Title:
新規な17β-ヒドロキシステロイドデヒドロゲナーゼI型阻害剤
Document Type and Number:
Japanese Patent JP4778438
Kind Code:
B2
Abstract:
The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17beta-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17beta-estradiol concentration. In addition, the present invention relates to the general use of selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.
Inventors:
Josef Messinger
Heinrich-Hubert Torre
Bettina Fusen
Bartholomew Johannes van Steen
Jura Schneider
Johannes Bernardus Everaldus Furshof
Pashko Skimmies
Nina Johansson
Yelzi Adam Ski
Heinrich-Hubert Torre
Bettina Fusen
Bartholomew Johannes van Steen
Jura Schneider
Johannes Bernardus Everaldus Furshof
Pashko Skimmies
Nina Johansson
Yelzi Adam Ski
Application Number:
JP2006538862A
Publication Date:
September 21, 2011
Filing Date:
November 11, 2004
Export Citation:
Assignee:
Solvay Pharmaceuticals GmbH
International Classes:
C07J1/00; A61K31/565; A61K31/5685; A61K31/58; A61P5/00; A61P5/30; A61P35/00; A61P43/00; C07J41/00; C07J43/00
Other References:
POIRIER D,JOURNAL OF STEROID BIOCHEM. MOLEC. BIOL.,1998年,V64 N1/2,P83-90
POIRIER D,CURRENT MEDICINAL CHEMISTRY,2003年,V10 N6,P453-477
SAM K-M,DRUG DESIGN AND DISCOVERY,1998年,V15,P157-180
TREMBLAY M R,JOURNAL OF STEROID BIOCHEMISTRY,英国,PERGAMON PRESS PLC,1998年,V66 N4,P179-191
POIRIER D,TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS,1991年,V47 N37,P7751-7766
J. Med. Chem.,2003年,Vol.46, No.10,p.1886-1904,Publication Date (web) April 5, 2003
POIRIER D,CURRENT MEDICINAL CHEMISTRY,2003年,V10 N6,P453-477
SAM K-M,DRUG DESIGN AND DISCOVERY,1998年,V15,P157-180
TREMBLAY M R,JOURNAL OF STEROID BIOCHEMISTRY,英国,PERGAMON PRESS PLC,1998年,V66 N4,P179-191
POIRIER D,TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS,1991年,V47 N37,P7751-7766
J. Med. Chem.,2003年,Vol.46, No.10,p.1886-1904,Publication Date (web) April 5, 2003
Attorney, Agent or Firm:
Toshio Yano
Takuya Kuno
Einzel Felix-Reinhard
Takuya Kuno
Einzel Felix-Reinhard