1999 pyridine derivatives

pyridine derivativesR 0380

44 - 144Orally Bioavailable Nonpeptide Vitronectin Receptor Antagonistswith Efficacy in an Osteoporosis Model. — Title antagonists suchas (XII) and (XIV), based on a novel carbocyclic Gly-Asp mimetic, aresynthesized. The (S)-enantiomer of (XIV) displays 100% oral bioavailabilityand is orally active in vivo in an ovariectomized rat model of osteoporosis.The enantiomers of (XIV) are prepared in a similar fashion from the corre-sponding enantiomerically pure phenols of racemic phenol (VII). — (MILLER,WILLIAM H.; ET AL.; Bioorg. Med. Chem. Lett. 9 (1999) 13, 1807-1812;Res. Dev. Div., SmithKline Beecham Pharm., Collegeville, PA 19426, USA; EN)

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