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    • 5. 发明授权
    • Viral polymerase inhibitors
    • 病毒聚合酶抑制剂
    • US07576079B2
    • 2009-08-18
    • US11333163
    • 2006-01-17
    • Pierre Louis BeaulieuGulrez FazalSylvie GouletGeorge KukoljMartin PoirierYoula S. TsantrizosJames GillardMarc-Andre Poupart
    • Pierre Louis BeaulieuGulrez FazalSylvie GouletGeorge KukoljMartin PoirierYoula S. TsantrizosJames GillardMarc-Andre Poupart
    • A61K31/5377A61K31/454C07D417/14
    • C07D333/62C07D209/08C07D209/30C07D209/42C07D401/04C07D403/04C07D405/04C07D409/04C07D413/04C07D417/04C07D471/04
    • An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein;  represents either a single or a double bond; R2 is selected from 6 or 10-membered aryl and Het, each optionally substituted with R20; provided that Het is not a 5- or 6-membered monocyclic heterocycle having 1 or 2 nitrogen heteroatoms; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of which optionally substituted with R90; or R9 is covalently bonded to either of R7 or R8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
    • 由式I表示的化合物的异构体,对映体,非对映异构体或互变异构体:其中:A是O,S,NR1或CR1,其中R1如本文所定义; “img id =”CUSTOM-CHARACTER-00001“he =”2.46mm“wi =”6.35mm“file =”US07576079-20090818-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示单键或双键; R2选自6或10元芳基和Het,各自任选被R 20取代; 条件是Het不是具有1或2个氮杂原子的5或6元单环杂环; B是NR 3或CR 3,条件是A或B中的一个是CR 1或CR 3,其中R 3在本文中定义; K是N或CR 4,其中R 4在本文中定义; L是N或CR5,其中R5与R4具有相同的定义; M是N或CR7,其中R7与R4具有相同的定义; Y1为O或S; Z是N(R6a)R6或OR6,其中R6a是H或烷基或NR61R62,其中R61和R62在本文中定义; 且R 6为H,烷基,环烷基,烯基,Het,烷基 - 芳基,烷基-Het; 或R6是其中R7和R8和Q如本文所定义; Y2为O或S; R9是H,(C1-6烷基),(C3-7)环烷基或(C1-6)烷基 - (C3-7)环烷基,芳基,Het,(C1-6)烷基 - 芳基或(C1-6) 烷基-Het,它们全部被R90取代; 或R 9与R 7或R 8中的任一个共价连接以形成5-或6-元杂环; 其盐或其衍生物,作为HCV NS5B聚合酶的抑制剂。