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    • 7. 发明授权
    • Azetidinone derivatives for the treatment of HCMV infections
    • 氮杂环丁酮衍生物用于治疗HCMV感染
    • US06211170B1
    • 2001-04-03
    • US09167141
    • 1998-10-06
    • Christiane YoakimRobert DézielStephen KawaiWilliam W. OgilvieJeffrey O'MearaCatherine Chabot
    • Christiane YoakimRobert DézielStephen KawaiWilliam W. OgilvieJeffrey O'MearaCatherine Chabot
    • C07D20508
    • C07D205/08C07D403/12
    • A compound of formula I: wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or C1-3 alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or phenyl (lower alkyl); or R6 is Het or Het(lower alkyl; or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with benzyloxycarbonyl or with phenyl optionally substituted among other group with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; X is selected from the group consisting of O, S, SO, SO2, NR8, wherein R8 is H or lower alkyl; and Y is C1-10 non-cyclic or cyclic alkyl; [(CH2)0-1]-phenyl, said phenyl ring optionally substituted; Het or Het(lower alkyl); or when X is NR8, wherein R8 is lower alkyl and Y is lower alkyl or lower alkoxy, X and Y are joined together to form a morpholino or piperidino ring; or a therapeutically acceptable acid addition salt thereof, which compound is useful in the treatment of HCMV infection.
    • 式I的化合物:其中R 1是氢,甲基,乙基,甲氧基或甲硫基; R2和R3各自独立地为氢或C1-3烷基; R4是氢,低级烷基,甲氧基,乙氧基或苄氧基; R5是低级烷基,低级环烷基,(CH2)mC(O)OR6,其中m是整数1或2,R6是低级烷基,任选被C(O)OR 7取代的苯基,其中R 7是低级烷基或苯基(低级烷基) ; 或R6是Het或Het(低级烷基;或R4和R5与它们所连接的氮原子一起形成任选被苄氧基羰基取代的含氮环或与C(O)OR 7任选取代的苯基,其中R 7是 低级烷基或(低级烷基)苯基; X选自O,S,SO,SO 2,NR 8,其中R 8为H或低级烷基; Y为C 1-10非环状或环状烷基; [(CH 2 )0-1] - 苯基,所述苯环任选被取代; Het或Het(低级烷基);或当X是NR8时,其中R8是低级烷基,Y是低级烷基或低级烷氧基,X和Y连接在一起形成 吗啉或哌啶子基环;或其治疗上可接受的酸加成盐,该化合物可用于治疗HCMV感染。