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Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone |
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| Authors: | Whitman David B Askew Ben C Duong Le T Fernandez-Metzler Carmen Halczenko Wasyl Hartman George D Hutchinson John H Leu Chih-Tai Prueksaritanont Thomayant Rodan Gideon A Rodan Sevgi B Duggan Mark E |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. david_whitman@merck.com |
| Abstract: | A series of alphaVbeta3 receptor antagonists lacking the amide bond of previously-reported 'chain-shortened' compounds is described. Replacement of the lone amide bond with two methylene groups in this series yields more lipophilic compounds that have longer half-lives, lower clearance, and greater oral bioavailability when administered to dogs. |
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