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    • 1. 发明申请
    • Non-Nucleotide Reverse Transcriptase Inhibitors
    • 非核苷酸逆转录酶抑制剂
    • US20080070951A1
    • 2008-03-20
    • US10584933
    • 2004-12-30
    • Christian SundNathalie RoueStefan LindstromDmitry AntonovChrister SahlbergKatarina Jansson
    • Christian SundNathalie RoueStefan LindstromDmitry AntonovChrister SahlbergKatarina Jansson
    • A61K31/44A61P31/18C07D211/00
    • C07D409/12C07D405/12C07D405/14C07D409/14
    • Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(═O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(═O)ORx, —NRxOH; —C(═O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(═O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(═O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(═O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)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, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(═O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8′)n-D-(CR8R8′)m-; D is a bond, —NR9—, —O—, —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)n R a的A的环中的碳原子的取代基,其中R a是-C 1 - -O - , - NR x R x,-NHNR x R x,-NHNHC(-O)OR x,-NR x OH; -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,C 1 -C 4烷基,-NR x R x; -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-COOR x; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯(OC 烷基)qO-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; R 3 -R 7是说明书中定义的取代基; X是 - (CR 8 R 8 8)n-D-(CR 8 R 8)m - ; D是键,-NR 9 - , - O - , - S - , - S(= O) - 或-S(= O)2 - 其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。
    • 2. 发明授权
    • Non-nucleotide reverse transcriptase inhibitors
    • 非核苷酸逆转录酶抑制剂
    • US07915295B2
    • 2011-03-29
    • US10584933
    • 2004-12-30
    • Christian SundNathalie RoueStefan LindstromDmitry AntonovChrister SahlbergKatarina Jansson
    • Christian SundNathalie RoueStefan LindstromDmitry AntonovChrister SahlbergKatarina Jansson
    • A61K31/453C07D405/12
    • C07D409/12C07D405/12C07D405/14C07D409/14
    • Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(═O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(═O)ORx, —NRxOH; —C(═O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(═O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(═O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(═O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)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, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, —S(═O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8′)n-D-(CR8R8′)m-; D is a bond, —NR9—, -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,-NHNHC(= O)OR x, NR x OH; -C(= O)-R b,其中R b是-CT-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 )ORx,-C1-C3-烷基-COORx; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯(O-C 1 -C 3烷基)q-O-R 1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。