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1. 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。

2. 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.

3. 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。

4. 发明申请

US20060063776A1 Piperidine-piperazine ligands for neurotransmitter receptors 有权
公开(公告)号：US20060063776A1
公开(公告)日：2006-03-23
申请号：US11215358
申请日：2005-08-29
申请人： Paul Persons , Heike Radeke
发明人： Paul Persons , Heike Radeke
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D211/26
摘要： One aspect of the present invention relates to piperidine-piperazine compounds. 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.

5. 发明申请

US20050080271A1 Peptidomimetic ligands for cellular receptors and ion channels 有权
标题翻译：肽模拟配体的细胞受体和离子通道
公开(公告)号：US20050080271A1
公开(公告)日：2005-04-14
申请号：US10203279
申请日：2001-02-27
申请人： Paul Persons , Joanne Holland , James Hauske
发明人： Paul Persons , Joanne Holland , James Hauske
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07D207/14 , C07D207/16 , C07D213/56 , C07D217/26 , C07D295/185 , C07D401/12 , A61K31/4025 , A61K31/40 , C07D207/22 , C07D43/02
CPC分类号： C07D295/185 , C07B2200/07 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07D207/14 , C07D207/16 , C07D213/56 , C07D217/26 , C07D401/12
摘要： One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize $gm-opioid receptors.
摘要翻译：本发明的一个方面涉及新的拟肽化合物。本发明的第二方面涉及新型拟肽化合物作为配体 - 激动剂或拮抗剂 - 用于各种细胞受体，例如G-蛋白偶联受体和阿片受体，以及各种细胞离子通道（例如钠和钙。在某些实施方案中，本发明的化合物优选或选择性地抑制钠离子或钙离子通道。在某些实施方案中，本发明的化合物优选地或选择性地激动或拮抗$ g阿片受体。在某些实施方案中，本发明的化合物优选地或选择性地抑制钠离子通道或钙离子通道，并且激动或拮抗$ g-阿片受体。

6. 发明申请

US20070093522A1 Peptidomimetic ligands for cellular receptors and ion channels 有权
标题翻译：肽模拟配体的细胞受体和离子通道
公开(公告)号：US20070093522A1
公开(公告)日：2007-04-26
申请号：US11512056
申请日：2006-08-29
申请人： Paul Persons , Joanne Holland , James Hauske
发明人： Paul Persons , Joanne Holland , James Hauske
IPC分类号： A61K31/4709 , C07D403/02 , C07D401/02
CPC分类号： C07D295/185 , C07B2200/07 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07D207/14 , C07D207/16 , C07D213/56 , C07D217/26 , C07D401/12
摘要： One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize μ opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize μ-opioid receptors.
摘要翻译：本发明的一个方面涉及新颖的肽模拟化合物。本发明的第二方面涉及新型拟肽化合物作为配体 - 激动剂或拮抗剂用于各种细胞受体，例如G-蛋白偶联受体和阿片受体，以及各种细胞离子通道（例如钠和钙。在某些实施方案中，本发明的化合物优选或选择性地抑制钠离子或钙离子通道。在某些实施方案中，本发明的化合物优选地或选择性地激动或拮抗μ阿片受体。在某些实施方案中，本发明的化合物优选地或选择性地抑制钠离子通道或钙离子通道并且激动或拮抗μ-阿片受体。

7. 发明申请

US20050182054A1 Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases 失效
标题翻译：抑制血小板衍生生长因子和/或p56lck酪氨酸激酶的喹啉和喹喔啉化合物
公开(公告)号：US20050182054A1
公开(公告)日：2005-08-18
申请号：US11043473
申请日：2005-01-25
申请人： Michael Myers , Alfred Spada , Paul Persons , Martin Maguire
发明人： Michael Myers , Alfred Spada , Paul Persons , Martin Maguire
IPC分类号： A61K31/47 , A61K31/498 , A61P9/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D215/20 , C07D215/38 , C07D241/44 , C07D241/52 , C07D241/54 , C07D403/04 , C07D405/12 , A61K31/5377 , C07D413/02
CPC分类号： C07D215/38 , C07D215/20 , C07D241/44 , C07D241/52 , C07D241/54 , C07D403/04 , C07D405/12
摘要： This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
摘要翻译：本发明涉及抑制血小板衍生生长因子酪氨酸激酶和/或Lck酪氨酸激酶的喹啉/喹喔啉化合物，包含这些化合物的药物组合物，以及这些化合物用于治疗患有或患有疾病/ 涉及细胞分化，增殖，细胞外基质产生或介体释放和/或T细胞活化和增殖的条件。

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