Invention Grant
- Patent Title: Bicyclic pyridine compound
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Application No.: US15551222Application Date: 2015-11-27
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Publication No.: US10023583B2Publication Date: 2018-07-17
- Inventor: Kenichi Kawaguchi , Akihiro Ishihata , Akira Kanai , Yusuke Inagaki , Masashi Hiramoto , Kentaro Enjo , Hajime Takamatsu
- Applicant: Astellas Pharma Inc. , KOTOBUKI PHARMACEUTICAL CO., LTD.
- Applicant Address: JP Chuo-ku JP Hanishina-gun
- Assignee: Astellas Pharma Inc.,KOTOBUKI PHARMACEUTICAL CO., LTD.
- Current Assignee: Astellas Pharma Inc.,KOTOBUKI PHARMACEUTICAL CO., LTD.
- Current Assignee Address: JP Chuo-ku JP Hanishina-gun
- Agency: Oblon, McClelland, Maier & Neustadt, L.L.P.
- Priority: JP2015-046121 20150309
- International Application: PCT/JP2015/083345 WO 20151127
- International Announcement: WO2016/143200 WO 20160915
- Main IPC: C07D213/02
- IPC: C07D213/02 ; C07D407/04 ; A61K31/5365 ; C07D491/048 ; C07D495/04

Abstract:
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.
Public/Granted literature
- US20180022755A1 BICYCLIC PYRIDINE COMPOUND Public/Granted day:2018-01-25
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