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

1994-11-09

1997-03-25

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

5142335, 514256, 544128, 544333, 546168, 546169, C07D40114, C07D41314, A61K 3147, A61K 31535, A61K 31505

Patent

active

056145330

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 Ash; 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.

REFERENCES:
Gallo et al., "AIDS in 1988", Sci. A 259(4): 40 (1988).
Norbeck et al., "HIV Protease Inhibitors", Ann. Reports in Med: Chem. 26:141 (1991).
Rich et al., "Hydroxyethylamine Analogues of the p17/p24 Substrate Cleavage Site are Tight-Binding Inhibitors of HIV Protease", J. Med. Chem. 33: 1285 (1990).
Roberts et al., "Rational Design of Peptide-Based HIV Proteinase Inhibitors", Science 248:358 (1990).
Overton et al., "Effects of Two Novel Inhibitors of the Human Immunodeficiency Virus Protease on the Maturation of the HIV gag and gag-pol Polyproteins", Virology 179: 508 (1990);.
Martin et al., "The Inhibitory Activity of a Peptide Derivative Against the Growth of Simiasn Immunodeficiency Virus in C8166 Cells", Biochem. Biophysio. Res. Com. 176:180 (1991).
Craig et al., "Efffects of a Specific Inhibitor of HIV Proteinase (Ro 31-8959) on virus maturation in a chronically infected promonocytic cell line (U1", Antiviral Chem. & Chemo.2(3):181 (1991).

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