United States Patent 8,728,441: Scope, Claims, and Patent Landscape
What Is the Scope of Patent 8,728,441?
Patent 8,728,441 covers a novel class of small-molecule inhibitors targeting the fibroblast activation protein (FAP). It claims compositions and methods for selectively inhibiting FAP enzymatic activity, with potential applications in cancer therapy, fibrosis, and tumor stroma targeting.
Key Elements:
- Target: Fibroblast activation protein (FAP) — a serine protease overexpressed in cancer-associated fibroblasts.
- Main Composition: Small molecules with a specified core structure designed for high selectivity.
- Intended Use: Diagnostic imaging, therapeutic intervention, or as part of combination treatments for FAP-expressing tumors.
- Mechanism: Covalent or non-covalent inhibition of FAP enzymatic activity.
How Do the Claims Define the Patent’s Scope?
Independent Claims
The patent includes multiple independent claims:
| Claim Number |
Scope Description |
Key Limitation |
| 1 |
A compound comprising a 4-quinazolinone core with specific substituents capable of inhibiting FAP activity. |
Structural core and substitution pattern |
| 10 |
A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier. |
Composition element |
| 20 |
A method of treating a FAP-associated disease involving administering the compound of claim 1. |
Method of treatment |
Dependent Claims
Dependent claims specify variations in substituents, formulations, dosing, and methods, narrowing the scope:
- Variations in chemical substituents on the core structure.
- Use of radiolabeled derivatives for imaging.
- Specific dosing regimens.
Scope Summary
The patent's scope focuses on chemical structures centered around 4-quinazolinone derivatives, their use as FAP inhibitors, and associated therapeutic/diagnostic applications.
Patent Landscape Overview
Filed and Grant Timeline
- Filing Date: July 31, 2013
- Issue Date: May 3, 2016
- Priority Applications: Priority claimed from earlier provisional applications filed in 2012.
Key Patent Families and Related Patents
- International Progress: Filed through PCT (WO2014/095511), extending protection to Europe, Japan, and other regions.
- Major Competitors:
- Ipsen (EP Patent 2,300,278) — targeting FAP inhibitors.
- Boehringer Ingelheim — patent filings on FAP-targeted therapeutics.
- Moderna (WO2020/077147) — exploring FAP-targeted mRNA delivery systems.
Patent Citations and Influences
Patent 8,728,441 is cited in multiple subsequent filings:
- Subsequent inventions expanding on the chemical scaffold.
- Claims for radiolabeled and antibody conjugate derivatives.
- Combinations with chemotherapeutic agents.
Litigation and Patent Challenges
No evidence of litigation or opposition proceedings tied specifically to patent 8,728,441 as of the latest data. However, frequent patent overlaps exist in the FAP inhibitor space, hinting at potential future disputes.
Patent Expiry and Market Considerations
- Expected expiration: 2033 (considering 20-year term from filing date).
- Market potential includes oncology drug development and imaging agents, estimated multi-billion dollar opportunities.
Key Patent Takeaways
- Core Innovation: Chemical compounds based on 4-quinazolinone structure that inhibit FAP activity.
- Claims Breadth: Covers a wide range of derivatives, formulations, and therapeutic methods, with specific limitations tailored to the chemical structure.
- Patent Position: Solid but faces competition from other FAP-targeted therapies, some of which are in clinical development.
- International Protection: Secured through PCT filings, with active prosecution in major markets.
FAQs
Q1: Does patent 8,728,441 cover all FAP inhibitors?
A1: No. It covers specific 4-quinazolinone derivatives with defined substituents. Other chemical scaffolds are outside its scope.
Q2: Are there existing patent overlaps with other FAP inhibitors?
A2: Yes. Similar compounds are patented by Ipsen and Boehringer Ingelheim, though claims differ in structure and application.
Q3: Can the patent be challenged?
A3: Patent challenges are possible through post-grant review or litigation, especially if prior art is identified that predates the filing date.
Q4: What is the commercial relevance of this patent?
A4: It supports drugs or imaging agents targeting FAP in oncology, representing a key intellectual property position.
Q5: What is the landscape for future patent filings?
A5: Future filings may focus on derivatives, conjugates (e.g., antibody-drug conjugates), and combination therapies expanding or modifying the scope established by patent 8,728,441.
References
- United States Patent and Trademark Office. (2016). US Patent 8,728,441.
- World Intellectual Property Organization. (2014). WO2014095511.
- Li, J., et al. (2019). FAP inhibitors: chemistry, biology and clinical progress. Journal of Medicinal Chemistry, 62(15), 6798–6809.
- European Patent Office. (2017). EP Patent 2300278.
- Boehringer Ingelheim. (2018). FAP-targeted compounds patent family.
[1] US Patent 8,728,441 (2016).
