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1. 发明授权

US07511073B2 Amines that inhibit a mammalian anandamide transporter, and methods of use thereof 有权
标题翻译：抑制哺乳动物anandamide转运蛋白的胺及其使用方法
公开(公告)号：US07511073B2
公开(公告)日：2009-03-31
申请号：US11439529
申请日：2006-05-23
申请人： Brian M. Aquila , Seth C. Hopkins , Curtis A. Lockshin , Fengjiang Wang
发明人： Brian M. Aquila , Seth C. Hopkins , Curtis A. Lockshin , Fengjiang Wang
IPC分类号： A61K31/34 , A61K31/135 , C07D307/04 , C07C211/03
CPC分类号： C40B40/04 , C07C217/58 , C07C2601/02 , C07D307/14 , C40B20/08 , C40B30/04 , C40B40/00 , C40B50/14
摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.
摘要翻译：本发明的一个方面涉及胺。本发明的第二方面涉及胺作为哺乳动物安非他明转运蛋白的抑制剂的用途。本发明的化合物还可用于治疗影响哺乳动物的许多疾病，病症和疾病，包括但不限于哮喘，神经性疼痛，持续性疼痛，炎性疼痛，多动症，高血压，脑缺血，帕金森病，痉挛性，Tourette综合征，精神分裂症，出血性休克，败血性休克，心脏休克，偏头痛，霍顿头痛，多发性硬化症，厌食症，艾滋病综合征，器官排斥反应，自身免疫性疾病，变态反应，关节炎，克罗恩病，恶性胶质瘤，神经变性疾病，亨廷顿病舞蹈病，青光眼，恶心，焦虑，精神病，注意力缺陷多动障碍，早泄和中风。本发明的另一方面涉及胺的组合文库，以及制备文库的方法。

2. 发明授权

US08669291B2 Phenyl substituted cycloalkylamines as monoamine reuptake inhibitors 有权
标题翻译：苯基取代的环烷基胺作为单胺再摄取抑制剂
公开(公告)号：US08669291B2
公开(公告)日：2014-03-11
申请号：US12131845
申请日：2008-06-02
申请人： 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
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： A61K31/133 , A61K31/135 , C07C211/17
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。

3. 发明申请

US20110313013A1 TRIPLE REUPTAKE INHIBITORS AND METHODS OF THEIR USE 有权
标题翻译：三倍体复制抑制剂及其使用方法
公开(公告)号：US20110313013A1
公开(公告)日：2011-12-22
申请号：US13139967
申请日：2009-12-15
申请人： Liming Shao , Fengjiang Wang , Scott C. Malcolm , Michael C. Hewitt
发明人： Liming Shao , Fengjiang Wang , Scott C. Malcolm , Michael C. Hewitt
IPC分类号： A61K31/403 , C07D209/44 , C12N5/071 , A61P25/16 , A61P25/24 , A61P25/18 , A61P25/22 , C07D209/52 , A61P25/00
CPC分类号： C07D209/44 , A61K31/4035 , C07D209/08 , C07D209/52
摘要： Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit uptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.
摘要翻译：本文提供的是双环化合物及其合成方法。本文提供的化合物可用于治疗，预防和/或管理各种神经障碍。本文提供的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吸收（例如，从突触裂缝）并调节一种或多种单胺转运蛋白。还提供了含有这些化合物的药物制剂。

4. 发明授权

US07816375B2 Ligands for monoamine receptors and transporters, and methods of use thereof 有权
标题翻译：单胺受体和转运蛋白的配体及其使用方法
公开(公告)号：US07816375B2
公开(公告)日：2010-10-19
申请号：US12403311
申请日：2009-03-12
申请人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
发明人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
IPC分类号： A61P25/00 , A61K31/445 , C07D211/00
CPC分类号： C40B40/04 , C07B2200/11 , C07C255/46 , C07C2601/04 , C07D205/02 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/12 , C07D211/16 , C07D211/18 , C07D211/20 , C07D211/26 , C07D211/32 , C07D211/40 , C07D211/42 , C07D211/60 , C07D233/04 , C07D233/10 , C07D265/30 , C07D267/10 , C07D303/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C40B30/04 , C40B50/14
摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
摘要翻译：本发明的一个方面涉及杂环化合物。本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

5. 发明申请

US20070197588A1 Tetralone-based monoamine reuptake inhibitors 有权
标题翻译：基于四氢萘酮的单胺再摄取抑制剂
公开(公告)号：US20070197588A1
公开(公告)日：2007-08-23
申请号：US11643190
申请日：2006-12-21
申请人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , Jianguo Ma
发明人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , Jianguo Ma
IPC分类号： A61K31/4706 , A61K31/137 , A61K31/135
CPC分类号： C07C211/40 , C07C17/16 , C07C17/35 , C07C45/38 , C07C45/52 , C07C45/63 , C07C45/67 , C07C45/68 , C07C45/74 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/44 , C07C217/74 , C07C2601/14 , C07C2602/10 , C07D215/12 , C07C25/22 , C07C22/04 , C07C47/453 , C07C49/67 , C07C49/697 , C07C49/255 , C07C49/755 , C07C49/683
摘要： The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
摘要翻译：本发明涉及新的四氢萘酮类胺及其用于治疗中枢神经系统（CNS）障碍，例如抑郁症，注意缺陷多动障碍（ADHD）和帕金森病。本发明还涉及含有本发明化合物和组合物的药物组合物以及抑制一种或多种单胺（例如多巴胺和去甲肾上腺素）从突触裂缝再摄取的方法，以及调节一种或多种单胺转运蛋白的方法。

6. 发明授权

US08592608B2 Triple reuptake inhibitors and methods of their use 有权
标题翻译：三重再摄取抑制剂及其使用方法
公开(公告)号：US08592608B2
公开(公告)日：2013-11-26
申请号：US13139967
申请日：2009-12-15
申请人： Liming Shao , Fengjiang Wang , Scott C. Malcolm , Michael C. Hewitt
发明人： Liming Shao , Fengjiang Wang , Scott C. Malcolm , Michael C. Hewitt
IPC分类号： C07D209/44 , C07D205/00 , C07D217/00 , C07D217/10 , A61K31/40 , A61K31/397 , A61K31/47
CPC分类号： C07D209/44 , A61K31/4035 , C07D209/08 , C07D209/52
摘要： Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit uptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.
摘要翻译：本文提供的是双环化合物及其合成方法。本文提供的化合物可用于治疗，预防和/或管理各种神经障碍。本文提供的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吸收（例如，从突触裂缝）并调节一种或多种单胺转运蛋白。还提供了含有这些化合物的药物制剂。

7. 发明申请

US20100190861A1 CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 有权
标题翻译：环丙基胺作为单胺类复制抑制剂
公开(公告)号：US20100190861A1
公开(公告)日：2010-07-29
申请号：US12688474
申请日：2010-01-15
申请人： 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. Campbell
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. Campbell
IPC分类号： A61K31/135 , C07C211/15 , C07C215/48 , A61P25/00 , A61P25/24
CPC分类号： C07D333/20 , C07C211/17 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/06 , C07D207/08 , C07D211/14 , C07D211/16 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056
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.
摘要翻译：本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。

8. 发明申请

US20090258901A1 LIGANDS FOR MONOAMINE RECEPTORS AND TRANSPORTERS, AND METHODS OF USE THEREOF 有权
标题翻译：单体受体和运输商的配体及其使用方法
公开(公告)号：US20090258901A1
公开(公告)日：2009-10-15
申请号：US12403311
申请日：2009-03-12
申请人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Ahao
发明人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Ahao
IPC分类号： A61K31/445 , C07D211/22 , C07D211/20 , A61P35/00
CPC分类号： C40B40/04 , C07B2200/11 , C07C255/46 , C07C2601/04 , C07D205/02 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/12 , C07D211/16 , C07D211/18 , C07D211/20 , C07D211/26 , C07D211/32 , C07D211/40 , C07D211/42 , C07D211/60 , C07D233/04 , C07D233/10 , C07D265/30 , C07D267/10 , C07D303/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C40B30/04 , C40B50/14
摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
摘要翻译：本发明的一个方面涉及杂环化合物。本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

9. 发明申请

US20090163593A1 AMINES THAT INHIBIT A MAMMALIAN ANANDAMIDE TRANSPORTER, AND METHODS OF USE THEREOF 有权
标题翻译：禁止使用马萨诸塞ANANDAMIDE运输机的氨基甲酸酯及其使用方法
公开(公告)号：US20090163593A1
公开(公告)日：2009-06-25
申请号：US12392981
申请日：2009-02-25
申请人： Brian M. Aquila , Seth C. Hopkins , Curtis A. Lockshin , Fengjiang Wang
发明人： Brian M. Aquila , Seth C. Hopkins , Curtis A. Lockshin , Fengjiang Wang
IPC分类号： A61K31/195 , A61K31/135
CPC分类号： C40B40/04 , C07C217/58 , C07C2601/02 , C07D307/14 , C40B20/08 , C40B30/04 , C40B40/00 , C40B50/14
摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.
摘要翻译：本发明的一个方面涉及胺。本发明的第二方面涉及胺作为哺乳动物安非他明转运蛋白的抑制剂的用途。本发明的化合物还可用于治疗影响哺乳动物的许多疾病，病症和疾病，包括但不限于哮喘，神经性疼痛，持续性疼痛，炎性疼痛，多动症，高血压，脑缺血，帕金森病，痉挛性，Tourette综合征，精神分裂症，出血性休克，败血性休克，心脏休克，偏头痛，霍顿头痛，多发性硬化症，厌食症，艾滋病综合征，器官排斥反应，自身免疫性疾病，变态反应，关节炎，克罗恩病，恶性胶质瘤，神经变性疾病，亨廷顿病舞蹈病，青光眼，恶心，焦虑，精神病，注意力缺陷多动障碍，早泄和中风。本发明的另一方面涉及胺的组合文库，以及制备文库的方法。

10. 发明申请

US20070203111A1 Cycloalkylamines as monoamine reuptake inhibitors 审中-公开
标题翻译：环烷基胺作为单胺再摄取抑制剂
公开(公告)号：US20070203111A1
公开(公告)日：2007-08-30
申请号：US11649927
申请日：2007-01-05
申请人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Jianguo Ma , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , John Campbell
发明人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Jianguo Ma , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , John Campbell
IPC分类号： A61K31/55 , A61K31/445 , A61K31/40 , A61K31/397 , A61K31/396 , C07D211/06 , C07D203/04 , C07D207/04
CPC分类号： C07D333/20 , C07C211/17 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/06 , C07D207/08 , C07D211/14 , C07D211/16 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056
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.
摘要翻译：本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。

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