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    • 2. 发明申请
    • SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
    • 作为OREXIN受体拮抗剂的替代制剂/哌啶
    • WO2015123355A1
    • 2015-08-20
    • PCT/US2015/015500
    • 2015-02-11
    • EOLAS THERAPEUTICS, INC.
    • KAMENECKA, Theodore, M.HE, YuanjunJIANG, RongNGUYEN, WilliamSONG, XinyiHERR, Robert, JasonBARNES, KeithYOUNG, Steven, D.JIANG, Qin
    • C07D211/04C07D209/02A61K31/445C07D277/02
    • C07D417/14C07D401/12C07D413/14C07D417/12
    • The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX 1 or OX 2 , or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention. For example, orexin receptor- modulatory compounds of the present invention can be used in treatment of an eating disorder, obesity, alcoholism or an alcohol-related disorder, drug abuse or addiction including addiction to cocaine, opiates, amphetamines, or nicotine, a sleep disorder, a cognitive dysfunction in a psychiatric or neurologic disorder, depression, anxiety, post-traumatic stress disorder, seasonal affective disorder, an eating disorder, panic disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, headache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases, cancer, hypertension, behavior disorder, mood disorder, manic depression, dementia, sex disorder, psychosexual disorder, or renal disease.
    • 本发明涉及调节食欲肽受体如OX1或OX2或两者的生物活性的化合物; 涉及包含本发明化合物的药物组合物和组合; 涉及食管蛋白受体调节在医学上指示的患者中的病情治疗方法; 以及制备本发明化合物的方法。 例如,本发明的食欲素受体调节化合物可用于治疗进食障碍,肥胖,酒精中毒或酒精相关疾病,药物滥用或成瘾,包括对可卡因,阿片剂,苯丙胺或尼古丁的成瘾,睡眠 精神病或神经障碍的认知功能障碍,抑郁症,焦虑症,创伤后应激障碍,季节性情感障碍,进食障碍,恐慌症,精神分裂症,阿尔茨海默病,帕金森病,亨廷顿舞蹈病,头痛,偏头痛,疼痛, 胃肠道疾病,癫痫,炎症,免疫相关疾病,内分泌相关疾病,癌症,高血压,行为障碍,情绪障碍,躁狂抑郁,痴呆,性障碍,心理性功能障碍或肾脏疾病。