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US 11,124,489 B2Granted
EPAC antagonists
AssigneeBoard of Regents, The University of Texas System
InventorsJia Zhou, Zhiqing Liu, Na Ye, Fang Mei, Xiaodong Cheng
Life of this patent
Estimating the term…
Abstract
Embodiments are directed to a series of novel EPAC antagonists that are designed, synthesized and evaluated in an effort to develop diversified analogues based on the scaffold of the previously identified high-throughput (HTS) hit ESI-09.
Claims8
An Exchange Protein Activated by cAMP (EPAC) antagonist
- selected from N-(4-Chloro-3-(trifluoromethyl)phenyl)-2-oxo-2-(5-(4-(tert-butyl)phenyl)isoxazol-3-yl)acetohydrazonoyl cyanide (NY0617), N-(3-trifluromethyl-4-chlorophenyl)-2-oxo-2-(5-phenylisoxazol-3-yl)acetohydrazonoyl cyanide (NY0460), N-(3,5-Bis(trifluoromethyl)phenyl)-2-oxo-2-(5-phenylisoxazol-3-yl)acetohydrazonoyl cyanide (NY0457), N-(4-Chloro-3-(trifluoromethyl)phenyl)-2-oxo-2-(5-(4-methoxyphenyl)isoxazol-3-yl)acetohydrazonoyl cyanide (NY0654), N-(3,5-bis(trifluoromethyl)phenyl)-2-(5-(4-methoxyphenyl)isoxazol-3-yl)-2-oxoacetohydrazonoyl cyanide (NY0655), N-(3-Chloro-5-(trifluoromethyl)phenyl)-2-(5-(furan-2-yl)isoxazol-3-yl)-2-oxoacetohydrazonoyl cyanide (NY0725), N-(4-Chloro-3-(trifluoromethyl)phenyl)-2-(5-(furan-2-yl)isoxazol-3-yl)-2-oxoacetohydrazonoyl cyanide (NY0726), or N-(3-Chloro-4-(trifluoromethyl)phenyl)-2-(5-(4-fluorophenyl)isoxazol-3-yl)-2-oxoacetohydrazonoyl cyanide (NY0541).
An Exchange Protein Activated by cAMP (EPAC) antagonist having a formula of:
- where R7 and R11 are H;
- R8, R9, and R10 are independently selected from H, halogen, CF3, C1 to C4 alkyl, C1 to C4 heteroalkyl, or C1 to C4 alkoxy.
Dependencies are inferred from the claim text.