公开(公告)号：EP1695966A1

公开(公告)日：2006-08-30

申请号：EP05025004.2

申请日：2004-07-21

申请人： Arena Pharmaceuticals, Inc.

发明人： Teegarden, Bradley ,  Jayakumar, Honnappa ,  Li, Hongmei ,  Strah-Pleynet, Sonja ,  Dosa, Peter Ian

IPC分类号： C07D231/16 ,  A61K31/415

CPC分类号： C07D231/12 ,  C07D231/16 ,  C07D405/12

摘要： The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like. The present invention also relates to the method of prophylaxis or treatment of 5-HT 2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

摘要翻译： 本发明涉及式（I）的某些吡唑衍生物及其药物组合物做了调制的5-HT 2A血清素受体的活性。 化合物及其药物组合物涉及在血小板aggreagation，冠状动脉病，心肌梗塞，短暂性缺血发作，心绞痛，中风，心房纤维性颤动的预防或治疗有用的方法，降低血液凝块形成，哮喘或症状的危险物， 搅拌或症状，行为障碍，药物诱发的精神病，兴奋型精神病，抽动秽语综合征的，躁狂症，器质性或NOS精神病，精神障碍，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关病症，和睡眠障碍， 睡眠障碍，糖尿病相关疾病等。 因此，本发明涉及预防或治疗5-HT 2A血清素受体介导的病症的组合与多巴胺D2受体拮抗剂的方法：如氟哌啶醇，分开或一起给药。

公开(公告)号：EP1978019A1

公开(公告)日：2008-10-08

申请号：EP08010784.0

申请日：2005-11-17

申请人： Arena Pharmaceuticals, Inc.

发明人： Teegarden, Bradley ,  Xiong, Yifeng ,  Strah-Pleynet, Sonja ,  Jayakumar, Honnappa ,  Dosa, Peter I. ,  Feichtinger, Konrad ,  Casper, Martin ,  Lehmann, Juerg ,  Jones, Robert M. ,  Unett, David J.

IPC分类号： C07D231/16 ,  C07D231/12 ,  C07D403/12 ,  C07D487/08 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61P29/00 ,  A61K31/4155

CPC分类号： C07D231/12 ,  A61K31/5377 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula ( Ia ) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及式的某些3-苯基 - 吡唑衍生物（Ia）和其药物组合物做了调制的5-HT 2A血清素受体的活性。 化合物及其药物组合物涉及在血小板聚集，冠状动脉病，心肌梗塞，短暂性缺血发作，心绞痛，中风，心房纤维性颤动，降低血液凝块形成，哮喘或其症状，搅动或风险的治疗有用的方法 症状，行为障碍，药物诱发的精神病，兴奋型精神病，图雷特氏综合征，躁狂性障碍，器质性或NOS精神病，精神障碍，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关病症，和睡眠障碍，睡眠障碍 ，糖尿病相关疾病，进行性多灶性白质脑病等。 因此，本发明涉及一种用于与分开或一起给药其它药物试剂联合治疗5-HT 2A血清素受体介导的病症的方法。