公开(公告)号：WO2008027483A1

公开(公告)日：2008-03-06

申请号：PCT/US2007/019084

申请日：2007-08-30

Applicant: ARENA PHARMACEUTICALS, INC. ,  DOSA, Peter, I. ,  TEEGARDEN, Bradley

Inventor： DOSA, Peter, I. ,  TEEGARDEN, Bradley

IPC: C07D405/04 ,  A61K31/4155 ,  A61P25/00

CPC classification number: C07D405/04

Abstract: The present invention relates to benzofuran derivatives of the following formula (I) which are modulators of the serotonin 5-HT 2A receptor and are useful in the treatment of various diseases and disorders related to the 5-HT 2A receptor.

Abstract translation: 本发明涉及作为5-羟色胺5-HT 2A受体的调节剂的下式（I）的苯并呋喃衍生物，可用于治疗与5-HT 2A受体相关的各种疾病和病症， SUB> 2A 受体。

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：WO2007136680A3

公开(公告)日：2008-01-10

申请号：PCT/US2007011789

申请日：2007-05-17

Applicant: ARENA PHARM INC ,  TEEGARDEN BRADLEY ,  CHAPMAN DENNIS ,  DECAIRE MARC ,  DOSA PETER I ,  FEICHTINGER KONRAD ,  JAYAKUMAR HONNAPPA ,  STRAH-PLEYNET SONJA ,  TRAN THUY-ANH ,  XU JINGDONG

Inventor： TEEGARDEN BRADLEY ,  CHAPMAN DENNIS ,  DECAIRE MARC ,  DOSA PETER I ,  FEICHTINGER KONRAD ,  JAYAKUMAR HONNAPPA ,  STRAH-PLEYNET SONJA ,  TRAN THUY-ANH ,  XU JINGDONG

IPC: 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 classification number: C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

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

Applicant: ARENA PHARMACEUTICALS, INC. ,  TEEGARDEN, Bradley ,  CHAPMAN, Dennis ,  DECAIRE, Marc ,  DOSA, Peter, I. ,  FEICHTINGER, Konrad ,  JAYAKUMAR, Honnappa ,  STRAH-PLEYNET, Sonja ,  TRAN, Thuy-Anh ,  XU, Jingdong

Inventor： TEEGARDEN, Bradley ,  CHAPMAN, Dennis ,  DECAIRE, Marc ,  DOSA, Peter, I. ,  FEICHTINGER, Konrad ,  JAYAKUMAR, Honnappa ,  STRAH-PLEYNET, Sonja ,  TRAN, Thuy-Anh ,  XU, Jingdong

IPC: C07D413/12 ,  C07D231/12 ,  C07D231/16 ,  C07D403/12 ,  C07D411/12 ,  A61K31/42 ,  A61K31/4192 ,  A61K31/427

CPC classification number: C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2007120600A2

公开(公告)日：2007-10-25

申请号：PCT/US2007/008718

申请日：2007-04-09

Applicant: ARENA PHARMACEUTICALS, INC. ,  DOSA, Peter I. ,  TEEGARDEN, Bradley

Inventor： DOSA, Peter I. ,  TEEGARDEN, Bradley

IPC: C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4439 ,  A61P9/00

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D413/14

Abstract: The present invention pertains to certain 3-pyridinyl-pyrazole derivatives 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, 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, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also pertains to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

Abstract translation: 本发明涉及式（Ia）的某些3-吡啶基 - 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，药物诱发的精神病，兴奋性精神病，吉列斯·杜列特综合征，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，精神分裂症精神分裂症和相关疾病，睡眠障碍，糖尿病相关 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。

公开(公告)号：WO2007120600A3

公开(公告)日：2008-01-03

申请号：PCT/US2007008718

申请日：2007-04-09

Applicant: ARENA PHARM INC ,  DOSA PETER I ,  TEEGARDEN BRADLEY

Inventor： DOSA PETER I ,  TEEGARDEN BRADLEY

IPC: C07D401/04 ,  A61K31/4439 ,  A61P9/00 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D413/14

Abstract: The present invention pertains to certain 3-pyridinyl-pyrazole derivatives 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, 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, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also pertains to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

Abstract translation: 本发明涉及式（Ia）的某些3-吡啶基 - 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，药物诱发的精神病，兴奋性精神病，吉列斯·杜列特综合征，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，精神分裂症精神分裂症和相关疾病，睡眠障碍，糖尿病相关 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。

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

Applicant: ARENA PHARMACEUTICALS, INC. ,  UNETT, David J. ,  TEEGARDEN, Bradley ,  JAYAKUMAR, Honnappa ,  LI, Hongmei ,  STRAH-PLEYNET, Sonja ,  DOSA, Peter I.

Inventor： UNETT, David J. ,  TEEGARDEN, Bradley ,  JAYAKUMAR, Honnappa ,  LI, Hongmei ,  STRAH-PLEYNET, Sonja ,  DOSA, Peter I.

IPC: A61K31/415 ,  A61P25/28

CPC classification number: A61K31/415

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2008042388A1

公开(公告)日：2008-04-10

申请号：PCT/US2007/021182

申请日：2007-10-02

Applicant: ARENA PHARMACEUTICALS, INC. ,  XIONG, Yifeng ,  CHERRIER, Martin, C. ,  CHOI, Jin Sun, Karoline ,  DOSA, Peter, I. ,  SMITH, Brian, M. ,  STRAH-PLEYNET, Sonja ,  ULLMAN, Bret ,  TEEGARDEN, Bradley

Inventor： XIONG, Yifeng ,  CHERRIER, Martin, C. ,  CHOI, Jin Sun, Karoline ,  DOSA, Peter, I. ,  SMITH, Brian, M. ,  STRAH-PLEYNET, Sonja ,  ULLMAN, Bret ,  TEEGARDEN, Bradley

IPC: C07D231/14 ,  A61K31/415 ,  A61P25/00

CPC classification number: C07D231/16 ,  C07D231/14 ,  C07D231/54 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04

Abstract: Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT 2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related 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: 式（Ia）的吡唑衍生物及其药物组合物，其调节5-羟色胺5HT 2A受体的活性。 式（Ia）。 化合物及其药物组合物涉及可用于治疗失眠和相关睡眠障碍，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，心房颤动，降低血块形成风险，哮喘的方法 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，以及其它疾病，或其症状，激动或其症状，行为障碍，药物诱导的精神病，兴奋性精神病，Gilles de Ia Tourette综合征，躁狂症，有机或NOS精神病，精神病，精神病， 糖尿病相关疾病，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-HT 2A 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。