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1. 发明申请

WO2016069875A1 COMPOSITIONS AND METHODS FOR CEASING TOBACCO SMOKING 审中-公开
标题翻译：烟草吸烟的组合物和方法
公开(公告)号：WO2016069875A1
公开(公告)日：2016-05-06
申请号：PCT/US2015/058016
申请日：2015-10-29
申请人： ARENA PHARMACEUTICALS, INC.
发明人： BEHAN, Dominic P. , GLICKLICH, Alan , GROTTICK, Andrew J. , KAM, Maria Matilde Sanchez , SHANAHAN, William R.
IPC分类号： A61K45/06 , A61K31/55 , A61P25/34 , A61K31/135 , A61K31/137 , A61K31/4168 , A61K9/28
CPC分类号： A61K31/55 , A61K9/2054 , A61K31/135 , A61K31/137 , A61K31/4168 , A61K45/06 , A61K2300/00
摘要： Provided are compositions comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate, or hydrate thereof, 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 (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate, or hydrate thereof, optionally in combination with a supplemental agent.
摘要翻译：提供了包含（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂或其药学上可接受的盐，溶剂化物或水合物的组合物，任选地与补充剂组合以及减少试图减少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/或戒断的个人中治疗尼古丁依赖，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（R）-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂或其药学上可接受的盐，溶剂合物或水合物，任选地与补充剂组合。

2. 发明申请

WO2015066344A1 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： 5-HT2C受体激动剂及其组合物和使用方法
公开(公告)号：WO2015066344A1
公开(公告)日：2015-05-07
申请号：PCT/US2014/063191
申请日：2014-10-30
申请人： ARENA PHARMACEUTICALS, INC.
发明人： SEMPLE, Graeme , BEHAN, Dominic P. , FEICHTINGER, Konrad , GLICKLICH, Alan , GROTTICK, Andrew J. , KAM, Maria Matilde Sanchez , KASEM, Michelle , LEHMANN, Juerg , REN, Albert S. , SCHRADER, Thomas O. , SHANAHAN, William R. , WONG, Amy Siu-Ting , ZHU, Xiuwen
IPC分类号： A61K31/5517 , C07D487/06 , A61P25/30 , A61P25/34 , A61P3/04
CPC分类号： A61K31/5517 , C07D487/06
摘要： 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.
摘要翻译：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。

3. 发明申请

WO2016112075A1 METHODS OF TREATING CONDITIONS RELATED TO THE S1P1 RECEPTOR 审中-公开
标题翻译：治疗与S1P1受体有关的病症的方法
公开(公告)号：WO2016112075A1
公开(公告)日：2016-07-14
申请号：PCT/US2016/012289
申请日：2016-01-06
申请人： ARENA PHARMACEUTICALS, INC.
发明人： GLICKLICH, Alan , KAM, Maria Matilde Sanchez , SHANAHAN, William R.
IPC分类号： A61K31/473 , A61P37/00 , A61P29/00
CPC分类号： A61K31/403 , A61K9/4825
摘要： Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P 1 ) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[ b ]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to about 1.5 to about 2.5 mg of Compound 1, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, ankylosing spondylitis, biliary cirrhosis, cancer, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, inflammatory bowel disease, ulcerative colitis, type I diabetes, hypertensive nephropathy, glomerulosclerosis, myocardial ischemia-reperfusion injury, and acne.
摘要翻译：提供了治疗1-磷酸鞘磷脂亚型1（S1P1）受体相关疾病的方法，包括向有需要的个体处方和/或施用标准剂量的（R）-2-（7-（4-环戊基 - 3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸（化合物1）或其药学上可接受的盐，水合物或溶剂合物，约1.5至约2.5mg化合物1，例如由淋巴细胞介导的疾病或病症，自身免疫性疾病或病症，炎症性疾病或病症，强直性脊柱炎，胆汁性肝硬化，癌症，牛皮癣，银屑病关节炎，类风湿性关节炎，克罗恩氏病疾病，移植排斥，多发性硬化，系统性红斑狼疮，炎性肠病，溃疡性结肠炎，I型糖尿病，高血压性肾病，肾小球硬化，心肌缺血再灌注损伤和痤疮。

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