (2013.01); A61K 45/06 (2013.01)
Citation (search report)
See references of WO 0066166A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
AU 4686700 A 20001117; CA 2372591 A1 20001109; CN 1349417 A 20020515; EP 1173211 A1 20020123; JP 2002543157 A 20021217; MX PA01011297 A 20030714
DOCDB simple family (application)
AU 4686700 A 20000501; CA 2372591 A 20000501; CN 00807136 A 20000501; EP 00928667 A 20000501; JP 2000615050 A 20000501; MX PA01011297 A 20000501