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    • 4. 发明授权
    • Non-nucleoside reverse transcriptase inhibitors
    • 非核苷逆转录酶抑制剂
    • US06806265B2
    • 2004-10-19
    • US10430116
    • 2003-05-06
    • Bruno SimoneauSerge LandryEric MalenfantJulie NaudJeffrey O'MearaBounkham ThavonekhamChristiane Yoakim
    • Bruno SimoneauSerge LandryEric MalenfantJulie NaudJeffrey O'MearaBounkham ThavonekhamChristiane Yoakim
    • C07D47114
    • C07D471/14
    • Compounds represented by formula I: wherein R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)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 CONR12R13; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; 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(C1- 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 并且E是CONR 12 R 13; CONHNR 14 R 15; NR 16 COR 17; NR 18(C 1-6)烷基; SO 2 NR 19 R 20; 或SO2R 21; 或者n为1时:环C如上所定义,E为单键或连接基团; 且R D为具有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逆转录酶的抑制剂提供。