The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines. A preferred specific N,N-disubstituted diamine is the compound: ##STR1##

 
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> Use of substituted N, N-disubstituted cycloalkyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity

> Use of substituted N, N-bis-benzyl aminoalcohol compounds inhibiting cholesteryl ester transfer protein activity

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