The 17 hydroxyl fluoro- female steroids -4,9 of -17- ethyl diphenylamines (10)-diene -11- aryl derivatives, for treating their preparation and their method used of disease
SCHWEDE, WOLFGANG,KLAR, ULRICH,MOELLER, CARSTEN,ROTGERI, ANDREA,BONE, WILHELM
申请号：
ES10735198
公开号：
ES2416461T3
申请日:
2010.07.07
申请国别(地区):
ES
年份:
2013
代理人:
摘要：
17 hydroxyl -17-pentafluoroethyl- female steroids -4,9 (10)-diethylenetriamines -11- aryl derivatives (I) are new. 17 hydroxyl -17-pentafluoroethyl- female steroids -4,9 (10)-diethylenetriamines -11- aryl derivatives of public formula (I) and their stereoisomer, the solvent of salt, solvent or salt is new including all crystal modifications. R 1 >: by 1 or 2 Y 1 Y 1 > replaced or a benzyl ring > Y 1 >: SR 2 >, S (O) R 3 >, S (O) 2R 3 >, S (O) (NH) R 3 >, 9 > R of S (O) (NR 4 >) R 3 > or S (O) 2NR 10 > R 2 >: H, 1-6C- alkyl, 7-10C- aralkyl or aryl R 3 >: 1-6C alkyl or aryls R 4 >: S (O) 2R 6 > R 6 >: phenyl or 4 aminomethyl phenyls X: O or non-7 > or NNHSO 2R 7 > Any one R 9 >, R 10 >: H, 1-10C- alkyl or aryl Or the 3-8 membered heterocyclic rings that 9 > R of R 10 > N: one are optionally saturated R 7 >: H, 1-10C- alkyl or aryl. It includes (I) in conjunction with another activator and an auxiliary material that one independent claims, which are put into a medicament,. [image] activity: gynaecology Inhibit cell Contraceptive. Mechanism of action: progesterone receptor antagonist. (I) progesterone receptor A antagonistic activity is tested using stable transfection thing human neuroblastoma cell. The result shows that 4[(11beta, 17beta) -3 oxygen containing -17 figure (pentafluoroethyl) female steroid -4,9 diethylenetriamines -11-yl of -17- hydroxyls]-N, N- dimethylbiphenyl -4- sulphanilamides show 0.01 one IC of nanomole/l, 5 0value.
