- DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT
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The present invention relates to novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV), methods of preparing the same and pharmaceutical compositions containing the same as an active agent.
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Page/Page column 59
(2010/11/24)
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- Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
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A series of β-aminoacylpiperidines bearing various fused five-membered heterocyclic rings was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective inhibition could be obtained, depending on choice of heterocycle, regioisomerism, and substitution. In particular, one analog (74, DPP-IV IC50 = 26 nM) exhibited good oral bioavailability and acceptable half-life in the rat, albeit with rather high clearance.
- Ashton, Wallace T.,Sisco, Rosemary M.,Dong, Hong,Lyons, Kathryn A.,He, Huaibing,Doss, George A.,Leiting, Barbara,Patel, Reshma A.,Wu, Joseph K.,Marsilio, Frank,Thornberry, Nancy A.,Weber, Ann E.
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p. 2253 - 2258
(2007/10/03)
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