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PYRIDINE DERIVATIVE
专利权人:
ASTELLAS PHARMA INC.;KOTOBUKI PHARMACEUTICAL CO., LTD.
发明人:
KAWAGUCHI, KENICHI,ISHIHATA, AKIHIRO,INAGAKI, YUSUKE,TSUCHIYA, KAZUYUKI,HANADATE, TADAATSU,KANAI, AKIRA,KAIZAWA, HIROYUKI,KAZAMI, JUNICHI,MORIKAWA, HIROSHI,HIRAMOTO, MASASHI,ENJO, KENTARO,TAKAMATSU, H
申请号:
PH12016502344
公开号:
PH12016502344A1
申请日:
2016.11.25
申请国别(地区):
PH
年份:
2017
代理人:
摘要:
The present invention addresses the problem of providing a medicinal composition and, in particular, a compound suitable for treating nocturia. Under the expectation that nocturnal urinary frequency could be reduced via an antidiuretic action, said antidiuretic action being induced by inhibiting placental leucine aminopeptidase (P-LAP) that is an AVP-metabolic enzyme at night and thus maintaining and/or increasing endogenous AVP concentration, extensive studies were made on compounds capable of inhibiting P-LAP. As a result, it was discovered that a (2R)-3-amino-2-[(4-substituted pyridin-2-yl)methyl]-2-hydroxypropanoic acid derivative has an excellent P-LAP inhibiting effect. By testing the antidiuretic action using drinking water-loaded rats, furthermore, it was discovered that the aforesaid compound has an effect of suppressing urine production due to an increase in endogenous AVP concentration based on the inhibition of P-LAP. Thus, the present invention provides a compound that is likely usable as a therapeutic agent for nocturia based on a mechanism of inhibiting P-LAP.
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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