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    • 9. 发明申请
    • Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
    • 二芳胺和芳基杂芳基吡唑衍生物作为5ht2a的调节剂
    • US20060229335A1
    • 2006-10-12
    • US10540650
    • 2003-12-22
    • Bradley TeegardenSonja Strah-PleynetHonnappa Jayakumar
    • Bradley TeegardenSonja Strah-PleynetHonnappa Jayakumar
    • A61K31/4709A61K31/428A61K31/423A61K31/4178A61K31/415C07D417/02C07D413/02C07D403/02C07D231/12
    • C07D231/12C07D401/12C07D403/12C07D405/12C07D413/12C07D417/12
    • 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.
    • 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。