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Crystalline Solid Forms Of 6-Carboxy-2-(3,5-Dichlorophenyl)-Benzoxazole For Use As A Medicament

Patent No. EP3977993 (titled "Crystalline Solid Forms Of 6-Carboxy-2-(3,5-Dichlorophenyl)-Benzoxazole For Use As A Medicament") was filed by Pfizer on Aug 31, 2015. The application was issued on Jan 31, 2024.

Patent Summary

This invention provides a crystalline form (Form 1) of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole for use as a medicament, specifically to stabilize transthyretin (TTR) and inhibit TTR amyloid fibril formation in treating transthyretin amyloid diseases. Form 1 is characterized by a powder X-ray diffraction (PXRD) pattern with peaks at 2θ of 15.4 ± 0.2, 20.2 ± 0.2, 28.6 ± 0.2, and 29.0 ± 0.2, and a solid-state NMR spectrum with $^{13}$C chemical shifts at 120.8 ± 0.2 and 127.7 ± 0.2 ppm. The form may be substantially pure, consist of needles, or exist in mixtures with other polymorphs (e.g., Forms 2, 4, 6). Form 1 is utilized to ensure pharmaceutical stability, purity, and consistent dissolution rates in dosage forms.

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Patent Oppositions (3)

Patent oppositions filed by competitors challenge the validity of a granted patent. These oppositions are typically based on claims of prior art, lack of novelty, or non-obviousness. They are a key part of the process for determining a patent's strength and enforceability.

CompanyOpposition DateRepresentative
KELTIEOct 31, 2024KELTIE
QUIMICA SINTETICAOct 29, 2024AERA
QUIMICA SINTETICAOct 29, 2024BARDEHLE PAGENBERG SL

Dossier Documents

The dossier documents provide a comprehensive record of the patent's prosecution history - including filings, correspondence, and decisions made by patent offices - and are crucial for understanding the patent's legal journey and any challenges it may have faced during examination.

  • Date

    Description

EP3977993

PFIZER
Application Number
EP21203965A
Filing Date
Aug 31, 2015
Status
Granted And Under Opposition
Dec 29, 2023
Publication Date
Jan 31, 2024
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