公开(公告)号：US20100266504A1

公开(公告)日：2010-10-21

申请号：US12742781

申请日：2008-11-14

申请人： Takahiro Matsumoto ,  Hiroyuki Nagamiya ,  Hironobu Maezaki ,  Tomokazu Kusumoto ,  Kyoko Yoshikawa ,  Hideki Furukawa ,  Izumi Kamo

发明人： Takahiro Matsumoto ,  Hiroyuki Nagamiya ,  Hironobu Maezaki ,  Tomokazu Kusumoto ,  Kyoko Yoshikawa ,  Hideki Furukawa ,  Izumi Kamo

IPC分类号： A61K49/00

CPC分类号： A61K31/5377 ,  A61K31/4545 ,  A61K31/55 ,  C07D471/04 ,  G01N33/5088 ,  G01N33/6893 ,  G01N2800/34

摘要： Provided are a condensed pyridine derivative having a serotonin 5-HT2C receptor activation action, a prophylactic or therapeutic agent for a lower urinary tract symptom, obesity and/or organ prolapse and the like containing the condensed pyridine derivative, a screening method for a substance that increases leak point pressure upon a rise in the intravesical pressure or a prophylactic or therapeutic drug for stress urinary incontinence, a prophylactic or therapeutic drug for cystoceles or enteroceles, containing a substance that activates serotonin 5-HT2C receptor, and a method of screening for a therapeutic drug for cystoceles or enteroceles, including increasing an intravesical pressure after bilateral transection of the hypogastric nerve and pudendal nerve of an animal, and measuring a closure response in the urethra, the rectum or the vagina observed at that time. A serotonin 5-HT2c receptor activator containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

摘要翻译： 提供具有5-羟色胺5-HT 2C受体活化作用的缩合吡啶衍生物，含有缩合吡啶衍生物的下尿路症状，肥胖症和/或器官脱垂等的预防或治疗剂， 增加膀胱内压的上升时的泄漏点压力或压力性尿失禁的预防或治疗药物，包含激活5-羟色胺5-HT 2C受体的物质的用于膀胱或肠的预防或治疗药物的筛选方法 用于膀胱或肠道的治疗药物，包括在双侧横断动物的下腹神经和阴部神经之后增加膀胱内压力，并测量当时观察到的尿道，直肠或阴道中的闭合反应。 含有下式表示的化合物的5-羟色胺5-HT 2C受体活化剂：其中每个符号如说明书中所定义，或其盐。