Title:
PYRIDINE DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2015/182686
Kind Code:
A1
Abstract:
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.
Inventors:
KAWAGUCHI KENICHI (JP)
ISHIHATA AKIHIRO (JP)
INAGAKI YUSUKE (JP)
TSUCHIYA KAZUYUKI (JP)
HANADATE TADAATSU (JP)
KANAI AKIRA (JP)
KAIZAWA HIROYUKI (JP)
KAZAMI JUNICHI (JP)
MORIKAWA HIROSHI (JP)
HIRAMOTO MASASHI (JP)
ENJO KENTARO (JP)
TAKAMATSU HAJIME (JP)
ISHIHATA AKIHIRO (JP)
INAGAKI YUSUKE (JP)
TSUCHIYA KAZUYUKI (JP)
HANADATE TADAATSU (JP)
KANAI AKIRA (JP)
KAIZAWA HIROYUKI (JP)
KAZAMI JUNICHI (JP)
MORIKAWA HIROSHI (JP)
HIRAMOTO MASASHI (JP)
ENJO KENTARO (JP)
TAKAMATSU HAJIME (JP)
Application Number:
PCT/JP2015/065344
Publication Date:
December 03, 2015
Filing Date:
May 28, 2015
Export Citation:
Assignee:
ASTELLAS PHARMA INC (JP)
KOTOBUKI PHARMACEUTICAL CO LTD (JP)
KOTOBUKI PHARMACEUTICAL CO LTD (JP)
International Classes:
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
Domestic Patent References:
| WO2011136307A1 | 2011-11-03 | |||
| WO2010053120A1 | 2010-05-14 | |||
| WO2014133056A1 | 2014-09-04 |
Foreign References:
| JP2009057282A | 2009-03-19 |
Other References:
HECKER, S. J. ET AL.: "Total Synthesis of (±)- Leuhistin", J. ORG. CHEM., vol. 58, no. 7, 1993, pages 1762 - 1765, XP055360884
See also references of EP 3150581A4
See also references of EP 3150581A4
Attorney, Agent or Firm:
ONO, Shinjiro et al. (JP)
Ono Shinjiro (JP)
Ono Shinjiro (JP)
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