Cholesterol ester hydrolase inhibitors

Details Cholesterol ester hydrolase inhibitors Cholesterol ester hydrolase inhibitors

C - Chemistry, Metallurgy

07

C

167/208, 167/249

C07C 271/40 (2006.01) A61K 31/27 (2006.01) A61K 31/395 (2006.01) C07D 211/16 (2006.01) C07D 221/20 (2006.01) C07D 295/205 (2006.01) C07D 295/215 (2006.01)

Patent

CA 2029934

Abstract of the Disclosure The compounds of the formula: Image in which R1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl,phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R2 is hydrogen, alkyl or R1 taken with R2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: Image wherein X is Image , -NR9- , -O- or -S- ; in which R7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R8 is hydrogen or alkyl or R7 and R8 taken together are polymethylene; R9 is hydrogen, alkyl, phenyl or substituted phenyl, in which thesubstituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and K3, R4, R5 and R6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is -NR9- or R7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; useful as inhibitors of cholesterol esterhydrolase.

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