P2Y14 Receptor Antagonists Containing A Biaryl Core

The technology discloses composition of compounds that fully antagonize the human P2Y14 receptor, with moderate affinity with insignificant antagonism of other P2Y receptors. Therefore, they are highly selective P2Y14 receptor antagonists. Even though there is no P2Y14 receptor modulators in clinical use currently, selective P2Y14 receptor antagonists are sought as potential therapeutic treatments for asthma, cystic fibrosis, inflammation and possibly diabetes and neurodegeneration.

Potential Commercial Applications: Competitive Advantages:
  • Development of P2Y14 receptor antagonist for treatment of disorders, such as:
  • Inflammation
  • diabetes
  • cystic fibrosis
  • asthma
  • neurodegeneration


Kenneth Jacobson (NIDDK)  ➽ more inventions...

Jinha Yu (NIDDK)  ➽ more inventions...

Antonella Ciancetta (NIDDK)  ➽ more inventions...

Zhiwei Wen (NIDDK)  ➽ more inventions...

Young-Hwan Jung (NIDDK)  ➽ more inventions...

Intellectual Property:
US Pat: - issued -
PCT Application No. PCT/US19/17422 filed on 2019-02-11
US Application No. 16/967,177 filed on 2020-08-04

Yu J, et al, Structure-guided modification of heterocyclic antagonists of the P2Y14 receptor. J. Med. Chem., 2018, 61: 4860−4882, doi: 10.1021/acs.jmedchem.8b00168
Jung, Y.H., et al, Exploration of alternative scaffolds for P2Y14 receptor antagonists containing a biaryl core. J. Med. Chem., 2020, 63:9563–9589 doi: 10.1021/acs.jmedchem.0c00745

Collaboration Opportunity:

The NIDDK is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize P2Y14 Receptor Antagonists Containing A Biaryl Core. For collaboration opportunities, please contact Kenneth A. Jacobson, Ph.D. at ,a href="mailto:kennethj@niddk.nih.gov">kennethj@niddk.nih.gov

Licensing Contact:
Betty Tong, Ph.D.
Email: tongb@niddk.nih.gov
Phone: 301-451-7836

OTT Reference No: E-028-2018-0
Updated: Nov 20, 2020