Substituted pipecolinic acid derivatives as HIV protease inhibit

Details Substituted pipecolinic acid derivatives as HIV protease inhibit Substituted pipecolinic acid derivatives as HIV protease inhibit

1996-12-11

1998-09-15

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514256, 514314, 514326, 544242, 544333, 544335, 546168, 546169, 546193, 546209, 546212, A61K 31445, A61K 31505, C07D40112, C07D40312

Patent

active

058078703

ABSTRACT:
Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Asn; R.sup.1 is hydrogen or a ring substituent, for example, fluoro or methyl; R.sup.2 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 compounds useful for combating HIV infections.

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Singh et al. "Improvements of oligodeoxyribonucleotied synthesis using phenoxyacetyl as amino protecting group" CA 110:57984, 1988. acid protease inhibvitors . . . " J. Med. Chem. v.38, pp. 1427-1430, 1995.

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