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：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.