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    • 2. 发明申请
    • NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS
    • 非核苷酸逆转录酶抑制剂
    • WO2005066131A1
    • 2005-07-21
    • PCT/SE2004/002034
    • 2004-12-30
    • MEDIVIR ABSUND, ChristianROUE, NathalieLINDSTRÖM, StefanANTONOV, DmitrySAHLBERG, ChristerJANSSON, Katarina
    • SUND, ChristianROUE, NathalieLINDSTRÖM, StefanANTONOV, DmitrySAHLBERG, ChristerJANSSON, Katarina
    • C07D213/75
    • C07D409/12C07D405/12C07D405/14C07D409/14
    • Compounds of the formula Z: where; A is CH or N; R 1 is a substituent to a carbon atom in the ring containing A selected from -S(=O) p Ra, where Ra is -C 1 -C 4 alkyl, -ORx, -NRxRx, -NHNRxRx, - NHNHC(=O)ORx, -NRxOH; -C(=O)-Rb, where Rb is -CT-C4-alkyl, ORx, -NRxRx, -NHNRxRx, -NHC 1 -C 3 -alkyl-C(=O)Orx -NRxRc, where Rc is H, C 1 -C 4 alkyl, -NRxRx; -C(=0)Rd, -CN, S(=O)pRx where Rd is Rd is C1-C4-alkyl, -ORx, -NRxRx C 1 -C 3 -alkyl-O-Cl-C3alkylC(=O)ORx, -C 1 -C 3 -alkyl-COORx; -C 1 -C 3 alkyl-OH or C 1 -C 4 alkyl ethers or esters thereof (O-C l -C 3 alkyl)q-O-Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C 1 -C 4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, -S(=O),- or -CH 2 -, where r is 0, 1 or 2; R 3 -R 7 are substituents as defined in the specification; X is -(CR 8 R 8 ')n-D-(CR 8 R 8 ')m-; D is a bond, -NR 9 -, -0-, -S-, -S(=0)- or -S(=0) 2 -; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
    • 式Z的化合物:其中; A是CH或N; R 1是含有选自-S(= O)p R a的A的环中的碳原子的取代基,其中R a是-C 1 -C 4烷基,-OR x,-NR x R x,-NHNR x R x,-NH NH(= O)OR x, NRxOH; -C(= O)-R b,其中R b是-C 1 -C 4 - 烷基,OR x,-NR x R x,-NHNR x R x,-NHC 1 -C 3 - 烷基-C(= O)OR x -NR x R c,其中R c是H, C4烷基,-NRxRx; -C(= O)R d,-CN,S(= O)p R x其中Rd是Rd是C 1 -C 4 - 烷基,-OR x,-NR x R x C 1 -C 3烷基-O-C 1 -C 3烷基C(= O)OR x, -C 1 -C 3 - 烷基 - COORx; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯(O-Cl-C 3烷基)q-O-Rx具有1-3个杂原子的5或6元芳环p为1或2; R x独立地选自H,C 1 -C 4烷基或乙酰基; 或一对Rx可与相邻的N原子一起形成环; L是-O - , - S(= O), - 或-CH 2 - ,其中r是0,1或2; R3-R7是说明书中定义的取代基; X是 - (CR8R8')n-D-(CR8R8')m-; D是键,-NR 9 - , - O - , - S - , - S(= O) - 或-S(= O) 其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。