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    BICYCLIC PYRIDINE COMPOUND
    4.
    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.

    2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF
    6.
    发明公开
    2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF 审中-公开

    公开(公告)号：EP3153511A4

    公开(公告)日：2017-12-06

    申请号：EP15803484

    申请日：2015-06-05

    申请人： ASTELLAS PHARMA INC

    发明人： TAKAHASHI TAISUKE ,  KOIKE TAKANORI ,  NEGORO KENJI ,  TANAKA HIROAKI ,  MAEDA JUN ,  YOKOYAMA KAZUHIRO ,  TAKAMATSU HAJIME

    IPC分类号： C07D417/14 ,  A61K31/497 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00

    CPC分类号： C07D417/14 ,  A61K31/497

    摘要： To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors perfected the present invention after discovering that thiazole derivatives substituted at position 2 by pyrazinylcarbonylamino are exceptional muscarinic M 3 receptor positive allosteric modulators and can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M 3 receptors. The 2-acylaminothiazole derivatives or salts thereof of the present invention can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M 3 receptors, e.g., underactive bladder and the like.