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1. 发明申请

WO2006010641A3 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：新型环状尿素衍生物及其制备方法和作为激酶抑制剂的药物用途
公开(公告)号：WO2006010641A3
公开(公告)日：2006-10-26
申请号：PCT/EP2005008720
申请日：2005-07-25
申请人： AVENTIS PHARMA SA , STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
发明人： STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
IPC分类号： C07D401/06 , A61K31/4166 , C07D401/14
CPC分类号： C07D403/04
摘要： The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
摘要翻译：本发明涉及式（I）的产物：其中p = 0,1和2; A =芳基，杂芳基，碳环或杂环; X =单键; -N（R 6） - ; -NH-烷 - ; 亚; -O-; -C（O） - ; -儿子-; -N（R 6）-C（O） - ; -NH-CO-alk-，-N（R 6）-C（O）-N（R 6'） - ; -N（R6）-C（S）-N（R6' ） - ; -N（R 6）-C（O）O-; -N（R 6）-SO 2 - ; -N（R6）-SO2-N（R6' ） - ; -C（O）-N（R6） - ; -SO 2 NR 6 - ; 和-C（O）O-; L1 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚杂芳基; 全部任选被取代; R1 =氢，烷基，烯基，炔基或环烷基，芳基，杂芳基，芳基烷基，杂芳基烷基; -SO 2 R 9，-C（O）R 9; -C（O）OR 9，-C（O）NR 10 R 11，-C（S）NR 10 R 11，-SO 2 NR 10 R 11; R 2 =氢，烷基，烯基，炔基，环烷基，R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O，N，S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基，烯基，炔基，环烷基，烷氧基，亚烷基二氧基，杂环，芳基和杂芳基，全部任选被取代; S（O）n-烷基; 氨基，烷基氨基，二烷基氨基，任选与N环形成的二烷基氨基，全部任选被取代; R4，R4'和R4“=氢，卤素，烷基，烯基，炔基，环烷基，芳基，杂芳基，氧代; 其中R4，R4'和R4“中的两个可能与C形成可能含有O，N或S的环; L2 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，-O - ， - NR17-，-C（O） - ，SO2; Y =可能含有O，N或S的N-杂环; R5 =氢，卤素，烷基，烯基，炔基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基; 所有这些基团任选地被取代，这些产物以所有异构形式和盐作为医药产品。

2. 发明申请

WO0168655A3 CAPROLACTAM DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：卡波拉明衍生物及其用途
公开(公告)号：WO0168655A3
公开(公告)日：2002-08-01
申请号：PCT/US0107935
申请日：2001-03-12
申请人： ARIAD PHARMA INC , DEPREZ PIERRE , LESUISSE DOMINIQUE , BENARD DIDIER
发明人： DEPREZ PIERRE , LESUISSE DOMINIQUE , BENARD DIDIER
IPC分类号： A61K38/00 , C07F9/12 , C07F9/40 , C07F9/553 , C07K5/06 , C07K5/065 , A61K31/675 , A61K38/05 , C07C233/47 , C07D223/12 , C07K5/068
CPC分类号： C07K5/06191 , A61K38/00 , C07F9/12 , C07F9/4056 , C07F9/5532 , C07K5/06078
摘要： The invention involves derivatives of caprolactam of the formula (I) in which [A ], A and R have the meanings indicated in the description, their salts and their prodrugs. The invention also relates to the preparation of such compounds, synthetic intermediates, their use, and in particular, antagonists of the Src SH2 domain and inhibitors of bone resorption and pharmaceutical compounds containing such compounds.
摘要翻译：本发明涉及式（I）的己内酰胺的衍生物，其中[A 1]，A 2和R 1具有说明书中所述的含义及其盐及其前药。本发明还涉及制备这些化合物，合成中间体，它们的用途，特别是Src SH2结构域的拮抗剂和骨吸收抑制剂以及含有这些化合物的药物化合物。

3. 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。

4. 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。

5. 发明申请

WO2004070050A2 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL USE OF SAME AS KINASE INHIBITORS 审中-公开
标题翻译：新型循环尿素衍生物，其制备方法及其作为激酶抑制剂的药物应用
公开(公告)号：WO2004070050A2
公开(公告)日：2004-08-19
申请号：PCT/FR2004000188
申请日：2004-01-28
申请人： AVENTIS PHARMA SA
发明人： PATEK MARCEL , NAIR ANIL , HITTINGER AUGUSTIN , NEMECEK CONCEPTION , BOND DANIEL , HARLOW GREG , BOUCHARD HERVE , MAUGER JACQUES , MALLERON JEAN-LUC , PALERMO MARK , AL-OBEIDI FAHAD , FAITG THOMAS , STROBEL HARTMUT , RUF SVEN , RITTER KURT , EL-AHMAD YOUSSEF , LESUISSE DOMINIQUE , BENARD DIDIER
IPC分类号： A61P3/00 , A61P7/02 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P35/00 , C07D401/06 , C07D401/14 , C12Q
CPC分类号： C07D401/06 , C07D401/14
摘要： The invention relates to novel products having formula (I), wherein: p denotes 0 to 2; R and R1 denote O or NH; R2 and R3 denote hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, or R2 and R3, together with the carbon atom to which they are bound, form a carbocyclic or heterocyclic radical, all of said radicals being optionally substituted; A1 denotes a single bond, alkyl, allyl and propynyl; Y and Y1 denote H, OCF3, S(O)nCF3, S(O)nAlk, SO2CHF2, SO2CF2CF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5 and SO2NR5R6, whereby R5 and R6 are selected from among hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl and heteroaryl, which are optionally substituted, or R5 and R6, together with N to which they are bound, form a heterocyclic radical; A2 denotes Al, CO and SO2; B2 denotes a heterocyclic radical which is optionally substituted with one or more substituents which are selected from the values of Y2; Y2 denotes hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -O-alkenyl, -O-alkynyl, O-cycloalkyl, S(O)n-alkyl, -S(O)n-alkenyl, -S(O)n-alkynyl, S(O)n-cycloalkyl, -COOR13,-OCOR13, NR5R6, CONR5R6, S(O)n-NR5R6,-NR10-CO-R13, -NR10-SO2-R13, -NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of said radicals being optionally substituted; and n denotes an integer of between 0 and 2. The aforementioned products are in all the isomeric forms and the salts thereof for use as medicaments.
摘要翻译：本发明涉及具有式（I）的新产品，其中：p表示0至2; R和R1表示O或NH; R 2和R 3表示氢，烷基，烯基，炔基，环烷基，芳基和杂芳基，或者R 2和R 3与它们所连接的碳原子一起形成碳环或杂环基，所有基团都是任选被取代的; A1表示单键，烷基，烯丙基和丙炔基; Y和Y1表示H，OCF3，S（O）nCF3，S（O）nAlk，SO2CHF2，SO2CF2CF3，-O-CF2-CHF2，-O-CHF2，-O-CH2-CF3，SF5和SO2NR5R6， R 6选自任选取代的氢，烷基，烯基，环烷基，环烯基，杂环烷基，芳基和杂芳基，或R 5和R 6与它们所连接的N一起形成杂环基; A2表示Al，CO和SO2; B2表示任选被一个或多个选自Y2的取代基取代的杂环基; 环烷基，杂环烷基，芳基，杂芳基，-O-烯基，-O-炔基，O-环烷基，S（O）n - 烷基，-S（O）n - 烯基，-S（O）n - 炔基，S（O）n-环烷基，-COOR 13，-OCOR 13，NR 5 R 6，CONR 5 R 6，S（O）n -NR 5 R 6，-NR 10 -CO-R 13，-NR 10 -SO 2 - R13，-NH-SO2-NR5R6，-NR10-CO-NR5R6，-NR10-CS-NR5R6，-NR10-COOR13，所有所述基团任选被取代; 并且n表示0和2之间的整数。上述产物是全部异构形式及其盐，用作药物。

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