Brian R. Smith

TL;DR: Reduced molecular flexibility, as measured by the number of rotatable bonds, and low polar surface area or total hydrogen bond count are found to be important predictors of good oral bioavailability, independent of molecular weight.

TL;DR: This is the first report of an orally active alpha(v)beta(3) antagonist that is effective at inhibiting bone resorption when dosed in a pharmaceutically acceptable fashion and may provide a novel therapeutic agent for the treatment of postmenopausal osteoporosis.

TL;DR: Pharmacokinetic characterization of 38 in the rat revealed that this molecule had a large volume of distribution, which resulted in a prolonged systemic exposure, protracted increases in the plasma levels of PTH, and an overall lack of net bone formation effect in a rodent model of osteoporosis.

TL;DR: The reasonable correlation found between the FTC dissolution results and the oral bioavailability data demonstrate that FTC dissolution testing can be a valuable tool for aiding in salt (solid-state form) and formulation selection in the early stages of development of drug candidates.

TL;DR: A new series of phenylbutyrate derivatives, exemplified by 16, which have good potency and excellent oral bioavailability and are derived conceptually from opening of the seven-membered ring of SB-265123.