8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin- 2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting, and orally active DPP-4 inhibitor that shows considerable blood glucose lowering in different animal species. 1 is currently undergoing clinical phase IIb trials and holds the potential for once-daily treatment of type 2 diabetics.
8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PRODUCTION THEREOF AND THE USE OF THE SAME AS MEDICAMENTS
The invention relates to substituted xanthines of general formula (I) wherein R1 to R3 have the designations cited in patent claims 1 to 16, and to the tautomers, stereoisomers, mixtures, prodrugs and salts thereof, which have precio
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(2008/06/13)
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