发明名称 PYRIDINE DERIVATIVE
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.
申请公布号 CA2950259(A1) 申请公布日期 2015.12.03
申请号 CA20152950259 申请日期 2015.05.28
申请人 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, HAJIME
分类号 C07D213/68;A61K31/4355;A61K31/436;A61K31/437;A61K31/439;A61K31/44;A61K31/443;A61K31/4433;A61K31/4436;A61K31/4439;A61K31/444;A61K31/4545;A61K31/4725;A61K31/497;A61K31/506;A61K31/5377;A61P13/00;A61P43/00;C07D213/70;C07D213/74;C07D401/04;C07D401/06;C07D401/12;C07D407/06;C07D407/12;C07D409/12;C07D471/04;C07D491/048;C07D491/056;C07D491/08 主分类号 C07D213/68
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