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    • 9. 发明申请
    • 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE
    • 5-HT2C受体激动剂及其组合物和使用方法
    • WO2017023679A1
    • 2017-02-09
    • PCT/US2016/044426
    • 2016-07-28
    • ARENA PHARMACEUTICALS, INC.
    • LEHMANN, JuergFEICHTINGER, KonradREN, Albert S.SEMPLE, Graeme
    • C07D223/16C07D223/32C07D491/052A61K31/55A61P3/04
    • C07D223/16C07D223/32C07D491/052
    • Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.
    • 在一些实施方案中提供了调节5-HT 2C受体活性的式A定义的化合物。 在一些实施方案中还提供了一些方法,例如用于体重管理,诱导饱腹感和减少食物摄取,以及用于预防和治疗肥胖,抗精神病药物引起的体重增加,2型糖尿病,Prader-Willi综合征,烟草/尼古丁依赖性, 吸毒成瘾,酒精成瘾,病态赌博,奖励缺乏综合征和性成瘾),强迫症频谱障碍和冲动控制障碍(包括指甲和精神病),睡眠障碍(包括失眠,分散的睡眠结构和慢性紊乱 睡眠障碍),尿失禁,精神障碍(包括精神分裂症,神经性厌食症和神经性贪食症),阿尔茨海默病,性功能障碍,勃起功能障碍,癫痫,运动障碍(包括帕金森综合征和抗精神病诱发的运动障碍),高血压,血脂异常, 非酒精性脂肪性肝病,肥胖相关性肾病和睡眠呼吸暂停。
    • 10. 发明申请
    • 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE
    • 5-HT2C受体激动剂及其组合物和使用方法
    • WO2015066344A1
    • 2015-05-07
    • PCT/US2014/063191
    • 2014-10-30
    • ARENA PHARMACEUTICALS, INC.
    • SEMPLE, GraemeBEHAN, Dominic P.FEICHTINGER, KonradGLICKLICH, AlanGROTTICK, Andrew J.KAM, Maria Matilde SanchezKASEM, MichelleLEHMANN, JuergREN, Albert S.SCHRADER, Thomas O.SHANAHAN, William R.WONG, Amy Siu-TingZHU, Xiuwen
    • A61K31/5517C07D487/06A61P25/30A61P25/34A61P3/04
    • A61K31/5517C07D487/06
    • Provided are 5-HT 2C receptor agonists. Also provided are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea. Also provided are compositions comprising a selective 5-HT 2C receptor agonist, optionally in combination with a supplemental agent, and methods for reducing the frequency of smoking tobacco in an individual attempting to reduce frequency of smoking tobacco; aiding in the cessation or lessening of use of a tobacco product in an individual attempting to cease or lessen use of a tobacco product; aiding in smoking cessation and preventing associated weight gain; controlling weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; reducing weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; treating nicotine dependency, addiction and/or withdrawal in an individual attempting to treat nicotine dependency, addiction and/or withdrawal; or reducing the likelihood of relapse use of nicotine by an individual attempting to cease nicotine use comprising administering a selective 5-HT 2C receptor agonist, optionally in combination with a supplemental agent.
    • 提供5-HT 2C受体激动剂。 还提供了用于体重管理,诱导饱腹感和减少食物摄入以及预防和治疗肥胖,抗精神病药物引起的体重增加,2型糖尿病,Prader-Willi综合征,烟草/尼古丁依赖,药物成瘾,酒精成瘾,病理学 赌博,奖励缺陷综合征和性成瘾),强迫性频谱障碍和冲动控制障碍(包括指甲和精神病),睡眠障碍(包括失眠,零散睡眠结构和慢波睡眠障碍),尿失禁 ,精神障碍(包括精神分裂症,神经性厌食和神经性贪食),阿尔茨海默病,性功能障碍,勃起功能障碍,癫痫,运动障碍(包括帕金森综合征和抗精神病诱发的运动障碍),高血压,血脂异常,非酒精性脂肪性肝病, 相关的肾脏疾病和睡眠呼吸暂停。 还提供了包含选择性5-HT 2C受体激动剂,任选地与补充剂组合的组合物,以及降低试图降低吸烟频率的个体吸烟的频率的方法; 协助在试图停止或减少使用烟草制品的个人中停止或减少使用烟草制品; 协助戒烟和预防相关体重增加; 控制一个企图停止吸烟的个人与戒烟相关的体重增加; 减轻试图戒烟的个人与戒烟相关的体重增加; 在试图治​​疗尼古丁依赖,成瘾和/或戒断的个体中治疗尼古丁依赖,成瘾和/或戒断; 或减少试图停止尼古丁使用的个体复发使用尼古丁的可能性,包括施用选择性的5-HT 2C受体激动剂,任选地与补充剂组合。