Peptide compound its preparation pharmaceutical composition containing it and its application in medicine for the treatment of retrovirus infections

摘要

COMPOUNDS OF THE FORMULA : (FORMULA 1)AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND BIOPRECURSORS THEREOF, WHEREIN-: RI IS C1-C6 ALKYL, C3-C8 CYCLOALKYL, ARYL, HETEROCYCLYL OR CONR9R10;R2 IS CI-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 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 TRIALZOLYL GROUP EITHER OF WHICH MAY OPTIONALLY BE SUBSTITUTED BY C1-C6 ALKYL, C3-C7 CYCLOALKYL, NR9R10 0R 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 O, 1 OR 2; WHEREIN ANY ALKYL OR CYCLOALKYL GROUP INCLUDED IN THE AFOREMENTIONED DEFINITIONS MAY OPTIONALLY BE FULLY OR PARTIALLY SUBSTITUTED BY FLUORINE;ARE INHIBTORS OF RETROVIRAL PROTEASES OF UTILITY IN THE TREATMENT AND PROPYLAXIC OF HUMAN RETROVIRAL INFECTIONS.