Peptidyl activated ketone inhibitors containing natural and...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/06 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07C 271/18 (2006.01) C07C 271/22 (2006.01) C07C 279/14 (2006.01) C07D 295/205 (2006.01) C07D 295/215 (2006.01) C07K 4/00 (2006.01) C07K 5/08 (2006.01)

Patent

CA 2142839

2142839 9404172 PCTABS00030 A method of treating medical conditions with proteinase inhibitors of formula (I), 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 analogues 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 analogues 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.

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