Polymorph of EP4 receptor antagonist, preparation method and use
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.
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
Archived snapshot
Mar 31, 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.
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.
CPC Classifications
C07D 495/04 C07B 2200/13 A61P 35/00 A61P 37/00 A61P 19/00
Filing Date
2021-01-29
Application No.
17797804
Claims
12
Named provisions
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