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Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes II: Optimisation of the PK profile

Sutton, J and Clark, D and Dunsdon, J and Fenton, G and Fillmore, A and Harris, N and Higgs, C and Hurley, C and Krintel, S and MacKenzie, R and Duttaroy, Alokesh and Gangl, Eric and Maniara, Wieslawa and Sedrani, Richard and Namoto, Kenji and Ostermann, Nils and Sirockin, Finton and Trappe, Joerg and Hassiepen, Ulrich and Baeschlin, Daniel (2011) Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes II: Optimisation of the PK profile. Bioorganic and medicinal chemistry letters, 22 (3). pp. 1464-1468. ISSN 0960-894X

Abstract

Optimisation of compounds from a series of deazaxanthines is described. SAR from the deazahypoxanthine series described previously was used to design improved deazaxanthine-based DPP-4 inhibitors which not only exhibited excellent activity and selectivity but showed improved in vivo activity due to an improved PK profile. Optimization of compound 1 resulted in the identification of compound 9i, which displayed good ex vivo DPP-4 inhibition and a superior PK profile in rat, potentially suitable for once daily dosing in man.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Dipeptidyl peptidase IV inhibitor; diabetes
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/5549

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