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1. 发明申请

WO2006081335A2 PROCESSES FOR PREPARING SUBSTITUTED PHENYLPYRAZOLE UREAS 审中-公开
标题翻译：制备取代的苯基脲的方法
公开(公告)号：WO2006081335A2
公开(公告)日：2006-08-03
申请号：PCT/US2006/002721
申请日：2006-01-25
申请人： ARENA PHARMACEUTICALS, INC. , GHARBAOUI, Tawfik , AVERBUJ, Claudia , CARLOS, Marlon V. , LALLY, Edward A. , SENGUPTA, Dipanjan , FRITCH, John R.
发明人： GHARBAOUI, Tawfik , AVERBUJ, Claudia , CARLOS, Marlon V. , LALLY, Edward A. , SENGUPTA, Dipanjan , FRITCH, John R.
IPC分类号： C07D231/16
CPC分类号： C07D231/16
摘要： The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.
摘要翻译：本发明涉及用于制备用作治疗疾病的5-HT2A 5-羟色胺受体调节剂的式（I）的取代的苯基吡唑脲的方法。

2. 发明申请

WO2009111004A1 PROCESSES FOR THE PREPARATION OF INTERMEDIATES RELATED TO THE 5-HT2C AGONIST (R)-8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE 审中-公开
标题翻译：制备与5-羟色胺-8-CH-1-甲基-2,3,4,5-四氢-1H-苯并恶唑相关的中间体的方法
公开(公告)号：WO2009111004A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/001340
申请日：2009-03-03
申请人： ARENA PHARMACEUTICALS, INC. , CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
发明人： CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
IPC分类号： C07C17/16 , C07C215/08 , C07C209/68 , C07C211/29 , C07D223/16
CPC分类号： C07C209/74 , C07C17/16 , C07C17/38 , C07C213/08 , C07C25/02 , C07C211/29 , C07C215/08
摘要： The present invention provides processes and intermediates useful in the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H -3-benzazepine, a serotonin (5-HT) receptor agonist that is useful in the treatment or prophylaxis of, for example, central nervous system disorders, such as obesity.
摘要翻译：本发明提供了可用于制备8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因的方法和中间体，5-羟色胺（5-HT）受体激动剂可用于治疗或预防例如中枢神经系统疾病，例如肥胖症。

3. 发明申请

WO2010062321A1 PROCESSES USEFUL FOR THE PREPARATION OF 1-[3-(4-BROMO-2-METHYL-2H-PYRAZOL-3-YL)-4-METHOXY-PHENYL]-3-(2,4-DIFLUORO-PHENYL)-UREA AND CRYSTALLINE FORMS RELATED THERETO 审中-公开
标题翻译：用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基苯基] -3-（2,4-二氟苯基） - 乙烯的方法和与其相关的晶体形式
公开(公告)号：WO2010062321A1
公开(公告)日：2010-06-03
申请号：PCT/US2009/005809
申请日：2009-10-27
申请人： ARENA PHARMACEUTICALS, INC. , CARLOS, Marlon V. , DONG, Weitong , MACIAS, Mark , SATO, Suzanne Michiko , SILVEY, Gary
发明人： CARLOS, Marlon V. , DONG, Weitong , MACIAS, Mark , SATO, Suzanne Michiko , SILVEY, Gary
IPC分类号： C07D231/16
CPC分类号： A61K31/415 , C07D231/12 , C07D231/16
摘要： The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
摘要翻译：本发明涉及可用于制备1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4 - 二氟 - 苯基） - 脲（化合物I），其结晶形式和溶剂合物形式; 和包含1- [3-（4-溴-2-甲基-2H-吡唑-3-基）-4-甲氧基 - 苯基] -3-（2,4-二氟 - 苯基） - 脲的结晶的组合物，其通过如本文所述的方法制备的溶剂合物形式。

4. 发明申请

WO2010062323A2 COMPOSITIONS OF A 5-HT2A SEROTONIN RECEPTOR MODULATOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗与其有关的病症的5-HT2A血清素受体调节剂的组合物
公开(公告)号：WO2010062323A2
公开(公告)日：2010-06-03
申请号：PCT/US2009/005811
申请日：2009-10-27
申请人： ARENA PHARMACEUTICALS, INC. , SILVEY, Gary L. , CARLOS, Marlon V. , MAFFUID, Paul , SHAN, Yun
发明人： SILVEY, Gary L. , CARLOS, Marlon V. , MAFFUID, Paul , SHAN, Yun
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , A61K9/1635 , A61K9/2027 , A61K9/2054 , C07D231/16
摘要： The present invention relates to certain compositions of a 5-HT 2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating 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 la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.
摘要翻译：本发明涉及5-HT 2 A 5-羟色胺受体调节剂的某些组合物及其制备方法。本文公开的组合物可用于增加慢波睡眠，改善睡眠巩固，改善睡眠维持和改善睡眠质量，并用于治疗失眠和相关的睡眠障碍，睡眠异常，异嗜睡和非消除性睡眠等。本文公开的组合物还用于治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房纤颤，血栓形成，哮喘或其症状，激动或其症状，行为障碍，药物诱导的精神病，兴奋抽动秽语综合征，狂躁症，机体或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精神分裂症和相关障碍，糖尿病相关障碍和进行性多灶性白质脑病等等。

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