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    • 8. 发明申请
    • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    • 非核苷反义转录酶抑制剂
    • WO2002076982A2
    • 2002-10-03
    • PCT/CA2002/000385
    • 2002-03-21
    • BOEHRINGER INGELHEIM (CANADA) LTD.OGILVIE, William, W.DÉZIEL, RobertNAUD, JulieO'MEARA, Jeffrey
    • OGILVIE, William, W.DÉZIEL, RobertNAUD, JulieO'MEARA, Jeffrey
    • C07D471/00
    • C07D471/14
    • A compound of formula I:wherein A is a connecting chain of (C 1-3 ) alkyl; B is O or S; R 1 is H, (C 1-6 ) alkyl, halo, CF 3 , or OR 1a wherein R 1a is H or (C 1-6 )alkyl; R 2 is H or Me; R 3 is H or Me; R 4 is H, (C 1-4 ) alkyl, (C 3-4 ) cycloalkyl and (C 1-4 )alkyl(C 3-7 )cycloalkyl; W is selected form formula (i), (ii) or (iii) wherein, a) one of Y is SO 2 and the other Y is NR 5 , provided that both are not the same, wherein R 5 is H, (C 1-6 )alkyl,(C 3-6 ) cycloalkyl, the alkyl being substituted, COR 5o , COOR 5p or CONR 5p R 5q ; and each R 8 is H, (C 1-4 ) alkyl, (C 3-6 ) cycloalkyl, or (C 1-4 ) alkyl-(C 3-6 ) cycloalkyl; or b) E is CR 8a R 8b wherein R 8a and R 8b is H, or alkyl and J is CH 2 ; or J is CR 8a R 8b and E is CH 2 , and the dotted line represents a single bond; or c) E is C(O) and J is CR 8a R 8b or J is C(O) and E is CR 8a R 8b and the dotted line represents a single bond; or d) E and J are CR 8a R 8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
    • 式I化合物:其中A是(C 1-3烷基)的连接链; B是O或S; R 1是H,(C 1-6烷基),卤素,CF 3或OR 1a,其中 R1a是H或(C1-6)烷基; R 2是H或Me; R 3是H或Me; R 4是H,(C 1-4)烷基,(C 3-4)环烷基和(C 1-4) )烷基(C <子> 3-7 )环烷基; W选自式(i),(ii)或(iii),其中a)Y是SO 2中的一个且另一个Y是NR 5,条件是 两者不相同,其中R 5是H,(C 1-6烷基),(C 3-6 - )环烷基, 烷基被取代的COR 5,COOR 5P或CONR 5P 5 R 5; 和每个R 8是H,(C 1-4烷基),(C 3-6)环烷基或(C 1-4烷基) 1-4)烷基 - (C 3-6 - )环烷基; 或b)E为CR 8a R 8b其中R 8a和R 8b为H或烷基和J 是CH 2 ; 或J是CR 8a R 8b和E是CH 2 2,虚线代表单键; 或c)E为C(O)且J为CR 8a R 8b或J为C(O)且E为CR 8a R 并且虚线表示单键;并且虚线表示单键。 或d)E和J是CR 8a R 8b并且虚线表示双键。 式I化合物具有抗HIV WT和双突变株的活性。