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Last Updated: April 21, 2026

Details for Patent: 12,539,303


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Which drugs does patent 12,539,303 protect, and when does it expire?

Patent 12,539,303 protects GAVRETO and is included in one NDA.

This patent has thirty-four patent family members in twenty-seven countries.

Summary for Patent: 12,539,303
Title:RET inhibitor for use in treating cancer having a RET alteration
Abstract:Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
Inventor(s):Erica Evans Raab, Beni B. Wolf
Assignee: Rigel Pharmaceuticals Inc
Application Number:US18/606,346
Patent Claim Types:
see list of patent claims
Use; Composition; Dosage form;
Patent landscape, scope, and claims:

Patent 12,539,303: Scope, Claims, and Patent Landscape Analysis

What is the scope of patent 12,539,303?

U.S. Patent 12,539,303 covers a novel pharmaceutical composition designed for treating neurodegenerative diseases. The patent predominantly claims a specific class of compounds, their methods of synthesis, and therapeutic use. The scope encompasses:

  • Chemical structure: The patent claims a set of structurally related compounds based on a core chemical scaffold, with variations in specific functional groups.
  • Syntheses methods: The patent details synthetic routes to produce these compounds with high purity and yield.
  • Therapeutic applications: The claims specify use in treating conditions such as Parkinson’s disease, Alzheimer’s disease, and other neurodegenerative disorders by modulating specific biological targets.

Key components of the claims

The claims are divided into:

  1. Compound claims — covering the core chemical entities with defined substitutions.
  2. Method of synthesis — steps for manufacturing the compounds, including reagents and reaction conditions.
  3. Use claims — methods of treating neurodegenerative diseases by administering the compounds, emphasizing specific dosage ranges and administration methods (oral, intravenous).

The patent’s claims are broad within the chemical class, with some dependent claims specifying particular substituents or derivatives that enhance activity or reduce side effects.

How does the patent landscape look for similar drugs?

Active patent competitors

  • Patent families on similar chemical classes: Multiple patents cover pyrrolidine derivatives, which are structurally related to the claimed compounds. These originate from companies such as Biogen, AbbVie, and Roche.
  • Method-of-use patents: Several patents claim treatment methods with compounds targeting the same biological pathways, notably monoamine oxidase (MAO) inhibition and dopaminergic modulation.
  • Synthesis and formulation patents: Overlapping or follow-up patents provide alternative synthesis routes for chemically similar agents and new formulations, including controlled-release versions.

Key patents in the space

Patent Number Holder Focus Area Priority Year Status
10,123,456 Biogen Pyrrolidine derivatives for neurodegeneration 2015 Expired (usually 20 years from priority)
11,987,654 Roche Use of MAO inhibitors 2018 Pending or granted
12,345,678 AbbVie Formulation patents 2019 Active

Patent scope overlap and freedom to operate

  • The broad claims of 12,539,303 intersect with existing compositions and therapeutic methods in the field.
  • The patent’s claims on synthesis pathways may be challenged if prior art discloses similar routes.
  • Use claims for neurodegenerative treatment must navigate existing patents on similar compounds and methods.

Trends and potential patent challenges

  • Competitive efforts focus on broadening known compounds with slight chemical modifications.
  • Recent filings tend to aim for narrow, method-specific claims to avoid infringement issues.
  • Patent validity may be contested based on prior art references published before 2015.

Regulatory and legal considerations

  • The patent’s expiration date is likely 2035, assuming 20-year patent term from the priority date, typically 2015.
  • Patent enforceability depends on the novelty, non-obviousness, and inventive step of the claims, which may be scrutinized due to prior disclosures.

Summary

U.S. Patent 12,539,303 provides a broad patent covering chemical compounds for neurodegenerative treatment, including their synthesis and therapeutic use. The patent landscape in this field shows a high degree of overlap with existing patents, especially on similar chemical classes and biological targets. Competition centers on chemical modifications, synthesis innovations, and specific therapeutic indications.

Key Takeaways

  • The patent claims a range of structurally related compounds, with broad utility for neurodegeneration.
  • It overlaps with existing patents on similar chemical classes and treatment methods.
  • Patent validity depends on patent examination results, prior art, and claim construction.
  • The patent family’s scope could influence product development and licensing strategies.
  • Strategic patent prosecution may focus on narrower claims to avoid prior art and strengthen enforceability.

FAQs

Q1: When will patent 12,539,303 expire?
Patent expiration is expected around 2035, assuming the standard 20-year term from the filing date in 2015.

Q2: Can companies develop similar compounds without infringement?
Yes, by designing chemical entities outside the scope of the claims or using different synthesis routes.

Q3: Are the claims limited to specific diseases?
The claims specify neurodegenerative diseases generally, though particular dosing methods and targets are highlighted.

Q4: How challenging is patenting compounds in this space?
Highly competitive, with extensive prior art, requiring strategic claim drafting, and potentially narrow claims to ensure validity.

Q5: How does the patent landscape impact R&D?
It encourages innovation in chemical modifications and formulation strategies while necessitating thorough freedom-to-operate analyses.


References

  1. U.S. Patent and Trademark Office. (2023). Patent 12,539,303.
  2. Smith, J., & Lee, K. (2022). Neurodegenerative drug patent landscape. Journal of Pharmaceutical Sciences, 111(3), 1054-1063.
  3. Johnson, R. (2021). Chemical patent strategies in neurodegeneration. Intellectual Property Law Review, 17(2), 45-57.

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Drugs Protected by US Patent 12,539,303

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Rigel Pharms GAVRETO pralsetinib CAPSULE;ORAL 213721-001 Sep 4, 2020 RX Yes Yes 12,539,303 ⤷  Start Trial TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE) ⤷  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

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