287379-33-3

Upstream product

• 20481-15-6 ethyl 4-chloro-1,3-dimethylpyrazolo[3,4-b]pyridine-5-carboxylate 
• 287379-32-2 4-But-2-ynyloxy-N-methyl-benzenesulfonamide 
• 3524-32-1 5-Amino-1,3-dimethylpyrazole 
• 19736-06-2 4-hydroxy-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl ester 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 

Downstream Products

• 287379-34-4 4-[(4-but-2-ynyloxy-benzenesulfonyl)-methyl-amino]-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid 

Relevant academic research and scientific papers

Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors

Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.

Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors

Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

ACETYLENIC ORTHO-SULFONAMIDO AND PHOSPHINIC ACID AMIDO BICYCLIC HETEROARYL HYDROXAMIC ACIDS AS TACE INHIBITORS

Compounds of the formula are provided wherein P and Q are provided that when P is Q is and vice versa; which are useful in disease conditions mediated by TNF- alpha , such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.