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US 5,648,497 AGranted
Retroviral protease inhibiting compounds
AssigneeAbbott Laboraotries
InventorsDale J. Kempf, Daniel W. Norbeck, Lynn M. Codacovi, Hing L. Sham, Steven J. Wittenberger
Life of this patent
Estimating the term…
Abstract
A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.
Claims8
A compound of the formula:
- ##STR17## wherein R.sub.2 and R.sub.3 are independently selected from C.sub.3 -to-C.sub.7 -cycloalkyl-C.sub.1 -to-C.sub.6 -alkyl and (C.sub.6 -monocyclic or C.sub.9 - or C.sub.10 -bicyclic)aryl-C.sub.1 -to-C.sub.6 -alkyl;
- and
- (a) A is thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-R.sub.9 --C(O)--NH--CH(R.sub.5)--C(O)-- or (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-R.sub.9 --C(O)--NH--CH(R.sub.5)--C(O)-- wherein R.sub.9 is --O--, --NH-- or --N(C.sub.1 -to-C.sub.6 -loweralkyl)- and R.sub.5 is C.sub.1 -to-C.sub.6 -loweralkyl and B is thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-O--C(O)--, thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-NH--C(O)--, thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-N(C.sub.1 -to-C.sub.6 -loweralkyl)-C(O)--, (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-O--C(O)--, (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-NH--C(O)-- or (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-N(C.sub.1 -to-C.sub.6 -loweralkyl)-C(O)-- and wherein at each occurrence substituted-thiazolyl is independently selected from a thiazolyl ring substituted with one or two substituents independently selected from C.sub.1 -to-C.sub.6 -loweralkyl, hydroxy, halo, amino, C.sub.1 -to-C.sub.6 -alkylamino, di-C.sub.1 -to-C.sub.6 -alkylamino, C.sub.1 -to-C.sub.6 -alkoxy, halo-C.sub.1 -to-C.sub.6 -alkyl, unsubstituted-C.sub.3 -to-C.sub.7 -cycloalkyl, unsubstituted (C.sub.6 -monocyclic or C.sub.9 - or C.sub.10 -bicyclic)aryl, unsubstituted (C.sub.6 -monocyclic or C.sub.9 - or C.sub.10 -bicyclic)aryl-C.sub.1 -to-C.sub.6 -alkyl, --COOH and --SO.sub.3 H;
- or
- (b) A is thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-O--C(O)--, thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-NH--C(O)--, thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-N(C.sub.1 -to-C.sub.6 -loweralkyl)-C(O)--, (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-O--C(O)--, (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-NH--C(O)-- or (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-N(C.sub.1 -to-C.sub.6 -loweralkyl)-C(O)-- and B is thiazolyl-C.sub.1 -to-C.sub.6 -alkyl-R.sub.9 --C(O)--NH--CH(R.sub.5)--C(O)-- or (substituted-thiazolyl)-C.sub.1 -to-C.sub.6 -alkyl-R.sub.9 -C(O)--NH--CH(R.sub.5)--C(O)-- wherein R.sub.9 is --O--, --NH-- or --N(C.sub.1 -to-C.sub.6 -loweralkyl)- and R.sub.5 is C.sub.1 -to-C.sub.6 -loweralkyl and wherein at each occurrence substituted-thiazolyl is independently selected from a thiazolyl ring substituted with one or two substituents independently selected from C.sub.1 -to-C.sub.6 -loweralkyl, hydroxy, halo, amino, C.sub.1 -to-C.sub.6 -alkylamino, di-C.sub.1 -to-C.sub.6 -alkylamino, C.sub.1 -to-C.sub.6 -alkoxy, halo-C.sub.1 -to-C.sub.6 -alkyl, unsubstituted-C.sub.3 -to-C.sub.7 -cycloalkyl, unsubstituted (C.sub.6 -monocyclic or C.sub.9 - or C.sub.10 -bicyclic)aryl, unsubstituted (C.sub.6 -monocyclic or C.sub.9 - or C.sub.10 -bicyclic)aryl-C.sub.1 -to-C.sub.6 -alkyl, --COOH and --SO.sub.3 H;
- or a pharmaceutically acceptable salt thereof.
3 more elements
The compound (2S,3S,5S)-2-(N-(N-((N-Methyl-N-((2-amino-4-thiazolyl)methyl)amino)carbony l)valinyl)amino)-5-(N-((5-thiazolyl)-methoxycarbonyl)amino)-1,6-diphenyl-3- hydroxyhexane;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.