专利检索 ap:("ASTELLAS PHARMA INC" OR "KOTOBUKI PHARMACEUTICAL CO LTD") AND inv:"KAWAGUCHI KENICHI" 第 1 页

1.

发明公开
PYRIDINE DERIVATIVES 有权

公开(公告)号：EP3228616A4

公开(公告)日：2018-04-25

申请号：EP15865019

申请日：2015-12-04

申请人： 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

IPC分类号： C07D213/55 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4418 , A61K31/4433 , A61K31/444 , A61K31/472 , A61K31/4747 , A61P7/12 , A61P13/00 , A61P43/00 , C07D213/63 , C07D217/16 , C07D221/02 , C07D221/04 , C07D221/20 , C07D401/04 , C07D405/04

CPC分类号： C07D405/04 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4418 , A61K31/4433 , A61K31/444 , A61K31/472 , A61K31/4747 , A61P7/12 , C07D213/55 , C07D213/63 , C07D217/16 , C07D217/24 , C07D221/02 , C07D221/04 , C07D221/20 , C07D401/04

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.

2.

发明公开
BICYCLIC PYRIDINE COMPOUND 审中-公开

公开(公告)号：EP3269721A4

公开(公告)日：2018-08-01

申请号：EP15884684

申请日：2015-11-27

申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD

发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME

IPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D495/04

CPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , C07D495/04

摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition 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-(bi-cyclic 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.

3.

发明公开
PYRIDINE DERIVATIVE 审中-公开

公开(公告)号：EP3150581A4

公开(公告)日：2018-01-17

申请号：EP15799163

申请日：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

IPC分类号： C07D213/68 , A61K31/4355 , A61K31/436 , A61K31/437 , 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

CPC分类号： C07D495/04 , 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 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12 , C07D409/12 , C07D471/04 , C07D491/048 , C07D491/056 , C07D491/08

摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition 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-{[4-(substituted pyridine)-2-yl]methyl}-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.