C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 235/12 (2006.01) A61K 31/4184 (2006.01) A61K 31/4439 (2006.01) A61P 5/08 (2006.01) A61P 13/08 (2006.01) A61P 15/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/10 (2006.01) C07D 409/06 (2006.01)
Patent
CA 2568590
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.
Destiné à fournir un composé utile en tant qu'antagoniste de récepteur GnRH Suite aux résultats des études sur les dérivés de propane-1, dione-3, il est confirmé que, parmi les composés de propane-1, dione-3 ayant 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), un composé dont un anneau de benzène ou de thiophène est remplacé par un groupe dérivé de 1-hydroxyalkyl possède d'excellentes propriétés de transfusion sanguine en plus d'un excellent antagonisme du récepteur de GnRH. Du fait de ses excellentes propriétés de transfusion sanguine en plus de son puissant antagonisme de récepteur de GnRH, le composé ci-dessus devrait démontrer d'excellents effets médicamenteux in vivo et s'avérer utile dans le traitement de maladies dépendantes d'hormones sexuelles comme les cancers de la prostate, du sein, de l'endomètre utérin, le myome utérin et l'hypertrophie de la prostate De plus, ce composé est excellent dans la stabilité métabolique chez l'être humain et de faibles interactions parmi les médicaments. Nommément, il compte des propriétés préférées additionnelles comme les médicaments à employer pour les maladies ci-dessus.
Hirano Masaaki
Kawaminami Eiji
Kinoyama Isao
Kusayama Toshiyuki
Matsumoto Shunichiro
Astellas Pharma Inc.
Dennison Associates
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