Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

Abstract: 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 non-fused heterocyclo amines.

Abstract: Five independent transgenic founder lines were created which have all developed cardiac hypertrophy and heart failure. The line with the most severe phenotype was analyzed in detail. Transgenic cardiac 11&bgr;HSD2 mRNA expression is increased 4,000 fold over non-transgenic mice and the expressed enzyme was found to possess catalytic activity. At five months of age transgenic mice had developed severe myocardial hypertrophy in the absence of an increase in blood pressure. Interstitial fibrosis in the left ventricle of transgenic mice was revealed by picrosirius red staining. The hearts of the mice were severely dilated and cardiomyocyte size was increased.