Enzyme inhibitors

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/02 (2006.01) A61K 38/06 (2006.01) A61K 38/07 (2006.01) A61K 38/08 (2006.01) C07D 217/26 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2016656

Disclosed herein are peptide derivatives which inhibit the activity of human immunodeficiency virus (HIV) protease. The peptide derivatives can be represented by general formula R1-R2-Y-R3-R4 wherein R1 is an optionally substituted 3-(1,2,3,4-tetrahydro- isoquinolyl)carbonyl 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 [-NR17CH(R18)C(O)]p-2 wherein R17 is hydrogen or lower alkyl, R18 is an amino acid or analogous amino acid side chain, p is zero or 1 and 2 is a terminal group (e.g. hydroxy or amino), or R4 is -NR17CR18(R21)CH2OH wherein R17 and R18 are as noted hereinabove and R25 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives also inhibit renin activity. Accordingly, the derivatives can be used for combating HIV infections or for treating hypertension or congestive heart failure.

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