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Pyridine derivatives
专利权人:
Astellas Pharma Inc.;KOTOBUKI PHARMACEUTICAL CO., LTD.
发明人:
Kawaguchi Kenichi,Ishihata Akihiro,Kanai Akira,Tsuchiya Kazuyuki,Inagaki Yusuke,Kazami Junichi,Morikawa Hiroshi,Hiramoto Masashi,Enjo Kentaro,Takamatsu Hajime
申请号:
US201515532772
公开号:
US10005762(B2)
申请日:
2015.12.04
申请国别(地区):
美国
年份:
2018
代理人:
Oblon, McClelland, Maier & Neustadt, L.L.P.
摘要:
The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent 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-(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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