Apremilast is an oral small molecule specific PDE4 inhibitor. It is being studied in multiple Phase III clinical trials for the treatment of psoriasis, psoriatic arthritis and other chronic inflammatory diseases with promising clinical efficacy in psoriasis and psoriatic arthritis. Herein, we describe the discovery of Apremilast starting from the optimization of a series of �-amino-propionic acid PDE4 inhibitors. SAR exploration of three moieties, dialkoxyphenyl, phthalimide, and sulfone, will be presented.

Discovery of Apremilast, a selective PDE4 inhibitor

248th National Meeting (2014)

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