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1. 发明公开

EP2190844A2 IMIDAZO[L,2-a]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：咪唑并[1,2-a]吡啶衍生物作为参与与相关疾病CONNECTION的治疗5-HT 2A血清素受体调节剂的适合
公开(公告)号：EP2190844A2
公开(公告)日：2010-06-02
申请号：EP08795334.5
申请日：2008-08-14
申请人： Arena Pharmaceuticals, Inc.
发明人： XIONG, Yifeng , FEICHTINGER, Konrad , REN, Albert, S. , ULMANN, Brett
IPC分类号： C07D471/04 , A61K31/437 , A61P25/20
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： rmidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）和药物组合物的rmidazo [1,2-α]吡啶衍生物及其做调节5-HT 2A血清素受体的活性。化合物及其药物组合物涉及在失眠，睡眠障碍，深眠状态的治疗有用的方法和相关的睡眠障碍，血小板聚集，冠状动脉病，心肌梗塞，短暂性缺血发作，心绞痛，中风，心房纤维性颤动，血栓形成，哮喘或症状物，搅动或其症状，行为障碍，药物诱发的精神病，兴奋型精神病，图雷特氏综合征，躁狂性障碍，器质性或NOS精神病，精神障碍，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关病症，diabetic- 相关的疾病，进行性多灶性白质脑病等。因此，本发明涉及一种用于与分开或一起给药其它药物试剂联合治疗5-HT 2A血清素受体介导的病症的方法。

2. 发明公开

EP2051978A2 ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：的乙酰胺衍生物作为5-HT 2A血清素受体用于疾病治疗有关的调节剂
公开(公告)号：EP2051978A2
公开(公告)日：2009-04-29
申请号：EP07809149.3
申请日：2007-05-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , FEICHTINGER, Konrad , STRAH-PLEYNET, Sonja , ULLMAN, Brett , XIONG, Yifeng
IPC分类号： C07D413/12 , C07D213/12 , C07D401/12 , C07D403/12 , C07D407/14 , A61K31/415
CPC分类号： C07D231/16 , C07D231/12 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

3. 发明授权

EP1833799B1 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT-2a SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译： 3-苯基 - 吡唑衍生物作为治疗相关的病症的5-HT-2A血清素受体的调节剂
公开(公告)号：EP1833799B1
公开(公告)日：2008-09-10
申请号：EP05849546.6
申请日：2005-11-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , XIONG, Yifeng , STRAH-PLEYNET, Sonja , JAYAKUMAR, Honnappa , DOSA, Peter I. , FEICHTINGER, Konrad , CASPER, Martin , LEHMANN, Juerg , JONES, Robert M. , UNETT, David J. , CHOI, Jin, Sun, Karoline
IPC分类号： C07D231/16
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, 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, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

4. 发明公开

EP3395816A1 ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：EP3395816A1
公开(公告)日：2018-10-31
申请号：EP18164223.2
申请日：2007-05-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , CHAPMAN, Dennis , DECAIRE, Marc , DOSA, Peter I. , FEICHTINGER, Konrad , JAYAKUMAR, Honnappa , STRAH-PLEYNET, Sonja , TRAN, Thuy-Anh , XU, Jingdong
IPC分类号： C07D413/12 , C07D231/12 , C07D231/16 , C07D403/12 , C07D411/12 , A61K31/42 , A61K31/4192 , A61K31/427 , A61K31/454 , A61P7/02 , A61P9/10 , A61P25/00
CPC分类号： C07D231/12 , A61K31/415 , C07D207/335 , C07D207/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , Y02A50/415
摘要： The present invention pertains to certain compounds of Formula ( Ia ) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor.

Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

5. 发明授权

EP2018371B1 PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权转让
标题翻译：伯胺及其衍生物的5-HT 2A血清素受体用于治疗相关疾病的调节剂
公开(公告)号：EP2018371B1
公开(公告)日：2015-03-04
申请号：EP07777120.2
申请日：2007-05-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , CHAPMAN, Dennis , CHOI, Juyi , FEICHTINGER, Konrad , HAN, Sangdon , JAYAKUMAR, Honnappa , TRAN, Thuy-Anh , XU, Jingdong , ZOU, Ning
IPC分类号： C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/4155 , A61P7/00
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12

6. 发明公开

EP1833799A2 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT-2a SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译： 3-苯基 - 吡唑衍生物作为治疗相关的病症的5-HT-2A血清素受体的调节剂
公开(公告)号：EP1833799A2
公开(公告)日：2007-09-19
申请号：EP05849546.6
申请日：2005-11-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , XIONG, Yifeng , STRAH-PLEYNET, Sonja , JAYAKUMAR, Honnappa , DOSA, Peter I. , FEICHTINGER, Konrad , CASPER, Martin , LEHMANN, Juerg , JONES, Robert M. , UNETT, David J. , CHOI, Jin, Sun, Karoline
IPC分类号： C07D231/16
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, 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, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

7. 发明授权

EP2190844B1 IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：咪唑并[1,2-a]吡啶衍生物作为参与与相关疾病CONNECTION的治疗5-HT 2A血清素受体调节剂的适合
公开(公告)号：EP2190844B1
公开(公告)日：2013-04-10
申请号：EP08795334.5
申请日：2008-08-14
申请人： Arena Pharmaceuticals, Inc.
发明人： XIONG, Yifeng , FEICHTINGER, Konrad , REN, Albert, S. , ULMANN, Brett
IPC分类号： C07D471/04 , A61K31/437 , A61P25/20
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： rmidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

8. 发明公开

EP2018371A1 PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权转让
标题翻译：伯胺及其衍生物的5-HT 2A血清素受体用于治疗相关疾病的调节剂
公开(公告)号：EP2018371A1
公开(公告)日：2009-01-28
申请号：EP07777120.2
申请日：2007-05-17
申请人： Arena Pharmaceuticals, Inc.
发明人： TEEGARDEN, Bradley , CHAPMAN, Dennis , CHOI, Juyi , FEICHTINGER, Konrad , HAN, Sangdon , JAYAKUMAR, Honnappa , TRAN, Thuy-Anh , XU, Jingdong , ZOU, Ning
IPC分类号： C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/4155 , A61P7/00
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, 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, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

9. 发明公开

EP3328835A1 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE 有权转让
公开(公告)号：EP3328835A1
公开(公告)日：2018-06-06
申请号：EP16751083.3
申请日：2016-07-28
申请人： Arena Pharmaceuticals, Inc.
发明人： LEHMANN, Juerg , FEICHTINGER, Konrad , REN, Albert S. , SEMPLE, Graeme
IPC分类号： C07D223/16 , C07D223/32 , C07D491/052 , A61K31/55 , A61P3/04
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.

10. 发明授权

EP2190844B3 IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权
标题翻译：咪唑[1,2-A]吡啶衍生物作为用于治疗与其有关的病症的5-HT2A血清素受体调节剂
公开(公告)号：EP2190844B3
公开(公告)日：2013-07-17
申请号：EP08795334.5
申请日：2008-08-14
申请人： Arena Pharmaceuticals, Inc.
发明人： XIONG, Yifeng , FEICHTINGER, Konrad , REN, Albert, S. , ULMANN, Brett
IPC分类号： C07D471/04 , A61K31/437 , A61P25/20
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： rmidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

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