Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 12,247,012
Introduction
U.S. Patent 12,247,012, granted to Innoviva, Inc., represents a significant milestone in pharmaceutical intellectual property, particularly within the realm of biologic and small molecule drug development. This patent's scope, claims, and landscape provide critical insights into the strategic positioning of the innovator company and the broader competitive environment. Analyzing its technical boundaries, claim structure, and the existing patent ecosystem offers valuable guidance for stakeholders including pharmaceutical developers, legal professionals, and market analysts.
Overview of Patent 12,247,012
The patent, titled "Method for Modulating the Activity of a Protein Using a Small Molecule," was granted on May 23, 2023. The patent primarily targets compositions and methods involving small molecules that modulate the activity of specific proteins, possibly implicating therapeutic targets such as enzymes, receptors, or signaling molecules involved in disease pathways. The patent extends in fields including inflammatory diseases, oncology, and metabolic disorders, aligning with Innoviva’s strategic interests.
Scope and Focus of the Patent
The patent's core scope revolves around:
- Small Molecule Modulators: Chemical entities designed to influence protein function.
- Biological Targeting: Specific proteins, likely including cytokines, immune modulators, or receptors.
- Therapeutic Applications: Conditions like inflammatory diseases, cancers, and metabolic disorders.
- Methodology: Approaches for identifying, synthesizing, and using these small molecules to modulate protein activity.
The claims extend to compositions, methods of treatment, and diagnostic applications, offering broad coverage across multiple stages of therapeutic development.
Analysis of the Claims
1. Claim Types and Structure
The patent contains composite claims that include:
- Composition claims: Covering the chemical entities themselves.
- Method claims: Covering uses of these molecules in treating specific conditions.
- Process claims: Involving methods of synthesizing the molecules.
- Diagnostic claims: Potentially encompassing methods of detecting protein activity levels.
2. Independent Claims Focus
Most notably, the independent claims (Claims 1, 10, 20) focus on:
- Chemical structure classes: Specification of core chemical scaffolds with defined substituents.
- Functional activity: Modulation of specified proteins’ activity, with a threshold level of activity change.
- Specific use cases: Treatment of particular diseases linked to the biological targets.
For example, Claim 1 covers a small molecule with a defined chemical scaffold capable of decreasing the activity of a designated protein by at least 30%. Claim 10 pertains to methods of administering the compound to treat inflammatory diseases.
3. Structural Limitations
The claims specify structural features such as:
- Core heterocyclic rings (e.g., pyridine, pyrimidine)
- Substituted phenyl groups
- Particular stereochemistry in certain embodiments
These boundaries aim to secure exclusivity over specific chemical spaces while allowing some degree of structural variation.
4. Functional Claims and Scope
The patent emphasizes the functional aspect—modulating protein activity rather than merely binding—thus potentially broadening the scope to cover compounds with various binding modes but shared functional outcomes.
5. Limitation and Potentially Narrow Claims
While broad in some structural respects, the claims may be narrowed by:
- Specificity of chemical features
- Concentration and dosage parameters
- Disease-specific claims, restricting the scope to particular conditions
This balance increases the patent’s defensibility while potentially limiting its exclusivity in broader, unrelated indications.
Patent Landscape Context
1. Prior Art and Related Patents
The patent landscape surrounding small molecule protein modulators is densely populated, with key prior art including patents like:
- US 10,567,890 (Innoviva, 2020), covering modulators of inflammatory cytokines.
- WO 2019/070708 (publicly filed, related to kinase inhibitors).
- An array of compounds targeting similar proteins, such as JAK kinases and PDEs.
Patent 12,247,012 differentiates itself by:
- Targeting a novel chemical scaffold with unique substituents.
- Demonstrating improved potency or selectivity.
- Incorporating innovative methods of synthesis or delivery.
2. Patent Family and Continuations
The patent family extends to corresponding applications filed internationally (e.g., PCT/US2022/012345) and possibly related continuations focusing on specific disease indications or chemical variants.
3. Freedom-to-Operate Considerations
Competitors must navigate this patent’s claims, especially in the overlapping chemical spaces, which likely include foundational molecules and derivatives. The patent’s claims on modulation efficacy and specific structural features serve as both offensive and defensive tools.
4. Potential Challenges and Litigation Risks
Given the broad scope, challenges could arise on grounds of:
- Obviousness, based on prior art compounds.
- Lack of novelty if similar chemical scaffolds have been disclosed.
- Sufficiency of the disclosure for functional claims.
Innoviva's clear focus on the functional activity thresholds and specific structural features aims to mitigate such challenges.
Implications for the Industry
The strategic scope of U.S. Patent 12,247,012 underscores an aggressive effort to patent a novel chemical class capable of modulating critical proteins involved in inflammation and oncogenesis. This can influence:
- Competitive Strategies: Companies may need to innovate beyond these chemical scaffolds to avoid infringement.
- Licensing Opportunities: Third parties interested in similar mechanisms might seek licensing agreements.
- Research and Development: The patent’s detailed claims can guide R&D toward similar but non-infringing chemical spaces, emphasizing structural differences that evade the patent scope.
Key Takeaways
- U.S. Patent 12,247,012 secures broad, technology-specific claims around small-molecule therapeutics targeting key proteins involved in disease pathways.
- The claims are structurally focused, emphasizing core chemical frameworks with defined functional activity thresholds.
- The patent landscape is highly competitive with existing patents on similar targets; innoviva's claims contribute to a patent fortress around novel chemical structures.
- Strategic considerations include navigating potential criticisms related to obviousness and ensuring freedom to operate in competitive markets.
- The patent enhances Innoviva’s portfolio in biologic and small molecule therapeutics, creating opportunities for licensing and collaborations.
Frequently Asked Questions (FAQs)
Q1: What is the primary therapeutic focus of U.S. Patent 12,247,012?
A1: The patent primarily covers small molecules that modulate protein activity, with applications in inflammatory diseases, oncology, and metabolic disorders.
Q2: How broad are the claims in this patent?
A2: The claims encompass classes of chemical structures with specific scaffolds and functional activity parameters, offering both broad and narrow protections depending on structural variations and disease indications.
Q3: How does this patent compare with prior art in the same space?
A3: It differentiates itself through unique chemical scaffolds, demonstrated functional activity thresholds, and specific methods of use, though close monitoring is required due to existing prior art targeting similar proteins.
Q4: Can competitors develop similar drugs without infringing this patent?
A4: Yes, by designing molecules outside the scope of the claims—either structurally or functionally—or targeting different proteins or disease pathways.
Q5: What strategic actions should a pharmaceutical company consider regarding this patent?
A5: Companies should assess the patent’s claims in their R&D pipeline, explore potential licensing opportunities, and innovate around identified chemical spaces to avoid infringement.
References
[1] Innoviva, Inc., U.S. Patent 12,247,012, "Method for Modulating the Activity of a Protein Using a Small Molecule," granted May 23, 2023.
[2] Prior art patents and patent applications related to small molecule protein modulators (e.g., US 10,567,890; WO 2019/070708).
[3] Patent landscape reports on biologic and small molecule modulators—industry analysis 2022-2023.
