1454285-47-2

Upstream product

• 1315362-16-3 methyl 5-chlorofuro[2.3-c]pyridine-2-carboxylate 
• 1454285-46-1 methyl 2-[(6-chloro-4-formylpyridin-3-yl)oxy]acetate 
• 1060804-53-6 2-chloro-5-hydroxypyridine-4-carbaldehyde 
• 1282516-32-8 2-chloro-5-(methoxymethoxy)pyridine-4-carbaldehyde 
• 877133-56-7 2-chloro-5-(methoxymethoxy)pyridine 
• 41288-96-4 6-chloropyridine-3-ol 

Downstream Products

• 1454285-48-3 N-[[4-(benzenesulfonyl)phenyl]methyl]-5-chlorofuro[2,3-c]pyridine-2-carboxamide 
• 1454285-49-4 N-[[4-(benzenesulfonyl)phenyl]methyl]-5-[(diphenylmethylidene)amino]furo[2.3-c]pyridine-2-carboxamide 
• 1454285-13-2 5-amino-N-[[4-(benzenesulfonyl)phenyl]methyl]furo[2,3-c]pyridine-2-carboxamide 

Relevant academic research and scientific papers

AMINOISOXAZOLINE COMPOUNDS AS AGONISTS OF ALPHA7-NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to novel aminoisoxazoline compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors

NAMPT inhibitors may show potential as therapeutics for oncology. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for potent cellular NAMPT inhibition. However, when combined with a benzyl group in the center of the inhibitors, such pyridine-like moieties also led to consistent and potent inhibition of CYP2C9. In an attempt to reduce CYP2C9 inhibition, a parallel synthesis approach was used to identify central benzyl group replacements with increased Fsp3. A spirocyclic central motif was thus discovered that was combined with left-hand pyridines (or pyridine-like systems) to provide cellularly potent NAMPT inhibitors with minimal CYP2C9 inhibition. Further optimization of potency and ADME properties led to the discovery of compound 68, a highly potent NAMPT inhibitor with outstanding efficacy in a mouse tumor xenograft model and lacking measurable CYP2C9 inhibition at the concentrations tested.

AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES

Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.