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1. 发明公开

EP2185561A2 DÉRIVÉS DE 1,2,3,4-TETRAHYDROPYRROLOÝ1,2-A¨PYRAZINE-6-CARBOXAMIDES ET DE 2,3,4,5-TETRAHYDROPYRROLOÝ1,2-A¨Ý1,4¨-DIAZÉPINE-7-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 有权
标题翻译： 1,2,3,4-四氢吡咯并（1,2-a）的吡嗪-6-甲酰胺和2,3,4,5-四氢吡咯并（1,2-a）的二氮杂-7-甲酰胺衍生物，它们的制备和治疗用途
公开(公告)号：EP2185561A2
公开(公告)日：2010-05-19
申请号：EP08836692.7
申请日：2008-07-24
申请人： Sanofi-Aventis
发明人： BAUDOIN, Bernard , EVERS, Michel , GENEVOIS-BORELLA, Arielle , KARLSSON, Andreas , MALLERON, Jean-Luc , MATHIEU, Magali
IPC分类号： C07D487/04 , A61K31/551 , A61P25/00 , C07D243/08 , C07D207/36 , A61K31/4985 , C07D241/06 , C07D241/08
CPC分类号： C07D241/06 , C07D207/36 , C07D241/08 , C07D243/08 , C07D487/04
摘要： The invention relates to 1,2,3,4-tetrahydropyrrolo[1,2-
a ]pyrazine-6-carboxamide and 2,3,4,5-tetrahydropyrrolo[1,2-
a ][1,4]-diazépine-7-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 = a group COOR, S(O)
m R, aryl or aralkyl; R2 = one or more groups from 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 from O, N and S(O)
m , or R2 = halo(C
1 -C
6 )alkyl, halo(C
1 -C
6 )alkoxy, hydroxy, C
1 -C
6 alkoxy, nitro, cyano, amino, NR7R8, COOR, C(O)NR7R8, O-C(O)(C
1 -C
6 )alkyl, S(O)
m -NR7R8, aryl; R3 = trifluoromethyl; R4 and R5 independently = H, or R4 and R5 form a saturated ring with the carbon to which they are attached with 3 to 6 C optionally containing 0 to 1 heteroatoms from O, N or S; R6 = H, halogen, C
1 -C
6 alkyl, C
3 -C
7 cycloalkyl, nitro, amino, NR7R8, COOR, aryl, NR7(SO
2 )R8 or C(O)NR7R8; W = methylene or C(O); m = a whole number between 0 and 2, n = a whole number between 1 and 6, p= 2 or 3. Method for production and therapeutic application.

2. 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
标题翻译： 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
公开(公告)号：EP2185511A2
公开(公告)日：2010-05-19
申请号：EP08835551.6
申请日：2008-07-25
申请人： Sanofi-Aventis
发明人： BAUDOIN, Bernard , EVERS, Michel , GENEVOIS-BORELLA, Arielle , KARLSSON, Andreas , MALLERON, Jean-Luc , MATHIEU, Magali
IPC分类号： C07D209/46 , C07D217/24 , C07D413/12 , A61K31/4035 , A61K31/472 , A61P25/00 , A61P9/00 , A61P35/00
CPC分类号： C07D209/46 , C07D217/24 , C07D413/12
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.

3. 发明授权

EP2185561B1 Dérivés de 1,2,3,4-tétrahydropyrrolo(1,2-a)pyrazine-6-carboxamides et de 2,3,4,5-tétrahydropyrrolo(1,2-a)-diazépine-7-carboxamides, leur préparation et leur application en thérapeutique 有权
标题翻译： 1,2,3,4-四氢吡咯并（1,2-a）的吡嗪-6-甲酰胺和2,3,4,5-四氢吡咯并（1,2-a）的二氮杂-7-甲酰胺衍生物，它们的制备和治疗用途
公开(公告)号：EP2185561B1
公开(公告)日：2011-06-15
申请号：EP08836692.7
申请日：2008-07-24
申请人： Sanofi-Aventis
发明人： BAUDOIN, Bernard , EVERS, Michel , GENEVOIS-BORELLA, Arielle , KARLSSON, Andreas , MALLERON, Jean-Luc , MATHIEU, Magali
IPC分类号： C07D487/04 , A61K31/551 , A61P25/00 , C07D243/08 , C07D207/36 , A61K31/4985 , C07D241/06 , C07D241/08
CPC分类号： C07D241/06 , C07D207/36 , C07D241/08 , C07D243/08 , C07D487/04
摘要： The invention relates to 1,2,3,4-tetrahydropyrrolo[1,2-
a ]pyrazine-6-carboxamide and 2,3,4,5-tetrahydropyrrolo[1,2-
a ][1,4]-diazépine-7-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 = a group COOR, S(O)
m R, aryl or aralkyl; R2 = one or more groups from 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 from O, N and S(O)
m , or R2 = halo(C
1 -C
6 )alkyl, halo(C
1 -C
6 )alkoxy, hydroxy, C
1 -C
6 alkoxy, nitro, cyano, amino, NR7R8, COOR, C(O)NR7R8, O-C(O)(C
1 -C
6 )alkyl, S(O)
m -NR7R8, aryl; R3 = trifluoromethyl; R4 and R5 independently = H, or R4 and R5 form a saturated ring with the carbon to which they are attached with 3 to 6 C optionally containing 0 to 1 heteroatoms from O, N or S; R6 = H, halogen, C
1 -C
6 alkyl, C
3 -C
7 cycloalkyl, nitro, amino, NR7R8, COOR, aryl, NR7(SO
2 )R8 or C(O)NR7R8; W = methylene or C(O); m = a whole number between 0 and 2, n = a whole number between 1 and 6, p= 2 or 3. Method for production and therapeutic application.

4. 发明公开

EP2185523A2 DÉRIVÉS DE 1-0X0-1,2-DIHYDROISOQUINOLEINE-5-CARBOXAMIDES ET DE 4-OXO-3,4-DIHYDROQUINAZOLINE-8-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
标题翻译： 1-氧代-1,2-二氢异喹啉-5-羧酰胺和4-氧代-3,4-二氢喹唑啉-8-甲酰胺，其制备方法及其在治疗中的应用衍生物
公开(公告)号：EP2185523A2
公开(公告)日：2010-05-19
申请号：EP08835688.6
申请日：2008-07-25
申请人： Sanofi-Aventis
发明人： EVERS, Michel , GENEVOIS-BORELLA, Arielle , KARLSSON, Andreas , MALLERON, Jean-Luc
IPC分类号： C07D217/24 , C07D239/88 , A61K31/472 , A61K31/498 , A61P25/00 , A61K31/517 , A61P35/00 , A61P9/00
CPC分类号： C07D217/24 , C07D239/88
摘要： The invention relates to the derivatives of 1-oxo-1,2-dihydroisoquinoline-5-carboxamides and of 4-oxo-3,4-dihydroquinazoline-8-carboxamides, of general formula (I) in which: R1 represents a hydrogen atom, a (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 or (C
1 -C
6 )alkyl-Z-(C
1 -C
6 )alkyl group in which Z represents a heteroatom chosen from O, N and S(O)
m , or else R1 represents a COOR or S(O)
m R group, an aryl or an aralkyl, the (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, aryl or aralkyl groups; R2 represents one or more groups chosen from a hydrogen atom, a halogen atom, a (C
1 -C
6 )alkyl, (C
3 -C
7 )cycloalkyl, (C
1 -C
6 )alkenyl, (C
1 -C
6 )alkynyl or (C
1 -C
6 )alkyl-Z-(C
1 -C
6 )alkyl group, in which Z represents a heteroatom chosen from O, N and S(O)
m , or else R2 represents a halo(C
1 -C
6 )alkyl, halo(C
1 -C
6 )alkoxy, hydroxy, (C
1 -C
6 )alkoxy, nitro, cyano or amino group, an NR7R8, COOR, CONR7R8, OCO(C
1 -C
6 )alkyl or S(O)
m -NR7R8 group, or an aryl group; R4 and R5 represent, independently of one another, a hydrogen atom, or else R4 and R5 form, with the carbon atom which bears them, a saturated ring containing from 3 to 6 carbon atoms and optionally containing from 0 to 1 heteroatoms chosen from O, N or S; R6 represents a group chosen from a hydrogen atom, a halogen atom, a (C
1 -C
6 )alkyl, (C
3 -C
7 )cycloalkyl or (C
3 -C
7 )cycloalkyl(C
1 -C
6 )alkyl group, a halo(C
1 -C
6 )alkyl, nitro or amino group, an NR7R8 or COOR group, an NR7(SO
2 )R8 or CONR7R8 group, or an aryl group; X represents a carbon atom or a nitrogen atom; m represents an integer between 0 and 2 and n represents an integer between 1 and 6. The invention also relates to the method of producing said derivatives and the application thereof in therapeutics as β-secretase for treating neurodegenerative disorders such as Alzheimer's disease.

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