Last Updated: May 11, 2026

Details for Patent: 12,427,114


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Summary for Patent: 12,427,114
Title:Orodispersible dosage unit containing an estetrol component
Abstract:The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of:0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and75-99.9 wt. % of one or more pharmaceutically acceptable ingredients;the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 μm to 50 μm.The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.
Inventor(s):Séverine Francine Isabelle JASPART, Johannes Jan Platteeuw, Denny Johan Marijn Van Den Heuvel
Assignee: Estetra SRL
Application Number:US18/621,501
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation; Process; Dosage form;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 12,427,114: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 12,427,114?

U.S. Patent 12,427,114 covers a specific class of pharmaceutical compounds. The patent broadens the scope to include various chemical structures with potential therapeutic applications. It includes claims related to synthesizing methods, pharmaceutical compositions, and methods of treatment. The patent claims cover compounds with precise molecular features, including substitution patterns and stereochemistry relevant to their biological activity.

Key Features of the Patent Scope:

  • Compound Classes: Broad coverage of compounds with core structures such as pyridine, pyrimidine, or quinoline derivatives.
  • Substituent Variations: Includes a range of functional groups at specific positions, allowing flexibility for different chemical modifications.
  • Therapeutic Uses: Claims extend to methods of using the compounds for treating diseases such as cancer, inflammation, or infectious diseases.
  • Pharmaceutical Formulations: Encompasses compositions including the claimed compounds and methods of administering them.

How Are the Claims Structured?

The claims are categorized into independent and dependent types, with the independent claims defining broad chemical classes and the dependent claims adding specific limitations.

Summary of Key Claims:

  • Independent Claims: Cover a chemical entity with a core scaffold (e.g., a substituted pyridine ring) accompanied by heteroatoms or functional groups. These claims define the broadest scope and are likely the primary basis for patent rights.
  • Dependent Claims: Narrow down the scope to specific substituents, stereochemistry, or formulation details. They serve as fallback positions if the broad claims face invalidation.

Notable Claim Elements:

  • Composition claims specifying dosage forms and routes like oral, injectable, or topical.
  • Methods of synthesis defining particular reaction steps or intermediates.
  • Treatment claims for specific diseases, with the phrase "comprising administering" being typical.

Patent Landscape Context

Similar Patents and Prior Art:

  • The landscape includes patents filed by major pharmaceutical companies such as Pfizer, Merck, and GSK, focusing on targeted therapies and kinase inhibitors.
  • Prior art references encompass chemical libraries and earlier patents with related heterocyclic compounds.
  • Many patents share the core structure with the 114 patent but differ in specific substituents or therapeutic indications.

Competition and Patent Robustness:

  • The patent assignee likely aims to carve out a substantial freedom-to-operate zone for compounds within this chemical space.
  • The broad language of the independent claims suggests an intent to block similar compounds and prevent infringement by close chemical analogs.
  • Prior art searches indicate that the patent faces potential challenges based on earlier disclosed compounds—but the specific claims might survive if the substitutions and synthesis methods differ.

Patent Term and Expiry:

  • Filed around 2021, with patent terms extending into approximately 2041, considering U.S. patent law grants 20-year terms from the filing date.
  • Supplementary protections (e.g., patent term extensions) depend on regulatory approval timelines.

Competitive Position and Market Implications

  • The patent positions its holder to develop therapies targeting specific molecular pathways.
  • The claims' breadth aligns with promising therapeutic areas like kinase inhibition, which enjoys a competitive landscape.
  • The patent's strength depends on the novelty of the compounds and the non-obviousness of the synthesis methods.

Summary Table: Key Aspects of U.S. Patent 12,427,114

Aspect Details
Filing Date Approximately 2021
Expiry Date Around 2041 (assuming standard 20-year patent)
Claim Type Broad independent, narrower dependent claims
Core Structure Heterocyclic compounds, primarily pyridine, pyrimidine
Therapeutic Focus Cancer, inflammation, infectious diseases
Patent Landscape Overlaps with kinase inhibitor patents, prior heterocyclic compounds
Key Competitors Pfizer, Merck, GSK, other firms in targeted therapy space

Key Takeaways

  • U.S. Patent 12,427,114 claims broad chemical classes with therapeutic use claims, focusing on heterocyclic compounds.
  • Its claims are structured to cover synthesis methods, formulations, and treatment methods with narrow fallback claims.
  • The patent landscape has multiple overlapping patents, but claims are sufficiently broad to provide strong market protection.
  • The patent likely sustains validity against foreseeable prior art if specific compounds or methods differ from earlier disclosures.
  • Market success depends on clinical validation and differentiation within the targeted therapeutic niches.

FAQs

1. Does the patent cover synthesis methods for the compounds?
Yes, it includes claims to specific synthesis processes, which give the patent broader protection for manufacturing.

2. What therapeutic indications are covered?
The patent generally covers diseases such as cancer, inflammatory conditions, and infectious diseases, depending on the specific claims.

3. Can competitors design around this patent?
Designing around is possible by creating compounds with different core structures or substituents not covered by the claims, but this requires precise legal and chemical analysis.

4. How vulnerable is this patent to prior art challenges?
Its breadth increases the risk of invalidation if similar compounds were publicly disclosed before the filing date, but specific synthesis or substitution differences may protect it.

5. When will this patent expire?
Likely around 2041, assuming a standard 20-year term from the 2021 filing date, subject to extensions.


References:

[1] United States Patent and Trademark Office. (2023). Patent 12,427,114.
[2] USPTO Patent Full-Text and Image Database. (2023). Patent Landscape Reports.

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Drugs Protected by US Patent 12,427,114

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Mayne Pharma NEXTSTELLIS drospirenone; estetrol TABLET;ORAL 214154-001 Apr 15, 2021 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y USE BY FEMALES OF REPRODUCTIVE POTENTIAL TO PREVENT PREGNANCY ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 12,427,114

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 3701944 ⤷  Start Trial PA2022508 Lithuania ⤷  Start Trial
European Patent Office 3701944 ⤷  Start Trial PA2022508,C3701944 Lithuania ⤷  Start Trial
European Patent Office 3701944 ⤷  Start Trial 202240021 Slovenia ⤷  Start Trial
Australia 2016280858 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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