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21. 发明授权

EP1556380B1 DERIVES DE PYRIDOINDOLONE SUBSTITUES EN -3 PAR UN GROUPE HETEROCYCLIQUE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： IN 3-POSITION杂环取代pyridoindolone衍生物，生产和治疗用途
公开(公告)号：EP1556380B1
公开(公告)日：2006-04-12
申请号：EP03767851.3
申请日：2003-10-21
申请人： Sanofi-Aventis
发明人： BOURRIE, Bernard , CASELLAS, Pierre , DEROCQ, Jean-Marie , JEGHAM, Samir , MUNEAUX, Yvette
IPC分类号： C07D471/04 , A61K31/444 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, having general formula (I), wherein: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a mono or poly thienyl substituted by a methyl group, or a bicyclic or monocyclic heterocyclic radical selected from a pyridyl, an N-oxidopyridyl, a pyrazole, a (N-phenyl)pyrazole, a (N-halogenophenyl)pyrazole, a furyl, an indolyl, a (N-benzyl)indolyl, a (N-halogenobenzyl)indolyl, a benzothienyl, a benzofuryl, whereby said radicals are not substituted or are substituted one or more times by a halogen atom or a methyl or methoxy group; and R4 and R5 are identical or different and each represent independently of each other a hydrogen or halogen atom or a hydroxyl group, a hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, (C1-C4)alkoxy, (C1-C4)alkoxycarbonyl, a cyano. The invention also relates to the preparation method thereof and to the application of same in therapeutics.

22. 发明公开

EP1556382A1 DERIVES DE PYRIDOINDOLONE SUBSTITUES EN -3 PAR UN PHENYLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE. 有权
标题翻译： 3 PHENYLPYRIDOINDOLDERIVATE，生产和使用
公开(公告)号：EP1556382A1
公开(公告)日：2005-07-27
申请号：EP03810495.6
申请日：2003-10-21
申请人： Sanofi-Aventis
发明人： BOURRIE, Bernard , CASELLAS, Pierre , CIAPETTI, Paola , DEROCQ, Jean-Marie , JEGHAM, Samir , MUNEAUX, Yvette , WERMUTH, Camille-Georges
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00 , C07D471/16
CPC分类号： C07D471/04
摘要： The invention concerns compounds having an anticancer activity, of formula (I) wherein: R1 represents a hydrogen atom, a (C1-C4)alkyl group or a (CH2)nOH, (CH2)n-O-tetrahydropyran-2-yl, (CH2)nNR'6R'7, (CH2)nCN, (CH2)nCO2(C1-C4)Alk or (CH2)nCONR6R7 group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; or R1 and R2 together form a (CH2)3 group; R3 represents a phenyl monosubstituted by a hydroxyl, hydroxymethyl, carboxy, (C1-C4)alkanyl, azido, (C1-C4)alkoxycarbonyl, hydroxyiminomethyl, (C1-C4)alkylsulphonyl, trifluoromethyl, thiol, (C1-C4)alkylthio, cyano group or by a (CH2)mNR'7R10, CONR6R8 or O(CH2)nR9 group; a phenyl substituted by 2 to 5 identical or different substituents selected among a halogen atom, a (C1-C4)alkyl, trifluoromethyl, hydroxyl, hydroxymethyl, (C1-C4)alkoxy, carboxy, (C1-C4)alkanyl, azido, (C1-C4)alkoxycarbonyl, hydroxyiminomethyl, thiol, (C1-C4)alkylthio, (C1--C4)alkylsulphonyl, a phenyl, cyano group or by a (CH2)mNR'7R10, CONR6R8 or O(CH2)nR9 group; or R3 represents a benzodioxolyl group unsubstituted or substituted on the phenyl by a halogen atom; R4 and R5, identical or different, represent each independently a hydrogen or halogen or a hydroxyl, (C1-C4)alkyl, trifluoromethyl, phenyl, cyano, (C1-C4)alkoxy, (C1-C4)alkoxycarbonyl, (C1-C4) alkylsulphonyl group or a O-(CH2)nNR6R7 or (CH2)nNR6R7 group.

23. 发明公开

EP2307401A2 DERIVES ANTICANCEREUX DE 4-OXO-1,4-DIHYDRO-QUINOLINE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 审中-公开
标题翻译： 4-氧代-1,4-二氢喹啉抗癌衍生物，它们的制备和治疗用途
公开(公告)号：EP2307401A2
公开(公告)日：2011-04-13
申请号：EP09784468.2
申请日：2009-07-06
申请人： Sanofi-Aventis
发明人： BERNHART, Claude , BOUABOULA, Monsif , CASELLAS, Pierre , DUCLOS, Olivier , HERBERT, Jean Marc , JEGHAM, Samir , MCCORT, Gary
IPC分类号： C07D401/12 , C07D401/14 , C07D407/14 , C07D471/04 , A61K31/519 , A61K31/4709 , A61K31/4375 , A61P35/00 , C07D215/56 , C07D213/82 , C07D213/40
CPC分类号： C07D471/04 , C07D401/12 , C07D401/14 , C07D407/14
摘要： The invention relates to antineoplastic compounds of formula (I) where: - R1 is a (C
3 -C
7 )cycloalkyl or (C
1 -C
6 )alkyl group optionally substituted with –NR
a N
b ; - A is –NR
2 N
3 ; - B is -NR
4 R
5 or –OR
6 ; R
6 is H or a (C
1 -C
4 )alkyl group; - Z is N or CH, and Z’ is N or CH if Z is N and CH if Z is CH; - R
7 is H or a (C
1 -C
4 ) alkyl group; - L is a –CH=CH-, -CH
2 CH
2 -, -CH
2 CH[NHC(=O)O(C
1 -C
4 )alkyl]], or –(CH
2 )
n -Y- group (n=1-4, and y = O or NR
8 , with R
8 being H or a (C
1 -C
4 )alkyl group); - Ar is a group chosen from formula (II).

24. 发明授权

EP1940840B1 DERIVES DE 6-HETEROARYLPYRIDOINDOLONE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： 6 HETEROARYLPYRIDOINDOLON衍生物，生产和治疗应用
公开(公告)号：EP1940840B1
公开(公告)日：2010-07-21
申请号：EP06830970.7
申请日：2006-10-17
申请人： Sanofi-Aventis
发明人： MUNEAUX, Yvette , JEGHAM, Samir , BOURRIE, Bernard , CASELLAS, Pierre , CIAPETTI, Paola , DEROCQ, Jean-Marie , WERMUTH, Camille-Georges
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention concerns compounds of formula (I), wherein: R1 represents a hydrogen atom or a C1-C4 alkyl group, CN, CF3 or CHF2; R2 represents a hydrogen atom or a C1-C4 alkyl group; R3 represents an unsubtituted or substituted phenyl; R4 represents a heterocyclic radial; R5 represents a hydrogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group. The invention also concerns a method for preparing said compounds and the therapeutic use thereof.

25. 发明公开

EP1979352A2 DERIVES DE PYRIDO-PYRIMIDONE, LEUR PREPARATION, LEUR APPLICATION EN THERAPEUTIQUE. 审中-公开
标题翻译： PYRIDOPYRIMIDONDERIVATE，其制备方法和治疗用途
公开(公告)号：EP1979352A2
公开(公告)日：2008-10-15
申请号：EP07717935.6
申请日：2007-01-12
申请人： Sanofi-Aventis
发明人： PERREAUT, Pierre , JEGHAM, Samir , BOURRIE, Bernard , CASELLAS, Pierre , LABROSSE, Jean-Robert , DURAND, Florence
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： The invention relates to pyrido[2,3-d]pyrimidone derivatives, to the preparation thereof and to the therapeutic use thereof, wherein said derivatives are of general formula (I) which follows: (I), in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The invention also relates to the process for preparing said derivatives, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compositions.

26. 发明公开

EP1771425A1 DERIVES DE 2-CARBAMIDE-4-PHENYLTHIAZOLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： 2-脲基-4-苯基噻唑衍生物，其制备及其治疗用途
公开(公告)号：EP1771425A1
公开(公告)日：2007-04-11
申请号：EP05786078.5
申请日：2005-07-05
申请人： Sanofi-Aventis
发明人： CASELLAS, Pierre , FLOUTARD, Daniel , FRAISSE, Pierre , JEGHAM, Samir
IPC分类号： C07D277/40 , C07D277/44 , C07D417/12 , A61K31/551 , A61K31/427 , A61K31/496 , A61P37/00 , A61P29/00 , A61P31/00 , A61P9/00 , A61P3/04
CPC分类号： C07D417/12 , C07D277/40 , C07D277/46
摘要： The invention concerns 2-carbamide-4-phenylthiazole derivatives of general formula (I). The invention also concerns pharmaceutical compositions containing a compound of general formula (I).

27. 发明授权

EP1807421B1 DERIVES DE 2-AMIDO-4-PHENYLTHIAZOLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： 2-酰氨基-4-苯基噻唑衍生物，其制备和治疗用途及其
公开(公告)号：EP1807421B1
公开(公告)日：2011-03-16
申请号：EP05809089.5
申请日：2005-10-17
申请人： Sanofi-Aventis
发明人： CASELLAS, Pierre , FLOUTARD, Daniel , FRAISSE, Pierre , JEGHAM, Samir
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427
CPC分类号： C07D417/12 , C07D417/14
摘要： The invention relates to 2-amido-4-phenylthiazole derivatives of the following general formula (I) embodied in the form of a base or a salt additional to a pharmaceutically acceptable acid, in the form of hydrates or solvents and in the form of enantiomers, diastereoisomers and the mixture thereof. Pharmaceutical compositions containing a compound of general formula (I) and the therapeutic use thereof are also disclosed.

28. 发明公开

EP1984361A1 DERIVES DE 2-CARBAMIDE-4-PHENYLTHIAZOLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 审中-公开
标题翻译： 2-脲基-4-苯基噻唑衍生物，其制备及其治疗用途
公开(公告)号：EP1984361A1
公开(公告)日：2008-10-29
申请号：EP07712634.0
申请日：2007-01-04
申请人： Sanofi-Aventis
发明人： FRAISSE, Pierre , JEGHAM, Samir , CASELLAS, Pierre , FLOUTARD, Daniel , HOURCADE, Stéphane
IPC分类号： C07D417/12 , C07D277/46 , A61K31/427
CPC分类号： C07D277/46 , C07D417/12 , C07D417/14
摘要： The invention relates to 2-carbamide-4-phenylthiazole derivatives having the following general formula (I). The invention also relates to pharmaceutical compositions containing a compound of general formula (I).

29. 发明公开

EP1940840A1 DERIVES DE 6-HETEROARYLPYRIDOINDOLONE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： 6 HETEROARYLPYRIDOINDOLON衍生物，生产和治疗应用
公开(公告)号：EP1940840A1
公开(公告)日：2008-07-09
申请号：EP06830970.7
申请日：2006-10-17
申请人： Sanofi-Aventis
发明人： MUNEAUX, Yvette , JEGHAM, Samir , BOURRIE, Bernard , CASELLAS, Pierre , CIAPETTI, Paola , DEROCQ, Jean-Marie , WERMUTH, Camille-Georges
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention concerns compounds of formula (I), wherein: R1 represents a hydrogen atom or a C1-C4 alkyl group, CN, CF3 or CHF2; R2 represents a hydrogen atom or a C1-C4 alkyl group; R3 represents an unsubtituted or substituted phenyl; R4 represents a heterocyclic radial; R5 represents a hydrogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group. The invention also concerns a method for preparing said compounds and the therapeutic use thereof.

30. 发明授权

EP1556382B1 DERIVES DE PYRIDOINDOLONE SUBSTITUES EN -3 PAR UN PHENYLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE. 有权
标题翻译：衍生物DE吡啶酮取代物EN -3 PAR UN PHENYLE，LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUQUE。
公开(公告)号：EP1556382B1
公开(公告)日：2008-05-28
申请号：EP03810495.6
申请日：2003-10-21
申请人： Sanofi-Aventis
发明人： BOURRIE, Bernard , CASELLAS, Pierre , CIAPETTI, Paola , DEROCQ, Jean-Marie , JEGHAM, Samir , MUNEAUX, Yvette , WERMUTH, Camille-Georges
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00 , C07D471/16
CPC分类号： C07D471/04
摘要： The invention concerns compounds having an anticancer activity, of formula (I) wherein: R1 represents a hydrogen atom, a (C1-C4)alkyl group or a (CH2)nOH, (CH2)n-O-tetrahydropyran-2-yl, (CH2)nNR'6R'7, (CH2)nCN, (CH2)nCO2(C1-C4)Alk or (CH2)nCONR6R7 group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; or R1 and R2 together form a (CH2)3 group; R3 represents a phenyl monosubstituted by a hydroxyl, hydroxymethyl, carboxy, (C1-C4)alkanyl, azido, (C1-C4)alkoxycarbonyl, hydroxyiminomethyl, (C1-C4)alkylsulphonyl, trifluoromethyl, thiol, (C1-C4)alkylthio, cyano group or by a (CH2)mNR'7R10, CONR6R8 or O(CH2)nR9 group; a phenyl substituted by 2 to 5 identical or different substituents selected among a halogen atom, a (C1-C4)alkyl, trifluoromethyl, hydroxyl, hydroxymethyl, (C1-C4)alkoxy, carboxy, (C1-C4)alkanyl, azido, (C1-C4)alkoxycarbonyl, hydroxyiminomethyl, thiol, (C1-C4)alkylthio, (C1--C4)alkylsulphonyl, a phenyl, cyano group or by a (CH2)mNR'7R10, CONR6R8 or O(CH2)nR9 group; or R3 represents a benzodioxolyl group unsubstituted or substituted on the phenyl by a halogen atom; R4 and R5, identical or different, represent each independently a hydrogen or halogen or a hydroxyl, (C1-C4)alkyl, trifluoromethyl, phenyl, cyano, (C1-C4)alkoxy, (C1-C4)alkoxycarbonyl, (C1-C4) alkylsulphonyl group or a O-(CH2)nNR6R7 or (CH2)nNR6R7 group.
摘要翻译：本发明涉及具有式（I）的具有抗癌活性的化合物，其中：R 1表示氢原子，（C 1 -C 4）烷基或（CH 2）n OH，（CH 2）n O-四氢吡喃-2-基，）（CH 2）n CN，（CH 2）n CO 2（C 1 -C 4）Alk或（CH 2）n CONR 6 R 7基团; R2代表氢原子或（C1-C4）烷基; 或者R1和R2一起形成（CH2）3基团; （C1-C4）烷基，叠氮基，（C1-C4）烷氧基羰基，羟基亚氨基甲基，（C1-C4）烷基磺酰基，三氟甲基，硫醇，（C1-C4）烷硫基，氰基（CH2）mNR'7R10，CONR6R8或O（CH2）nR9基团; （C 1 -C 4）烷基，三氟甲基，羟基，羟甲基，（C 1 -C 4）烷氧基，羧基，（C 1 -C 4）烷基，叠氮基，（（C 1 -C 4）烷基磺酰基，苯基，氰基或被（CH 2）m NR 17 R 10，CONR 6 R 8或O（CH 2）n R 9基团取代的C 1 -C 4烷氧基羰基，羟基亚氨基甲基，硫醇，或者R3表示未被取代或在苯基上被卤素原子取代的苯并间二氧杂环戊烯基; （C 1 -C 4）烷基，三氟甲基，苯基，氰基，（C 1 -C 4）烷氧基，（C 1 -C 4）烷氧基羰基，（C 1 -C 4）烷氧基羰基，）烷基磺酰基或O-（CH 2）n NR 6 R 7或（CH 2）n NR 6 R 7基团。

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