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    • 5. 发明申请
    • VIRAL POLYMERASE INHIBITORS
    • 病毒聚合酶抑制剂
    • WO2003007945A1
    • 2003-01-30
    • PCT/CA2002/001129
    • 2002-07-18
    • BOEHRINGER INGELHEIM (CANADA) LTD.BEAULIEU, Pierre, LouisFAZAL, GulrezGOULET, SylvieKUKOLJ, GeorgePOIRIER, MartinTSANTRIZOS, Youla, S.
    • BEAULIEU, Pierre, LouisFAZAL, GulrezGOULET, SylvieKUKOLJ, GeorgePOIRIER, MartinTSANTRIZOS, Youla, S.
    • A61K31/4184
    • C07D401/04C07D235/18C07D403/04C07D405/04C07D405/14C07D409/04C07D409/14C07D417/14C07D471/04
    • An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula (I): wherein R 1 is selected from: H, haloalkyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 3-7 )cycloalkyl, (C 2-6 )alkynyl, (C 5-7 )cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 6-10 )bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR 5 , wherein R 5 is H, halogen, haloalkyl, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; X is N or CR 5 ; D is N or CR 5 ; each of Y 1 and Y 2 is independently O or S; Z is O, N, or NR z wherein R z is H, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; R 3 and R 4 are each independently H, (C 1-6 )alkyl, first (C 3-7 )cycloalkyl, 6- or 10-membered aryl, Het (C 1-6 )alkyl-6- or 10-membered aryl, (C 1-6 )alkyl-Het; or each R 3 and R 4 are independently covalently bonded together to form second (C 3-7 )cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R 3 or R 4 are independently covalently bonded thereto to form a nitrogen-containing heterocycle; R 7 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; or R 7 is covalently bonded to either of R 3 or R 4 to form a heterocycle; A is (C 1-6 ) alkyl-CONHR 8 wherein R 8 is-6- or 10-membered aryl, or Het; or A is a 6- or 10-membered aryl, or Het said aryl or Het being optionally substituted; or a salt or a derivative thereof; such compounds being potent inhibitors of HCV NS5B polymerase.
    • 由式(I)表示的化合物的异构体,对映异构体,非对映异构体或互变异构体:其中R 1选自:H,卤代烷基,(C 1-6)烷基,(C 2-6)烯基,(C 3 -C 6) 7)环烷基,(C 2-6)炔基,(C 5-7)环烯基,6或10元芳基,Het全部被取代; R 2选自(C 1-6)烷基,(C 3-7)环烷基,(C 6-10)双环烷基,6-或10-元芳基,或任选取代的Het; B是N或CR 5,其中R 5是H,卤素,卤代烷基,(C 1-6)烷基,(C 3-7)环烷基或(C 1-6)烷基 - (C 3-7)环烷基; X为N或CR <5>; D为N或CR 5; Y1和Y2各自独立地为O或S; Z是O,N或NR z,其中R z是H,(C 1-6)烷基,(C 3-7)环烷基或(C 1-6)烷基 - (C 3-7)环烷基; R 3和R 4各自独立地为H,(C 1-6)烷基,第一(C 3-7)环烷基,6-或10-元芳基,Het(C 1-6)烷基-6-或10- (C 1-6)烷基-Het; 或每个R 3和R 4独立地共价键合在一起形成全部任意取代的第二(C 3-7)环烷基或杂环; 或当Z为N时,R 3或R 4独立地与其共价键合形成含氮杂环; R 7是H,(C 1-6烷基),(C 3-7)环烷基或(C 1-6)烷基 - (C 3-7)环烷基; 或R 7共价键合到R 3或R 4中的任一个以形成杂环; A是(C 1-6)烷基-CONHR 8,其中R 8是6-元或10元芳基,或Het; 或A是6-或10-元芳基,或Het表示芳基或Het任选被取代; 或其盐或衍生物; 这些化合物是HCV NS5B聚合酶的有效抑制剂。