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1. 发明授权

US07517892B2 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：US07517892B2
公开(公告)日：2009-04-14
申请号：US09951130
申请日：2001-09-12
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 , C07D401/00
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。

2. 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。

3. 发明授权

US07812035B2 4-substituted piperidines, and methods of use thereof 有权
标题翻译： 4-取代的哌啶，及其使用方法
公开(公告)号：US07812035B2
公开(公告)日：2010-10-12
申请号：US10317014
申请日：2002-12-11
申请人： Heike Radeke , Liming Shao
发明人： Heike Radeke , Liming Shao
IPC分类号： A61K31/445 , C07D211/44 , C07D211/22
CPC分类号： C07D211/62 , C07D211/22 , C07D211/46
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。

4. 发明授权

US06703383B2 Antipsychotic sulfonamide-heterocycles, and methods of use thereof 有权
标题翻译：抗精神病药磺酰胺 - 杂环，及其使用方法
公开(公告)号：US06703383B2
公开(公告)日：2004-03-09
申请号：US09951137
申请日：2001-09-12
申请人： Xinhe Wu , Brian M. Aquila , Liming Shao , Heike Radeke , Gregory D. Cuny , James R. Hauske , Roger L. Xie
发明人： Xinhe Wu , Brian M. Aquila , Liming Shao , Heike Radeke , Gregory D. Cuny , James R. Hauske , Roger L. Xie
IPC分类号： A61K3133
CPC分类号： C07D401/04 , C07D211/28 , C07D401/12 , C07D409/12
摘要： One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
摘要翻译：本发明的一个方面涉及包含磺酰胺部分的杂环化合物。本发明的第二方面涉及包含磺酰胺部分的杂环化合物在至少部分地由一种或多种GPCR或配体门控离子通道的异常活性引起的疾病，病痛或疾病的用途。本发明的另一方面涉及包含磺酰胺部分的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，例如在精神病的动物模型中。

5. 发明申请

US20050080078A1 Method of treating addiction or dependence using a ligand for a monoamine receptor or transporter 有权
标题翻译：使用单胺受体或转运蛋白配体治疗成瘾或依赖的方法
公开(公告)号：US20050080078A1
公开(公告)日：2005-04-14
申请号：US10771519
申请日：2004-02-04
申请人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Joanne Holland , Paul Persons , Heike Radeke , Fengjiang Wang , Liming Shao
发明人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Joanne Holland , Paul Persons , Heike Radeke , Fengjiang Wang , Liming Shao
IPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , C07B61/00 , C07C255/46 , 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 , A61K31/54 , A61K31/495 , A61K31/496 , A61K31/537
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , 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 , C40B40/04
摘要： One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.
摘要翻译：本发明的一个方面涉及一种治疗哺乳动物药物成瘾或药物依赖的方法，其包括向有需要的哺乳动物施用治疗有效量的杂环化合物，例如3-取代哌啶的步骤。在优选的实施方案中，本发明的方法治疗可卡因成瘾或甲基苯丙胺成瘾。

6. 发明授权

US06872716B2 Antipsychotic sulfonamide-heterocycles, and methods of use thereof 有权
标题翻译：抗精神病药磺酰胺 - 杂环，及其使用方法
公开(公告)号：US06872716B2
公开(公告)日：2005-03-29
申请号：US10766300
申请日：2004-01-28
申请人： Xinhe Wu , Brian M. Aquila , Liming Shao , Heike Radeke , Gregory D. Cuny , James R. Hauske , Roger L. Xie
发明人： Xinhe Wu , Brian M. Aquila , Liming Shao , Heike Radeke , Gregory D. Cuny , James R. Hauske , Roger L. Xie
IPC分类号： A61P25/00 , C07D211/28 , C07D401/04 , C07D401/12 , C07D409/12 , A61K31/44 , C07D211/00 , C07D401/00
CPC分类号： C07D401/04 , C07D211/28 , C07D401/12 , C07D409/12
摘要： One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
摘要翻译：本发明的一个方面涉及包含磺酰胺部分的杂环化合物。本发明的第二方面涉及包含磺酰胺部分的杂环化合物在至少部分地由一种或多种GPCR或配体门控离子通道的异常活性引起的疾病，病痛或疾病的用途。本发明的另一方面涉及包含磺酰胺部分的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，例如在精神病的动物模型中。

7. 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。

8. 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。

9. 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。

10. 发明申请

US20060211864A1 Methods for the stereoselective synthesis of substituted piperidines 失效
公开(公告)号：US20060211864A1
公开(公告)日：2006-09-21
申请号：US11364506
申请日：2006-02-28
申请人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Michele Heffernan , Michael Hoemann , Donald Kessler , Liming Shao , Xinhe Wu , Roger Xie
发明人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Michele Heffernan , Michael Hoemann , Donald Kessler , Liming Shao , Xinhe Wu , Roger Xie
IPC分类号： C07D211/06 , C07D211/60 , C07D211/26 , C07D211/28
CPC分类号： C07D211/22 , C07D211/26
摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

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