公开(公告)号：EP2043745A2

公开(公告)日：2009-04-08

申请号：EP07759776.3

申请日：2007-03-30

申请人： SEPRACOR Inc

发明人： TARANTINO, Paul ,  CAMPBELL, Una ,  BUSH, Larry

IPC分类号： A61P25/00 ,  A61P25/06

CPC分类号： A61K31/135 ,  A61K31/165

摘要： Treatment of pain disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful in treatment of pain disorders.

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：EP2300470A2

公开(公告)日：2011-03-30

申请号：EP09751384.0

申请日：2009-05-19

申请人： Sepracor Inc.

发明人： FANG, Qun, Kevin ,  WU, Frank, Xinhe ,  GROVER, Paul, T. ,  HOPKINS, Seth, C. ,  CAMPBELL, Una ,  CHYTIL, Milan ,  SPEAR, Kerry, L.

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. Many of the compounds disclosed herein may be represented by the following generic formula: in which Y is a direct bond or heteroatom and A3 is usually a nitrogenous heterocycle.

摘要翻译： 公开了咪唑并[1,2-a]吡啶。 本发明的化合物是有用的治疗剂，并且它们包括在药物制剂中并用于治疗方法中。 本文公开的许多化合物可以由以下通式表示：其中Y是直接键或杂原子，A3通常是含氮杂环。

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。