公开(公告)号：EP1007518A1

公开(公告)日：2000-06-14

申请号：EP98940980.0

申请日：1998-08-18

申请人： SEPRACOR, INC.

发明人： WANG, Fengjiang

IPC分类号： C07D277/60 ,  C07D277/62 ,  C07D277/68 ,  C07D277/80 ,  C07D263/52 ,  C07D263/60 ,  C07D413/00 ,  C07D498/00

CPC分类号： C07D263/52 ,  C07D277/64

摘要： Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.

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：EP1509489A1

公开(公告)日：2005-03-02

申请号：EP03736639.0

申请日：2003-05-15

申请人： Sepracor, Inc.

发明人： AQUILA, Brian, A. ,  HOPKINS, Seth ,  LOCKSHIN, Curtis, A. ,  WANG, Fengjiang

IPC分类号： C07C215/00 ,  C07C211/00

CPC分类号： C40B40/04 ,  C07C217/58 ,  C07C2601/02 ,  C07D307/14 ,  C40B20/08 ,  C40B30/04 ,  C40B40/00 ,  C40B50/14

摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. 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 asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson’s disease, spasticity. Tourette’s syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton’s headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn’s disease, malignant gliomas, neurodegenerative diseases, Huntington’s chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

摘要翻译： 本发明的一个方面涉及胺。 本发明的第二方面涉及胺作为哺乳动物花生四烯酸转运蛋白抑制剂的用途。 本发明的化合物还可用于治疗哺乳动物患病，包括但不限于哮喘，神经性疼痛，持续性疼痛，炎性疼痛，活动过度，高血压，脑缺血，帕金森病， 痉挛。 抽动秽语综合征，精神分裂症，失血性休克，败血性休克，心脏休克，偏头痛，霍顿氏头痛，多发性硬化症， 青光眼，恶心，焦虑症，精神病，注意力缺陷多动症，早泄和中风。 本发明的另一方面涉及胺的组合文库，以及制备文库的方法。

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。