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.