| 摘要 |
Compounds of formula (I) wherein R<1> is C1-C6 alkyl, C3-C8 cycloalkyl, aryl, heterocyclyl, or R<7>R<8>NCO; 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; R<5> and R<6> are each independently H, C1-C6 alkyl, C3-C7 cycloalkyl, or C1-C6 alkyl substituted by C1-C4 alkoxy, hydroxy or NR<7>R<8>; or R<5> and R<6> are linked to form, together with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, morpholine, piperazine or N-(C1-C4 alkyl) piperazine group; each of R<7> and R<8> is independently H, C1-C6 alkyl or C3-C8 cycloalkyl or R<7> and R<8> may be joined together to form, with the nitrogen to which they are attached, a 4 to 8 membered nitrogen-containing heterocyclic group; each of R<9>, R<10>, R<11> and R<12> is independently H, C1-C6 alkyl or C3-C8 cycloalkyl; or R<9> and R<10>, or R<11> and R<12> 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<11>R<12>)m -NR<5>R<6> substituent, it may be substituted by up to 4 further substituents each independently chosen from F, C1-C6 alkyl, C3-C8 cycloalkyl, OH, C1-C6 alkoxy or NR<7>R<8>; and n and m are each independently 0, 1 or 2; and 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. |
