Disclosed are compounds of the formula I
##STR00001##
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.
