MERCK PATENT GESELLSCHAFT MIT BESCHRAENKTER HAFTUNG
发明人:
BUCHSTALLER, HANS-PETER,FINSINGER, DIRK,WIESNER, MATTHIAS,BURGDORF, LARS,AMENDT, CHRISTIANE,GRELL, MATTHIAS,SIRRENBERG, CHRISTIAN,ZENKE, FRANK
申请号：
CA2531859
公开号：
CA2531859C
申请日:
2004.06.15
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
The present invention relates to a benzimidazole derivative of formula I:(see formula I)wherein: R6 and R7 are independently H or A, A is alkyl, Ar2 is independentlyphenyl, pyridinylor pyrimidyl, R8 is alkyl, alkoxy or perhaloalkyl comprising 1 to 4 carbonatoms, Hal, CH2Hal,CH(Hal)2, NO2 or (CH2)n CN, R9 and R10 are independently H, A, cycloalkylcomprising 3 to 7carbon atoms, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)n CN, (CH2)nNR11R12, (CH2)n OR11,(CH2)n O(CH2)k NR11R12, (CH2)n COOR12, (CH2),CONR11R12, (CH2)n NR11COR13,(CH2)n NR11CONR11R12, (CH2)n NR11SO2A, (CH2)n SO2NR11R12, (CH2)n S(O)n R13,(CH2)n OC(O)R13, (CH2)n COR13, (CH2)n SR11, CH=N-OA, CH2CH=N-OA, (CH2)n NHOA,(CH2)n CH=N-R11, (CH2)n OC(O)n R11R12, (CH2)n NR11COOR12, (CH2)nN(R11)CH2CH2OR13,(CH2)n N(R11)CH2CH2OCF3, (CH2)n N(R11)C(R13)HCOOR12, C(R13)HCOR12,(CH2)n N(R11)CH2CH2N(R12)CH2COOR12, (CH2)n N(R11)CH2CH2NR11R12, CH=CHCOOR11,CH=CHCH2NR11R12, CH=CHCH2NR11R12, CH=CHCH2OR13, (CH2)n N(COOR11)COOR12,(CH2)n N(CONH2)COOR11, (CH2)n N(CONH2)CONH2, (CH2)n N(CH2COOR11)COOR12,(CH2)n N(CH2CONH2)COOR11, (CH2)n N(CH2CONH2)CONH2, (CH2)n CHR13COR11,(CH2)n CHR13COOR11, (CH2)n CHR13CH2OR14, (CH2)n OCN or (CH2)n NCO, wherein R11and R12are independently H, A, (CH2)m Ar3 or (CH2)m Het, or in NR11R12, R11 and R12form, together withthe N-atom they are bound to, a 5-, 6- or 7-membered heterocyclus, R13 and R14areindependently H, Hal, A, (CH2)m Ar4 or (CH2)m Het, Ar3 and Ar4 areindependently optionallysubstituted aromatic hydrocarbon residues comprising 5 to 12 carbon atoms, Hetis anoptionally substituted saturated, unsaturated or aromatic heterocyclicresidue, k, m and n areindependently 0, 1, 2, 3, 4, or 5, X is S, CH2 or O, Y is O, S or NR21, R21 isindependentlyselected from the meanings given for R13, R14 and p and r are independently 0,1, 2, 3, 4 or 5,q is 0, 1, 2, 3 or 4, u is 0, 1, 2 or 3, and Hal is independently F, CI, Br orI； or a
