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1. 发明申请

WO2006078610A1 DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS OR TREATMENT OF PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY 审中-公开
标题翻译：作为有利于预防或治疗进展性多发性白血病的5-HT2A丝氨酸受体的调节剂的二元和尿苷尿素衍生物
公开(公告)号：WO2006078610A1
公开(公告)日：2006-07-27
申请号：PCT/US2006/001516
申请日：2006-01-17
申请人： ARENA PHARMACEUTICALS, INC. , UNETT, David J. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter I.
发明人： UNETT, David J. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter I.
IPC分类号： A61K31/415 , A61P25/28
CPC分类号： A61K31/415
摘要： The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of progressive multifocal leukoencephalopathy.
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，其调节5-HT2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于预防或治疗进行性多灶性脑白质脑病的方法。

2. 发明申请

WO2007136703A1 PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗相关疾病的5-HT2A丝氨酸蛋白受体的调节剂的主要氨基酸及其衍生物
公开(公告)号：WO2007136703A1
公开(公告)日：2007-11-29
申请号：PCT/US2007/011834
申请日：2007-05-17
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , CHAPMAN, Dennis , CHOI, Juyi , FEICHTINGER, Konrad , HAN, Sangdon , JAYAKUMAR, Honnappa , TRAN, Thuy-Anh , XU, Jingdong , ZOU, Ning
发明人： TEEGARDEN, Bradley , CHAPMAN, Dennis , CHOI, Juyi , FEICHTINGER, Konrad , HAN, Sangdon , JAYAKUMAR, Honnappa , TRAN, Thuy-Anh , XU, Jingdong , ZOU, Ning
IPC分类号： C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/4155 , A61P7/00
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain compounds 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, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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 associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及调节5-HT 2A 2 5-羟色胺受体活性的某些式（Ia）化合物及其药物组合物。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，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法，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，糖尿病性精神病，精神病性精神病，精神病性精神病，精神病性精神病，相关疾病，进行性多灶性脑白质病等。本发明还涉及与分开或一起施用的其它药剂组合治疗5-HT 2A 5-羟色胺受体相关疾病的方法。

3. 发明申请

WO2006055734A2 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗相关疾病的5-HT2A丝氨酸受体的调节剂的3-苯基 - 吡唑衍生物
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
申请人： 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.
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.
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 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.
摘要翻译：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。

4. 发明申请

WO2005012254A1 DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERTO 审中-公开
标题翻译：作为有利于预防和治疗相关疾病的5-HT2A丝氨酸蛋白受体的调节剂的二元和尿苷尿素衍生物
公开(公告)号：WO2005012254A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/023488
申请日：2004-07-21
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter, Ian
发明人： TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , LI, Hongmei , STRAH-PLEYNET, Sonja , DOSA, Peter, Ian
IPC分类号： C07D231/16
CPC分类号： A61K31/415 , A61K31/4155 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/12 , C07D231/16 , C07D401/12 , 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，其调节5-HT2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于预防或治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状的方法，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NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症和精神分裂症以及相关疾病和睡眠障碍，睡眠障碍，糖尿病相关疾病等。本发明还涉及与单独或一起施用的多巴胺D2受体拮抗剂如氟哌啶醇组合预防或治疗5-HT2A 5-羟色胺受体介导的病症的方法。

5. 发明申请

WO2003062206A3 SMALL MOLECULE MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：WO2003062206A3
公开(公告)日：2003-07-31
申请号：PCT/US2003/002059
申请日：2003-01-23
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , DROUET, Keith , JAYAKUMAR, Honnappa , THOMSEN, William , MAFFUID, Paul , ELWELL, Katie , FOSTER, Richard , LAWLESS, Michael , LIU, Qian , SMITH, Julian , FEICHTINGER, Konrad
发明人： TEEGARDEN, Bradley , DROUET, Keith , JAYAKUMAR, Honnappa , THOMSEN, William , MAFFUID, Paul , ELWELL, Katie , FOSTER, Richard , LAWLESS, Michael , LIU, Qian , SMITH, Julian , FEICHTINGER, Konrad
IPC分类号： C07D231/16
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. Formula (I): Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of reducing 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 and NOS schizophrenia and related disorders. 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.

6. 发明申请

WO2006055734A3 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译： 3-苯基 - 吡唑衍生物作为用于治疗与其有关的疾病的5-HT2A血清素受体的调节剂
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
申请人： 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
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 , A61K31/4155 , A61P29/00 , C07D231/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08
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 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.
摘要翻译：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。

7. 发明申请

WO2007136680A3 3-PYRAZ0LYL-BENZAMIDE-4-ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗与相关疾病有关的5-HT2A丝氨酸受体有用的调节剂的3-氨基吡啶-4-酮，其次级胺和衍生物
公开(公告)号：WO2007136680A3
公开(公告)日：2008-01-10
申请号：PCT/US2007011789
申请日：2007-05-17
申请人： ARENA PHARM INC , TEEGARDEN BRADLEY , CHAPMAN DENNIS , DECAIRE MARC , DOSA PETER I , FEICHTINGER KONRAD , JAYAKUMAR HONNAPPA , STRAH-PLEYNET SONJA , TRAN THUY-ANH , XU JINGDONG
发明人： TEEGARDEN BRADLEY , CHAPMAN DENNIS , DECAIRE MARC , DOSA PETER I , FEICHTINGER KONRAD , JAYAKUMAR HONNAPPA , STRAH-PLEYNET SONJA , TRAN THUY-ANH , XU JINGDONG
IPC分类号： C07D413/12 , A61K31/4192 , A61K31/42 , A61K31/427 , A61K31/454 , A61P7/02 , A61P9/10 , A61P25/00 , C07D231/12 , C07D231/16 , C07D403/12 , C07D411/12
CPC分类号： C07D231/12 , A61K31/415 , C07D207/335 , C07D207/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A 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, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。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，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法，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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病，精神病，相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

8. 发明申请

WO2007136680A2 ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：其他作为5-HT2A丝氨酸受体调节剂的二级氨基酸和衍生物，用于治疗与相关疾病有关的疾病
公开(公告)号：WO2007136680A2
公开(公告)日：2007-11-29
申请号：PCT/US2007/011789
申请日：2007-05-17
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , CHAPMAN, Dennis , DECAIRE, Marc , DOSA, Peter, I. , FEICHTINGER, Konrad , JAYAKUMAR, Honnappa , STRAH-PLEYNET, Sonja , TRAN, Thuy-Anh , XU, Jingdong
发明人： TEEGARDEN, Bradley , CHAPMAN, Dennis , DECAIRE, Marc , DOSA, Peter, I. , FEICHTINGER, Konrad , JAYAKUMAR, Honnappa , STRAH-PLEYNET, Sonja , TRAN, Thuy-Anh , XU, Jingdong
IPC分类号： C07D413/12 , C07D231/12 , C07D231/16 , C07D403/12 , C07D411/12 , A61K31/42 , A61K31/4192 , A61K31/427
CPC分类号： C07D231/12 , A61K31/415 , C07D207/335 , C07D207/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A 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, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。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，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法，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，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病，精神病，相关疾病，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-HT2A 5-羟色胺受体相关疾病的方法。

9. 发明申请

WO2004058722A1 DIARYLAMINE AND ARYLHETEROARYLAMINE PYRAZOLE DERIVATIVES AS MODULATORS OF 5HT2A 审中-公开
标题翻译：作为5HT2A的调节剂的二胺和芳基胺胺吡唑衍生物
公开(公告)号：WO2004058722A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/040844
申请日：2003-12-22
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , STRAH-PLEYNET, Sonja
发明人： TEEGARDEN, Bradley , JAYAKUMAR, Honnappa , STRAH-PLEYNET, Sonja
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： One aspect of the present invention relates to certain diarylamine and arylheteroarylamine pyrazole derivatives of Formula (A) and pharmaceutical compositions that modulate the activity of the human 5HT2A serotonin receptor. Compounds and pharmaceutical compositions are directed to methods useful in the prophylaxis or treatment of reducing platelet aggreagation, sleep disorders, 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 and NOS schizophrenia and related disorders. Another aspect of the present invention is directed to the method of prophylaxis or treatment of 5HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.
摘要翻译：本发明的一个方面涉及式（A）的某些二芳基胺和芳基杂芳基胺吡唑衍生物以及调节人5HT2A血清素受体活性的药物组合物。化合物和药物组合物涉及可用于预防或治疗减少血小板凝集，睡眠障碍，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，减少血块形成风险，哮喘或症状，激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症和NOS精神分裂症及相关疾病。本发明的另一方面涉及与多巴胺D2受体拮抗剂如氟哌啶醇组合施用以分别或一起施用的5HT2A 5-羟色胺受体介导的病症的方法。

10. 发明申请

WO2003062206A2 SMALL MOLECULE MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于预防和治疗相关疾病的5-HT2A丝氨酸受体的小分子调节剂
公开(公告)号：WO2003062206A2
公开(公告)日：2003-07-31
申请号：PCT/US2003/002059
申请日：2003-01-23
申请人： ARENA PHARMACEUTICALS, INC. , TEEGARDEN, Bradley , DROUET, Keith , JAYAKUMAR, Honnappa , THOMSEN, William , MAFFUID, Paul , ELWELL, Katie , FOSTER, Richard , LAWLESS, Michael , LIU, Qian , SMITH, Julian , FEICHTINGER, Konrad
发明人： TEEGARDEN, Bradley , DROUET, Keith , JAYAKUMAR, Honnappa , THOMSEN, William , MAFFUID, Paul , ELWELL, Katie , FOSTER, Richard , LAWLESS, Michael , LIU, Qian , SMITH, Julian , FEICHTINGER, Konrad
IPC分类号： C07D231/16
CPC分类号： C07D231/12 , C07D231/14 , C07D231/16 , C07D401/12 , C07D409/04
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. Formula (I): Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of reducing 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 and NOS schizophrenia and related disorders. 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，其调节5-HT2Ba5-5羟色胺受体的活性。式（I）：其化合物及其药物组合物涉及可用于预防或治疗减少血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血凝块形成风险的方法，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，杜勒氏综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症和NOS精神分裂症及相关障碍。本发明还涉及与单独或一起施用的多巴胺D2受体拮抗剂如氟哌啶醇组合预防或治疗5-HT2,5α血清素受体介导的病症的方法。

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