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US 9,539,256 B2Granted
Modulators of exchange proteins directly activated by cAMP (EPACS)
AssigneeBoard of Regents, The University of Texas System
InventorsXiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
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Abstract
Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7(1):e30441).
Claims21
An Exchange Protein Activated by cAMP (EPAC) specific inhibitor (ESI) having a formula of:
- where W′ is a substituted or unsubstituted isoxazole and W″ is a 3-trifluoromethylphenyl;
- 3,5-di-trifluoromethylphenyl;
- 3-chlorophenyl;
- 2-chlorophenyl;
- 3,6-dichlorophenyl;
- 3,5-dichlorophenyl;
- 4-bromophenyl;
- 3-bromophenyl;
- 2,3-dichlorophenyl;
- or 3-chloro-4-hydroxyphenyl, wherein the compound is not 3-(5-tert-Butyl-isoxazol-3-yl)-2-[(3-chlorophenyl)-hydrazono]-3-oxo-propionitrile (ESI-09).
7 more elements
Dependencies are inferred from the claim text.