公开(公告)号：EP1318988A2

公开(公告)日：2003-06-18

申请号：EP01970926.0

申请日：2001-09-12

申请人： Sepracor, Inc.

发明人： AQUILA, Brian, M. ,  BANNISTER, Thomas, D. ,  CUNY, Gregory, D. ,  HAUSKE, James, R. ,  HOLLAND, Joanne, M. ,  PERSONS, Paul, E. ,  RADEKE, Heike ,  WANG, Fengjian ,  SHAO, Liming

IPC分类号： C07D295/16

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 formula A; whereof the substituents are defined in the description. 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 aliments, 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，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，肥胖症，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。

公开(公告)号：EP1976513A2

公开(公告)日：2008-10-08

申请号：EP07716419.2

申请日：2007-01-05

申请人： SEPRACOR, INC.

发明人： SHAO, Liming ,  WANG, Fengjiang ,  MALCOLM, Scott, Christopher ,  HEWITT, Michael, Charles ,  BUSH, Larry, R. ,  MA, Jianguo ,  VARNEY, Mark, A. ,  CAMPBELL, Una ,  ENGEL, Sharon, Rae ,  HARDY, Larry, Wendell ,  KOCH, Patrick ,  CAMPBELL, John, E.

IPC分类号： A61K31/381 ,  A61K31/335

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，以及抑制来自突触裂缝的内源性单胺如多巴胺，5-羟色胺和去甲肾上腺素的再摄取的方法以及调节一种或多种单胺转运蛋白的方法。

公开(公告)号：EP2154962A1

公开(公告)日：2010-02-24

申请号：EP08756635.2

申请日：2008-06-02

申请人： Sepracor Inc.

发明人： SHAO, Liming ,  WANG, Fengjiang ,  MALCOLM, Scott, Christopher ,  HEWITT, Michael, Charles ,  MA, Jianguo ,  RIBE, Seth ,  VARNEY, Mark, A. ,  CAMPBELL, Una ,  ENGEL, Sharon, Rae ,  HARDY, Larry, Wendell ,  KOCH, Patrick ,  SCHREIBER, Rudy ,  SPEAR, Kerry, L.

IPC分类号： A01N43/00

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（例如来自突触裂缝）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。

公开(公告)号：EP1978961A2

公开(公告)日：2008-10-15

申请号：EP06848050.8

申请日：2006-12-21

申请人： SEPRACOR, INC.

发明人： SHAO, Liming ,  WANG, Fengjiang ,  MALCOLM, Scott, Christopher ,  HEWITT, Michael, Charles ,  BUSH, Larry, R. ,  VARNEY, Mark ,  CAMPBELL, Una ,  ENGEL, Sharon, Rae ,  HARDY, Larry, Wendell ,  KOCH, Patrick ,  MA, Jianguo

IPC分类号： A61K31/4706

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.

公开(公告)号：EP1187810A2

公开(公告)日：2002-03-20

申请号：EP00937830.8

申请日：2000-05-25

申请人： SEPRACOR, INC.

发明人： CUNY, Gregory, D. ,  SHAO, Liming ,  HAUSKE, James, R. ,  HEFFERNAN, Michele, L., R. ,  AQUILA, Brian, M. ,  WU, Xinhe ,  WANG, Fengjian ,  BANNISTER, Thomas, D.

IPC分类号： C07D211/26 ,  C07D211/60 ,  C07D211/56 ,  C07D241/04 ,  C07D265/30 ,  C07D267/10 ,  C07D223/04 ,  C07D223/12 ,  C07D243/06 ,  C07D205/04 ,  C07D207/09 ,  C07D207/16 ,  C07D491/10 ,  A61K31/445 ,  A61K31/397 ,  A61K31/40 ,  A61K31/535 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61P25/04

CPC分类号： C07D221/04 ,  C07D205/04 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D223/04 ,  C07D241/04 ,  C07D243/08 ,  C07D265/30 ,  C07D267/10 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D491/10

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 the 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.