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BICYCLISCHE PYRIDINVERBINDUNG
专利权人:
Astellas Pharma Inc.;Kotobuki Pharmaceutical Co., Ltd.
发明人:
KAWAGUCHI, Kenichi,ISHIHATA, Akihiro,KANAI, Akira,INAGAKI, Yusuke,HIRAMOTO, Masashi,ENJO, Kentaro,TAKAMATSU, Hajime
申请号:
EP15884684
公开号:
EP3269721A4
申请日:
2015.11.27
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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