公开(公告)号：EP1761508A1

公开(公告)日：2007-03-14

申请号：EP05787985.0

申请日：2005-06-30

申请人： WISYS TECHNOLOGY FOUNDATION, INC.

发明人： COOK, James, M. ,  ZHOU, Hao ,  HUANG, Shengming ,  SARMA, P.V.V.S. ,  ZHANG, Chunchun

IPC分类号： C07D243/16 ,  C07D243/24 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14 ,  A61K31/5517 ,  A61P25/22

CPC分类号： C07D243/24 ,  C07D243/16 ,  C07D471/06 ,  C07D487/04 ,  C07D487/06

摘要： The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-XXI and a pharmaceutically-acceptable carrier.

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.