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    Amino cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
    1.
    发明公开
    Amino cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors 审中-公开
    氨基环脲衍生物，其制备方法及其药物用途作为激酶抑制剂的

    公开(公告)号：EP1621536A1

    公开(公告)日：2006-02-01

    申请号：EP04291904.3

    申请日：2004-07-27

    申请人： Aventis Pharma S.A.

    发明人： Strobel, Hartmut ,  Nemecek, Conception ,  Lesuisse, Dominique ,  Ruf, Sven ,  El-Ahmad, Youssef ,  Guessregen, Stefan ,  Lebrun, Anne ,  Ritter, Kurt ,  Benard, Didier ,  Hittinger, Augustin ,  Bouchard, Hervé

    IPC分类号： C07D401/06 ,  C07D401/14

    CPC分类号： C07D403/04

    摘要： The invention relates to novel products of formula (I):

    in which p = 0, 1 and 2;
    A = aryl, heteroaryl, carbocycle or heterocycle;
    X = single bond, -N(R6)-, -O-, -C(O)-, -S(O)n-, -N(R6)-C(O)-, -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-, -C(O)O-;
    L1 = alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene;
    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 L 1 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）的新颖的产品：其中p = 0，1和2; A =芳基，杂芳基，碳环或杂环; X =单键，-N（R6） - ， - O-，-C（O） - ， - S（O）N - ， - N（R6）-C（O） - ， - 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） - ， - SO 2 NR 6，-C（O）O-; L1 =亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚杂芳基; R1 =氢，烷基，烯基，炔基或环烷基，芳基，杂芳基，芳烷基，杂芳基烷基; -SO2R9，-C（O）R 9; -C（O）OR 9，-C（O）NR 10 R 11，-C（S）NR 10 R 11，-SO2NR10R11; R2 =氢，烷基，烯基，炔基，环烷基，要么R 1和R 2与N或NR 1 R 2与L 1可以形成饱和或不饱和的杂环可能含有O，N，S; R3 =氢; 卤素; 烷基，烯基，炔基，环烷基，烷氧基，亚烷二氧基，杂环，芳基和杂芳基，全部任选地substituiertem; S（O）N烷基; 氨基，烷基氨基，二烷基氨基，与用N二烷基氨基OPTIONALLY形成一个循环，全部任选substituiertem; R4，R4 '和R4'“=氢，卤素，烷基，烯基，炔基，环烷基，芳基，杂芳基，氧代; 有两个从R4，R4“和R4”中“可能与C形环可能包含O形成，N或S; L2 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，-O - ，-NR 17 - ， - C（O） - ，SO 2; Y = N杂环可能含有O，N或S; 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; 所有论文基团任选地substituiertem，论文产品在所有的同分异构形式和这些盐的，作为医药品。