Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
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United States of America Patent
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Jun 9, 1998
Issued Date -
N/A
app pub date -
Jun 20, 1996
filing date -
Dec 2, 1992
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Expired
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Abstract
Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or arly-substituted lower alkyl group; K and J are independently a group having the formula of ##STR2## wherein R.sup.18 is a lower alkyl group optionally substituted with an aryl radical; X is O, NH, or N--CH.sub.3 ; and R.sup.19 is an aromatic hetercyclic sysstem containing a nitrogen atom in its ring, or a lower alkyl group optionally substituted with an aryl radical, or a hydrogen; G is an amino acid which is linked to K-- and ##STR3## by peptide bonds in formula (I-3); Q is an amino acid which is linked to by peptide bonds in formula (I-3), or a group having the formula of wherein R.sup.20 is a lower alkyl group optionally substituted with an aromatic radical; and Y is CH.sub.2, O or NH; and r is 0 or 1, except that Q is a group having the formula of r is 0.
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