Invention Grant
US07709519B2 Benzimidazolylidene propane-1,3 dione derivative or salt thereof
失效
苯并咪唑基丙烷-1,3-二酮衍生物或其盐
- Patent Title: Benzimidazolylidene propane-1,3 dione derivative or salt thereof
- Patent Title (中): 苯并咪唑基丙烷-1,3-二酮衍生物或其盐
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Application No.: US10588485Application Date: 2005-06-02
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Publication No.: US07709519B2Publication Date: 2010-05-04
- Inventor: Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
- Applicant: Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
- Applicant Address: JP Tokyo
- Assignee: Astellas Pharma Inc.
- Current Assignee: Astellas Pharma Inc.
- Current Assignee Address: JP Tokyo
- Agency: Sughrue Mion, PLLC
- Priority: JP2004-166486 20040604; JP2005-099815 20050330
- International Application: PCT/JP2005/010184 WO 20050602
- International Announcement: WO2005/118556 WO 20051215
- Main IPC: A01N43/52
- IPC: A01N43/52

Abstract:
Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.
Public/Granted literature
- US20090018177A1 Propane-1,3-Dione Derivative or Salt Thereof Public/Granted day:2009-01-15
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