发明公开
EP2185511A2 DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
审中-公开
1-氧代异二氢吲哚-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺衍生物及其制备和治疗用途
- 专利标题： DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
- 专利标题（英）： 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives, preparation and therapeutic use thereof
- 专利标题（中）： 1-氧代异二氢吲哚-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺衍生物及其制备和治疗用途
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申请号： EP08835551.6申请日： 2008-07-25
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公开(公告)号： EP2185511A2公开(公告)日： 2010-05-19
- 发明人: BAUDOIN, Bernard , EVERS, Michel , GENEVOIS-BORELLA, Arielle , KARLSSON, Andreas , MALLERON, Jean-Luc , MATHIEU, Magali
- 申请人： Sanofi-Aventis
- 申请人地址： 174 Avenue de France 75013 Paris FR
- 专利权人： Sanofi-Aventis
- 当前专利权人： Sanofi-Aventis
- 当前专利权人地址： 174 Avenue de France 75013 Paris FR
- 代理机构： Le Coupanec, Pascale A.M.P.
- 优先权： FR0705499 20070727
- 国际公布： WO2009044019 20090409
- 主分类号： C07D209/46
- IPC分类号： C07D209/46 ; C07D217/24 ; C07D413/12 ; A61K31/4035 ; A61K31/472 ; A61P25/00 ; A61P9/00 ; A61P35/00
摘要：
The invention relates to 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives of general formula (I) where: R1 = H, C
1 -C
10 alkyl, C
3 -C
7 cycloalkyl, (CH
2 )
n -(C
1 -C
6 )alkenyl, (CH
2 )n-(C
1 -C
6 )alkynyl, (C
1 -C
6 )alkyl-Z-(C
1 -C
6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
m , or R1 = COOR, S(O)
m R, aryl or aralkyl, R2 = one or more of H, halogen, C
1 -C
6 alkyl, C
3 -C
7 cycloalkyl, C
1 -C
6 alkenyl, C
1 -C
6 alkynyl, C
1 -C
6 alkyl-Z-(C
1 -C
6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
m , or R2 = halo(C
1 -C
6 )alkyl, C
1 -C
6 alkoxy, halo(C
1 -C
6 )alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C
1 -C
6 )alkyl, S(O)
m -NR7R8, aryl; R3 = trifluoromethyl;R4 and R5 independently = H, or R4 and R5 together with the carbon to which they are attached form a saturated ring with 3 to 6 C and optionally containing O to 1 heteroatoms chosen from O, N or S; R6 = H,halogen, C
1 - C
6 alkyl, C
3 -C
7 cycloalkyl, C
3 -C
7 cycloalkyl-(C
1 -C
6 )alkyl, halo(C
1 -C
6 )alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C
1 -C
2 alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6. The invention further relates to a method for preparation and therapeutic application thereof as ß-secretase inhibitors for the treatment of neurodegenerative disorders such as Alzheimers.
1 -C
10 alkyl, C
3 -C
7 cycloalkyl, (CH
2 )
n -(C
1 -C
6 )alkenyl, (CH
2 )n-(C
1 -C
6 )alkynyl, (C
1 -C
6 )alkyl-Z-(C
1 -C
6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
m , or R1 = COOR, S(O)
m R, aryl or aralkyl, R2 = one or more of H, halogen, C
1 -C
6 alkyl, C
3 -C
7 cycloalkyl, C
1 -C
6 alkenyl, C
1 -C
6 alkynyl, C
1 -C
6 alkyl-Z-(C
1 -C
6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
m , or R2 = halo(C
1 -C
6 )alkyl, C
1 -C
6 alkoxy, halo(C
1 -C
6 )alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C
1 -C
6 )alkyl, S(O)
m -NR7R8, aryl; R3 = trifluoromethyl;R4 and R5 independently = H, or R4 and R5 together with the carbon to which they are attached form a saturated ring with 3 to 6 C and optionally containing O to 1 heteroatoms chosen from O, N or S; R6 = H,halogen, C
1 - C
6 alkyl, C
3 -C
7 cycloalkyl, C
3 -C
7 cycloalkyl-(C
1 -C
6 )alkyl, halo(C
1 -C
6 )alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C
1 -C
2 alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6. The invention further relates to a method for preparation and therapeutic application thereof as ß-secretase inhibitors for the treatment of neurodegenerative disorders such as Alzheimers.
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