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    BENZAZEPINE COMPOUND
    2.
    发明公开
    BENZAZEPINE COMPOUND 有权
    苯并氮杂

    公开(公告)号：EP2546255A1

    公开(公告)日：2013-01-16

    申请号：EP11753475.0

    申请日：2011-03-11

    申请人： Astellas Pharma Inc.

    发明人： KOSHIO, Hiroyuki ,  ASAI, Norio ,  TAKAHASHI, Taisuke ,  SHIMIZU, Takafumi ,  NAGAI, Yasuhito ,  KAWABATA, Keiko ,  THOR, Karl Bruce

    IPC分类号： C07D487/04 ,  A61K31/55 ,  A61P3/04 ,  A61P13/00 ,  A61P13/02 ,  A61P15/10 ,  A61P43/00 ,  C07D498/04

    CPC分类号： C07D498/04 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

    摘要： [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
    [Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

    PIPERAZINE DERIVATIVE
    5.
    发明公开
    PIPERAZINE DERIVATIVE 审中-公开

    公开(公告)号：EP3489231A1

    公开(公告)日：2019-05-29

    申请号：EP17830975.3

    申请日：2017-07-18

    申请人： Astellas Pharma Inc.

    发明人： SUGANE, Takashi ,  ASAI, Norio ,  MORITOMO, Hiroyuki ,  YAMASHITA, Daisuke ,  HOSOGAI, Naomi

    IPC分类号： C07D401/14 ,  A61K31/496 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00 ,  C07D403/06 ,  C07D405/14

    摘要： [Problem] To provide a compound useful as an MC 4 receptor agonist. [Solution] The present inventors have made studies on MC 4 receptor agonists. As a result, it is confirmed that a piperazine derivative has an MC 4 receptor agonist activity, which leads to the accomplishment of the present invention. The piperazine derivative according to the present invention has an MC 4 receptor agonist activity, and therefore can be used as a prophylactic or therapeutic agent for disturbance of urination in bladder and urinary tract diseases, particularly underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-sphincter dyssynergia and prostatic hyperplasia.

    OXADIAZOLIDINEDIONE COMPOUND
    7.
    发明公开
    OXADIAZOLIDINEDIONE COMPOUND 审中-公开
    恶二唑啉二酮化合物

    公开(公告)号：EP2011788A1

    公开(公告)日：2009-01-07

    申请号：EP07742129.5

    申请日：2007-04-23

    申请人： Astellas Pharma Inc.

    发明人： NEGORO, Kenji ,  IWASAKI, Fumiyoshi ,  OHNUKI, Kei ,  KUROSAKI, Toshio ,  YONETOKU, Yasuhiro ,  ASAI, Norio ,  YOSHIDA, Shigeru ,  SOGA, Takatoshi

    IPC分类号： C07D271/06 ,  A61K31/4245 ,  A61K31/4439 ,  A61P3/08 ,  A61P3/10 ,  A61P43/00 ,  C07D413/12

    CPC分类号： C07D271/06 ,  C07D271/07 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided.
    [Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

    摘要翻译： [问题]提供可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗糖尿病等涉及GPR40的疾病的药剂。 [解决手段]发现了一种恶二唑烷二酮化合物或其药学上可接受的盐，其特征在于在恶二唑烷二酮环的2位具有通过连接基团与环状基团结合的苄基或类似取代基， 具有优良的GPR40激动剂作用。 另外，由于本发明的恶二唑烷二酮化合物显示出优异的胰岛素分泌促进作用和血糖值降低作用，因此可用作胰岛素分泌促进剂或糖尿病的预防/治疗剂。