公开(公告)号：EP1888594A2

公开(公告)日：2008-02-20

申请号：EP06813185.3

申请日：2006-05-16

申请人： WISYS TECHNOLOGY FOUNDATION, INC.

发明人： COOK, James M. ,  HAN, Dongmei ,  CLAYTON, Terry

IPC分类号： C07D497/04 ,  C07D487/14 ,  A61K31/5517 ,  A61P25/28

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D519/00

摘要： The present invention provides imidazobenzodiazepine derivatives and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognizance. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.

公开(公告)号：EP1490344B1

公开(公告)日：2008-03-19

申请号：EP03723846.6

申请日：2003-03-28

申请人： Wisys Technology Foundation, Inc.

发明人： COOK, James, M. ,  HUANG, Qi ,  HE, Xiaohui ,  LI, Xioayan ,  YU, Jianming ,  HAN, Dongmei ,  LELAS, Snjezana ,  MCELROY, John, F.

IPC分类号： C07D243/14 ,  C07D243/18 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14 ,  A61K31/5513 ,  A61P25/22

CPC分类号： C07D471/04 ,  C07D243/12 ,  C07D243/20 ,  C07D243/24 ,  C07D487/04 ,  C07D487/06 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D519/00

摘要： Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects. Compounds of e.g. the following formula (I) are disclosed, wherein Y and Z are taken together with the two intervening carbon atoms to form a ring selected from phenyl and thienyl, which ring is substituted at the C(7) position with at least the substituent -C≡C-R where R is H, Si (CH3)3, t-butyl, isopropyl, methyl, or cyclopropyl; R1 is one of H, CH3, C2H4N (C2H5)2, CH2CF3, CH2CCH, or an alkyl cyclopropyl; R2 is a substituted or unsubstituted at least partially unsaturated 5 or 6 membered cyclic or heterocyclic ring, wherein if substituted the substituent is one or more of F, Cl, Br, or NO2 at the 2’ - position; R3 is one of H, OH, OCON(CH3)2, COOCH3, or COOC2H5.

公开(公告)号：EP1490344A2

公开(公告)日：2004-12-29

申请号：EP03723846.6

申请日：2003-03-28

申请人： Wisys Technology Foundation, Inc.

发明人： COOK, James, M. ,  HUANG, Qi ,  HE, Xiaohui ,  LI, Xioayan ,  YU, Jianming ,  HAN, Dongmei ,  LELAS, Snjezana ,  MCELROY, John, F.

IPC分类号： C07D243/14 ,  C07D243/18 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14 ,  A61K31/5513 ,  A61P25/22

CPC分类号： C07D471/04 ,  C07D243/12 ,  C07D243/20 ,  C07D243/24 ,  C07D487/04 ,  C07D487/06 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D519/00

摘要： Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects. Compounds of e.g. the following formula (I) are disclosed, wherein Y and Z are taken together with the two intervening carbon atoms to form a ring selected from phenyl and thienyl, which ring is substituted at the C(7) position with at least the substituent -C≡C-R where R is H, Si (CH3)3, t-butyl, isopropyl, methyl, or cyclopropyl; R1 is one of H, CH3, C2H4N (C2H5)2, CH2CF3, CH2CCH, or an alkyl cyclopropyl; R2 is a substituted or unsubstituted at least partially unsaturated 5 or 6 membered cyclic or heterocyclic ring, wherein if substituted the substituent is one or more of F, Cl, Br, or NO2 at the 2’ - position; R3 is one of H, OH, OCON(CH3)2, COOCH3, or COOC2H5.