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1. 发明授权

US07087623B2 Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof 有权
公开(公告)号：US07087623B2
公开(公告)日：2006-08-08
申请号：US10786612
申请日：2004-02-25
申请人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
发明人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
IPC分类号： A61K31/445 , C07D401/00
CPC分类号： C07D271/07 , C07D277/42 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors. 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 addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, senile dementia, peptic ulcers, pulmonary obstruction disorders, and asthma.

2. 发明申请

US20050038011A1 Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof 有权
标题翻译：用于σ受体的螺环配体，以及文库及其使用方法
公开(公告)号：US20050038011A1
公开(公告)日：2005-02-17
申请号：US10890408
申请日：2004-07-13
申请人： Heike Radeke , Paul Persons , James Hauske
发明人： Heike Radeke , Paul Persons , James Hauske
IPC分类号： A61P25/00 , C07B61/00 , C07D471/10 , A61K31/55 , A61K31/4747
CPC分类号： C07D471/10 , C40B40/00
摘要： One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.
摘要翻译：本发明的一个方面涉及螺环化合物。本发明的另一方面涉及螺环化合物作为哺乳动物G蛋白偶联受体或σ受体的配体的用途。本发明还涉及使用本发明的螺环化合物调节哺乳动物中G蛋白偶联受体或σ受体的活性的方法。本发明还涉及使用本发明的螺环化合物治疗哺乳动物中各种疾病的方法。

3. 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。

4. 发明申请

US20060194785A1 Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof 审中-公开
公开(公告)号：US20060194785A1
公开(公告)日：2006-08-31
申请号：US11343077
申请日：2006-01-30
申请人： Heike Radeke , Paul Persons , James Hauske
发明人： Heike Radeke , Paul Persons , James Hauske
IPC分类号： C07D487/10 , A61K31/55 , A61K31/4747
CPC分类号： C07D471/10 , C40B40/00
摘要： One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.

5. 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。

6. 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。

7. 发明申请

US20050191238A1 Contrast agents for myocardial perfusion imaging 有权
公开(公告)号：US20050191238A1
公开(公告)日：2005-09-01
申请号：US11055498
申请日：2005-02-10
申请人： David Casebier , Simon Robinson , Ajay Purohit , Heike Radeke , Michael Azure , Douglas Dischino
发明人： David Casebier , Simon Robinson , Ajay Purohit , Heike Radeke , Michael Azure , Douglas Dischino
IPC分类号： A61K49/00 , A61K51/00
CPC分类号： C07D237/16 , A61K49/00 , A61K49/0002 , A61K49/0052 , A61K49/10 , A61K49/22 , A61K51/04 , A61K51/0421 , A61K51/0453 , A61K51/0459 , C07B59/002
摘要： The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

8. 发明授权

US06713479B2 Piperidine-piperazine ligands for neurotransmitter receptors 有权
标题翻译：用于神经递质受体的哌啶 - 哌嗪配体
公开(公告)号：US06713479B2
公开(公告)日：2004-03-30
申请号：US10087609
申请日：2002-03-01
申请人： Paul E. Persons , Heike Radeke
发明人： Paul E. Persons , Heike Radeke
IPC分类号： A61K31496
CPC分类号： C07D211/26
摘要： One aspect of the present invention relates to piperidine-piperazine compounds generically represented by A. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. 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, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, 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 piperidine-piperazine compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine receptors or transporters or both.
摘要翻译：本发明的一个方面涉及通常由A表示的哌啶 - 哌嗪化合物。本发明的第二方面涉及哌啶 - 哌嗪化合物作为各种哺乳动物细胞受体或转运蛋白或两者的配体的用途，包括多巴胺，5-羟色胺或去甲肾上腺素受体或转运蛋白，它们的任何组合，或它们的全部组合。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，镇痛，精神分裂症，帕金森病，不宁腿综合征，睡眠障碍，注意缺陷多动障碍，肠易激综合征，早泄，月经性烦躁综合征，尿失禁，炎性疼痛，神经性疼痛，莱氏阴道炎，威尔逊氏病和图雷特综合征。本发明的另一方面涉及哌啶 - 哌嗪化合物的组合文库的合成，以及这些文库的生物活性的筛选，例如在基于多巴胺受体或转运蛋白或两者的测定中。

9. 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。

10. 发明授权

US06699866B2 Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof 有权
标题翻译：噻唑和其他哺乳动物多巴胺，毒蕈碱和5-羟色胺受体和转运蛋白的杂环配体及其使用方法
公开(公告)号：US06699866B2
公开(公告)日：2004-03-02
申请号：US10123089
申请日：2002-04-12
申请人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
发明人： Gregory D. Cuny , James R. Hauske , Michele L. R. Heffernan , Joanne M. Holland , Paul E. Persons , Heike Radeke
IPC分类号： A61K31535
CPC分类号： C07D271/07 , C07D277/42 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors. 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 addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, senile dementia, peptic ulcers, pulmonary obstruction disorders, and asthma.
摘要翻译：本发明的一个方面涉及新的杂环化合物。本发明的第二方面涉及新型杂环化合物作为各种哺乳动物细胞受体（包括G蛋白偶联受体）的配体的用途。本发明的第三方面涉及新型杂环化合物作为哺乳动物多巴胺，毒蕈碱或血清素受体或转运蛋白的配体的用途。本发明的另一方面涉及新型杂环化合物作为哺乳动物多巴胺，毒蕈碱或血清素受体的配体的用途。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，镇痛，精神分裂症，帕金森病，不宁腿综合征，睡眠障碍，注意力缺陷多动障碍，肠易激综合征，早泄，月经性烦躁综合征，尿失禁，炎性疼痛，神经性疼痛，Lesche-Nyhane疾病，Wilson氏病，Tourette综合征，精神障碍，中风，老年痴呆，消化性溃疡，肺梗阻障碍和哮喘。

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