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תולדות 17–הידרוקסי–17–פנטאפלואורואתיל–אסטרא–9,4 (10)–דיאן–11–אריל והשימוש בהן לטיפול במחלות
专利权人:
BAYER INTELLECTUAL PROPERTY GMBH;BAYER PHARMA AKTIENGESELLSCHAFT
发明人:
申请号:
IL21696711
公开号:
IL216967A
申请日:
2011.12.14
申请国别(地区):
IL
年份:
2018
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.
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