Polymorph of EP4 receptor antagonist, preparation method and use

ChangeBridge: Patent Grants - Therapeutics (A61P)

Published March 31st, 2026

Detected March 31st, 2026

Summary

USPTO granted patent US12590103B2 to Shanghai Yuyao Biotech Ltd. for a stable polymorph of an EP4 receptor antagonist. The patent covers the solid-state form with improved stability over the amorphous compound, with claims directed to oncology, immunology, and bone disease applications.

View original document View source feed page

What changed

USPTO granted Patent US12590103B2 on March 31, 2026, to Shanghai Yuyao Biotech Ltd. The patent claims a stable polymorph (Form B) of the EP4 receptor antagonist (S)-4-(1-(2-(4-fluorobenzyl)-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxamido)ethyl)benzoic acid. The polymorph offers superior chemical and physical stability compared to the amorphous form, making it suitable for pharmaceutical manufacturing. The 12 claims cover the polymorph itself, its preparation method, pharmaceutical compositions containing it, and methods of treating conditions including cancer (A61P 35/00), immune disorders (A61P 37/00), and bone diseases (A61P 19/00).

Patent holders and R&D teams should conduct freedom-to-operate analyses to ensure their EP4 antagonist programs do not infringe this granted patent. Generic pharmaceutical companies and biotech firms developing similar prostaglandin receptor antagonists should review claim scope and consider design-around strategies. The patent expires January 29, 2041 (20 years from filing).

What to do next

Conduct freedom-to-operate analysis for any EP4 receptor antagonist programs
Review patent claims to assess potential infringement exposure
Consider design-around strategies if developing competing compounds

Source document (simplified)

← USPTO Patent Grants

Polymorph of EP4 receptor antagonist, preparation method therefor and use thereof

Grant US12590103B2 Kind: B2 Mar 31, 2026

Assignee

SHANGHAI YUYAO BIOTECH LTD.

Inventors

Hankun Zhang, Junjie Yang, Mingyao Liu, Wenbo Zhou, Shihong Peng, Huang Chen, Jian Lu

Abstract

Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist(S)-4-(1-(2-(4-fluorobenzyl)-4, 7-dihydro-5H-thieno [2,3-c]pyran-3-carboxamido) ethyl) benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.