2009345-75-7

Upstream product

• 1124383-04-5 5,7-dichloro-[1,2,4]triazolo[1,5-a]pyridin-2-amine 
• 1124383-03-4 ethyl [N-((4,6-dichloropyridin-2-yl)carbamothioyl)]carbamate 
• 116632-24-7 2-amino-4,6-dichloropyridine 

Relevant academic research and scientific papers

TRIAZOLOPYRIDINE COMPOUNDS USEFUL AS PESTICIDES

The present disclosure provides a novel triazolopyridine compound as represented by formula (I) or a salt thereof that controls pests: wherein, R1 and R3 independently represent hydrogen, or the like; R2 represents C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 alkoxy, or the like; R4, R5, R7, and R8 independently represent hydrogen, halogen, or the like; R6 represents C1-C6 haloalkoxy, or the like; and Z represents an oxygen atom, a sulfur atom, SO, or SO2.

1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors with a Novel Monodentate Binding Interaction

Herein we describe the identification of 4-{[1,2,4]triazolo[1,5-a]pyridin-5-yl}benzonitrile-based inhibitors of the hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme. These inhibitors were shown to possess a novel binding mode by X-ray crystallography, in which the triazolo N1 atom coordinates in a hitherto unreported monodentate interaction with the active site Fe2+ ion, while the benzonitrile group accepts a hydrogen-bonding interaction from the side chain residue of Asn315. Further optimization led to potent PHD-1 inhibitors with good physicochemical and pharmacokinetic properties.

FUSED BICYCLIC HETEROARYL DERIVATIVES HAVING ACTIVITY AS PHD INHIBITORS

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, formula (I) wherein X1 , X2, X 3, Y1 , Y 2, R 1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.