1607004-33-0Relevant academic research and scientific papers
A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose
Durham, Timothy B.,Marimuthu, Jothirajah,Toth, James L.,Liu, Chin,Adams, Lisa,Mudra, Daniel R.,Swearingen, Craig,Lin, Chaohua,Chambers, Mark G.,Thirunavukkarasu, Kannan,Wiley, Michael R.
, p. 5933 - 5939 (2017/07/22)
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
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Page/Page column 17-18, (2014/05/24)
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.
