公开(公告)号：WO2006055734A3

公开(公告)日：2006-08-17

申请号：PCT/US2005041726

申请日：2005-11-17

Applicant: ARENA PHARM INC ,  TEEGARDEN BRADLEY ,  XIONG YIFENG ,  STRAH-PLEYNET SONJA ,  JAYAKUMAR HONNAPPA ,  DOSA PETER I ,  FEICHTINGER KONRAD ,  CASPER MARTIN ,  LEHMANN JUERG ,  JONES ROBERT M ,  UNETT DAVID J

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

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

Abstract: 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 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, 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.

Abstract translation: 本发明涉及调节5-HT 2A受体5-羟色胺受体活性的式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物。 其化合物和药物组合物涉及用于治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房纤颤，降低血块形成风险，哮喘或其症状，激动或 精神病，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关障碍，以及睡眠障碍，睡眠障碍，睡眠障碍，睡眠障碍，精神病症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉勒斯德拉图雷特综合征， ，糖尿病相关病症，进行性多灶性白质脑病等。 本发明还涉及与单独或一起施用的其他药剂联合治疗5-HT 2A受体5-羟色胺受体介导的病症的方法。

公开(公告)号：WO2006055734A2

公开(公告)日：2006-05-26

申请号：PCT/US2005/041726

申请日：2005-11-17

Applicant: ARENA PHARMACEUTICALS, INC. ,  TEEGARDEN, Bradley ,  XIONG, Yifeng ,  STRAH-PLEYNET, Sonja ,  JAYAKUMAR, Honnappa ,  DOSA, Peter I. ,  FEICHTINGER, Konrad ,  CASPER, Martin ,  LEHMANN, Juerg ,  JONES, Robert M. ,  UNETT, David J.

Inventor： TEEGARDEN, Bradley ,  XIONG, Yifeng ,  STRAH-PLEYNET, Sonja ,  JAYAKUMAR, Honnappa ,  DOSA, Peter I. ,  FEICHTINGER, Konrad ,  CASPER, Martin ,  LEHMANN, Juerg ,  JONES, Robert M. ,  UNETT, David J.

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

Abstract: 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 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, 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.

Abstract translation: 本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT 2A / 5-羟色胺受体的活性。 化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状，激动或 症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，以及睡眠障碍，睡眠障碍 ，糖尿病相关病症，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT 2A 5-羟色胺受体介导的病症的方法。

公开(公告)号：WO2004087680A1

公开(公告)日：2004-10-14

申请号：PCT/JP2004/004554

申请日：2004-03-30

Applicant: TAISHO PHARMACEUTICAL CO., LTD. ,  ARENA PHARMACEUTICALS INC. ,  SEKIGUCHI, Yoshinori ,  KANUMA, Kosuke ,  OMODERA, Katsunori ,  BUSUJIMA, Tsuyoshi ,  TRAN, Thuy-Anh ,  HAN, Sangdon ,  CASPER, Martin ,  KRAMER, Bryan, A.

Inventor： SEKIGUCHI, Yoshinori ,  KANUMA, Kosuke ,  OMODERA, Katsunori ,  BUSUJIMA, Tsuyoshi ,  TRAN, Thuy-Anh ,  HAN, Sangdon ,  CASPER, Martin ,  KRAMER, Bryan, A.

IPC: C07D239/84

CPC classification number: C07D239/95 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

Abstract: The present invention relates to novel compounds of Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

Abstract translation: 本发明涉及新的式（I）化合物：其作为MCH受体拮抗剂。 这些组合物可用于药物组合物，其用途包括预防或治疗改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖症，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗死， 包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

公开(公告)号：WO2004087669A1

公开(公告)日：2004-10-14

申请号：PCT/JP2004/004624

申请日：2004-03-31

Applicant: TAISHO PHARMACEUTICAL CO. LTD. ,  ARENA PHARMACEUTICALS INC. ,  SEKIGUCHI, Yoshinori, ,  KANUMA, Kosuke, ,  OMODERA, Katsunori, ,  BUSUJIMA, Tsuyoshi, ,  TRAN, Thuy-Anh, ,  HAN, Sangdon, ,  CASPER, Martin, ,  KRAMER, Bryan, A., ,  SEMPLE, Graeme, ,  ZOU, Ning,

Inventor： SEKIGUCHI, Yoshinori, ,  KANUMA, Kosuke, ,  OMODERA, Katsunori, ,  BUSUJIMA, Tsuyoshi, ,  TRAN, Thuy-Anh, ,  HAN, Sangdon, ,  CASPER, Martin, ,  KRAMER, Bryan, A., ,  SEMPLE, Graeme, ,  ZOU, Ning,

IPC: C07D215/42

CPC classification number: C07D239/48 ,  C07D215/42 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds of the Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

Abstract translation: 本发明涉及作为MCH受体拮抗剂的式（I）的新化合物。 这些组合物可用于药物组合物，其用途包括预防或治疗改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖症，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗塞， 包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。