Invention Grant
- Patent Title: Pyridine derivatives
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Application No.: US15532772Application Date: 2015-12-04
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Publication No.: US10005762B2Publication Date: 2018-06-26
- Inventor: Kenichi Kawaguchi , Akihiro Ishihata , Akira Kanai , Kazuyuki Tsuchiya , Yusuke Inagaki , Junichi Kazami , Hiroshi Morikawa , 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: JP2014-246463 20141205
- International Application: PCT/JP2015/084098 WO 20151204
- International Announcement: WO2016/088864 WO 20160609
- Main IPC: A01N43/42
- IPC: A01N43/42 ; A61K31/44 ; C07D405/04 ; C07D217/16 ; C07D213/55 ; C07D221/04 ; C07D221/20 ; C07D401/04 ; C07D217/24 ; A61K31/435

Abstract:
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.
Public/Granted literature
- US20170362209A1 PYRIDINE DERIVATIVES Public/Granted day:2017-12-21
Information query
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