ANTIVIRAL PEPTIDES

摘要

Compounds of formula (I) and pharmaceutically acceptable salts thereof and bioprecursors therefore wherein R<1> is C1-C6 alkyl, C3-C8 cycloalkyl, aryl, heterocyclyl or CONR<9>R<10>; R<2> is C1-C6 alkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl or heterocyclyl(C1-C4)alkyl; R<3> 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; R<4> is C1-C6 alkyl, C3-C8 cycloalkyl, aryl or heterocyclyl; each of R<5>, R<6>, R<7> and R<8> is independently H, C1-C6 alkyl or C3-C8 cycloalkyl; or R<5> and R<6>, or R<7> and R<8> 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 -(CR<7>R<8>)m-Het substituent, it may be substituted by up to 4 further substituents independently chosen from F, C1-C6 alkyl, C3-C8 cycloalkyl, OR<11> or NR<9>R<10>; Het is an imidazolyl or triazolyl group either of which may optionally be substituted by C1-C6 alkyl, C3-C7 cycloalkyl, NR<9>R<10> or CONR<9>R<10>, each of R<9> and R<10> is independently H, C1-C6 alkyl or C3-C8 cycloalkyl, or R<9> and R<10> may be joined together to form, with the nitrogen to which they are attached, a 4 to 8 membered nitrogen-containing heterocyclic group, R<11> 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.