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US 5,256,677 AGranted
Retroviral protease inhibiting compounds
AssigneeAbbott Laboratories
InventorsHing L. Sham, Daniel W. Norbeck, Dale J. Kempf, Chen Zhao
Life of this patent
Estimating the term…
Abstract
Compounds are disclosed which are retroviral protease inhibitors. Also disclosed are methods of using the compounds and compositions for inhibiting a retroviral protease and for treating an HIV infection.
Claims13
A compound of the formula:
- ##STR7## wherein R.sub.1 is loweralkyl, cycloalkyl, phenyl, substituted loweralkyl, substituted cycloalkyl or substituted phenyl wherein the loweralkyl, cycloalkyl or phenyl group is substituted with one or two substituents independently selected from group is substituted with one or two substituents independently selected from hydroxy, alkoxy, thioalkoxy and halo;
- R.sub.2 is phenyl or substituted phenyl wherein the phenyl ring is substituted with one or two substituents independently selected from hydroxy, alkoxy, thioalkoxy and halo;
- R.sub.3 is ##STR8## wherein m is 1 and R.sub.4 is hydrogen, loweralkyl, cycloalkylalkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl or aminocarbonylalkyl and
- T is ##STR9## wherein R.sub.6 is pyridyl or substituted pyridyl wherein the pyridyl ring is substituted with one or two substituents independently selected from hydroxy, alkoxy, amino, alkylamino, dialkylamino, polalkoxy, haloalkyl, cycloalkyl, aryl, arylalkyl, --COOH, --SO.sub.3 H, loweralkyl and halo, V is O or S, W is CH.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --D--CH.dbd.CH-- wherein D is O, S or NH and Y is absent, O, S or N(R.sub.7) wherein R.sub.7 is hydrogen or loweralkyl;
- and Z is --C(O)-- or --CH(OH)--;
- or a pharmaceutically acceptable salt thereof;
- wherein the term aryl as used herein refers to phenyl, naphthyl, tetrahydronaphthyl or indanyl.
4 more elements
A compound of the formula:
- ##STR10## wherein R.sub.1 is phenyl;
- R.sub.2 is phenyl;
- R.sub.3 is ##STR11## wherein m is 1, R.sub.4 is loweralkyl and T is ##STR12## wherein R.sub.6 is pyridyl or substituted pyridyl wherein the pyridyl ring is substituted with one or two substituents independently selected from hydroxy, alkoxy, amino, alkylamino, dialkylamino, polalkoxy, haloalkyl, cycloalkyl, aryl, arylalkyl, --COOH, --SO.sub.3 H, loweralkyl and halo, V is O or S, W is CH.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --D--CH.dbd.CH-- wherein D is O, S or NH and Y is absent, O, S or N(R.sub.7) wherein R.sub.7 is hydrogen or loweralkyl;
- or a pharmaceutically acceptable salt thereof;
- wherein the term aryl as used herein refers to phenyl, naphthyl, tetrahydronaphthyl or indanyl.
2 more elements
A compound of the formula:
- ##STR13## wherein R.sub.1 is phenyl;
- R.sub.2 is phenyl;
- R.sub.3 is ##STR14## wherein m is 1, R.sub.4 is isopropyl and T is ##STR15## wherein R.sub.6 is pyridyl, V is O or S, W is CH.sub.2 or --CH.sub.2 CH.sub.2 -- and Y is O, S or N(R.sub.7) wherein R.sub.7 is hydrogen or loweralkyl;
- or a pharmaceutically acceptable salt thereof.
1 more element
A compound selected from the group consisting of:
- 5(S)-(N-(2-Pyridyl)-methoxycaronbyl-(L)-valinyl)-amino-3,3-difluoro-1,6-dip henyl-4-oxo-hexane and 5(S)-(N-(2-Pyridyl)-methylamino-carbonyl-(L)-Valinyl)-amino-3,3-difluoro-1 ,6-diphenyl-4-oxo-hexane;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.