866040-20-2

Upstream product

• 62535-60-8 5-amino-3-methyl-1-p-tolylpyrazole 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 956574-51-9 2-[(5-methyl-2-p-tolyl-2H-pyrazol-3-ylamino)-methylene]-malonic acid diethyl ester 

Downstream Products

• 1224047-97-5 C₂₇H₂₄ClN₅O₂ 
• 851521-42-1 4-chloro-3-methyl-1-p-tolyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid amide 
• 1026227-69-9 4-chloro-3-methyl-1-p-tolyl-1H-pyrazolo[3,4-b]pyridine-5-carbonyl chloride 
• 1026640-39-0 4-chloro-3-methyl-1-p-tolyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid 

Relevant academic research and scientific papers

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.

Discovery of new orally active phosphodiesterase (PDE4) inhibitors

A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.