公开(公告)号：EP2948429A1

公开(公告)日：2015-12-02

申请号：EP14702219.8

申请日：2014-01-24

申请人： INSA (Institut National des Sciences Appliquees) de Rouen ,  Centre National de la Recherche Scientifique (CNRS) ,  Universite de Rouen ,  VFP Therapies

发明人： MARSAIS, Francis ,  LEVACHER, Vincent ,  PAPAMICAEL, Cyril ,  BOHN, Pierre ,  PEAUGER, Ludovic ,  GEMBUS, Vincent ,  LE FUR, Nicolas ,  DUMARTIN-LEPINE, Marie-Laurence

IPC分类号： C07D213/50 ,  C07D213/61 ,  C07D213/82 ,  C07D213/85 ,  C07D211/82 ,  C07D211/84 ,  C07D211/90 ,  C07D401/06 ,  C07D405/06 ,  A61K31/4425 ,  A61P25/28

CPC分类号： C07D213/50 ,  C07D211/82 ,  C07D211/84 ,  C07D211/90 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82 ,  C07D213/85 ,  C07D401/06 ,  C07D405/06

摘要： A compound of the formula (I) in which the dotted lines indicate the presence of at least one double bond; n = 0 to 4; R 3 and R 4 are H, or when n = 1, R 3 and R 4 can also form together a double bond between the carbon atoms, and m = 0, 1 or 2, Z is CH or N or Z is C and -CHR 3 - is =CH- linked by the double bond to the cyclopentanone; or -(-) m - is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N-heteroaryl; R 8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR', CN, COR, CF 3 , SOR, SO 2 R, SONRR', SO 2 NRR', NO 2 , halogen, heteroaryl; and the pharmaceutical salts or tautomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.

公开(公告)号：EP2948429B1

公开(公告)日：2018-08-15

申请号：EP14702219.8

申请日：2014-01-24

申请人： INSA (Institut National des Sciences Appliquees) de Rouen ,  Centre National de la Recherche Scientifique (C.N.R.S.) ,  Universite de Rouen ,  VFP Therapies

发明人： MARSAIS, Francis ,  LEVACHER, Vincent ,  PAPAMICAEL, Cyril ,  BOHN, Pierre ,  PEAUGER, Ludovic ,  GEMBUS, Vincent ,  LE FUR, Nicolas ,  DUMARTIN-LEPINE, Marie-Laurence

IPC分类号： C07D213/50 ,  C07D213/61 ,  C07D213/82 ,  C07D213/85 ,  C07D211/82 ,  C07D211/84 ,  C07D211/90 ,  C07D401/06 ,  C07D405/06 ,  A61K31/4425 ,  A61P25/28

CPC分类号： C07D213/50 ,  C07D211/82 ,  C07D211/84 ,  C07D211/90 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82 ,  C07D213/85 ,  C07D401/06 ,  C07D405/06

摘要： A compound of the formula (I) in which the dotted lines indicate the presence of at least one double bond; n = 0 to 4; R 3 and R 4 are H, or when n = 1, R 3 and R 4 can also form together a double bond between the carbon atoms, and m = 0, 1 or 2, Z is CH or N or Z is C and -CHR 3 - is =CH- linked by the double bond to the cyclopentanone; or -(-) m - is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N-heteroaryl; R 8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR', CN, COR, CF 3 , SOR, SO 2 R, SONRR', SO 2 NRR', NO 2 , halogen, heteroaryl; and the pharmaceutical salts or tautomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.