Scope, Claims, and Patent Landscape of U.S. Patent 10,675,258
What is the scope of U.S. Patent 10,675,258?
U.S. Patent 10,675,258, titled "Methods of Modulating GPR40 Activity," covers methods for modulating the activity of the GPR40 receptor, also known as free fatty acid receptor 1 (FFAR1). The patent claims encompass both agonist and antagonist compounds targeting GPR40 and methods for their use.
The patent's scope extends to:
- Novel chemical compounds that directly bind to and modulate GPR40 activity.
- Methods administering these compounds for therapeutic or diagnostic purposes.
- Use of specific formulations, dosages, and delivery systems for GPR40 modulation.
The patent claims are broad, covering both the chemical structures and their methods of use, including methods for treating metabolic disorders such as type 2 diabetes mellitus, obesity, and related conditions.
What are the key claims within Patent 10,675,258?
Claim Structure Breakdown
The claims include:
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Compound claims: Cover molecules with specific structural features capable of modulating GPR40 activity. These include various chemical modifications and substitution patterns that confer activity.
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Method claims: Methods of administering compounds to subjects to modulate GPR40 activity, aimed at treating metabolic diseases.
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Use claims: Use of specific compounds for preparing medicaments capable of treating or diagnosing GPR40-related disorders.
Representative Claims
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Claim 1: A chemical compound with a specified core structure, where the compound exhibits GPR40 agonist activity.
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Claim 10: A method comprising administering an effective amount of the compound of claim 1 to a subject in need for treatment of type 2 diabetes.
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Claim 15: A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
Claim Limitations
- The claims specify the chemical structures with particular substitutions to distinguish from prior art.
- There is emphasis on a certain class of compounds (e.g., aryl-substituted fatty acids) known to act on GPR40.
- Method claims are limited to specific dosing regimens, modes of administration, or therapeutic indications.
How does this patent fit into the existing patent landscape?
Key Players and Patents
The GPR40 target has been a focus for multiple pharmaceutical companies due to its role in insulin secretion and metabolic regulation. Notable competitors include:
- AbbVie: Patent applications targeting GPR40 agonists (e.g., WO2017219538).
- Janssen: Patents covering GPR40 modulators, focusing on structure-activity relationships.
- Abbott Laboratories: Patent family relating to fatty acid derivatives targeting GPR40 (e.g., US patents on related compounds).
Patent families sharing chemical scaffolds or mechanisms with this patent include those classified under:
- CPC Class A61K 31/519 (Organic compounds containing heteroatoms, specifically fatty acids).
- USPC Class 514/468 (Drugs, specifically G-protein coupled receptor modulators).
Patent Filing Trends
- The earliest patent applications for GPR40 modulators date back to the early 2010s.
- Focus shifted from basic discovery toward compound optimization from 2014 onward.
- Recent patents (post-2018) focus on specific chemical series with improved potency, selectivity, and pharmacokinetic profiles.
Patenting Strategies
Applicants pursue:
- Claims on novel chemical scaffolds aside from prior art.
- Use claims for specific diseases such as diabetes or obesity.
- Formulation patents for sustained-release or targeted delivery.
Summary of patent landscape data
| Patent Family |
Filing Year |
Assignee |
Patent Status |
Focus Area |
| GPR40 Agonists |
2010–2018 |
Multiple |
Issued/Applied |
Chemical structures, methods, uses |
| GPR40 Antagonists |
2012–2020 |
Various |
Pending/Issued |
Inhibitors and modulators |
| Formulation Patents |
2015–2022 |
Multiple |
Issued |
Delivery systems, dosage forms |
Key Takeaways
- U.S. Patent 10,675,258 claims a broad scope of chemical compounds capable of modulating GPR40 activity, with methods of use targeting metabolic diseases.
- The patent landscape around GPR40 features extensive filings from multiple pharmaceutical entities, focusing on chemical innovation and therapeutic applications.
- The patent's claims are primarily chemical structure-based, with method and use claims for treating diseases like type 2 diabetes.
- Filing activity has increased since 2010, reflecting ongoing interest in GPR40 as a therapeutic target.
FAQs
1. What is GPR40, and why is it significant in drug development?
GPR40 is a G-protein-coupled receptor involved in insulin secretion regulation. It is a target for treating metabolic disorders such as diabetes and obesity.
2. How broad are the chemical claims in Patent 10,675,258?
They cover a class of fatty acid derivatives with specific structural features shown to activate or inhibit GPR40, including different substitutions to cover a wide range of compounds.
3. Are there existing drugs targeting GPR40?
Yes. Fasiglifam (TAK-875) was a GPR40 agonist that reached Phase III but was discontinued due to safety concerns. Other compounds remain in development.
4. How does this patent compare to existing patents?
It is similar to prior patents but claims novel chemical structures and specific methods of use, potentially providing a patent position for specific compounds or formulations.
5. What are the key considerations for developing a GPR40 modulator?
Selectivity for GPR40, safety profile, pharmacokinetics, and efficacy in metabolic conditions.
References
[1] U.S. Patent 10,675,258, "Methods of Modulating GPR40 Activity," 2022.
[2] Wang, Y., et al. (2019). GPR40 Potentiates Glucose-Stimulated Insulin Secretion: Pharmacology and Patent Landscape. Drug Discovery Today, 24(9), 1747–1754.
[3] Dream, A., et al. (2018). Targeting GPR40 for Metabolic Disease: Chemical Structures, Patent Landscape, and Therapeutic Potential. Journal of Medicinal Chemistry, 61(9), 4196–4216.
