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    • 8. 发明申请
    • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    • 非核苷酸逆转录酶抑制剂
    • WO2003097644A2
    • 2003-11-27
    • PCT/CA2003/000718
    • 2003-05-14
    • BOEHRINGER INGELHEIM INTERNATIONAL GMBHSIMONEAU, BrunoLANDRY, SergeMALENFANT, ÉricNAUD, JulieO'MEARA, JeffreyTHAVONEKHAM, BounkhamYOAKIM, Christiane
    • SIMONEAU, BrunoLANDRY, SergeMALENFANT, ÉricNAUD, JulieO'MEARA, JeffreyTHAVONEKHAM, BounkhamYOAKIM, Christiane
    • C07D471/14
    • C07D471/14
    • Compounds represented by formula (I), wherein R 2 is selected from the group consisting of H, (C 1-4 )alkyl, halo, haloalkyl, OH, (C 1-6 )alkoxy, NH(C 1-4 alkyl) or N(C 1-4 alkyl) 2 ; R 4 is H or Me; R 5 is H or Me; R 11 is H, (C 1-4 )alkyl, (C 3-4 )cycloalkyl and (C 1-4 )alkyl-(C 3-4 )cycloalkyl; A is a connecting chain of (C 1-3 )alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR 12 R 13 ; CONHNR 14 R 15 ; NR 16 COR 17 ; NR 18 SO 2 (C 1-6 )alkyl; SO 2 NR 19 R 20 ; or SO 2 R 21 ; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.
    • 由式(I)表示的化合物,其中R 2选自H,(C 1-4)烷基,卤素,卤代烷基,OH,(C 1-6)烷氧基,NH(C 1-4烷基)或N (C 1-4烷基)2; R 4是H或Me; R 5是H或Me; R 11是H,(C 1-4)烷基,(C 3-4)环烷基和(C 1-4)烷基 - (C 3-4)环烷基; A是(C 1-3)烷基的连接链; B是O或S; n为0或1; 其中当n为0时:环C为具有1至4个选自O,N和S的杂原子的6-元或10元芳基或5-或6-元杂环,所述芳基和所述杂环任选地 取代; 并且E是CONR 12 R 13; CONHNR <14> - [R <15>; NR <16> COR <17>; NR <18> SO 2(C 1-6)烷基; SO 2 NR <19> - [R <20>; 或SO2R 21; 或当n为1时:环C如上定义,E为单键或连接基团; 环D是具有1至4个选自O,N和S的杂原子的6-或10-元芳基或5-或6-元杂环,所述芳基和所述杂环任选被1至 5个取代基; 或其盐或前药作为HIV逆转录酶的抑制剂。
    • 10. 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。