5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of .beta.-amyloid protein production
AssigneeBristol-Myers Squibb Company
InventorsKevin Felsenstein, David W. Smith, Michael A. Poss, Prasad Chaturvedula, Charles P. Sloan
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Abstract
A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.
Claims9
A compound of Formula I and its pharmaceutically
- acceptable acid addition salts and hydrates thereof wherein
- R.sup.1 is selected from C.sub.4-8 alkyl, C.sub.4-8 alkenyl, C.sub.1-4 alkoxy-C.sub.1-4 alkanediyl, R.sup.5 -substituted C.sub.3-6 cycloalkyl, R.sup.5 -substituted C.sub.3-6 cycloalkyl-lower-alkanediyl, and Ar--(CH.sub.2).sub.n -- in which Ar is ##STR62## with R.sup.5 being hydrogen, lower (C.sub.1-6) alkyl, and lower alkoxy, and n is 1 to 4;
- R.sup.2 is independently selected from hydrogen and methyl;
- R.sup.3 is selected from lower alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-lower-alkanediyl, C.sub.3-6 alkenyl, and Ar--(CH.sub.2).sub.n --;
- and
- R.sup.4 is selected from R.sup.3, lower alkyl-thio-lower alkyl, and ##STR63## wherein R.sup.6 is lower alkyl.
A compound of Formula I having the stereochemistry of Formula IA ##STR64##
Dependencies are inferred from the claim text.