公开(公告)号：EP1674456A2

公开(公告)日：2006-06-28

申请号：EP05016160.3

申请日：2002-09-19

申请人： Sanofi-Aventis ,  Mitsubishi Pharma Corporation

发明人： Gallet, Thierry ,  Lardenois, Patrick ,  Lochead, Alistair ,  Marguerie, Séverine ,  Nedelec, Alain ,  Saady, Mourad ,  Slowinski, Franck ,  Yaiche, Philippe

IPC分类号： C07D213/60 ,  C07D213/50

CPC分类号： A01N43/90 ,  C07D213/50 ,  C07D213/60 ,  C07D487/04

摘要： The invention relates to 3-ketoester of formula (IV)
   
wherein R1 represents a 2, 3 or 4-pyridine ring optionally substituted by a C 3-6 cycloalkyl group, a C 1-4 alkyl group, a C 1-4 alkoxy group, a benzyl group or a halogen atom, R5 is an halogen atom and R is an alkyl.

摘要翻译： 本发明涉及式（IV）的3-酮酯，其中R 1表示任选被C 3-6环烷基取代的2,3或4-吡啶环，C 1-4烷基， C 1-4烷氧基，苄基或卤素原子，R 5为卤素原子，R为烷基。

公开(公告)号：EP1557417A1

公开(公告)日：2005-07-27

申请号：EP03293236.0

申请日：2003-12-19

申请人： Sanofi-Aventis ,  Mitsubishi Pharma Corporation

发明人： Chereze, Nathalie ,  Lochead, Alistair W. ,  Saady, Mourad ,  Slowinski, Franck ,  Yaiche, Philippe

IPC分类号： C07D487/04 ,  A61K31/505 ,  A61P25/28

CPC分类号： A61K31/527 ,  A61K31/397 ,  C07D487/04 ,  Y02P20/142

摘要： The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom;
Y represents a bond, a carbonyl group, a methylene group optionally substituted;
R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted;
R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted;
R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom;
R4 represents a hydrogen atom, a C 1-4 alkoxy carbonyl group, a C 1-6 alkyl group optionally substituted;
o and m represent 1 to 2;
n represents 0 to 3;
p represents 0 to 2; and
q represents 0 to 2.

The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.