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1. 发明申请

WO2005077463A2 METHOD OF TREATING ADDICTION OR DEPENDENCE USING A LIGAND FOR A MONOAMINE RECEPTOR OR TRANSPORTER 审中-公开
标题翻译：使用配体对单胺受体或运输工具治疗接受或依赖的方法
公开(公告)号：WO2005077463A2
公开(公告)日：2005-08-25
申请号：PCT/US2005/003629
申请日：2005-02-04
申请人： SEPRACOR INC. , AQUILA, Brian, M. , BANNISTER, Thomas, D. , CUNY, Gregory, D. , HAUSKE, James, R. , HOLLAND, Joanne, M. , PERSONS, Paul, E. , RADEKE, Heike, S. , WANG, Fengjiang , SHAO, Liming
发明人： AQUILA, Brian, M. , BANNISTER, Thomas, D. , CUNY, Gregory, D. , HAUSKE, James, R. , HOLLAND, Joanne, M. , PERSONS, Paul, E. , RADEKE, Heike, S. , WANG, Fengjiang , SHAO, Liming
IPC分类号： A61P25/30
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 therapeutically 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

WO2002083071A3 HETEROCYCLIC ANALGESIC COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2002083071A3
公开(公告)日：2002-10-24
申请号：PCT/US2002/011618
申请日：2002-04-11
申请人： SEPRACOR, INC.
发明人： AQUILA, Brian, M. , HAUSKE, James, R. , SHAO, Liming
IPC分类号： C07D211/26
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 cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocylic compounds as analgesics.

3. 发明申请

WO2003016274A2 2-SUBSTITUTED PIPERIDINES THAT ARE LIGANDS FOR MONOAMINE RECEPTORS AND TRANSPORTERS 审中-公开
标题翻译：单取代哌啶为单胺类受体和转运蛋白的配体
公开(公告)号：WO2003016274A2
公开(公告)日：2003-02-27
申请号：PCT/US2002/027087
申请日：2002-08-06
申请人： SEPRACOR, INC.
发明人： HAUSKE, James, R. , AQUILA, Brian, M.
IPC分类号： C07D
CPC分类号： C07D241/04 , C07D211/12 , C07D211/14 , C07D211/16 , C07D211/22
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, 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 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，血清素或去甲肾上腺素转运蛋白）的配体的用途。本发明化合物可用于治疗患有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，阿尔茨海默氏病，肥胖症，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，月经烦躁症，尿失禁，炎性疼痛，神经性疼痛，Lesche-Nyhane病，威尔逊氏病和图雷特综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及例如在基于多巴胺转运蛋白的测定中筛选那些文库的生物学活性。

4. 发明申请

WO2002069895A3 HETEROCYCLIC ANALGESIC COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2002069895A3
公开(公告)日：2002-09-12
申请号：PCT/US2002/006274
申请日：2002-03-01
申请人： SEPRACOR, INC.
发明人： AQUILA, Brian, M. , BANNISTER, Thomas, D. , CUNY, Gregory, D. , HAUSKE, James, R. , HEFFERMAN, Michele, L. , SHAO, Liming , WANG, Fengjian , WU, Xinhe
IPC分类号： C07D211/32
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 cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

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