1381795-32-9

Upstream product

• 824-94-2 p-methoxybenzyl chloride 
• 1381795-20-5 2-chloro-9-((2-(trimethylsilyl)ethoxy)methyl)-1H-purin-6(9H)-one 
• 1381795-30-7 C₂₀H₂₀BrN₅O₂ 
• 1381795-31-8 3-(R)-piperidinyl phthalimide hydrochloride 
• 1381795-23-8 C₂₂H₃₃N₅O₄Si 
• 442685-34-9 2,6-dichloro-9-{[2-(trimethylsilyl)ethoxy]methyl}-9H-purine 
• 1381795-31-8 3-(R)-piperidinyl phthalimide hydrochloride 
• 1381795-29-4 2-bromo-5-(4-methoxybenzyl)-5,7,8,9-tetrahydropyrimido[2,1-b]purin-4(3H)-one 
• 1381795-28-3 C₂₂H₃₀BrN₅O₃Si 
• 1381795-27-2 C₁₆H₁₇N₅O₂ 
• 1381795-25-0 5-(4-methoxybenzyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-5,7,8,9-tetrahydropyrimido[2,1-b]purin-4(1H)-one 

Downstream Products

• 1381794-99-5 (R)-2-(3-aminopiperidin-1-yl)-3-(but-2-yn-1-yl)-5-(4-methoxybenzyl)-5,7,8,9-tetrahydropyrimido[2,1-b]purin-4(3H)-one 

Relevant academic research and scientific papers

Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Molecular modeling of unbound tricyclic guanine scaffolds indicated that they can serve as effective bioisosteric replacements of xanthines. This notion was further confirmed by a combination of X-ray crystallography and SAR studies, indicating that tricyclic guanine DPP4 inhibitors mimic the binding mode of xanthine inhibitors, exemplified by linagliptin. Realization of the bioisosteric relationship between these scaffolds potentially will lead to a wider application of cyclic guanines as xanthine replacements in drug discovery programs for a variety of biological targets. Newly designed DPP4 inhibitors achieved sub-nanomolar potency range and demonstrated oral activity in vivo in mouse glucose tolerance test.

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. I