Substituted pyrrolidine derivatives as hiv protease inhibitors

Details Substituted pyrrolidine derivatives as hiv protease inhibitors Substituted pyrrolidine derivatives as hiv protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/40 (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 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2092653

Disclosed herein are compounds of formula 1 (see fig. I) wherein X is a terminal group, for example, an aryloxycarbonyl or an alkanoyl; B is absent or an amino acid residue, for example, Val or Asn; R1 is alkyl; and Y is a ring substituent, for example, benzyl, benzyloxy, 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 compounds useful for combating HIV infections.

Divulgation de composés de formule 1 (voir figure I), dans laquelle X est un groupement terminal, par exemple un aryloxycarbonyle ou un alcanoyle; B est absent ou est un résidu d'acide aminé, par exemple de la valine ou de l'asparagine; R1 est un groupement alkyle; et Y est un substituant cyclique, par exemple un benzyle, un benzyloxy, un phénylthio ou un 2-pyridinylthio. Ces composés inhibent l'activité de la protéase du virus de l'immunodéficience humaine (VIH) et interfèrent avec les effets cytopathogènes induits par le VIH sur les cellules humaines. Grâce à ces propriétés, ces composés sont utiles pour combattre les infections par le VIH.

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