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公开(公告)号：US08153621B2
公开(公告)日：2012-04-10
申请号：US11793941
申请日：2005-12-21
IPC分类号： A61K31/55
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译： 本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。 此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。 这些组合物可用于其用途包括治疗肥胖症的药物组合物中。
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公开(公告)号：US20090197868A1
公开(公告)日：2009-08-06
申请号：US11793941
申请日：2005-12-21
IPC分类号： A61K31/55 , A61K31/137 , A61K31/495
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译： 本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。 此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。 这些组合物可用于其用途包括治疗肥胖症的药物组合物中。
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3.发明申请MODULATORS OF THE HISTAMINE H3 RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开用于治疗相关疾病的组胺H3受体的调节剂公开(公告)号：US20100331312A1
公开(公告)日：2010-12-30
申请号：US12867570
申请日：2009-02-18
申请人： Vincent J. Santora , Brian J. Hofilena , Michelle Pulley , Graeme Semple , Yun Shan , Brian M. Smith
发明人： Vincent J. Santora , Brian J. Hofilena , Michelle Pulley , Graeme Semple , Yun Shan , Brian M. Smith
IPC分类号： A61K31/55 , C07D401/10 , C07D403/10 , A61P25/08 , A61P25/24 , A61P3/04 , A61P25/18 , A61P25/28 , A61P11/02 , A61K31/506 , C07D401/14 , A61K31/4725
CPC分类号： C07D401/10 , C07D217/14 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/14
摘要： Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
摘要翻译： 式（Ia）的酰胺衍生物及其药物组合物，其调节组胺H3受体的活性。 本发明化合物及其药物组合物涉及可用于治疗组胺H3相关疾病如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症如白天过度嗜睡，发作性睡病的方法 ，换班工作睡眠障碍，作为药物副作用的嗜睡，维持警惕以帮助完成任务等，猝倒，睡眠过多，嗜睡综合征，时差，睡眠呼吸暂停等，注意力缺陷多动障碍 （ADHD），精神分裂症，过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默病，疼痛等。
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4.发明申请N-Biaryl and N-Arylheteroaryl Piperazine Derivatives as Modulators of the 5Ht2c Receptor Useful For the Treatment of Disorders Related Thereto 审中-公开N-二芳基和N-芳基杂芳基哌嗪衍生物作为用于治疗相关疾病的5Ht2c受体的调节剂公开(公告)号：US20080119477A1
公开(公告)日：2008-05-22
申请号：US11792894
申请日：2005-12-09
申请人： Brian M. Smith , Vincent J. Santora , Rena Hayashi , Jason B. Ibarra , Jeffrey A. Schultz , Scott A. Estrada
发明人： Brian M. Smith , Vincent J. Santora , Rena Hayashi , Jason B. Ibarra , Jeffrey A. Schultz , Scott A. Estrada
IPC分类号： A61K31/496 , A61K31/495 , C07D409/02 , C07D403/02 , C07D405/02
CPC分类号： C07D295/073 , C07D213/38 , C07D295/096 , C07D307/52 , C07D333/20
摘要： The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.
摘要翻译： 本发明涉及作为5HT 2C受体的调节剂的式（Ia）的某些双芳基和芳基杂芳基哌嗪衍生物。 因此，本发明的化合物可用于治疗5HT 2C受体相关疾病或病症，例如肥胖症，阿尔茨海默病，勃起功能障碍和相关疾病。
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公开(公告)号：US08546378B2
公开(公告)日：2013-10-01
申请号：US13418151
申请日：2012-03-12
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译： 本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。 此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。 这些组合物可用于其用途包括治疗肥胖症的药物组合物中。
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公开(公告)号：US20120252786A1
公开(公告)日：2012-10-04
申请号：US13418151
申请日：2012-03-12
CPC分类号： A61K31/55 , A61K31/135 , A61K31/137
摘要： The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
摘要翻译： 本发明涉及包含苯丁胺和选择性5HT-2C受体激动剂的组合物。 此外，本发明涉及包含苯丁胺和具有式（I）的选择性5HT-2C受体激动剂或其药学上可接受的盐，溶剂合物或水合物的组合物。 这些组合物可用于其用途包括治疗肥胖症的药物组合物中。
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7.发明申请5-Ht6 Receptor and Modulators Thereof for the Treatment of Insulin-Related Disorders 审中-公开5-Ht6受体及其调节剂用于治疗胰岛素相关性疾病公开(公告)号：US20110319451A1
公开(公告)日：2011-12-29
申请号：US13055128
申请日：2009-07-22
申请人： James N. Leonard , Zhi-Liang Chu , Brian M. Smith
发明人： James N. Leonard , Zhi-Liang Chu , Brian M. Smith
CPC分类号： G01N33/942 , G01N2333/62 , G01N2500/04 , G01N2800/042
摘要： The present invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT6 receptor, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a single dose of a candidate compound with a 5-HT6 receptor, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT6 receptor in an isolated cell, b) determining whether 5-HT6 receptor functionality is increased, and c) determining whether a glycemic marker is directly modulated, where an increase in 5-HT6 receptor functionality and direct modulation of a glycemic marker identifies the candidate compound as the glycemic stabilizing compound.
摘要翻译： 本发明涉及通过以下方式来鉴定血糖稳定化合物的方法：a）使候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c）确定血糖标志物是否为 直接调节，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物鉴定为血糖稳定化合物。 此外，本发明涉及通过以下方式鉴定血糖稳定化合物的方法：a）使单剂量的候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c） 确定血糖标志物是否被直接调节，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物识别为血糖稳定化合物。 此外，本发明涉及通过以下方式鉴定血糖稳定化合物的方法：a）在分离的细胞中使候选化合物与5-HT 6受体接触，b）确定5-HT 6受体功能是否增加，以及c）确定 是否直接调节血糖标志物，其中5-HT 6受体功能的增加和血糖标志物的直接调节将候选化合物鉴定为血糖稳定化合物。
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8.发明申请BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开用于治疗相关疾病的组胺H3受体的联苯磺隆和苯并噻吩磺酸盐调节剂公开(公告)号：US20100240653A1
公开(公告)日：2010-09-23
申请号：US12445795
申请日：2007-10-16
申请人： Vincent J. Santora , Ryan M. Hart , Jason B. Ibarra , Douglas M. Park , Albert S. Ren , Graeme Semple , Jeffrey A. Schultz , Brian M. Smith , Jeffrey Smith
发明人： Vincent J. Santora , Ryan M. Hart , Jason B. Ibarra , Douglas M. Park , Albert S. Ren , Graeme Semple , Jeffrey A. Schultz , Brian M. Smith , Jeffrey Smith
IPC分类号： A61K31/4025 , A61K31/5377 , A61K31/506 , A61K31/454 , A61K31/4439 , A61K31/40 , C07D413/12 , C07D403/10 , C07D401/12 , C07D401/10 , C07D409/10 , C07D207/06 , A61P25/28 , C07D405/10 , A61P25/00 , A61P25/24 , A61P3/04 , A61P25/18 , A61P37/08 , A61P11/00
CPC分类号： C07D207/06 , C07D401/12 , C07D403/10 , C07D405/12 , C07D409/10 , C07D417/10
摘要： The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.
摘要翻译： 本发明涉及式（Ia）的某些联苯磺酰胺衍生物及其药物组合物，其调节组胺H3受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗组胺H3相关疾病例如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症如发作性睡眠， 工作综合征，作为药物副作用的睡意，维持警惕以完成任务等，猝倒，睡眠过多，嗜睡症，时差，睡眠呼吸暂停等，注意力缺陷多动障碍（ADHD），精神分裂症 过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默氏病等。
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9.发明申请PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权作为用于治疗与相关疾病相关的疾病的5-HT2A丝氨酸受体的调节剂的吡唑衍生物公开(公告)号：US20100004264A1
公开(公告)日：2010-01-07
申请号：US12444098
申请日：2007-10-02
申请人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： A61K31/497 , C07D403/06 , C07D403/14 , A61P25/20 , A61P7/02 , A61P7/12 , A61P9/12 , A61P29/00
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, 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 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 the 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）的吡唑衍生物及其药物组合物，其调节5-羟色胺5HT2A受体的活性。 式（Ia）。 化合物及其药物组合物涉及可用于治疗失眠和相关睡眠障碍，血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘的方法 精神病，精神病，精神分裂症，急性精神分裂症，慢性精神分裂症，精神分裂症，精神分裂症，精神分裂症及相关疾病，以及其它症状，症状或症状，激动或其症状，行为障碍，药物诱导的精神病，兴奋性精神病，Gilles de Ia Tourette综合征， 糖尿病相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体介导的病症的方法。
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10.发明申请N-Biaryl and N-Arylheteroaryl 2-Substituted Piperazine Derivatives as Modulators of the 5ht2c Receptor Useful for the Treatment of Disorders Related Thereto 审中-公开N-二芳基和N-芳基杂芳基2-取代的哌嗪衍生物作为用于治疗与其相关的疾病的5ht2c受体的调节剂公开(公告)号：US20080255137A1
公开(公告)日：2008-10-16
申请号：US11792742
申请日：2005-12-09
申请人： Brian M Smith , Vincent J. Santora , Rena Hayashi , Jason B. Ibarra , Jeffrey A. Schultz , Scott A. Estrada
发明人： Brian M Smith , Vincent J. Santora , Rena Hayashi , Jason B. Ibarra , Jeffrey A. Schultz , Scott A. Estrada
IPC分类号： A61K31/496 , C07D409/10 , C07D401/10 , C07D405/10 , C07D241/04 , A61P3/00 , A61P25/00
CPC分类号： C07D213/38 , C07D213/74 , C07D295/033 , C07D295/073 , C07D307/52 , C07D333/20
摘要： The present invention relates to certain N-biaryl and N-arylheteroaryl 2-substituted piperazine derivatives of Formula (Ia) that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2C receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.
摘要翻译： 本发明涉及作为5HT 2C受体的调节剂的式（Ia）的某些N-联芳基和N-芳基杂芳基2-取代的哌嗪衍生物。 因此，本发明的化合物可用于治疗5HT 2C受体相关疾病或障碍，如肥胖，阿尔茨海默病，勃起功能障碍和相关疾病。
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