公开(公告)号：EP2173170A2

公开(公告)日：2010-04-14

申请号：EP08796893.9

申请日：2008-07-30

申请人： Sepracor Inc.

发明人： HEFFERNAN, Michele, L.R. ,  DORSEY, James, M. ,  FANG, Qun, Kevin ,  FOGLESONG, Robert, J. ,  HOPKINS, Seth, C. ,  OGBU, Cyprian, O. ,  SOUKRI, Mustapha ,  SPEAR, Kerry, L.

IPC分类号： A01N43/16 ,  A61K31/35

CPC分类号： A61K31/407 ,  C07D491/04 ,  C07D495/04

摘要： This invention provides fused heterocycles having the formula: in which R
1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R
2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R
3 is a member selected from the group consisting of H
1 C
1 -C
6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R
4 is a member selected from OH and O
- X
+ , in which X
+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4. Formulae A, B.

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：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：EP2074092A2

公开(公告)日：2009-07-01

申请号：EP08727954.3

申请日：2008-01-18

申请人： Sepracor Inc.

发明人： HEFFERNAN, Michele, L.R. ,  FANG, Qun, Kevin ,  FOGLESONG, Robert, J. ,  HOPKINS, Seth, C. ,  OGBU, Cyprian, O. ,  SOUKRI, Mustapha ,  SPEAR, Kerry, L.

IPC分类号： C07D209/42 ,  C07D491/04 ,  C07D495/04 ,  A61K31/403 ,  A61P25/00

CPC分类号： C07D209/52 ,  C07D209/42 ,  C07D209/94 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  G01N21/253 ,  G01N21/255 ,  G01N21/3151

摘要： The present invention provides novel inhibitors of the enzyme D- amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/ or conditions, wherein modulation of D- serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatry diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

公开(公告)号：EP2057162A2

公开(公告)日：2009-05-13

申请号：EP07796659.6

申请日：2007-07-02

申请人： Sepracor Inc.

发明人： DORSEY, James, M. ,  HOPKINS, Seth, C. ,  FOGLESONG, Robert, J. ,  HEFFERNAN, Michele, L.r. ,  JONES, Michael, L. ,  PERALES, Joseph, B. ,  FANG, Qun, Kevin ,  OGBU, Cyprian, O. ,  JONES, Steven, W. ,  SOUKRI, Mustapha ,  VARNEY, Mark, A. ,  SPEAR, Kerry, L.

IPC分类号： C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/381 ,  A61K31/407 ,  A61K31/429 ,  A61K31/4162 ,  A61P25/00

CPC分类号： C07D491/04 ,  C07D495/04

摘要： This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure wherein Q is a member selected from O, S, CR1 and N, X and Y are members independently selected from CR2, O, S, N and NR3.