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Phenylbutyrates as potent,orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists |
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| Authors: | Miller William H Manley Peter J Cousins Russell D Erhard Karl F Heerding Dirk A Kwon Chet Ross Stephen T Samanen James M Takata Dennis T Uzinskas Irene N Yuan Catherine C K Haltiwanger R Curtis Gress Catherine J Lark Michael W Hwang Shing Mei James Ian E Rieman David J Willette Robert N Yue Tian Li Azzarano Leonard M Salyers Kevin L Smith Brian R Ward Keith W Johanson Kyung O Huffman William F |
| Affiliation: | GlaxoSmithKline Pharmaceuticals, 1250 S. Collegeville Rd., PO Box 5089, PA 19426, USA. william_h_miller@gsk.com |
| Abstract: | In our continuing efforts to identify small molecule vitronectin receptor antagonists, we have discovered a series of phenylbutyrate derivatives, exemplified by 16, which have good potency and excellent oral bioavailability (approximately 100% in rats). This new series is derived conceptually from opening of the seven-membered ring of SB-265123. |
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