1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability |
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| Authors: | Ghosh Shyamali Santulli Rosemary J Kinney William A Decorte Bart L Liu Li Lewis Joan M Proost Jef C Leo Gregory C Masucci John Hageman William E Thompson Andrew S Chen Ian Kawahama Reiko Tuman Robert W Galemmo Robert A Johnson Dana L Damiano Bruce P Maryanoff Bruce E |
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| Affiliation: | Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477-0776, USA. |
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| Abstract: | Reduction of the quinoline ring in an alpha(v)beta(3) antagonist yielded a 1,2,3,4-tetrahydro derivative as two diastereomers, the four isomers of which were separated by sequential chiral HPLC. Two isomers had significant alpha(V)beta(3) antagonist activity with improved oral bioavailability, relative to the corresponding quinoline derivative. |
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