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1.发明申请COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF 审中-公开用于治疗由代谢谷氨酸受体5介导的疾病的化合物及其使用方法公开(公告)号：US20140349992A1
公开(公告)日：2014-11-27
申请号：US14299364
申请日：2014-06-09
发明人： Larry Wendell Hardy , Michele L.R. Heffernan , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D239/88 , C07D405/06 , C07D413/04 , C07D401/14 , C07D471/14 , C07D471/20 , C07D487/08 , C07D498/04 , C07D491/20 , C07D417/06 , C07D487/04
CPC分类号： C07D239/88 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/04 , C07D417/06 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/04 , C07D487/08 , C07D487/20 , C07D491/20 , C07D498/04
摘要： Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
摘要翻译： 本文提供的化合物及其合成方法。 本文所述的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍，神经变性疾病，神经精神障碍，认知障碍，学习或记忆障碍，胃肠道疾病，下尿路障碍和癌症 。 本文所述的化合物调节代谢型谷氨酸受体5（mGluR5）在中枢神经系统或周边的活性。 本文还提供了含有化合物及其使用方法的药物制剂。
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公开(公告)号：US11186564B2
公开(公告)日：2021-11-30
申请号：US16322278
申请日：2016-08-04
IPC分类号： C07D211/22 , C07D401/08 , C07D401/14 , C07D401/06 , C07D401/12 , C07D405/06 , C07D471/04 , C07D487/10 , C07D491/107 , C07D311/22 , C07D217/24 , C07D223/08 , C07D235/12 , C07D237/14 , C07D413/06 , C07D241/04 , C07D243/08 , C07D471/08 , C07D491/048 , C07D267/10 , C07D275/04 , C07D211/58 , C07D403/06 , C07D405/12 , A61P25/28 , C07D417/04 , A61P25/18 , C07D513/04 , C07D211/42 , C07D295/104 , C07D207/36 , C07D213/81 , C07D491/20 , C07D249/12 , C07D221/20 , C07D295/088 , C07D311/58 , C07D207/12 , C07D211/44 , C07D265/30 , C07D277/66 , C07D295/027 , C07D295/073 , C07D295/096 , C07D295/108 , C07D307/83 , C07D311/08 , C07D413/08 , C07D471/10
摘要： Compounds of formula I: are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
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公开(公告)号：US20180037585A1
公开(公告)日：2018-02-08
申请号：US15625604
申请日：2017-06-16
发明人： Michele L.R. Heffernan , Larry Wendell Hardy , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D487/04 , C07D498/04 , C07D491/22 , C07D491/20 , C07D491/147 , C07D487/18 , C07D487/14 , C07D471/20 , C07D471/14 , C07D487/10 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/10 , C07D487/14 , C07D487/18 , C07D491/147 , C07D491/20 , C07D491/22 , C07D498/04
摘要： Compounds that modulate GluR5 activity and methods of using the same are disclosed.
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公开(公告)号：US09708331B2
公开(公告)日：2017-07-18
申请号：US15013741
申请日：2016-02-02
发明人： Michele L. R. Heffernan , Larry Wendell Hardy , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D487/14 , C07D487/04 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/18 , C07D491/147 , C07D491/20 , C07D491/22 , C07D498/04 , C07D487/10
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/10 , C07D487/14 , C07D487/18 , C07D491/147 , C07D491/20 , C07D491/22 , C07D498/04
摘要： Compounds that modulate GluR5 activity and methods of using the same are disclosed.
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公开(公告)号：US10562878B2
公开(公告)日：2020-02-18
申请号：US15836261
申请日：2017-12-08
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campell
IPC分类号： C07D333/20 , C07C211/17 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07D207/06 , C07D207/08 , C07D211/14 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056 , C07C211/29 , C07D211/16
摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
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6.发明申请公开(公告)号：US20190055204A1
公开(公告)日：2019-02-21
申请号：US16107385
申请日：2018-08-21
发明人： Larry Wendell Hardy , Michele L.R. Heffernan , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D239/88 , C07D487/20 , C07D471/20 , C07D491/20 , C07D413/04 , C07D471/04 , C07D471/14 , C07D487/08 , C07D498/04 , C07D417/06 , C07D487/04 , C07D401/14 , C07D405/06 , C07D403/06
摘要： Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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公开(公告)号：US20190135815A1
公开(公告)日：2019-05-09
申请号：US16211338
申请日：2018-12-06
发明人： Michele L.R. Heffernan , Larry Wendell Hardy , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D487/04 , C07D487/10 , C07D498/04 , C07D491/22 , C07D491/20 , C07D471/04 , C07D487/18 , C07D487/14 , C07D471/20 , C07D471/14 , C07D491/147
摘要： Compounds that modulate GluR5 activity and methods of using the same are disclosed.
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公开(公告)号：US10196399B2
公开(公告)日：2019-02-05
申请号：US15625604
申请日：2017-06-16
发明人： Michele L. R. Heffernan , Larry Wendell Hardy , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/14 , C07D487/18 , C07D491/147 , C07D491/20 , C07D491/22 , C07D498/04 , C07D487/10
摘要： Compounds that modulate GluR5 activity and methods of using the same are disclosed.
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公开(公告)号：US10077243B2
公开(公告)日：2018-09-18
申请号：US14299364
申请日：2014-06-09
发明人： Larry Wendell Hardy , Michele L. R. Heffernan , Frank Xinhe Wu , Lakshmi D. Saraswat , Kerry L. Spear
IPC分类号： A61K31/517 , C07D487/04 , C07D239/88 , C07D403/06 , C07D405/06 , C07D417/06 , C07D471/04 , C07D487/20 , C07D401/14 , C07D413/04 , C07D471/14 , C07D471/20 , C07D487/08 , C07D491/20 , C07D498/04
CPC分类号： C07D239/88 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/04 , C07D417/06 , C07D471/04 , C07D471/14 , C07D471/20 , C07D487/04 , C07D487/08 , C07D487/20 , C07D491/20 , C07D498/04
摘要： Provided herein are compounds of formula (I): and pharmaceutical compositions thereof, useful for the treatment of disorders mediated by metabotropic glutamate receptor 5.
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10.发明授权公开(公告)号：US09586888B2
公开(公告)日：2017-03-07
申请号：US14149492
申请日：2014-01-07
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Jianguo Ma , Seth Ribe , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , Rudy Schreiber , Kerry L. Spear
IPC分类号： C07C215/42 , C07C217/52 , C07C217/76 , A61K31/135
CPC分类号： C07C215/42 , A61K31/135 , A61P25/24 , A61P25/28 , C07B2200/07 , C07C217/52 , C07C217/76 , C07C2601/14
摘要： Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
摘要翻译： 公开了苯基取代的环己胺衍生物及其合成和表征的方法。 本文阐述了这些化合物治疗/预防神经系统疾病及其合成方法的用途。 本发明的示例性化合物抑制内源性单胺如多巴胺，5-羟色胺和去甲肾上腺素的再摄取（例如，从突触腭裂）并调节一种或多种单胺转运蛋白。 还提供了掺入本发明化合物的药物制剂。
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