Technology Bundle ID

Creation and Use of 12-LO inhibitors (4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives) for the Treatment of Diabetes and Large Platelet-Derived Clots

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Lead Inventors
David Maloney (NCATS)
Adam Yasgar (NCATS)
Ajit Jadhav (NCATS)
Anton Simeonov (NCATS)
David Taylor-Fishwick (Eastern Virginia Medical School)
Diane Luci (NCATS)
Jerry Nadler (Eastern Virginia Medical School)
Michael Holinstat (Thomas Jefferson University)
Theodore Holman (University of California, Santa Cruz)
This technology includes the discovery and use of novel selective 12-LO (lipoxygenase) inhibitors, 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives, for attenuating large clots and for the treatment of Type 1/2 diabetes. A 12-LO inhibitor could be a potent intracellular approach to block platelets from forming large clots in response to vessel injury or activation of the coagulation pathway, either due to diabetes and/or cardiovascular disease. Blocking clot formation can significantly decrease the occurrence of myocardial infarction and death.
Commercial Applications
With further development, the small molecules covered by this technology have the potential to be a therapeutic, but minimally can serve as a starting point to further validate 12-LO as a therapeutic target.
Competitive Advantages
The small molecules covered in this patent represent novel 12-LO inhibitors which are soluble, have favorable ADME properties, and good in vivo PK. There are no current commercially available 12-LO inhibitors, so these agents have the possibility of being first in class.

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