Disclosed are compounds of the formula I or a stereoisomer, tautomer, or
pharmaceutically acceptable salt or solvate thereof, wherein W is a
bond, --C(.dbd.S)--, --S(O)--, --S(O).sub.2--, --C(.dbd.O)--, --O--,
--C(R.sup.6)(R.sup.7)--, --N(R.sup.5)-- or --C(.dbd.N(R.sup.5))--; X is
--O--, --N(R.sup.5)-- or --C(R.sup.6)(R.sup.7)--; provided that when X is
--O--, U is not --O--, --S(O)--, --S(O).sub.2--, --C(.dbd.O)-- or
--C(.dbd.NR.sup.5)--; U is a bond, --S(O)--, --S(O).sub.2--, --C(O)--,
--O--, --P(O)(OR.sup.15)--, --C(.dbd.NR.sup.5)--,
--(C(R.sup.6)(R.sup.7)).sub.b-- or --N(R.sup.5)--; wherein b is 1 or 2;
provided that when W is --S(O)--, --S(O).sub.2--, --O--, or
--N(R.sup.5)--, U is not --S(O)--, --S(O).sub.2--, --O--, or
--N(R.sup.5)--; provided that when X is --N(R.sup.5)-- and W is --S(O)--,
--S(O).sub.2--, --O--, or --N(R.sup.5)--, then U is not a bond; and
R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as
defined in the specification; and pharmaceutical compositions comprising
the compounds of formula I. Also disclosed is the method of inhibiting
aspartyl protease, and in particular, the methods of treating
cardiovascular diseases, cognitive and neurodegenerative diseases, and
the methods of inhibiting of Human Immunodeficiency Virus, plasmepins,
cathepsin D and protozoal enzymes.
Also disclosed are methods of treating cognitive or neurodegenerative
diseases using the compounds of formula I in combination with a
cholinesterase inhibitor or a muscarinic m.sub.1 agonist or m.sub.2
antagonist.
