Enzyme inhibiting peptide derivatives

Details Enzyme inhibiting peptide derivatives Enzyme inhibiting peptide derivatives

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01) A61K 38/04 (2006.01) C07K 1/00 (2006.01) C07K 5/02 (2006.01)

Patent

CA 2016663

Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R1-R2-Y-R3-R4 wherein R1 is a derived amino acid based on an O4-(carboxymethyl)-tyrosyl residue, R2 and R3 are amino acid or analogous amino acid residues (R3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R4 is [NR17CHR18-C(O)]p-Z wherein R17 is hydrogen or lower alkyl, R18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R4 is NR17CR18(R21)CH2OH wherein R17 and R18 are as noted hereinabove and R21 is hydrogen, lower alkyl or hydroxy-(lower)alkyl. The derivatives are useful as agents for combating HIV infections and for treating renin-associated hypertension and congestive heart failure.

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