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    DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
    1.
    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
    2.
    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。

    PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    3.
    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：US20130217700A1

    公开(公告)日：2013-08-22

    申请号：US13614537

    申请日：2012-09-13

    申请人： Yifeng Xiong ,  Martin C. Cherrier ,  Jin Sun Karoline Choi ,  Peter I. Dosa ,  Brian M. Smith ,  Sonja Strah-Pleynet ,  Brett Ullman ,  Bradley Teegarden

    发明人： Yifeng Xiong ,  Martin C. Cherrier ,  Jin Sun Karoline Choi ,  Peter I. Dosa ,  Brian M. Smith ,  Sonja Strah-Pleynet ,  Brett Ullman ,  Bradley Teegarden

    IPC分类号： C07D231/14 ,  C07D403/06 ,  C07D405/04 ,  C07D403/12

    CPC分类号： C07D231/16 ,  C07D231/14 ,  C07D231/54 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04

    摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A 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 la 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-IIT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

    摘要翻译： 式（Ia）的吡唑衍生物及其药物组合物，其调节5-羟色胺5HT2A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，精神分裂症及相关疾病，以及其他症状，症状或症状，激动或其症状，行为障碍，药物诱发的精神病，兴奋性精神病， 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-IIT2A 5-羟色胺受体介导的病症的方法。

    Cannabinoid receptor modulators
    5.
    发明授权
    Cannabinoid receptor modulators 有权
    大麻素受体调节剂

    公开(公告)号：US08778950B2

    公开(公告)日：2014-07-15

    申请号：US13392074

    申请日：2010-08-27

    申请人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    发明人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    IPC分类号： A61K31/4965 ,  A01N43/56 ,  A61K31/415 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D231/54 ,  C07D487/00

    CPC分类号： C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

    摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

    摘要翻译： 本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。 本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于 与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏 异常性疼痛 炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受 骨质疏松症 多发性硬化相关性痉挛状态; 自身免疫性疾病 过敏反应; CNS炎症; 动脉粥样硬化 不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

    Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
    8.
    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
    10.
    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。