Substituted pipecolinic acid derivatives as hiv protease...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/60 (2006.01) A61K 31/435 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2131185

Disclosed herein are compounds of formula (I) wherein X is a terminal group, for exemple, an aryloxycarbonyl, an alka- noyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue,for example, Val or Asn; R1 is hy- drogen or a ring substituent, for example, fluoro or methyl; R2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the com- pounds useful for combating HIV infections.

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