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1. 发明申请

WO2004072027A2 CHEMICAL DERIVATIVES BINDING VERY SPECIFICALLY WITH G-QUADRUPLEX DNA STRUCTURES AND USE THEREOF AS A SPECIFIC ANTI-CANCER AGENT 审中-公开
标题翻译：化学衍生物与G-四联体DNA结构结合非常明确，并将其用作特异性抗癌药
公开(公告)号：WO2004072027A2
公开(公告)日：2004-08-26
申请号：PCT/FR2004000260
申请日：2004-02-05
申请人： AVENTIS PHARMA SA , CENTRE NAT RECH SCIENT , MUSEUM NAT D HISTOIRE NATURELL , INST CURIE , COMMISSARIAT ENERGIE ATOMIQUE , UNIV REIMS CHAMPAGNE ARDENNE , HITTINGER AUGUSTIN , CAULFIELD THOMAS , MAILLIET PATRICK , BOUCHARD HERVE , MANDINE ELIANE , MERGNY JEAN-LOUIS , GUITTAT LIONEL , RIOU JEAN-FRANCOIS , GOMEZ DENNIS , BELMOKHTAR CHAFKE
发明人： HITTINGER AUGUSTIN , CAULFIELD THOMAS , MAILLIET PATRICK , BOUCHARD HERVE , MANDINE ELIANE , MERGNY JEAN-LOUIS , GUITTAT LIONEL , RIOU JEAN-FRANCOIS , GOMEZ DENNIS , BELMOKHTAR CHAFKE
IPC分类号： A61K45/06 , A61P35/00 , A61P37/00 , C07D215/38 , C07D401/12 , C07D401/14 , C07D
CPC分类号： C07D401/12 , A61K45/06 , C07D215/38 , C07D401/14
摘要： The invention relates to cancer therapy and concerns novel anti-cancer agents exhibiting a highly specific action mechanism. The invention also relates to novel chemical compounds and the therapeutic use thereof in man. The invention describes the preparation of heterocylic diamides of general formula (IB) as highly specific G quadruplex DNA ligands and the use thereof as telomerase inhibitors in man. (IB) nitrogenous aromatic cycle comprising a nitrogen atom in a quaternary form (NR3)p CO distributor (CO)m NR'3)qu X- aromatic or non-aromatic cycle.
摘要翻译：本发明涉及癌症治疗并且涉及展现出高度特异性作用机制的新型抗癌剂。本发明还涉及新型化合物及其在人体中的治疗用途。本发明描述了通式（IB）的杂环二酰胺作为高度特异的G四链体DNA配体的制备及其在人体中作为端粒酶抑制剂的用途。（IB）包含氮原子的季氮形式（NR 3）p CO分配器（CO）m NR'3）q-芳族或非芳族循环的含氮芳族环。

2. 发明申请

WO2009118475A3 PLATINUM-N-HETEROCYCLIC CARBENE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：铂 - N-杂环碳源衍生物，其制备方法及其治疗用途
公开(公告)号：WO2009118475A3
公开(公告)日：2009-11-19
申请号：PCT/FR2009000220
申请日：2009-03-02
申请人： SANOFI AVENTIS , CENTRE NAT RECH SCIENT , MAILLIET PATRICK , MARINETTI ANGELA , SKANDER MYRIEM
发明人： MAILLIET PATRICK , MARINETTI ANGELA , SKANDER MYRIEM
IPC分类号： C07F15/00 , A61K31/4164 , A61K31/4196 , A61P35/00
CPC分类号： C07F15/0086 , A61K31/555
摘要： The invention relates to the platinum N-heterocycle derivatives of general formula (I) in which - R1 and/or R2 are, independently of one another, an aryl or aralkyl group, each optionally substituted, a linear or branched C1-C6 alkyl group, a monocyclic C3-C7 cycloalkyl group or a linear or branched C2-C6 alkenyl group, - or else R' is a hydrogen atom and R is a group selected from the following groups: cycloalkyl or heterocycloalkyl, which is monocyclic or bicyclic and has from 3 to 8 carbon atoms, or benzyl, which is optionally substituted, - or else R and R' form, together with NH, a C3-C8 monocyclic or bicyclic heterocycloalkyl, - V is a nitrogen atom or a C-R4 radical, - R3 and/or R4 are hydrogen or a phenyl group or R3 and R4 may also together form a C3-C6 alkylene radical or a C3-C6 heteroalkylene radical with one or more nitrogenous heteroatoms, it being possible for the carbon atoms of the heteroalkylene radical to be modified in the form of a carbonyl radical, - X is iodine, bromine, chlorine or a nitrato (-ONO2) group.
摘要翻译：本发明涉及通式（I）的铂N-杂环衍生物，其中-R 1和/或R 2彼此独立地为芳基或芳烷基，各自任选被取代为直链或支链C 1 -C 6烷基，单环C 3 -C 7环烷基或直链或支链C 2 -C 6烯基，或者R'是氢原子，R是选自以下基团的基团：环烷基或杂环烷基，其为单环或双环并且具有或任选取代的苄基，或者R和R'与NH一起与C 3 -C 8单环或双环杂环烷基一起形成，-V是氮原子或C-R 4基团， -R 3和/或R 4是氢或苯基，或者R 3和R 4也可以一起形成一个或多个含氮杂原子的C 3 -C 6亚烷基或C 3 -C 6亚杂烷基，杂亚烷基的碳原子是可能的自由基以羰基的形式被修饰，-X是碘，溴，氯或硝基（-ONO 2）基团。

3. 发明申请

WO2006108948A3 NOVEL ISOINDOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME, PREPARATION THEREOF AND PHARMACEUTICAL USES THEREOF IN PARTICULAR AS INHIBITORS OF CHAPERONE PROTEIN HSP90 ACTIVITIES 审中-公开
标题翻译：新颖的衍生物，含有它们的组合物，其制备方法及其在特定的作为CHAPERONE蛋白质HSP90活性的抑制剂中的药物用途
公开(公告)号：WO2006108948A3
公开(公告)日：2007-10-11
申请号：PCT/FR2006000750
申请日：2006-04-05
申请人： AVENTIS PHARMA SA , MAILLIET PATRICK , BERTIN LUC , BENARD DIDIER , CARREZ CHANTAL , VALLEE FRANCOIS , BACQUE ERIC
发明人： MAILLIET PATRICK , BERTIN LUC , BENARD DIDIER , CARREZ CHANTAL , VALLEE FRANCOIS , BACQUE ERIC
IPC分类号： C07D471/04 , A61K31/4184 , A61P35/00 , C07D519/00
CPC分类号： C07D471/04
摘要： The invention concerns novel products of formula (I), wherein: A1, A2, A3 and A4 represent CRa or N; n represents 1 or 2; R1 represents O, S or NRb; R2 represents H, halogen, CF3, nitro, cyano, methyl, ethyl, hydroxy, mercapto, amino, methoxy, thiomethoxy, methylamino, dimethylamino, acetylamino, carboxy and carboxamido; Ra represents in particular H, halogen, CF3, hydroxy, mercapto, nitro, amino, NH-OH, NH-CO-H, NH-CO-OH, NH-CO-NH2, carboxy, cyano, carboxamido, Y-(CH2)p-alkyl, Y (CH2)p-cycloalkyl, Y-(CH2)p-heterocycloalkyl, Y-(CH2)p-aryl or Y-(CH2)p-heteroaryl, with Y = O, S, NH, O-C(O), C(O)-NH, NH-C(O), NH-S(O) or NH-S(O)2, and p = 1, 2, or 3; Rb represents H, (CH2)m-cycloalkyl, (CH2)m-heterocycloalkyl, (CH2)m-aryl or (CH2)m-heteroaryl, with m = 0, 1, 2; said products being in all isomeric forms and the salts thereof, as medicines.
摘要翻译：本发明涉及式（I）的新产物，其中：A1，A2，A3和A4表示CRa或N; n表示1或2; R1表示O，S或NRb; R 2表示H，卤素，CF 3，硝基，氰基，甲基，乙基，羟基，巯基，氨基，甲氧基，硫代甲氧基，甲基氨基，二甲基氨基，乙酰氨基，羧基和甲酰氨基; R a特别表示H，卤素，CF 3，羟基，巯基，硝基，氨基，NH-OH，NH-CO-H，NH-CO-OH，NH-CO-NH 2，羧基，氰基，甲酰氨基，）对 - 烷基，Y（CH 2）对 - 环烷基，Y-（CH 2）p-杂环烷基，Y-（CH 2）p - 芳基或Y-（CH 2）p - 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，p = 1,2或3。 R b表示H，（CH 2）m - 环烷基，（CH 2）m - 杂环烷基，（CH 2）m - 芳基或（CH 2）m - 杂芳基，其中m = 0,1,2; 所述产物为所有异构体形式及其盐，作为药物。

4. 发明申请

WO2006075094A3 PURINE DERIVATIVES COMPOSITIONS CONTAINING THE SAME AND USE THEREOF AGAINST CANCER 审中-公开
标题翻译：含有它们的嘌呤衍生物组合物及其对癌症的用途
公开(公告)号：WO2006075094A3
公开(公告)日：2006-12-07
申请号：PCT/FR2006000065
申请日：2006-01-11
申请人： AVENTIS PHARMA SA , CARREZ CHANTAL , FASSY FLORENCE , MAILLIET PATRICK , THOMPSON FABIENNE
发明人： CARREZ CHANTAL , FASSY FLORENCE , MAILLIET PATRICK , THOMPSON FABIENNE
IPC分类号： C07D473/34 , A61K31/519 , A61K31/52 , A61P35/00 , C07D471/04 , C07D473/40 , C07D487/04
CPC分类号： C07D473/40
摘要： Purine derivatives of formula (IA1) or (IB1), compositions containing the same and use thereof as medicaments, in particular in oncology, where Y and Z = N or CH, X = halogen, in (IA), A = N or CH and in (IB), A = O, S, NH, CH 2 or CHR, B = O, S, NR', CH 2 or CHR', R = H or alkyl, R' = H, alkyl, alkenyl, alkynyl, (CH 2 ) n -aryl or heteroaryl, CH(aryl) 2 , C(Z)-aryl or heteroaryl, optionally substituted, n= 0, 1, 2 and Z = O, S or NR'.
摘要翻译：式（IA1）或（IB1）的嘌呤衍生物，其中Y和Z = N或CH，X =卤素，在（IA）中，A = N或CH 和（IB）中，A = O，S，NH，CH 2或CHR，B = O，S，NR'，CH 2或CHR'，R = H或烷基，R'= H，烷基，烯基，炔基，（CH 2）n - 芳基或杂芳基，CH（芳基）2 ，C（Z） - 芳基或杂芳基，任选取代的n = 0,1,2且Z = O，S或NR'。

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

WO2004099193A2 1-ARYL-3-(INDOL-5-YL)-PROP-2-EN-1-ONES, COMPOSITIONS COMPRISING THE SAME AND USE THEREOF 审中-公开
标题翻译： 1-ARYL-3-（INDOL-5-YL）-PROP-2-EN-1-ONES，包含它们的组合物及其用途
公开(公告)号：WO2004099193A2
公开(公告)日：2004-11-18
申请号：PCT/FR2004001012
申请日：2004-04-27
申请人： AVENTIS PHARMA SA
发明人： MAILLIET PATRICK , THOMPSON FABIENNE , BERTIN LUC , LECLERE GERARD , TIRABOSCHI GILLES
IPC分类号： A61P35/00 , C07D209/08 , C07D405/06 , C07D405/12
CPC分类号： C07D405/06 , C07D209/08
摘要： The invention relates to 1-aryl-3-(indol-5-yl)-prop-2-en-1-ones, compositions comprising the same and use thereof. The invention particularly relates to novel substituted 1-aryl-3-(indol-5-yl)-prop-2-en-1-ones with a therapeutic activity, of use, in particular, in oncology.
摘要翻译：本发明涉及1-芳基-3-（吲哚-5-基） - 丙-2-烯-1-酮，其组合物及其用途。本发明特别涉及具有治疗活性的新型取代的1-芳基-3-（吲哚-5-基） - 丙-2-烯-1-酮，尤其涉及肿瘤学。

7. 发明申请

WO2005009947A3 ARYL HETEROAROMATIC PRODUCTS, COMPOSITIONS COMPRISING THE SAME AND USE THEREOF 审中-公开
标题翻译： ARYL杂芳族产品，包含其的组合物及其用途的组合物
公开(公告)号：WO2005009947A3
公开(公告)日：2005-03-31
申请号：PCT/FR2004001944
申请日：2004-07-22
申请人： AVENTIS PHARMA SA
发明人： MAILLIET PATRICK , LE-BRUN ALAIN , THOMPSON FABIENNE , TIRABOSCHI GILLES
IPC分类号： A61K31/496 , A61K31/52 , A61K31/53 , A61P35/00 , A61P43/00 , C07D209/42 , C07D231/56 , C07D333/68 , C07D471/04 , A61K31/33
CPC分类号： C07D209/42 , C07D231/56 , C07D333/68 , C07D471/04
摘要： The invention relates to aryl heteroaromatic products, compositions comprising the same and to the use thereof. Said invention relates, in particular, to novel aryl heteroaromatic products having an anticancer activity, and especially, a tubulin polymerization inhibition activity.
摘要翻译：本发明涉及芳基杂芳族产物，包含其的组合物及其用途。本发明特别涉及具有抗癌活性，特别是微管蛋白聚合抑制活性的新型芳基杂芳族产物。

8. 发明申请

WO2004078732B1 N-ARYL HETEROAROMATIC PRODUCTS, COMPOSITIONS CONTAINING SAME AND USE THEREOF 审中-公开
标题翻译： N-ARYL异构产品，其组合物及其用途
公开(公告)号：WO2004078732B1
公开(公告)日：2004-10-28
申请号：PCT/FR2004000168
申请日：2004-01-26
申请人： AVENTIS PHARMA SA
发明人： LE-BRUN ALAIN , THOMPSON FABIENNE , TIRABOSCHI GILLES , MAILLIET PATRICK , SALVINO JOSEPH M
IPC分类号： C07D207/34 , C07D231/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , A61K31/40 , A61K31/415 , C07D401/06 , C07D417/12
CPC分类号： C07D403/04 , C07D207/34 , C07D231/14 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04
摘要： The invention relates to N-aryl heteroaromatic products, compositions containing same and the use thereof. More specifically, the invention relates to novel chemical compounds, particularly novel N-aryl heteroaromatic products, compositions containing same and the use thereof as medicaments, particularly in oncology.
摘要翻译：本发明涉及N-芳基杂芳族产物，含有它们的组合物及其用途。更具体地，本发明涉及新颖的化合物，特别是新颖的N-芳基杂芳族产物，含有它们的组合物及其作为药物的用途，特别是在肿瘤学中。

9. 发明申请

WO0247604A2 NOVEL USE OF CHALCONE CLASS COMPOUNDS 审中-公开
标题翻译： CHALCONE类化合物的新用途
公开(公告)号：WO0247604A2
公开(公告)日：2002-06-20
申请号：PCT/FR0103909
申请日：2001-12-11
申请人： AVENTIS PHARMA SA
发明人： CHIRON MARIELLE , COMBEAU CECILE , MAILLIET PATRICK
IPC分类号： A61K31/136 , A61P9/10 , A61P35/00 , A61K
CPC分类号： A61K31/136
摘要： The invention concerns the use of chalcone class compounds for inhibiting tumoral mass vascularization.
摘要翻译：本发明涉及查耳酮类化合物用于抑制肿瘤质量血管化的用途。

10. 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。

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