The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jul. 17, 2018
Filed:
Nov. 27, 2015
Astellas Pharma Inc., Chuo-ku, JP;
Kotobuki Pharmaceutical Co., Ltd., Hanishina-gun, JP;
Kenichi Kawaguchi, Tokyo, JP;
Akihiro Ishihata, Tokyo, JP;
Akira Kanai, Tokyo, JP;
Yusuke Inagaki, Tokyo, JP;
Masashi Hiramoto, Tokyo, JP;
Kentaro Enjo, Ibaraki, JP;
Hajime Takamatsu, Tokyo, JP;
Astellas Pharma Inc., Chuo-ku, JP;
KOTOBUKI PHARMACEUTICAL CO., LTD., Hanishina-gun, JP;
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.