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Biomedical subjects

David P Rotella

Publications and source records attributed to David P Rotella.

At least 19 recordsLinked to original sources
PubMed2005

Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.

A structure-activity relationship study of the amine portion of the calcilytic compound NPS-2143 resulted in the discovery of substituted 2-benzylpyrrolidines as replacements for the 1,1-dimethyl-2-naphthalen-2-yl-ethylamine. When compared to NPS-2143, a newly discovered compound, 3h, exhibited similar potency as a calcium-sensing receptor (CaR) antagonist and a superior human ether-a-go-go related gene (hERG) profile.

Calcium Signaling↗
PubMed2004

SB-480848. GlaxoSmithKline.

SB-480848 is a reversible lipoprotein-associated phospholipase A2 inhibitor under development by GlaxoSmithKline for the potential treatment of atherosclerosis. Phase II trials with SB-480848 are currently underway.

Animals↗
PubMed2003

Tadalafil Lilly ICOS.

Tadalafil is a phosphodiesterase type 5 inhibitor in development by Lilly ICOS for the potential treatment of erectile dysfunction. The compound will be marketed in North America and Europe by a collaboration formed by Eli Lilly & Co and ICOS Corp. Eli Lilly & Co has marketing rights in all other territories. Marketing approval in Europe was granted in November 2002, with launch expected in the first half of 2003. An approvable letter was issued by the FDA in April 2002, with a US launch anticipated in the first half of 2003.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMed2002

Phosphodiesterase 5 inhibitors: current status and potential applications.

Phosphodiesterase enzymes convert cyclic GMP and cyclic AMP to the corresponding nucleotide monophosphates. Phosphodiesterase 5 (PDE5) inhibition is now a widely accepted and efficacious therapeutic option for the treatment of erectile dysfunction in men, as a result of extensive clinical experience with sildenafil and other new PDE5 inhibitors. Research in the field continues at a substantial level to identify new, selective PDE5 inhibitors and to investigate their usefulness and activity in other areas. This review summarizes recent clinical trials with PDE5 inhibitors, advances in medicinal chemistry, and other activities and potential applications of this class of compounds.

Carbolines↗