1607004-48-7

Upstream product

• 90719-32-7 (S)-4-Benzyl-2-oxazolidinone 
• 111292-87-6 (S)-4-benzyl-3-butyryloxazolidin-2-one 
• 402-49-3 4-bromomethyltrifluoromethylbenzene 

Downstream Products

• 1607004-49-8 (2R)-2-[[4-(trifluoromethyl)phenyl]methyl]butanoic acid 
• 1607004-33-0 (2R)-N-[[(4R)-4-cyclopropyl-2,5-dioxo-imidazolidin-4-yl]methyl]-2-[[4-(trifluoromethyl)phenyl]methyl]butanamide 

Relevant academic research and scientific papers

A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose

Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means of altering the progression of osteoarthritis. We report the identification of 7 which had good oral pharmacokinetics in rats and showed efficacy in a rat chemical model of osteoarthritis. The projected human dose required to achieve sustained plasma levels ≥10 times the hADAMTS-5 IC50 is 5 mg q.d.

AGGRECANASE INHIBITORS

The present invention provides compounds having the formula: wherein R1 is selected from methyl, ethyl, propyl, cyclopropyl, and dimethyl, or a pharmaceutically acceptable salt thereof, along with methods and intermediates for their preparation, and uses thereof.