942586-07-4Relevant academic research and scientific papers
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes
Sutton, Jon M.,Clark, David E.,Dunsdon, Stephen J.,Fenton, Garry,Fillmore, Amanda,Harris, Neil V.,Higgs, Chris,Hurley, Chris A.,Krintel, Sussie L.,MacKenzie, Robert E.,Duttaroy, Alokesh,Gangl, Eric,Maniara, Wiesia,Sedrani, Richard,Namoto, Kenji,Ostermann, Nils,Gerhartz, Bernd,Sirockin, Finton,Trappe, J?rg,Hassiepen, Ulrich,Baeschlin, Daniel K.
scheme or table, p. 1464 - 1468 (2012/03/26)
Novel deazaxanthine-based DPP-4 inhibitors have been identified that are potent (IC50 10 nM) and highly selective versus other dipeptidyl peptidases. Their synthesis and SAR are reported, along with initial efforts to improve the PK profile through decoration of the deazaxanthine core. Optimisation of compound 3a resulted in the identification of compound (S)-4i, which displayed an improved in vitro and ADME profile. Further enhancements to the PK profile were possible by changing from the deazahypoxanthine to the deazaxanthine template, culminating in compound 12g, which displayed good ex vivo DPP-4 inhibition and a superior PK profile in rat, suggestive of once daily dosing in man.
CONDENSED HETEROCYCLIC COMPOUNDS USEFUL AS DPP-IV INHIBITORS
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Page/Page column 206, (2008/06/13)
The invention provides novel deazaxanthine and deazahypoxanthine compounds, of formula (I), wherein X is -CH= and Y is =N-; or X is -C(O)- and Y is -N(R3)-; The compounds may be useful in the therapy of diseases and conditions in wich dipeptidy
