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    Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
    2.
    发明申请
    Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a 审中-公开
    二芳胺和芳基杂芳基吡唑衍生物作为5ht2a的调节剂

    公开(公告)号：US20060229335A1

    公开(公告)日：2006-10-12

    申请号：US10540650

    申请日：2003-12-22

    申请人： Bradley Teegarden ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar

    发明人： Bradley Teegarden ,  Sonja Strah-Pleynet ,  Honnappa Jayakumar

    IPC分类号： A61K31/4709 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4178 ,  A61K31/415 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  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 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。

    DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
    3.
    发明申请
    DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 有权
    作为有用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：US20150073141A1

    公开(公告)日：2015-03-12

    申请号：US14332207

    申请日：2014-07-15

    申请人： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

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

    IPC分类号： C07D405/12 ,  C07D401/12 ,  C07D231/12

    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-HT2A 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-HT2A 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，哮喘或其症状的方法， 激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，杜蕾特勒杜勒特综合征，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。

    Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
    4.
    发明授权
    Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto 有权
    二芳基和芳基杂芳基脲衍生物作为可用于预防和治疗与之相关的疾病的5-HT2A 5-羟色胺受体的调节剂

    公开(公告)号：US08754238B2

    公开(公告)日：2014-06-17

    申请号：US10895789

    申请日：2004-07-21

    申请人： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter Ian Dosa

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

    IPC分类号： C07D231/12

    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-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or 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 and the like.The present invention also relates to the method of prophylaxis or treatment of 5-HT2A 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，哮喘或其症状的方法， 激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，杜蕾特勒杜勒特综合征，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。

    Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
    6.
    发明授权
    Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto 有权
    二芳基和芳基杂芳基脲衍生物作为可用于预防和治疗与之相关的疾病的5-HT2A 5-羟色胺受体的调节剂

    公开(公告)号：US08871797B2

    公开(公告)日：2014-10-28

    申请号：US13619137

    申请日：2012-09-14

    申请人： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

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

    IPC分类号： A61K31/415

    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-HT2A 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-HT2A 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，哮喘或其症状的方法， 激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，杜蕾特勒杜勒特综合征，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。