Hiv protease inhibitors containing derived amino acid units

Details Hiv protease inhibitors containing derived amino acid units Hiv protease inhibitors containing derived amino acid units

C - Chemistry, Metallurgy

07

K

167/103.05, 530/

C07K 5/02 (2006.01) A61K 38/04 (2006.01) A61K 38/06 (2006.01) C07C 237/22 (2006.01) C07C 271/22 (2006.01) C07C 327/42 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2036397

Disclosed herein are compounds of the general formula X-A-B-C'-Y wherein X is lower alkanoyl optionally substituted with one or two hydroxyls, A is an amino acid residue having a lower alkyl side chain, e.g. Ala or Val, B is a non-peptide linking unit, e.g. statyl or Phe~[CH2NH]Leu, C' is an amino acid residue of .alpha.-amino-.beta.-cycloalkylpropionic acid, glutamic acid or .alpha.- aminoadipic acid, or a related derivative thereof, and Y is alkoxy, cycloalkoxy, a substituted alkoxy or a substituted amino group, e.g. cycloalkylalkoxy, arylalkoxy, alkylamino, (cycloalkyl)alkylamino or arylalkylamino. The compounds inhibit the activity of human immuno-deficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.

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