Title:
１７−ヒドロキシ−１７−ペンタフルオロエチル−エストラ−４，９（１０）−ジエン−１１−アリール誘導体、その製造方法、その誘導体を利用した諸疾患の治療
Document Type and Number:
Japanese Patent JP5795312
Kind Code:
B2
Abstract:
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.
Inventors:
Wolfgang Schwede
Ulrich Klar
Karsten Mellar
Andrea Rothgeri
Bilhelm Bourne
Ulrich Klar
Karsten Mellar
Andrea Rothgeri
Bilhelm Bourne
Application Number:
JP2012520921A
Publication Date:
October 14, 2015
Filing Date:
July 07, 2010
Export Citation:
Assignee:
Bayer Intellectual Property GmbH
International Classes:
C07J7/00; A61K31/573; A61P5/36; A61P15/00; A61P15/12; A61P15/18; A61P35/00; A61P43/00
Domestic Patent References:
| JP60226893A | ||||
| JP8311094A | ||||
| JP6157587A |
Foreign References:
| WO1998034947A1 | ||||
| US6172052 | ||||
| WO2002067910A2 |
Other References:
野崎正勝ら,創薬化学,化学同人,1995年,p.98-99
Attorney, Agent or Firm:
Yasuhiko Murayama
Shinya Mitsuhiro
Tatsuhiko Abe
Shinya Mitsuhiro
Tatsuhiko Abe