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公开(公告)号：US20220356172A1
公开(公告)日：2022-11-10
申请号：US17215759
申请日：2021-03-29
发明人： Kai Gerlach , Graeme Semple , Yifeng Xiong , Barbara Bertani , Marco Ferrara , Giacomo Fossati , Scott Hobson , Uta Friederike Lessel , Frank Runge , Ursula Mueller-Vieira , Julian Wippich
IPC分类号： C07D403/14
摘要： The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
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2.发明申请公开(公告)号：US20230131465A1
公开(公告)日：2023-04-27
申请号：US17941860
申请日：2022-09-09
发明人： Kai Gerlach , Daniela Gavina Berta , Marco Ferrara , Kirsten Gutsche , Ursula Mueller-Vieira , Scott Hobson , Frank Runge , Graeme Semple , Viktor Vintonyak , Yifeng Xiong
IPC分类号： A61K31/497 , C07D403/14 , C07D487/08 , C07D417/14 , A61K45/06 , A61K31/433
摘要： The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases.
In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.-
公开(公告)号：US20200078368A1
公开(公告)日：2020-03-12
申请号：US16299880
申请日：2019-03-12
IPC分类号： A61K31/55 , A61P25/08 , A61P3/10 , A61P3/04 , A61P25/32 , C07D491/052 , C07D223/32 , C07D223/16
摘要： 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.
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公开(公告)号：US10272094B2
公开(公告)日：2019-04-30
申请号：US15748205
申请日：2016-07-28
IPC分类号： C07D223/16 , C07D223/32 , C07D491/052 , A61K31/55 , A61P25/32 , A61P25/08 , A61P3/04 , A61P3/10
摘要： 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.
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公开(公告)号：US20180214455A1
公开(公告)日：2018-08-02
申请号：US15748205
申请日：2016-07-28
CPC分类号： A61K31/55 , A61K2121/00 , A61P3/04 , A61P3/10 , A61P25/08 , A61P25/32 , C07D223/16 , C07D223/32 , C07D491/052
摘要： 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.
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公开(公告)号：US11608339B2
公开(公告)日：2023-03-21
申请号：US17073458
申请日：2020-10-19
发明人： Graeme Semple , Albert S. Ren , Thomas O. Schrader , Michelle Kasem , Xiuwen Zhu
IPC分类号： C07D471/14 , A61P3/00
摘要： The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a 5-HT2C receptor-mediated disorder, such as, 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 and the like, obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders, 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 compound herein, optionally in combination with a supplemental agent.
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7.发明申请1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO 有权作为GPR52调节剂的1-HETEROARYL-INDOLINE-4-CARBOXAMIDES可用于治疗或预防相关疾病公开(公告)号：US20160318911A1
公开(公告)日：2016-11-03
申请号：US15143026
申请日：2016-04-29
发明人： Yifeng Xiong , Andrew J. Grottick , Henry Korman , Juerg Lehmann , Albert S. Ren , Graeme Semple
IPC分类号： C07D405/14 , C07D403/04 , C07D401/14 , C07D401/04
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g., posttraumatic stress disorder (PTSD)); a disruptive, impulse-control, or conduct disorder; a sleep-wake disorder; a substance-related disorder; an addictive disorder; a behavioral disorder; hypofrontality; an abnormality in the tuberoinfundibular, mesolimbic, mesocortical, or nigrostriatal pathway; decreased activity in the striatum; cortical dysfunction; neurocognitive dysfunction; and conditions related thereto
摘要翻译： 本发明涉及调节GPR52活性的式（Ia）化合物及其药物组合物。 本发明的化合物及其药物组合物涉及可用于治疗GPR52介导的病症（例如亨廷顿氏病，精神分裂症，双相情感障碍，注意缺陷多动障碍（ADHD）或图雷特综合征）的方法）。 锥体外系或运动障碍; 运动障碍 运动障碍; 精神障碍 紧张症; 情绪障碍 抑郁障碍 焦虑症 强迫症（OCD）; 自闭症谱系障碍 催乳素相关病症（例如高催乳素血症）; 神经认知障碍 创伤或压力相关障碍（如创伤后应激障碍（PTSD））; 破坏性，冲动控制或行为障碍; 睡眠障碍 物质相关疾病; 成瘾性障碍 行为障碍 次方数 结节性下颌，中脑边缘，中皮质或黑质纹状体通路异常; 纹状体活动减少; 皮质功能障碍 神经认知功能障碍 和相关条件
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公开(公告)号：US20230055376A1
公开(公告)日：2023-02-23
申请号：US17837622
申请日：2022-06-10
IPC分类号： A61K31/55 , C07D223/16 , C07D223/32 , C07D491/052 , A61P25/32 , A61P3/04 , A61P3/10 , A61P25/08
摘要： 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.
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公开(公告)号：US20210214355A1
公开(公告)日：2021-07-15
申请号：US17073458
申请日：2020-10-19
发明人： Graeme Semple , Albert S. Ren , Thomas O. Schrader , Michelle Kasem , Xiuwen Zhu
IPC分类号： C07D471/14 , A61P3/00
摘要： The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a 5-HT2C receptor-mediated disorder, such as, 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, chug addiction, alcohol addiction and the like, obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders, urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction,
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公开(公告)号：US10392390B2
公开(公告)日：2019-08-27
申请号：US15567116
申请日：2016-04-26
发明人： Albert S. Ren , Graeme Semple , Xiuwen Zhu , Carleton R. Sage
IPC分类号： C07D487/06 , C07D487/04 , A61P3/04
摘要： Provided in some embodiments are compounds herein. Also provided in some embodiments 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 in some embodiments are compositions comprising a compound herein, 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 compound herein, optionally in combination with a supplemental agent.
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