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1. 发明申请

WO2009004146A3 NOVEL HERBIMYCIN A ANALOGUE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF 审中-公开
标题翻译：新的除虫霉素A类似物衍生物，含有它们的组合物及其用途
公开(公告)号：WO2009004146A3
公开(公告)日：2009-08-20
申请号：PCT/FR2008000709
申请日：2008-05-23
申请人： SANOFI AVENTIS , BELLOSTA VERONIQUE , BIGOT ANTONY , CANOVA SOPHIE , COSSY JANINE , MAILLIET PATRICK , MIGNANI SERGE , MINOUX HERVE
发明人： BELLOSTA VERONIQUE , BIGOT ANTONY , CANOVA SOPHIE , COSSY JANINE , MAILLIET PATRICK , MIGNANI SERGE , MINOUX HERVE
IPC分类号： C07D225/06 , A61K31/395 , A61P35/00
CPC分类号： C07D225/06
摘要： The invention relates to products having formula (I), in which A represents one of the following three rings: ring a, ring b, ring c and W represents hydrogen or -(C1-C4)alkyl, -(C1-C4)alkenyl, -CO-(C1-C3)alkyl, - CO-(C1-C3)alkenyl, -CO-NH-(C1-C2)alkyl, -CO-NH-(C1-C2)alkenyl or -CO-NH2, carbon C15 having stereochemical configuration R or S and the double bond between carbons C4 and C5 having geometry E or Z, providing that W does not represent hydrogen or methyl when A represents ring b and carbon C15 has stereochemical configuration R. The invention relates to all of the isomeric forms of the products and the salts thereof for use as drugs.
摘要翻译：本发明涉及具有式（I）的产物，其中A表示以下三个环之一：环a，环b，环c，W表示氢或 - （C1-C4）烷基， - （C1-C4）链烯基（C 1 -C 3）烷基，-CO-（C 1 -C 3）链烯基，-CO-NH-（C 1 -C 2）烷基，-CO-NH-（C 1 -C 2）烯基或-CO- 具有立体化学构型R或S的碳C15以及具有几何E或Z的碳C4和C5之间的双键，条件是当A表示环b且碳C15具有立体化学构型R时W不表示氢或甲基。本发明涉及全部用作药物的产品及其盐的异构体形式。

2. 发明申请

WO2006056697A8 SUBSTITUTED THIENO[2,3-C]PYRAZOLES, METHOD FOR THE PREPARATION THEREOF, COMPOSITIONS CONTAINING THEM AND USE THEREOF 审中-公开
标题翻译：取代的噻吩并[2,3-C]吡唑，其制备方法，包含它们的组合物及其用途
公开(公告)号：WO2006056697A8
公开(公告)日：2007-07-05
申请号：PCT/FR2005002933
申请日：2005-11-25
申请人： AVENTIS PHARMA SA , CARRY JEAN-CHRISTOPHE , DOERFLINGER GILLES , BIGOT ANTONY , BARBALAT-DAMOUR DOMINIQUE , CLERC FRANCOIS , GENEVOIS-BORELLA ARIELLE , RONAN BAPTISTE , MINOUX HERVE , BARBERIS CLAUDE , JANIN YVES
发明人： CARRY JEAN-CHRISTOPHE , DOERFLINGER GILLES , BIGOT ANTONY , BARBALAT-DAMOUR DOMINIQUE , CLERC FRANCOIS , GENEVOIS-BORELLA ARIELLE , RONAN BAPTISTE , MINOUX HERVE , BARBERIS CLAUDE , JANIN YVES
IPC分类号： C07D495/04 , A61K31/4162
CPC分类号： C07D495/04
摘要： Products of formula (I), wherein R1 represents R2, NHCO(R2), CH=CH-(R2) and NH-R4 with R2 represents alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylene, aryl, heteroaryl, arylalkyl and heteroarylalkyl; R3 represents alkyl, alkyl-aryl, alkyl-heteroaryl, -aryl, -heteroaryl; R4 represents aryl, heteroaryl,cycloalkyl, heterocycloalkyl, all of which are optionally substituted; said products being in all forms isomeric and the salts thereof; the preparation thereof; as medicaments acting as inhibitors for kinase proteins; the preparation of hydroxamates that are substituted by condensed heterocycles, a method for the preparation thereof, compositions containing them, and the use thereof as a medicament, particularly as anti canceral agents
摘要翻译：式（I）的产物，其中R1表示R2，NHCO（R2），CH = CH-（R2）和具有R2的NH-R4表示烷基，环烷基，杂环烷基，杂环亚烷基，芳基，杂芳基，芳基烷基和杂芳基烷基; R3代表烷基，烷基 - 芳基，烷基 - 杂芳基， - 芳基， - 杂芳基; R 4表示芳基，杂芳基，环烷基，杂环烷基，它们均为任选取代的; 所述产物为所有形式的异构体及其盐; 其制备方法作为用作激酶蛋白抑制剂的药物; 由稠合杂环取代的异羟肟酸盐的制备，其制备方法，含有它们的组合物及其作为药物的用途，特别是作为抗癌剂

3. 发明申请

WO2011027081A3 DERIVATIVES OF 5,6,7,8-TETRAHYDROINDOLIZINE INHIBITING HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF 审中-公开
标题翻译： 5,6,7,8-四氢吲哚啉抑制HSP90的衍生物，含有它们的组合物及其用途
公开(公告)号：WO2011027081A3
公开(公告)日：2011-05-12
申请号：PCT/FR2010051833
申请日：2010-09-03
申请人： SANOFI AVENTIS , BERTIN LUC , MAILLIET PATRICK , MINOUX HERVE , RUXER JEAN-MARIE
发明人： BERTIN LUC , MAILLIET PATRICK , MINOUX HERVE , RUXER JEAN-MARIE
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/4709 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to the novel materials of formula (I), Het and Het' being an aromatic or partially unsaturated, dihydro or tetrahydro, mono- or bicyclic heterocyclic compound having 5 to 11 members, containing 1 to 4 heteroatoms, selected from among N, O or S, optionally substituted by one or more identical or different radicals R1 or R'1 such as expressed below, X being NH-CO or CO-NH, R1 and/or R'1 belonging to the group consisting of H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, free carboxy or carboxy esterified by an alkyl radical, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulphonamide, NH-SO2-alkyl, S(O)2-NH-alkyl or S(O2)-N(alkyl)2, all the alkyl, alkoxy and alkylthio radicals in turn being optionally substituted by one or more identical or different radicals selected from among halogen, hydroxy, alkoxy, amino, alkylamino and dialkylamino, wherein said materials are in any isomer and salt form and used as drugs.
摘要翻译：本发明涉及式（I）的新型材料，Het和Het是具有5至11个成员的芳族或部分不饱和的二氢或四氢，单环或双环杂环化合物，其含有1至4个选自N ，O或S，任选被一个或多个相同或不同的基团R 1或R 11取代，如下文表示的，X是NH-CO或CO-NH，R 1和/或R'1属于由H，卤素，CF 3，硝基，氰基，烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，烷硫基，游离的羧基或被烷基酯化的羧基，羧酰胺，CO-NH（烷基），CON（烷基） -CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH-烷基或S（O 2）-N（烷基）2，所有烷基，烷氧基和烷硫基依次任选地被一个或更多相同或不同的选自卤素，羟基，烷氧基，氨基，烷基氨基和二烷基氨基的基团，其中所述材料为任何异构体和盐形式，而我们作为药物。

4. 发明申请

WO2009122034A8 NOVEL HSP90 INHIBITORY CARBAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME, AND USE THEREOF 审中-公开
标题翻译：新型HSP90抑制性卡波醇衍生物，其组合物及其用途
公开(公告)号：WO2009122034A8
公开(公告)日：2010-08-19
申请号：PCT/FR2009000267
申请日：2009-03-13
申请人： SANOFI AVENTIS , ALASIA MARCEL , BERTIN LUC , CERTAL VICTOR , HALLEY FRANK , MAILLIET PATRICK , MENDEZ PEREZ MARIA , MINOUX HERVE , RUXER JEAN-MARIE
发明人： ALASIA MARCEL , BERTIN LUC , CERTAL VICTOR , HALLEY FRANK , MAILLIET PATRICK , MENDEZ PEREZ MARIA , MINOUX HERVE , RUXER JEAN-MARIE
IPC分类号： C07D401/04 , A61K31/4184 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D451/04 , C07D453/00 , C07D471/04 , C07D493/08
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D451/04 , C07D453/00 , C07D471/04 , C07D493/08
摘要： The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R'1; R is selected from the group comprising Formula (II) with R1 and/or R'1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkythio, or carboxy that is free or esterified by an alkyl, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH-SO2-alkyl, S(O)2-NHalkyl, or S(O2)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is O, S, NR2, C(O), S(O), or S(O)2; Z is optionally substituted H, HaI, -O-R2 or -NH-R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.
摘要翻译：本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自包含式（II）的基团，其中R 1和/或R 1选自H，卤素，CF 3，硝基，氰基，烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，羧基，其被烷基，羧酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（ O 2）-N（烷基）2基; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X是O，S，NR2，C（O），S（O）或S（O）2; Z是任选取代的H，H 1，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。

5. 发明申请

WO2006123061A3 FLUORENE DERIVATIVES, COMPOSITION CONTAINING SAID DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：氟衍生物，含有该衍生物的组合物及其用途
公开(公告)号：WO2006123061A3
公开(公告)日：2007-01-11
申请号：PCT/FR2006001137
申请日：2006-05-19
申请人： AVENTIS PHARMA SA , MAILLIET PATRICK , BERTIN LUC , GUYON THIERRY , THOMPSON FABIENNE , RUXER JEAN-MARIE , PILORGE FABIENNE , BENARD DIDIER , MINOUX HERVE , CARREZ CHANTAL , GOULAOUIC HELENE
发明人： MAILLIET PATRICK , BERTIN LUC , GUYON THIERRY , THOMPSON FABIENNE , RUXER JEAN-MARIE , PILORGE FABIENNE , BENARD DIDIER , MINOUX HERVE , CARREZ CHANTAL , GOULAOUIC HELENE
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D401/12
摘要： The invention relates to novel products of formula (1), wherein A1, A2, A3 and A4 are CRa or N, R1 and R1' are such that one represents H, Hal, C1C3-alkyl, C1C3-alkoxy, alkyl-OH, CF3, cyano, carboxy or carboxamido and the other represents Hal; CF3 ; OH ; SH; nitro; amino ; NH-OH ; NH-CO-H ; NH-CO-OH, NH-CO-O alkyl , NH-CO-NH2 ; carboxy ; CN ; CO-NH2 ; X-(CH2)m-alkyl; X-(CH2)m-cycloalkyl ; X-(CH2)m-heterocycloalkyl ; X-(CH2)m-aryl or X-(CH2)m-heteroaryl with X = simple bond, CH2, CH=CH, CH2-O, CH2-NH, CH2-C(O), CH2-C(O)-O, CH2-C(O)-NH, CH2-NH-(CO), CH2-NH-S(O), CH2-NH-S(O)2, O, S, NH, O-C(O), C(O)-NH, -NH-C(O), -NH-C(O)-C(O)-, -NH-C(O)-NH-, ; NH-CS, NH-S(O) or NH-S(O)2 ; m = 0, 1 or 2, or R1 and R'1 form with C to which they are bound either a radical =O ; =S ; =N-OH ; =N-NH2 ; =N-NH-CO-NH2, =CH-OH ; =Y1-(CH2)m-aryl or =Y1-(CH2)m heteroaryl, wherein Y1 represents CH, CH-CO-, CH-CO-NH, N, N-O or N-NH-, where m = 0, 1 or 2, or a cycle, R2 et R'2 represent H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, free or esterified carboxy, carboxamide, CO-NH(alkyl) et CO N(alkyl)2, p= 1 à 3 et p'= 1 à 4; Ra represents H ; halogen ; CF3 ; hydroxy ; mercapto ; nitro ; amino ; NH-OH ; NH-CO-H ; NH-CO-NH2 ; carboxy ; CN ; CO-NH2 ; Y-(CH2)n-alkyl ; Y-(CH2)n-cycloalkyl, Y-(CH2)n-heterocycloalkyl, Y-(CH2)n-aryl or Y-(CH2)n-heteroaryl, with Y = O, S, NH, O-C(O), C(O)-NH, NH-C(O), NH-S(O) or NH-S(O)2, with n = 0, 1, 2 or 3, wherein all alkyl, alkoxy, alkylthio, cycloalkyl, heterocycloalkyl, aryl and heteroaryl radicals are optionally substituted and all products in any forms are tautomers and isomers and the salts, which are used in the form of drugs.
摘要翻译：本发明涉及式（1）的新产物，其中A 1，A 2，A 3和A 4为CR a或N，R 1和R 1'表示H，Hal，C 1 -C 3 - 烷基，C 1 -C 3 - 烷氧基，烷基-OH， CF 3，氰基，羧基或甲酰氨基，另一个表示Hal; CF3; OH; SH; 硝基; 氨基; NH-OH; NH-CO-H; NH-CO-OH，NH-CO-O烷基，NH-CO-NH2; 羧基 CN; CO-NH2; X-（CH 2）M-烷基; X-（CH 2）m - 环烷基; X-（CH 2）m - 杂环烷基; X =简单键，CH2，CH = CH，CH2-O，CH2-NH，CH2-C（O），CH2-C（O）的X-（CH2）m-芳基或X- -O，CH 2 -C（O）-NH，CH 2 -NH-（CO），CH 2 -NH-S（O），CH 2 -NH-S（O）2，O，S，NH，OC（O） C（O）-NH，-NH-C（O），-NH-C（O）-C（O） - ， - NH-C（O） NH-CS，NH-S（O）或NH-S（O）2; m = 0,1或2，或者R1和R'1与它们所结合的C形成基团= O; = S; = N-OH; = N-NH 2; = N-NH-CO-NH 2 = CH-OH; = Y1-（CH2）m-芳基或= Y1-（CH2）m杂芳基，其中Y1表示CH，CH-CO-，CH-CO-NH，N，NO或N-NH-，其中m = R 2和R 2代表H，卤素，CF 3，硝基，氰基，烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，烷硫基，游离或酯化羧基，羧酰胺，CO-NH 烷基）和CO N（烷基）2，p = 1à3 et p'= 1à4; Ra表示H; 卤素 CF3; 羟基; 巯基硝基; 氨基; NH-OH; NH-CO-H; NH-CO-NH2; 羧基 CN; CO-NH2; Y-（CH 2）n - 烷基; Y - （CH 2）n - 环烷基，Y-（CH 2）n - 杂环烷基，Y-（CH 2）n - 芳基或Y-（CH 2）n - 杂芳基，其中Y = O，S，NH，OC（O） C（O）-NH，NH-C（O），NH-S（O）或NH-S（O）2，其中n = 0,1,2或3，其中全部烷基，烷氧基，烷硫基，环烷基，杂环烷基，芳基和杂芳基任选被取代，并且任何形式的所有产物都是以药物形式使用的互变异构体和异构体和盐。

6. 发明申请

WO2009122034A2 NOVEL DHSP90 INHIBITORY CARBAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME, AND USE THEREOF 审中-公开
标题翻译：新型DHSP90抑制卡博唑衍生物，含有它们的组合物及其用途
公开(公告)号：WO2009122034A2
公开(公告)日：2009-10-08
申请号：PCT/FR2009000267
申请日：2009-03-13
申请人： SANOFI AVENTIS , ALASIA MARCEL , BERTIN LUC , CERVAL VICTOR , HALLEY FRANK , MAILLIET PATRICK , MENDEZ PEREZ MARIA , MINOUX HERVE , RUXER JEAN-MARIE
发明人： ALASIA MARCEL , BERTIN LUC , CERVAL VICTOR , HALLEY FRANK , MAILLIET PATRICK , MENDEZ PEREZ MARIA , MINOUX HERVE , RUXER JEAN-MARIE
IPC分类号： C07D401/04 , A61K31/4184 , A61K31/437 , A61K31/4709 , A61P35/00 , C07D209/88 , C07D213/16 , C07D215/12 , C07D231/56 , C07D233/64 , C07D235/18 , C07D261/20 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D413/14 , C07D471/04
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D451/04 , C07D453/00 , C07D471/04 , C07D493/08
摘要： The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R'1; R is selected from the group comprising Formula (II) with R1 and/or R'1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkythio, or carboxy that is free or esterified by an alkyl, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH-SO2-alkyl, S(O)2-NHalkyl, or S(O2)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is O, S, NR2, C(O), S(O), or S(O)2; Z is optionally substituted H, HaI, -O-R2 or -NH-R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.
摘要翻译：本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自包含式（II）的基团，其中R 1和/或R 1选自H，卤素，CF 3，硝基，氰基，烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，羧基，其被烷基，羧酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（ O 2）-N（烷基）2基; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X是O，S，NR2，C（O），S（O）或S（O）2; Z是任选取代的H，H 1，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。

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