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US 5,151,438 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 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 2 and R.sub.4 is independently selected at each occurrence from hydrogen, loweralkyl, cycloalkylalkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl and 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, halo, amino, alkylamino, dialkylamino, alkoxy, polyalkoxy, haloalkyl, cycloalkyl, aryl, arylalkyl, --COOH, --SO.sub.3 H and loweralkyl, 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 alkyl as used herein refers to a straight or branched chain alkyl radical containing from 1 to 6 carbon atoms;
- wherein the terms alkoxy and thioalkoxy as used herein refer to R.sub.32 is an alkyl group or benzyl and wherein the term aryl as used herein refers to phenyl, naphthyl, tetrahydronaphthyl or indanyl.
5 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 2, R.sub.4 is independently selected at each occurrence from hydrogen and loweralkyl and
- T is ##STR12## R.sub.6 is pyridyl or substituted pyridyl wherein the pyridyl ring is substituted with one or two substituents independently selected from hydroxy, alkoxy, thioalkoxy 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;
- wherein the term alkyl as used herein refers to a straight or branched chain alkyl radical containing from 1 to 6 carbon atoms;
- and wherein the terms alkoxy and thioalkoxy as used herein refer to R.sub.32 O--and R.sub.32 S--, respectively, wherein R.sub.32 is an alkyl group or benzyl;
- or a pharmaceutically acceptable salt thereof.
4 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 R.sub.4 is isopropyl and
- T is ##STR15## 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, thioalkoxy 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;
- wherein the term alkyl as used herein refers to a straight or branched chain alkyl radical containing from 1 to 6 carbon atoms;
- wherein the terms alkoxy and thioalkoxy as used herein refer to R.sub.32 O--and R.sub.32 S--, respectively, wherein R.sub.32 is an alkyl group or benzyl;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound selected from the group consisting of:
- 5(S)-(N-(2-pyridyl)methoxycarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluoro-1 ,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(3-pyridyl)methoxycarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluoro-1 ,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(4-pyridyl)methoxycarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluoro-1 ,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(2-pyridylmethyl)aminocarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluo ro-1,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(3-pyridylmethyl)aminocarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluo ro-1,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(4-pyridylmethyl)aminocarbonyl-glycyl-(L)-valinyl)-amino-3,3-difluo ro-1,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(2-pyridylmethyl)-N-(methyl)aminocarbonyl-glycyl-(L)-valinyl)-amino -3,3-difluoro-1,6-diphenyl-4-oxo-hexane;
- 5(S)-(N-(3-pyridylmethyl)-N-(methyl)aminocarbonyl-glycyl-(L)-valinyl)-amino -3,3-difluoro-1,6-diphenyl-4-oxo-hexane;
- and
- 5(S)-(N-(4-pyridylmethyl)-N-(methyl)aminocarbonyl-glycyl-(L)-valinyl)-amino -3,3-difluoro-1,6-diphenyl-4-oxo-hexane;
- or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.