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    INDAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    1.
    发明申请
    INDAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    作为用于治疗相关疾病的5-HT2A丝氨酸受体有用的调节剂的吲哚衍生物

    公开(公告)号：WO2008054748A2

    公开(公告)日：2008-05-08

    申请号：PCT/US2007/022921

    申请日：2007-10-30

    Applicant: ARENA PHARMACEUTICALS, INC. ,  FEICHTINGER, Konrad ,  XIONG, Yifeng ,  CHOI, Jin Sun, Karoline ,  SMITH, Brian, M. ,  STRAH-PLEYNET, Sonja ,  TEEGARDEN, Bradley

    Inventor： XIONG, Yifeng ,  CHOI, Jin Sun, Karoline ,  SMITH, Brian, M. ,  STRAH-PLEYNET, Sonja ,  TEEGARDEN, Bradley

    CPC classification number: C07D231/56 ,  C07D403/06

    Abstract: Indazole 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-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

    Abstract translation: 式（Ia）的吲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，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血液风险的方法 凝块形成，哮喘或其症状，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，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，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-羟色胺受体介导的病症的方法。

    ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    2.
    发明申请
    ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    作为用于治疗相关疾病的5-HT2A丝氨酸受体的调节剂的乙酰胺衍生物

    公开(公告)号：WO2007136875A3

    公开(公告)日：2008-04-10

    申请号：PCT/US2007012230

    申请日：2007-05-17

    Applicant: ARENA PHARM INC ,  TEEGARDEN BRADLEY ,  FEICHTINGER KONRAD ,  STRAH-PLEYNET SONJA ,  ULMANN BRETT ,  XIONG YIFENG

    Inventor： TEEGARDEN BRADLEY ,  FEICHTINGER KONRAD ,  STRAH-PLEYNET SONJA ,  ULMANN BRETT ,  XIONG YIFENG

    IPC: C07D413/12 ,  A61K31/415 ,  C07D213/12 ,  C07D401/12 ,  C07D403/12 ,  C07D407/14

    CPC classification number: C07D231/16 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-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.

    Abstract translation: 本发明涉及某些式（Ia）的化合物及其药物组合物，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-HT 2A 5-羟色胺受体相关疾病的方法。

    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    5.
    发明申请
    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    作为用于治疗与相关疾病相关的疾病的5-HT2A丝氨酸受体的调节剂的吡唑衍生物

    公开(公告)号：WO2006060762A2

    公开(公告)日：2006-06-08

    申请号：PCT/US2005043893

    申请日：2005-12-01

    Applicant: ARENA PHARM INC ,  STRAH-PLEYNET SONJA ,  TEEGARDEN BRADLEY ,  UNETT DAVID J

    Inventor： STRAH-PLEYNET SONJA ,  TEEGARDEN BRADLEY ,  UNETT DAVID J

    IPC: C07D231/38 ,  A61K31/415 ,  A61P25/00 ,  C07D401/12

    CPC classification number: C07D231/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    Abstract: The present invention relates to certain 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 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, 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 mediated disorders in combination with other pharmaceutical agents administered separately or together.

    Abstract translation: 本发明涉及式（Ia）的某些吡唑衍生物及其调节5-HT2A 5-羟色胺受体活性的药物组合物。 化合物及其药物组合物涉及可用于治疗血小板聚集，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-羟色胺受体介导的病症的方法。

    ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    7.
    发明申请
    ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    作为用于治疗相关疾病的5-HT2A硒同位素受体的调节剂的乙酰胺衍生物

    公开(公告)号：WO2007136875A2

    公开(公告)日：2007-11-29

    申请号：PCT/US2007/012230

    申请日：2007-05-17

    Applicant: ARENA PHARMACEUTICALS, INC. ,  TEEGARDEN, Bradley ,  FEICHTINGER, Konrad ,  STRAH-PLEYNET, Sonja ,  ULMANN, Brett ,  XIONG, Yifeng

    Inventor： TEEGARDEN, Bradley ,  FEICHTINGER, Konrad ,  STRAH-PLEYNET, Sonja ,  ULMANN, Brett ,  XIONG, Yifeng

    CPC classification number: C07D231/16 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-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.

    Abstract translation: 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。

    DIARYLAMINE AND ARYLHETEROARYLAMINE PYRAZOLE DERIVATIVES AS MODULATORS OF 5HT2A
    9.
    发明申请
    DIARYLAMINE AND ARYLHETEROARYLAMINE PYRAZOLE DERIVATIVES AS MODULATORS OF 5HT2A 审中-公开
    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

    Applicant: ARENA PHARMACEUTICALS, INC. ,  TEEGARDEN, Bradley ,  JAYAKUMAR, Honnappa ,  STRAH-PLEYNET, Sonja

    Inventor： TEEGARDEN, Bradley ,  JAYAKUMAR, Honnappa ,  STRAH-PLEYNET, Sonja

    IPC: C07D231/12

    CPC classification number: C07D231/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    Abstract: 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.

    Abstract translation: 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。

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