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    Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
    3.
    发明专利
    Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors 未知

    公开(公告)号：NZ505776A

    公开(公告)日：2003-06-30

    申请号：NZ50577698

    申请日：1998-03-09

    Applicant: VERTEX PHARMA

    Inventor： SPALTENSTEIN ANDREW ,  TUNG ROGER D ,  HALE MICHAEL R ,  BAKER CHRISTOPHER T ,  FURFINE ERIC STEVEN ,  KALDOR ISTVAN ,  KAZMIERSKI WIESLAW WIECZYSLAW

    IPC: A61K31/18 ,  A61K31/215 ,  A61K31/265 ,  A61K31/27 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4025 ,  A61K31/496 ,  A61K31/66 ,  A61K31/661 ,  A61K31/664 ,  A61K31/7048 ,  A61K45/00 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07C311/15 ,  C07C311/18 ,  C07C311/37 ,  C07D277/30 ,  C07D307/20 ,  C07D405/12 ,  C07D407/12 ,  C07D417/12 ,  C07F9/655 ,  C07F9/6584 ,  C07H15/04 ,  C07H15/26 ,  A61K31/665 ,  A61K31/70 ,  C07H15/18

    Abstract: The compound of Formula I wherein: A is selected from H; Ht; -R1-Ht; -R1-(C1-C6)-alkyl, which is optionally substituted; -R1-(C2-C6)-alkenyl, which is optionally substituted; R1 is selected from -C(O)-, -S(O)2-, -C(O)-C(O)-, -O-C(O)-, -O-S(O)2, -N(R2)-S(O)2-, -N(R2)-(O)- or -N(R2)-C(O)-C(O)-; Ht is selected from C3-C7 cycloalkyl; C5-C7 cycloalkenyl; C6-C10 aryl; or a 5-7 membered heterocycle, containing 1 or more heteroatoms selected from N, N(R2), O, S and S(O)n; wherein said aryl or said heterocycle is optionally fused to Q; and wherein any member of said Ht is optionally substituted with one or more substituents selected from oxo, -OR2, SR2, -R2, -N(R2)2, -R2-OH, -CN, -C(O)O-R2, -C(O)-N(R2)2, -S(O)2-N(R2)2, -N(R2)-C(O)-R2, -C(O)-R2, -S(O)n-R2, -OCF3, -S(O)n-Q, methylenedioxy, -N(R2)-S(O)2-R2, halo, -CF3, -NO2, Q, -OQ, -OR7, -SR7, -R7, -N(R2)(R7) or -N(R7)2; R2 is selected from H, or (C1-C4)-alkyl optionally substituted with Q; B, when present, is -N(R2)-C(R3)2-C(O)-; x is 0 or 1; R3 is selected from H, Ht, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C6)-cycloalkyl or (C5-C6)-cycloalkenyl; wherein any member of said R3, except H, is optionally substituted; n is 1 or 2; G, when present, is selected from H, R7 or (C1-C4)-alkyl, or, when G is (C1-C4)-alkyl, G and R are bound to one another either directly or through a C1-C3 linker to form a heterocyclic ring; or when G is absent, the atom to which G is attached is bound directly to the R7 group in ?OR7 with the concomitant displacement of one -ZM group from R7; D and D' are selected from Q; (C1-C6)-alkyl, which is optionally substituted; (C2-C4)-alkenyl, which is optionally substituted; Q is selected from a 3-7 membered carbocyclic ring system; or a 5-7 membered heterocyclic ring containing one or more heteroatoms selected from O, N, S, S(O)n or N(R2); wherein any ring in Q is optionally substituted; E is selected from Ht; O-Ht; Ht-Ht; -O-R3; -N(R2)(R3); (C1-C6)-alkyl, which is optionally substituted; (C2-C6)-alkenyl, which is optionally substituted; (C3-C6)-saturated carbocycle, which is optionally substituted; or (C5-C6)-unsaturated carbocycle, which is optionally substituted; R4 is selected from ?OR2, -SR2, -C(O)-NHR2, -S(O)2-NHR2, halo, -N(R2)-C(O)-R2, -N(R2)2 or -CN; R7 is selected from formulas (ii) or (iii) wherein each M is selected from H, Li, Na, K, Mg, Ca, Ba, -N(R2)4, (C1-C12)-alkyl, (C2-C12)-alkenyl, or ?R6; wherein 1 to 4 -CH2 radicals of the alkyl or alkenyl group, other than the -CH2 that is bound to Z, is optionally replaced by a heteroatom group selected from O, S, S(O), S(O)2, or N(R2); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced with a substituent selected from oxo, -OR2, -R2, N(R2)2, N(R2)3, R2OH, -CN, -C(O)OR2, -C(O)-N(R2)2, S(O)2-N(R2)2, N(R2)-C(O)-R2, C(O)R2, -S(O)n-R2, OCF3, -S(O)n-R6, N(R2)-S(O)2-R2, halo, -CF3, or -NO2; M' is H, (C1-C12)-alkyl, (C2-C12)alkenyl, or ?R6; wherein 1 to 4 -CH2 radicals of the alkyl or alkenyl group is optionally replaced by a heteroatom group selected from O, S, S(O), S(O)2, or N(R2); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced with a substituent selected from oxo, -OR2, -R2, -N(R2)2, N(R2)3, -R2OH, -CN, -CO2R2, -C(O)-N(R2)2, -S(O)2-N(R2)2, -N(R2)-C(O)-R2, -C(O)R2, -S(O)n-R2, -OCF3, -S(O)n-R2, -N(R2)-S(O)2-R2, halo, -CF3, or -NO2; Z is CH3, O, S, N(R2)2, or, when M is not present, H. Y is P or S; X is O or S; and R9 is C(R2)2, O or N(R2); and wherein when Y is S, Z is not S; and R6 is a 5-6 membered carbocyclic or heterocyclic ring system, or an 8-10 membered bicyclic ring system; wherein any of said heterocyclic ring systems contains one or more heteroatoms selected from O, N, S, S(O)n or N(R2); and wherein any of said ring systems optionally contains 1 to 4 substituents independently selected from OH, C1-C4 alkyl, O-(C1-C4)alkyl or O-C(O)-(C1-C4)-alkyl. Also described are pharmaceutical compositions comprising the compounds. The compounds are useful for inhibiting aspartyl protease activity and for treating HIV infection. The compounds may also be combined with other anti-viral or HIV protease inhibitors.

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