| 摘要 |
2131154 9319059 PCTABS00025 Compounds of formula (I) and pharmaceutically acceptable salts thereof and bioprecursors therefore wherein R1 is C1-C6 alkyl, C3-C8 cycloalkyl, aryl, heterocyclyl or CONR9R10; R2 is C1-C6 alkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl or heterocyclyl(C1-C4)alkyl; R3 is C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl, aryl(C2-C4)-alkenyl, heterocyclyl(C1-C4)alkyl or heterocyclyl(C2-C4)-alkenyl; R4 is C1-C6 alkyl, C3-C8 cycloalkyl, aryl or heterocyclyl; each of R5, R6, R7 and R8 is independently H, C1-C6 alkyl or C3-C8 cycloalkyl; or R5 and R6, or R7 and R8 may be joined together to form a 3 to 8 membered carbocyclic ring; X is a 4-10 membered mono or bicyclic heterocyclic group containing carbon ring atoms and one ring nitrogen atom through which the group is attached to the adjacent carbonyl group; the group may be saturated or partially unsaturated and, in addition to the -(CR7R8)m-Het substituent, it may be substituted by up to 4 further substituents independently chosen from F, C1-C6 alkyl, C3-C8 cycloalkyl, OR11 or NR9R10; Het is an imidazolyl or triazolyl group either of which may optionally be substituted by C1-C6 alkyl, C3-C7 cycloalkyl, NR9R10 or CONR9R10, each of R9 and R10 is independently H, C1-C6 alkyl or C3-C8 cycloalkyl, or R9 and R10 may be joined together to form, with the nitrogen to which they are attached, a 4 to 8 membered nitrogen-containing heterocyclic group, R11 is H, C1-C6 alkyl or C3-C8 cycloalkyl; n and m are each independently 0, 1 or 2; wherein any alkyl or cycloalkyl group included in the aforementioned definitions may optionally be fully or partially substituted by fluorine; are inhibitors of retroviral proteases of utility in the treatment and prophylaxis of human retroviral infections.
|
