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1. 发明申请

WO2007083017A3 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF 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用途
公开(公告)号：WO2007083017A3
公开(公告)日：2008-02-14
申请号：PCT/FR2007000079
申请日：2007-01-17
申请人： AVENTIS PHARMA SA , HALLEY FRANK , EL-AHMAD YOUSSEF , CERTAL VICTOR , STROBEL HARTMUT , RITTER KURT , RUF SVEN , DAGALLIER ANNE , VENOT CORINNE
发明人： HALLEY FRANK , EL-AHMAD YOUSSEF , CERTAL VICTOR , STROBEL HARTMUT , RITTER KURT , RUF SVEN , DAGALLIER ANNE , VENOT CORINNE
IPC分类号： C07D401/06 , A61K31/4166 , C07D401/14 , C07D403/06 , C07D403/14
CPC分类号： C07D401/14 , C07D401/06 , C07D403/06 , C07D403/14
摘要： The invention relates to the novel products of formula (I): in which X1 and X2 represent: either one hydrogen and the other alkyl; or one -OCF 3 or -SCF 3 and the other NH-CO-alkyl-R3; or X1 and X2 form, with the phenyl radical to which they are attached, an optionally substituted dihydro-indole radical; R represents pyridyl or pyrimidinyl substituted with NR1R2, with R1 representing hydrogen or alkyl, and R2 representing optionally substituted alkyl, cycloalkyl, heterocycloalkyl, phenyl, pyrimidinyl, pyridyl, and CO-R3 with R3 representing in particular amine, alkoxy, heterocycloalkyl, aryl, aryloxy and heteroaryl; all these radicals being optionally substituted; and salts thereof.
摘要翻译：本发明涉及式（I）的新产物：其中X 1和X 2表示：一个氢和另一个烷基; 或一个-OCF 3 - 或-SCF 3 - 和另一个NH-CO-烷基-R 3; 或X 1和X 2与它们所连接的苯基形成任选取代的二氢 - 吲哚基; R代表被NR 1 R 2取代的吡啶基或嘧啶基，其中R1代表氢或烷基，R2表示任选取代的烷基，环烷基，杂环烷基，苯基，嘧啶基，吡啶基和CO-R3，其中R3表示特别是胺，烷氧基，杂环烷基，芳基，芳氧基和杂芳基; 所有这些基团任选被取代; 及其盐。

2. 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。

3. 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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