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1. 发明申请

WO2009044019A3 1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译： 1-OXO-ISOINDOLINE-4-羧酰胺和1-氧代-1,2,3,4-四氢喹啉-5-羧酰胺衍生物，其制备和治疗用途
公开(公告)号：WO2009044019A3
公开(公告)日：2009-06-18
申请号：PCT/FR2008001110
申请日：2008-07-25
申请人： SANOFI AVENTIS , BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
发明人： BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
IPC分类号： C07D209/46 , A61K31/4035 , A61K31/472 , A61P25/00 , C07D217/24 , C07D413/12
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, C1-C10alkyl, C3-C7cycloalkyl, (CH2)n-(C1-C6)alkenyl, (CH2)n-(C1-C6)alkynyl, (C1-C6)alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R1 = COOR, S(O)mR, aryl or aralkyl, R2 = one or more of H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkenyl, C1-C6alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R2 = halo(C1-C6)alkyl, C1-C6alkoxy, halo(C1-C6)alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C1-C6)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, C1- C6alkyl, C3-C7cycloalkyl, C3-C7cycloalkyl-(C1-C6)alkyl, halo(C1-C6)alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C1-C2alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6.
摘要翻译：本发明涉及通式（I）的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，其中：R1 = H，C1-C10烷基，C3- C7-环烷基，（CH2）n-（C1-C6）烯基，（CH2）n-（C1-C6）炔基，（C1-C6）烷基-Z-（C1-C6）烷基，其中Z =选自O ，N和S（O）m，或R1 = COOR，S（O）mR，芳基或芳烷基，R2 = H，卤素，C1-C6烷基，C3-C7环烷基，C1-C6烯基，C1-C6炔基， C 1 -C 6烷基Z-（C 1 -C 6）烷基，其中Z =选自O，N和S（O）m的杂原子，或R 2 =卤代（C 1 -C 6）烷基，C 1 -C 6烷氧基，）烷氧基，羟基，硝基，氰基，氨基，NR 7 R 8，COOR，CONR 7 R 8，O CO（C 1 -C 6）烷基，S（O）m -NR 7 R 8， R3 =三氟甲基; R 4和R 5独立地为H或R 4和R 5与它们所连接的碳一起形成具有3至6个碳原子的饱和环，并任选地含有O至1个选自O，N或S的杂原子; R 6 = H，卤素，C 1 -C 6烷基，C 3 -C 7环烷基，C 3 -C 7环烷基 - （C 1 -C 6）烷基，卤代（C 1 -C 6）烷基，硝基，氨基，NR 7 R 8，COOR，NR 7（SO 2）R 8，CONR 7 R 8，芳基或杂环; X = C1-C2亚烷基; m =从0到2的整数，n = 1到6的整数。

2. 发明申请

WO2009044019A9 1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译： 1-OXO-ISOINDOLINE-4-羧酰胺和1-氧代-1,2,3,4-四氢喹啉-5-羧酰胺衍生物，其制备和治疗用途
公开(公告)号：WO2009044019A9
公开(公告)日：2010-10-14
申请号：PCT/FR2008001110
申请日：2008-07-25
申请人： SANOFI AVENTIS , BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
发明人： BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
IPC分类号： C07D209/46 , A61K31/4035 , A61K31/472 , A61P25/00 , C07D217/24 , C07D413/12
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, C1-C10alkyl, C3-C7cycloalkyl, (CH2)n-(C1-C6)alkenyl, (CH2)n-(C1-C6)alkynyl, (C1-C6)alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R1 = COOR, S(O)mR, aryl or aralkyl, R2 = one or more of H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkenyl, C1-C6alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R2 = halo(C1-C6)alkyl, C1-C6alkoxy, halo(C1-C6)alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C1-C6)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, C1- C6alkyl, C3-C7cycloalkyl, C3-C7cycloalkyl-(C1-C6)alkyl, halo(C1-C6)alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C1-C2alkylene; 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.
摘要翻译：本发明涉及通式（I）的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，其中：R1 = H，C1-C10烷基，C3- C7-环烷基，（CH2）n-（C1-C6）烯基，（CH2）n-（C1-C6）炔基，（C1-C6）烷基-Z-（C1-C6）烷基，其中Z =选自O ，N和S（O）m，或R1 = COOR，S（O）mR，芳基或芳烷基，R2 = H，卤素，C1-C6烷基，C3-C7环烷基，C1-C6烯基，C1-C6炔基， C 1 -C 6烷基Z-（C 1 -C 6）烷基，其中Z =选自O，N和S（O）m的杂原子，或R 2 =卤代（C 1 -C 6）烷基，C 1 -C 6烷氧基，）烷氧基，羟基，硝基，氰基，氨基，NR 7 R 8，COOR，CONR 7 R 8，O CO（C 1 -C 6）烷基，S（O）m -NR 7 R 8， R3 =三氟甲基; R 4和R 5独立地为H或R 4和R 5与它们所连接的碳一起形成具有3至6个碳原子的饱和环，并任选地含有O至1个选自O，N或S的杂原子; R 6 = H，卤素，C 1 -C 6烷基，C 3 -C 7环烷基，C 3 -C 7环烷基 - （C 1 -C 6）烷基，卤代（C 1 -C 6）烷基，硝基，氨基，NR 7 R 8，COOR，NR 7（SO 2）R 8，CONR 7 R 8，芳基或杂环; X = C1-C2亚烷基; m = 0至2的整数，n = 1至6的整数。本发明还涉及其用于治疗神经变性疾病如阿尔茨海默病的β-分泌酶抑制剂的制备和治疗应用的方法。

3. 发明申请

WO2009044007A3 1,2,3,4-TETRAHYDROPYRROLO[1,2- 审中-公开
标题翻译： 1,2,3,4-四氢吡咯并[1,2 <我
公开(公告)号：WO2009044007A3
公开(公告)日：2009-09-17
申请号：PCT/FR2008001096
申请日：2008-07-24
申请人： SANOFI AVENTIS , BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
发明人： BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/551 , A61P25/00
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, C1-C10alkyl, C3-C7 cycloalkyl, (CH2)n-(C1-C6)alkenyl, (CH2)n-(C1-C6)alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R1 = a group COOR, S(O)mR, aryl or aralkyl; R2 = one or more groups from H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkenyl, C1-C6alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom from O, N and S(O)m, or R2 = halo(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy, C1-C6alkoxy, nitro, cyano, amino, NR7R8, COOR, C(O)NR7R8, O-C(O)(C1-C6)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, C1-C6alkyl, C3-C7cycloalkyl, nitro, amino, NR7R8, COOR, aryl, NR7(SO2)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.
摘要翻译：本发明涉及1,2,3,4-四氢吡咯并[1,2-a]吡嗪-6-甲酰胺和2,3,4,5-四氢吡咯并[1,2-a] [1,4] 其中R1 = H，C1-C10烷基，C3-C7环烷基，（CH2）n-（C1-C6）烯基，（CH2）n-（C1-C6）炔基，C1 C 1-6烷基-Z-（C 1 -C 6）烷基，其中Z =选自O，N和S（O）m的杂原子，或R 1 = COOR，S（O）m R，芳基或芳烷基; R 2 = H，卤素，C 1 -C 6烷基，C 3 -C 7环烷基，C 1 -C 6烯基，C 1 -C 6炔基，C 1 -C 6烷基Z-（C 1 -C 6）烷基中的一个或多个基团，其中Z =来自O，N的杂原子， S（O）m或R 2 =卤代（C 1 -C 6）烷基，卤代（C 1 -C 6）烷氧基，羟基，C 1 -C 6烷氧基，硝基，氰基，氨基，NR 7 R 8，COOR，C（O）NR 7 R 8，OC ）（C 1 -C 6）烷基，S（O）m -NR 7 R 8，芳基; R3 =三氟甲基; R4和R5独立地为H，或R4和R5与它们连接的碳形成饱和的环，其中3至6个C任选地含有0至1个O，N或S的杂原子; R6 = H，卤素，C1-C6烷基，C3-C7环烷基，硝基，氨基，NR7R8，COOR，芳基，NR7（SO2）R8或C（O）NR7R8; W =亚甲基或C（O）; m = 0到2之间的整数，n = 1到6之间的整数，p = 2或3.生产和治疗应用的方法。

4. 发明申请

WO03000695A8 PYRROLOPYRIMIDINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的吡咯烷酮
公开(公告)号：WO03000695A8
公开(公告)日：2004-03-11
申请号：PCT/GB0202835
申请日：2002-06-21
申请人： AVENTIS PHARMA INC , COX PAUL JOSEPH , MAJID TAHIR NADEEM , AMENDOLA SHELLEY , DEPRETS STEPHANIE DANIELE , EDLIN CHRIS , PEDGRIFT BRIAN LESLIE , HALLEY FRANK , EDWARDS MICHAEL , BAUDOIN BERNARD , MCLAY IAIN MCFARLANE , ALDOUS DAVID JOHN
发明人： COX PAUL JOSEPH , MAJID TAHIR NADEEM , AMENDOLA SHELLEY , DEPRETS STEPHANIE DANIELE , EDLIN CHRIS , PEDGRIFT BRIAN LESLIE , HALLEY FRANK , EDWARDS MICHAEL , BAUDOIN BERNARD , MCLAY IAIN MCFARLANE , ALDOUS DAVID JOHN
IPC分类号： A61K31/519 , A61K31/5377 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D487/04 , A61K31/505 , C07D209/00
CPC分类号： C07D487/04
摘要： This invention is directed to compounds of the formula (I) to N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and to methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.
摘要翻译：本发明涉及式（I）化合物与这些盐或溶剂合物的N-氧化物，前体药物，酸性生物电子等排物，这些化合物的药学上可接受的盐或溶剂化物，或N-氧化物，前体药物或酸性生物电子等排体，这些化合物，以及治疗方法，包括向有需要的患者施用此类化合物和组合物。

5. 发明专利

ES2367338T3 DERIVADOS DE 1,2,3,4-TETRAHIDROPIRROLO[1,2-a]-PIRAZINA-6-CARBOXAMIDAS Y DE 2,3,4,5-TETRAHIDROPIRROLO[1,2,-a][1,4]-DIAZEPINO-7-CARBOXAMIDAS, SU PREPARACION Y SU APLICACION EN TERAPEUTICA. 未知
公开(公告)号：ES2367338T3
公开(公告)日：2011-11-02
申请号：ES08836692
申请日：2008-07-24
申请人： SANOFI AVENTIS , SANOFI SA
发明人： BAUDOIN BERNARD , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/551 , A61P25/00 , C07D207/36 , C07D241/06 , C07D241/08 , C07D243/08
摘要： Compuesto que responde a la fórmula (I) **Fórmula** en la que: R1 representa un átomo de hidrógeno, un grupo alquilo (C1-C10), cicloalquilo (C3-C7), (CH2)n-alquenilo (C1C6), (CH2)n-alquinilo (C1-C6), alquil (C1-C6)-Z-alquilo (C1-C6), en el que Z representa un heteroátomo elegido entre O, N y S(O)m, o bien R1 representa un grupo COOR, S(O)mR, un arilo o un aralquilo; estando los grupos alquilo (C1-C10), cicloalquilo (C3-C7), (CH2)n-alquenilo (C1-C6), (CH2)n-alquinilo (C1-C6), alquil (C1-C6)Z- alquilo (C1-C6), arilo o aralquilo sustituidos opcionalmente con uno o varios grupos elegidos entre un átomo de halógeno, un grupo alquilo (C1-C6), cicloalquilo (C3-C7), halo-alquilo (C1-C6), alcoxi (C1-C6), haloalcoxi (C1-C6), NR7R8, nitro, ciano, OR, COOR, C(O)NR7R8 o S(O)mNR7R8, R2 representa uno o varios grupos elegidos entre un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo (C1-C6), cicloalquilo (C3-C7), alquenilo (C1-C8), alquinilo (C1-C6) o alquil (C1-C6)-Z-alquilo (C1-C6), en el que Z representa un heteroátomo elegido entre O, N y S(O)m, o bien R2 representa un grupo halo-alquilo (C1-C6), halo-alcoxi (C1-C6), hidroxi, alcoxi (C1-C6), nitro, ciano, amino, un grupo NR7R8, COOR, C(O)NR7R8, O-C(O)-alquilo (C1-C6), S(O)m-NR7R8 o un grupo arilo, pudiendo estar el grupo arilo sustituido opcionalmente con uno o varios grupos elegidos entre un átomo de halógeno, un grupo alquilo (C1-C6), cicloalquilo (C3-C7), halo-alquilo (C1-C6), alcoxi (C1-C6), halo-alcoxi (C1-C6), NR7R8, OR, nitro, ciano, COOR, C(O)NR7R8 o S(O)mNR7R8, R3 representa un grupo trifluorometilo, R4 y R5 representan un átomo de hidrógeno, o bien R4 y R5 forman con el átomo de carbono al que están unidos un ciclo saturado que contiene de 3 a 6 átomos de carbono y que contiene opcionalmente de 0 a 1 heteroátomo elegido entre O, N o S, R6 representa un grupo elegido entre un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo (C1C6), cicloalquilo (C3-C7), cicloalquil (C3-C7)-alquilo (C1-C6), nitro, amino, un grupo NR7R8, COOR, un grupo arilo, un grupo NR7(SO2)R8 o C(O)NR7R8, R, R7 y R8 representan, independientemente uno del otro, uno o varios grupos elegidos entre un átomo de hidrógeno, un grupo alquilo (C1-C6), cicloalquilo (C3-C7), cicloalquil (C3-C7)-alquilo (C1-C6), un grupo arilo o aril-alquileno (C1-C6), o bien R7 y R8 pueden formar con el átomo al que están unidos un ciclo saturado, parcialmente insaturado o insaturado, que contiene de 5 a 7 átomos de carbono y que contiene opcionalmente además un heteroátomo elegido entre O, N o S(O)m, W representa un grupo metileno o C(O), m representa un número entero que puede tomar los valores 0, 1 ó 2, n representa un número entero que puede tomar los valores 1, 2, 3, 4, 5 ó 6, p representa un número entero que puede tomar los valores 2 ó 3, el carbono al que está unido el grupo bencilo sustituido con R2 tiene la configuración absoluta S, el carbono al que está unido el grupo hidroxilo tiene la configuración absoluta R, en estado de base o de sal de adición a un ácido.

6. 发明专利

CO6290689A2 DERIVADOS DE 1,2,3,4-TETRAHIDROPIRROLO[1,2]PIRAZINA-6-CARBOXAMIDAS Y DE 2,3,4,5-TETRAHIDROPIRROL[1,2][1,4]-DIAZEPINA -7-CARBOXAMIDAS SU PREPARACION Y SU APLICACION EN TERAPEUTICA 未知
公开(公告)号：CO6290689A2
公开(公告)日：2011-06-20
申请号：CO10007695
申请日：2010-01-26
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： A61K31/4985 , A61P25/00 , C07D487/04
摘要： La invención se refiere a los derivados de 1,2,3,4-tetrahidropirrolo-[1,2-a]-pirazina-6-carboxamidas y de 2,3,4,5-tetrahidropirrolo[1,2-a][1,4]-diazepina-7-carboxamidas, de fórmula general (I), en la que R1 representa un átomo de hidrogeno, un grupo alquilo(C1-C10), cicloalquilo(C3-C7), (CH2)n-alquenilo(C1-C6), (CH2)n-alquinilo(C1-C6), alquilo(C1-C6)-Z-alquilo(C1-C6), en el que Z representa un heteroátomo elegido entre O, N y S(O)m, o bien R1 representa un grupo COOR, S(O)mR, un arilo o un aralquilo; R2 representa uno o varios grupos elegidos entre un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo(C1-C6), cicloalquilo(C3-C7), alquenilo(C1-C6), alquinilo(C1-C6), alquilo(C1-C6)-Z-alquilo(C1-C6), en el que Z representa un heteroátomo elegido entre O, N y S(O)m, o bien R2 representa un grupo haloalquilo(C1-C6), haloalcoxi(C1-C6), hidroxi, alcoxi(C1-C6), nitro, ciano, amino, un grupo NR7R8, COOR, C(O)NR7R8, O-C(O)alquilo(C1-C6), S(O)m-NR7R8, un grupo arilo; R3 representa un grupo trifluorometilo; R4 y R5 representan, independientemente uno del otro, un átomo de hidrógeno o bien R4 y R5 forman con el átomo de carbono que les lleva un ciclo saturado que contiene 3 a 6 átomos de carbono y que contiene opcionalmente de 0 a 1 heteroátomos elegidos entre O, N o S; R6 representa un grupo elegido entre un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo(C1-C6), cicloalquilo(C3-C7), nitro, amino, un grupo NR7R8, COOR, un grupo arilo, un grupo NR7(SO2)R8 o C(O)NR7R8; W representa un grupo metileno o C(O); m representa un número entero comprendido entre 0 y 2, n representa un número entero comprendido entre 1 y 6, p representa un número entero comprendido entre 2 o 3. Procedimiento de preparación y aplicación en terapéutica.

7. 发明专利

ZA201000581B 1,2,3,4-TETRAHYDROPYRROLO[1,2-A]PYRAZINE-6-CARBOXAMIDE AND 2,3,4,5-TETRAHYDROPYRROLO[1,2-A][1,4]-DIAZEPINE-7-CARBOXAMIDE DERIVATIVES,PREPARATION AND THERAPEUTIC USE THEREOF 未知
公开(公告)号：ZA201000581B
公开(公告)日：2011-04-28
申请号：ZA201000581
申请日：2010-01-26
申请人： SANOFI-AVENTIS
发明人： MATHIEU MAGALI , KARLSSON ANDREAS , EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , BAUDOIN BERNARD , MALLERON JEAN-LUC
摘要： The present invention relates to derivatives of 1,2,3,4-tetrahydropyrrolo-[1,2-a]pyrazine-6-carboxamides and of 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]diazepine-7-carboxamides, to the preparation thereof and to the therapeutic use thereof.

8. 发明专利

HK1143163A1 未知
公开(公告)号：HK1143163A1
公开(公告)日：2010-12-24
申请号：HK10109764
申请日：2010-10-15
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： C07D20060101 , A61K20060101 , A61P20060101
摘要： 1-Oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide compounds (I) and their base or acid addition salts, hydrates or solvates are new. 1-Oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide compounds of formula (I) and their base or acid addition salts, hydrates or solvates are new. R 1>H, 1-10C alkyl, 3-7C cycloalkyl, (CH 2) n-(1-6C)alkenyl, (CH 2) n-(1-6C)alkynyl, 1-6C alkyl-Z-(1-6C alkyl), aryl or aralkyl (all optionally substituted by halo, 1-6C alkyl, 3-7C cycloalkyl, halo(1-6C)alkyl, 1-6C alkoxy, halo(1-6C)alkoxy, NR 7>R 8>, nitro, cyano, OR, COOR, CONR 7>R 8>or S(O) mNR 7>R 8>), COOR or S(O) mR; Z : heteroatom comprising O, N or S(O) m; R 2>halo(1-6C)alkyl, halo(1-6C)alkoxy, OH, 1-6C alkoxy, NO 2, CN, NH 2, NR 7>R 8>, COOR, CONR 7>R 8>, OCO(1-6C)alkyl, S(O) mNR 7>R 8>or aryl (all optionally substituted by one or more halo, 1-6C alkyl, 3-7C cycloalkyl, halo(1-6C)alkyl, (1-6C)alkoxy, halo(1-6C)alkoxy, NR 7>R 8>, NO 2, CN, OR, COOR, CONR 7>R 8>or S(O) mNR 7>R 8>), H (preferred), halo, 1-6C alkyl, 3-7C cycloalkyl, (1-6C)alkenyl, (1-6C)alkynyl or 1-6C alkyl-Z-(1-6C alkyl); R 3>CF 3; either R 4>, R 5>H; or CR 4>R 5>ring containing 3-6 carbon atoms (optionally saturated and optionally containing 0 or 1 heteroatom comprising O, N or S); R 6>H (preferred), halo, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-6C alkyl, NO 2, NH 2, NR 7>R 8>, COOR, NR 7>(SO 2)R 8>, CONR 7>R 8>or aryl; either R 7>, R 8>, R : H, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-6C alkyl, aryl, aryl(1-6C)alkylene or COR; or R 7>R 8>ring containing 5-7 carbon atoms (optionally saturated and substituted by heteroatom of O, N or S(O) m); X : 1-2C alkylene (optionally substituted by one or more 1-6C alkyl group); m : 0-2; and n : 1-6. Where the carbon carrying the benzyl substituted by R2 is absolute configuration S and the carbon carrying the hydroxyl is absolute configuration R. Independent claims are included for: (1) substituted 1-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid compounds of formula (IIIa); and (2) substituted 1-oxo-1,2,3,4-tetrahydro-isoquinoline-5-carboxylic acid of formula (IIIb) and (IIIc). [Image] [Image] ACTIVITY : Neuroprotective; Nootropic; Antiparkinsonian; Cerebroprotective; Vasotropic; Cardiovascular-gen.; Anticonvulsant; Antimigraine; Antidepressant; Tranquilizer; Antiarteriosclerotic; Cytostatic. MECHANISM OF ACTION : Beta-secretase inhibitor. The ability of (I) to inhibit beta-secretase was tested using fluorescence resonance energy transfer assay. The result showed that N-[(1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-3-({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)propyl]-7-[methyl(methylsulfonyl)amino]-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide hydrochloride exhibited an IC 5 0value of 0.048 mu M.

9. 发明专利

MA31630B1 Dérivés de 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamides et de 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]-diazépine-7-carboxamides, leur préparation et leur application en thérapeutique 未知
公开(公告)号：MA31630B1
公开(公告)日：2010-08-02
申请号：MA32647
申请日：2010-02-24
申请人： SANOFI AVENTIS
发明人： EVERS MICHEL , GENEVOIS-BORELLA ARIELLE , KARLSSON ANDREAS , MALLERON JEAN-LUC , MATHIEU MAGALI , BAUDOIN BERNARD
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/551 , A61P25/00
摘要： L'invention concerne les dérivés de 1, 2, 3,4-tétrahydropyrrolo- [1, 2-a] -pyrazine-6-carboxamides et de 2, 3, 4, 5-tétrahydropyrrolo [1, 2-a] [1, 4] -diazépine-7-carboxamides, de formule générale (i) selon la revendication 1 ayant une activité inhibitrice vis-à-vis de l'activité ß-secrétax.

10. 发明专利

MX2010001076A DERIVADOS DE 1,2,3,4-TETRAHIDROPIRROLO-[1,2-A]-PIRAZINA-6-CARBOXAM IDA Y 2,3,4,5-TETRAHIDROPIRROLLO [1,2,A] [1,4]-DIAZEPINA-7-CARBOXA MIDA, PREPARACION Y SU USO TERAPEUTICO. 未知
公开(公告)号：MX2010001076A
公开(公告)日：2010-03-09
申请号：MX2010001076
申请日：2008-07-24
申请人： SANOFI AVENTIS
发明人： GENEVOIS-BORELLA ARIELLE , MALLERON JEAN-LUC , EVERS MICHEL , BAUDOIN BERNARD , KARLSSON ANDREAS , MATHIEU MAGALI
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/551 , A61P25/00 , C07D207/36 , C07D241/06 , C07D241/08 , C07D243/08
摘要： La invención se refiere a derivados de 1 2,3,4-tetrahidropirrolo[1 ,2-a]pirazina-6-carboxamida y 2,3,4,5- tetrahidropirrolo[1 ,2-a][1 ,4]-diazepina-7-carboxamida de fórmula general (I), donde R1 = H, alquilo de 1 a 10 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono, (CH2)n-aIquenilo(1 a 6 átomos de carbono), (CH2)n-alquinilo(1 a 6 átomos de carbono), alquilo de 1 a 6 átomos de carbono-Z-alquilo(de 1 a 6 átomos de carbono), donde Z = un heteroátomo elegido de O, N y S(O)m, o R1 = un grupo COOR, S(O)mR, arilo o aralquilo; R2 = uno o varios grupos H, halógeno, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono, alquenilo de 1 a 6 átomos de carbono, alquinilo de 1 a 6 átomos de carbono, alquilo de 1 a 6 átomos de carbono-Z-alquilo(de 1 a 6 átomos de carbono), donde Z = un heteroátomo de O, N y S (O) m, o R2 = halo-alquilo(de 1 a 6 átomos de carbono), halo-alcoxi(de 1 a 6 átomos de carbono), hidroxi, alcoxi de 1 a 6 átomos de carbono, nitro, ciano, amino, NR7R8, COOR, C(O)NR7R8, O-C(O)alquilo(de a 6 átomos de carbono), S(O)m-NR7R8, arilo; R3 = trifluorometilo; R4 y R5 independientemente = H, o R4 y R5 forman un anillo saturado con el carbono al cual se unen con 3 a 6 C opcionalmente que contienen O a 1 heteroátomos de O, N o S; R6 = H, halógeno, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono, nitro, amino, NR7R8, COOR, arilo, NR7(SO2)R8 o C(O)NR7R8 W = metileno o C(O); m = un m = un número entero entre O y 2, n = un número entero entre 1 y 6, p = 2 ó 3. El método para producción y aplicación terapéutica.

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