SCHWEDE, WOLFGANG,KLAR, ULRICH,MÖLLER, CARSTEN,ROTGERI, ANDREA,BONE, WILHELM
申请号：
PL17176264
公开号：
PL3252069T3
申请日:
2010.07.07
申请国别(地区):
PL
年份:
2019
代理人:
摘要：
17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives (I) are new. 17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) and their stereoisomers, salts, solvate or solvate of the salts, including all crystal modifications, are new. R 1>； : Y 1>；or a phenyl ring substituted by 1 or 2 Y 1>；； Y 1>； : SR 2>；, S(O)R 3>；, S(O) 2R 3>；, S(O)(NH)R 3>；, S(O)(NR 4>；)R 3>；or S(O) 2NR 9>；R 10>；； R 2>； : H, 1-6C-alkyl, 7-10C-aralkyl or aryl； R 3>； : 1-6C-alkyl or aryl； R 4>； : S(O) 2R 6>；； R 6>； : phenyl or 4-methylphenyl； X : O, NOR 7>；or NNHSO 2R 7>；； either R 9>；, R 10>； : H, 1-10C-alkyl or aryl； or R 9>；R 10>；N : an optionally saturated 3-8-membered heterocyclic ring； and R 7>； : H, 1-10C-alkyl or aryl. An independent claim is included for a medicament comprising (I) in combination with a further active agent and an auxiliary material. [Image] ACTIVITY : Gynecological； Cytostatic； Contraceptive. MECHANISM OF ACTION : Progesterone receptor antagonist. The progesterone receptor A antagonistic activity of (I) was tested using stable transfectant human neuroblastoma cells. The results showed that 4'-[(11beta , 17beta )-17-hydroxy-3-oxo-17-(pentafluoroethyl)estra-4,9-dien-11-yl]-N,N-dimethylbiphenyl-4-sulfonamide exhibited an IC 5 0value of 0.01 nmole/l.
