PEPTIDYL ACTIVATED KETONE INHIBITORS CONTAINING NATURAL AND UNNATURAL PEPTIDE SEQUENCES.

摘要

A method of treating medical conditions with proteinase inhibitors of the formula: IMAGE wherein B is H or an amino acid blocking group for the N-terminal amino acid nitrogen; R1 is an optionally protected alpha -amino acid side chain such that P2 is the residue of an alpha -amino acid selected from the group consisting of phenylalanine (Phe), leucine (Leu), tyrosine (Tyr) and valine (Val), and substituted analogs thereof, particularly including Tyr(OMe); R2 is an optionally protected alpha -amino acid side chain such that P1 is the residue of an alpha -amino acid selected from the group consisting of alanine (Ala), arginine (Arg), aspartic acid (Asp), glutamic acid (Glu), histidine (His), homophenylalanine (HPhe), phenylalanine (Phe), ornithine (Orn), serine (Ser) and threonine (Thr), and substituted analogs thereof; X is a fluorine-free leaving group selected from the group consisting of phenoxy, substituted phenoxy and heterophenoxy; E and G are one or more atoms more electronegative than carbon; and D is hydrogen, methyl or a substituted methyl.