1417715-75-3

Upstream product

• 1417715-70-8 C₁₇H₁₈N₆O₂ 
• 421552-12-7 2-(bromomethyl)-4-fluorobenzonitrile 
• 1417715-69-5 2-(2-chloro-9-(4-methoxybenzyl)-6-oxo-6,9-dihydro-1H-purin-1-yl)acetonitrile 
• 115204-74-5 2,6-dichloro-9-(4-methoxyphenylmethyl)-9H-purine 

Downstream Products

• 1417715-76-4 tert-butyl (R)-(1-(1-(2-cyano-5-fluorobenzyl)-5-methyl-6,9-dioxo-5,6,7,9-tetrahydro-1H-imidazo[1,2-a]purin-2-yl)piperidin-3-yl)carbamate 

Relevant academic research and scientific papers

Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes

In our efforts to develop second generation DPP-4 inhibitors, we endeavored to identify distinct structures with long-acting (once weekly) potential. Taking advantage of X-ray cocrystal structures of sitagliptin and other DPP-4 inhibitors, such as alogliptin and linagliptin bound to DPP-4, and aided by molecular modeling, we designed several series of heterocyclic compounds as initial targets. During their synthesis, an unexpected chemical transformation provided a novel tricyclic scaffold that was beyond our original design. Capitalizing on this serendipitous discovery, we have elaborated this scaffold into a very potent and selective DPP-4 inhibitor lead series, as highlighted by compound 17c.

TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS

The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.