PDIA4 Inhibitors Treat Diabetes, Preserve Beta Cells
Summary
USPTO has granted Patent US12605353B2 to Academia Sinica, covering disulfide-isomerase A4 (PDIA4) inhibitors for inhibiting pancreatic beta-cell pathogenesis and treating diabetes. The patent discloses drug candidates with IC50 values ranging from 4 micrometers to 300 nanomolars that augment insulin secretion from pancreatic beta-cells.
Pharmaceutical companies developing diabetes or metabolic disease therapeutics should monitor this IP landscape for potential licensing, freedom-to-operate, or R&D pathway considerations.
What changed
USPTO issued Patent US12605353B2 to Academia Sinica on April 21, 2026, covering disulfide-isomerase A4 (PDIA4) inhibitors for treating diabetes and preserving pancreatic beta-cell function. The patent discloses drug candidates with IC50 values between 4 micrometers and 300 nanomolars that augment insulin secretion, including representative compound No. 8 (4,5-dimethoxy-2-propiolamidobenzoic acid) which, alone or combined with metformin, was effective in normalizing blood glucose in diabetic subjects.
Pharmaceutical companies engaged in diabetes or metabolic disease drug development should review this patent for potential freedom-to-operate implications, licensing opportunities, or competitive landscape considerations in the PDIA4 inhibitor space.
Archived snapshot
Apr 21, 2026GovPing captured this document from the original source. If the source has since changed or been removed, this is the text as it existed at that time.
PDIA4 inhibitors and use thereof for inhibiting β-cell pathogenesis and treating diabetes
Grant US12605353B2 Kind: B2 Apr 21, 2026
Assignee
ACADEMIA SINICA
Inventors
Wen-Chin Yang, Keng-Chang Tsai
Abstract
Disulfide-Isomerase A4 (PDIA4) inhibitors and use thereof for inhibiting pancreatic β-cell pathogenesis and treating diabetes are disclosed. Drug candidates that inhibit PDIA4 with IC50 values ranging from 4 μM to 300 nM are identified. The compounds are highly active in augmenting insulin secretion from pancreatic β-cells. The representative compound No. 8 (4,5-dimethoxy-2-propiolamidobenzoic acid), alone or in combination with metformin, is effective in preserving pancreatic β-cell function, treating and/or reversing, returning blood glucose concentration to a normal level in a diabetic.
CPC Classifications
A61K 31/216 A61K 31/196 A61K 31/155 A61K 31/4035 A61K 31/695 A61P 3/10
Filing Date
2020-11-15
Application No.
17780482
Claims
18
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