Back to results
US 5,914,332 AGranted
Retroviral protease inhibiting compounds
AssigneeAbbott Laboratories
InventorsHing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner
Life of this patent
Estimating the term…
Abstract
A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Claims17
A compound of the formula:
- ##STR84## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of loweralkyl, cycloalkylalkyl and arylalkyl;
- R.sub.3 is loweralkyl, hydroxyalkyl or cycloalkylalkyl;
- R.sub.4 is aryl;
- R.sub.5 is ##STR85## wherein n is 1, 2 or 3, X is O, S or NH and Y is --O-- or --N(R.sub.6)-- wherein R.sub.6 is hydrogen, loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl;
- and
- L.sub.1 is
- a) --O--,
- b) --S--,
- c) --N(R.sub.7)-- wherein R.sub.7 is hydrogen, loweralkyl, cycloalkyl or cycloalkylalkyl,
- d) --O-alkylenyl-,
- e) --S-alkylenyl-
- f) --S(O)-alkylenyl-,
- g) --S(O).sub.2 -alkylenyl-,
- h) --N(R.sub.7)-alkylenyl- wherein R.sub.7 is defined as above,
- i) -alkylenyl-O--,
- j) -alkylenyl-S--,
- k) alkylenyl-N(R.sub.7)-- wherein R.sub.7 is defined as above,
- l) alkylenyl or
- m) alkenylenyl;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
17 more elements
A compound selected from the group consisting of:
- (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-2S-(1-tetrahydro -pyrimid-2-onyl)-3-methyl butanoyl!amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(2,6-Dimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-imidazolid in-2-onyl)-3,3dimethyl butanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-imidazolid in-2-thionyl)-3-methyl butanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(2,4,6-trimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-imidazo lidin-2-onyl-3-methylbutanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(4-fluoro-2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-i mmidazolidin-2-onyl)-3-methylbutanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(trans-3-(2,6-dimethylphenyl)propenoyl)amino-3-hydroxy-5-(2S-1 -tetrahydropyrimidin-2-onyl)-3-methyl-butanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(3-(2,6-dimethylphenyl)propanoyl)amino-3-hydroxy-5-(2S-(1-tetr ahydropyrimidin-2-onyl)-3-methyl-butanoyl)amino-1,6-diphenylhexane;
- (2S,3S,5S)-2-(2,6-Dimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-tetrahydro -pyrimid-2-onyl)-3-methylbutanoyl)amino-1-phenyl-6-methylheptane;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
6 more elements
The compound (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-(2S-(1-tetrahydr o-pyrimid-2-onyl)-3-methyl butanoyl)amino-1,6-diphenylhexane;
- or a pharmaceutically acceptable salt, ester or pyodrug thereof.
The compound (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-(2-(1-tetrahydro -pyrimid-2-onyl)-3-methyl butanoyl)amino-1,6-diphenylhexane;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.