The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 04, 2010
Filed:
Jun. 02, 2005
Masaaki Hirano, Chuo-ku, JP;
Eiji Kawaminami, Chuo-ku, JP;
Isao Kinoyama, Chuo-ku, JP;
Shunichiro Matsumoto, Chuo-ku, JP;
Kei Ohnuki, Chuo-ku, JP;
Kazuyoshi Obitsu, Chuo-ku, JP;
Toshiyuki Kusayama, Chuo-ku, JP;
Masaaki Hirano, Chuo-ku, JP;
Eiji Kawaminami, Chuo-ku, JP;
Isao Kinoyama, Chuo-ku, JP;
Shunichiro Matsumoto, Chuo-ku, JP;
Kei Ohnuki, Chuo-ku, JP;
Kazuyoshi Obitsu, Chuo-ku, JP;
Toshiyuki Kusayama, Chuo-ku, JP;
Astellas Pharma Inc., Tokyo, JP;
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.