公开(公告)号：EP2365973A1

公开(公告)日：2011-09-21

申请号：EP09752667.7

申请日：2009-11-11

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  GREENLEE, William, J. ,  LI, Hongmei ,  VICAREL, Monica, L. ,  QIN, Jun ,  DHONDI, Pawan, Kumar ,  HUANG, Xianhai ,  PALANI, Anandan ,  LIU, Xiaoxiang ,  SUN, Zhong-Yue ,  JOSIEN, Hubert B. ,  XU, Ruo ,  COLE, David, James ,  BURNETT, Duane, A. ,  BENNETT, Chad, E. ,  MCCRACKEN, Troy, M. ,  MACCOSS, Malcolm

IPC分类号： C07D409/14 ,  C07D413/10 ,  C07D498/04 ,  C07D498/14 ,  C07D498/20 ,  A61K31/5395 ,  A61K31/553 ,  A61P25/28

CPC分类号： C07D498/04 ,  C07D409/14 ,  C07D413/10 ,  C07D498/14 ,  C07D498/20

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

公开(公告)号：EP2217604A1

公开(公告)日：2010-08-18

申请号：EP08848226.0

申请日：2008-11-03

申请人： Schering Corporation

发明人： GREENLEE, William J. ,  ZHU, Zhaoning ,  ASBEROM, Theodros ,  HUANG, Xianhai ,  JOSIEN, Hubert B.

IPC分类号： C07D487/10 ,  C07D487/20 ,  C07D493/20 ,  C07D495/20 ,  C07D498/10 ,  C07D498/20 ,  C07D498/22 ,  C07F7/08 ,  C07F9/6571

CPC分类号： C07D498/10 ,  C07D487/10 ,  C07D487/20 ,  C07D493/20 ,  C07D495/20 ,  C07D498/20 ,  C07D498/22 ,  C07F7/0812 ,  C07F9/657181

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

公开(公告)号：EP1789404B1

公开(公告)日：2010-03-24

申请号：EP05790194.4

申请日：2005-06-28

申请人： Schering Corporation

发明人： JOSIEN, Hubert B. ,  CLADER, John W. ,  BARA, Thomas A. ,  XU, Ruo ,  LI, Hongmei ,  PISSARNITSKI, Dmitri ,  ZHAO, Zhiqiang

IPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08 ,  A61K31/5377 ,  A61P25/28

CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

公开(公告)号：EP1789404A2

公开(公告)日：2007-05-30

申请号：EP05790194.4

申请日：2005-06-28

申请人： SCHERING CORPORATION

发明人： JOSIEN, Hubert B. ,  CLADER, John W. ,  BARA, Thomas A. ,  XU, Ruo ,  LI, Hongmei ,  PISSARNITSKI, Dmitri ,  ZHAO, Zhiqiang

IPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08 ,  A61K31/5377 ,  A61P25/28

CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.