Patent ID: 6121417
Filing Date: 2000-09-19
Classification: A61K,C07K,C12N

Abstract:
The method of preparing an inhibitor of HIV protease comprising introducing an internal CH.sub.2 NH bond isostere into a peptide substrate for HIV Protease derived from a HIV-1 or HIV-2 cleavage site in which the peptide is selected from the group consisting ofAc-Gln-Asn-Tyr-Pro-Ile-Val-NH.sub.2,Ac-Gly-Asn-Tyr-Pro-Val-Gln-NH.sub.2,Ac-Thr-Ile-Met-Met-Gln-Arg-NH.sub.2,Ac-Thr-Ile-Nle-Nle-Gln-Arg-NH.sub.2,Ac-Thr-Ile-PnF-Nle-Gln-Arg-NH.sub.2,Ac-Thr-Ile-Nle-PnF-Gln-Arg-NH.sub.2,Aba-Thr-Ile-Nle-[Pnf]-PnF-Gln-Arg-NH.sub.2,Ac-Phe-Asn-Phe-Pro-Gln-Ile-NH.sub.2,Ac-Ser-Phe-Asn-Phe-Pro-Gln-Ile-NH.sub.2,Ac-Leu-Ala-Ala-Pro-Gln-Phe-NH.sub.2,Ac-Leu-Asn-Phe-Pro-Ile-Ser-OH, andAc-Leu-Asn-Leu-Pro-Val-Ala-NH.sub.