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COMPOSE PYRIDINE BICYCLIQUE
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:
CA2976746
公开号:
CA2976746A1
申请日:
2015.11.27
申请国别(地区):
CA
年份:
2016
代理人:
摘要:
The present invention addresses the problem of providing a pharmaceutical composition, particularly a compound suitable for the treatment of nocturia. Extensive and intensive studies have been made on compounds capable of inhibiting placental leucineaminopeptidase (P-LAP), in the anticipation that an antidiuretic activity associated with the maintenance of or increase in an endogenous AVP concentration can be exerted by inhibiting P-LAP, which is a metabolic enzyme for AVP, in the nighttime and the urination frequency in the nighttime can be decreased through the antidiuretic activity. As a result, it is found that a (2R)-3-amino-2-(bicyclic pyridylmethyl)-2-hydroxypropanoic acid derivative has a good P-LAP inhibition activity, and it is also found that, in an antidiuretic test using a drinking water-fed rat, the compound has a urine production inhibition activity associated with the increase in an endogenous AVP concentration which is resulted from the P-LAP inhibition by the compound. Thus, the present invention provides a compound which is expected to be used as a therapeutic agent for nocturia and of which the mechanism of action against nocturia is through the inhibition of 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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