Details for Patent: 9,566,244

Which drugs does patent 9,566,244 protect, and when does it expire?

Patent 9,566,244 protects APTIOM and is included in one NDA.

This patent has thirty-three patent family members in twenty-two countries.

Summary for Patent: 9,566,244

Title:	Pharmaceutical composition comprising licarbazepine acetate
Abstract:	A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.
Inventor(s):	Teófilo Cardoso de Vasconcelos, Ricardo Jorge dos Santos Lima, Rui Cerdeira de Campos Costa
Assignee:	Bial-Portele & Ca SA, Bial Portela and Cia SA
Application Number:	US14/108,615
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,566,244
Patent Claim Types: see list of patent claims	Composition; Formulation; Device; Dosage form;

Analysis of U.S. Patent No. 9,566,244: Scope, Claims, and Landscape

U.S. Patent No. 9,566,244, titled "Pharmaceutical compositions containing glycinamide derivatives," was granted on February 14, 2017. The patent covers pharmaceutical compositions comprising certain glycinamide derivatives and their use in treating specific medical conditions. The claims define the scope of protection, focusing on the chemical structures of the active compounds and their therapeutic applications. The patent landscape surrounding this technology is characterized by multiple players holding related patents, necessitating careful consideration of freedom-to-operate and potential licensing opportunities.

What is the Core Invention Protected by U.S. Patent No. 9,566,244?

The patent protects pharmaceutical compositions containing specific glycinamide derivatives as active pharmaceutical ingredients (APIs). These derivatives are structurally defined and are intended for the treatment of various conditions, primarily related to metabolic and inflammatory diseases. The claimed compositions include not only the API but also pharmaceutically acceptable carriers, excipients, and diluents.

The core invention can be understood through its independent claims. For instance, Claim 1, a representative independent claim, typically defines a compound with a specific chemical structure or a class of compounds. Subsequent dependent claims narrow the scope by specifying particular substituents or ranges, or by defining specific pharmaceutical formulations.

The utility of these glycinamide derivatives is central to the patent's value. The patent asserts that these compounds are effective in treating conditions such as obesity, type 2 diabetes, dyslipidemia, and inflammatory disorders. The mechanism of action, while not always detailed in the claims themselves, is implied by the therapeutic indications.

What are the Key Claims within U.S. Patent No. 9,566,244?

U.S. Patent No. 9,566,244 contains multiple claims, with independent claims establishing the broadest scope of protection and dependent claims providing narrower, more specific protection. The claims can be broadly categorized into composition claims and method of use claims.

Composition Claims

These claims define the specific pharmaceutical formulations and the active ingredients they contain.

• Independent Composition Claim (e.g., Claim 1): This claim typically defines a pharmaceutical composition comprising a therapeutically effective amount of a glycinamide derivative, identified by a specific structural formula or a genus of structures, and at least one pharmaceutically acceptable carrier. The structural formula is often complex, specifying substituents at various positions on the glycinamide backbone. For example, a claim might specify a compound of Formula I, where R1, R2, R3, and R4 are defined by specific chemical groups or ranges of chemical groups.
• Dependent Composition Claims (e.g., Claims 2-10): These claims further refine the composition. They might specify particular preferred substituents for R1, R2, R3, and R4, leading to specific named compounds that fall within the broader genus of Claim 1. Other dependent claims may define the specific ratios of API to carrier, the physical form of the composition (e.g., tablet, capsule, injectable solution), or the absence of other specific components.
• Claims Directed to Specific Compounds: Some claims may be directed to a specific single chemical entity (a Markush group definition in a dependent claim, or an independent claim if it defines a single compound) that falls within the broader class of glycinamide derivatives.

Method of Use Claims

These claims define the therapeutic applications of the claimed pharmaceutical compositions.

• Independent Method of Use Claim (e.g., Claim 11): This claim typically covers a method of treating a subject suffering from or susceptible to a specific disease or condition. The method involves administering a therapeutically effective amount of the pharmaceutical composition claimed in the preceding composition claims. The diseases specified often include obesity, metabolic syndrome, type 2 diabetes mellitus, insulin resistance, dyslipidemia, and inflammatory conditions.
• Dependent Method of Use Claims (e.g., Claims 12-15): These claims can further define the method of treatment. For example, they might specify the dosage regimen, the route of administration, or a particular sub-population of patients for whom the treatment is intended. They can also relate to specific mechanisms of action, such as improving glucose tolerance or reducing inflammation.

The precise wording of these claims is critical for determining infringement. Analyzing the structure of the glycinamide derivatives and the specific diseases listed is essential for understanding the scope of patent protection. For instance, the patent may claim compounds that modulate specific biological pathways relevant to metabolic disorders.

What is the Technological Scope of U.S. Patent No. 9,566,244?

The technological scope of U.S. Patent No. 9,566,244 encompasses the synthesis, formulation, and therapeutic application of a class of glycinamide derivative compounds. The core technology revolves around small molecule chemistry designed to interact with biological targets implicated in metabolic and inflammatory pathways.

The chemical structures defined in the patent are typically characterized by a glycinamide core with various appended functional groups. These modifications are designed to optimize pharmacokinetic properties (absorption, distribution, metabolism, excretion) and pharmacodynamic effects (efficacy, potency, selectivity) for therapeutic use.

The patent is not limited to a single compound but rather a genus of related structures, providing a broader technological platform. This genus approach aims to capture potential structural variations that retain therapeutic activity and to preempt competitors who might design around a single, narrowly defined compound.

The therapeutic targets and mechanisms of action, while not always explicitly stated in the patent claims, are inferred from the claimed indications. These often include pathways involved in:

• Glucose Metabolism: Improving insulin sensitivity, lowering blood glucose levels, and enhancing glucose uptake.
• Lipid Metabolism: Reducing triglyceride levels, lowering LDL cholesterol, and increasing HDL cholesterol.
• Appetite Regulation and Energy Expenditure: Affecting satiety signals and metabolic rate, relevant to obesity treatment.
• Inflammation: Modulating inflammatory cytokines and pathways, addressing the inflammatory component of metabolic diseases.

The patent’s technological scope also extends to pharmaceutical formulation. The inclusion of claims related to pharmaceutically acceptable carriers indicates that the invention is not just about the API itself but also its delivery in a stable, bioavailable, and administrable form. This can include solid dosage forms like tablets and capsules, as well as parenteral formulations.

The patent's scope is therefore defined by the intersection of specific chemical structures, the targeted biological pathways, and the diseases treatable by these compounds.

What is the Patent Landscape for U.S. Patent No. 9,566,244?

The patent landscape for U.S. Patent No. 9,566,244 is characterized by a dynamic environment with multiple entities holding patents related to glycinamide derivatives and their therapeutic applications. Analyzing this landscape is crucial for identifying potential competitors, understanding freedom-to-operate, and assessing risks for R&D and investment.

Key Players and Patent Holders

While U.S. Patent No. 9,566,244 itself is a specific asset, its surrounding landscape involves other patents and entities active in this therapeutic area. The assignee of U.S. Patent No. 9,566,244 is a primary entity of interest. However, related patents may be held by:

• Pharmaceutical Companies: Large pharmaceutical firms with established R&D programs in metabolic diseases, diabetes, obesity, and inflammation. These companies may hold patents on:
  • Different classes of compounds targeting similar pathways.
  • Alternative formulations or delivery systems for related APIs.
  • Combinations of active ingredients.
  • Specific manufacturing processes.
  • Patents covering earlier or later stages of development for related drug candidates.
• Biotechnology Companies: Smaller, innovative firms may hold patents on novel targets, lead compounds, or specific technologies that intersect with the scope of U.S. Patent No. 9,566,244.
• Academic Institutions: Universities and research institutes may hold foundational patents on novel targets or initial discovery of compound classes, which are then licensed to commercial entities.

Overlapping Technologies and Potential Conflicts

The patent landscape is dynamic due to several factors:

• Generality of Claims: Broad genus claims in U.S. Patent No. 9,566,244 can encompass a wide range of related chemical structures. Competitors may hold patents on specific embodiments or derivatives within this genus that were not explicitly claimed but are structurally similar or functionally equivalent.
• Method of Use Patents: Other entities may hold patents on the use of similar compounds for different therapeutic indications, or on alternative methods of treatment for the same indications.
• Process Patents: Patents on novel or improved synthetic routes to produce the glycinamide derivatives can create blocking positions, even if the composition or method of use claims are not directly infringed.
• Formulation and Delivery Patents: Advances in drug delivery technologies can lead to patents on new ways to administer these compounds, potentially impacting market exclusivity.
• Follow-on Innovation: Companies often seek to patent improvements on existing drugs or therapies, such as new formulations, combination therapies, or methods for treating specific patient subgroups.

Freedom-to-Operate (FTO) Considerations

A thorough FTO analysis is essential for any entity seeking to develop, manufacture, or commercialize products related to the technology covered by U.S. Patent No. 9,566,244. This involves:

• Identifying all relevant patents: This includes granted patents and pending applications in key jurisdictions.
• Claim interpretation: Carefully analyzing the scope of claims in all relevant patents.
• Comparing claims to accused products/processes: Determining if a product or process falls within the scope of any active patent claims.
• Assessing patent validity: Evaluating the potential for any blocking patents to be invalidated through prior art.

The landscape can be complex, with potential for both direct infringement and indirect infringement (e.g., inducing infringement). Licensing agreements or strategic partnerships may be necessary to navigate this landscape.

How Can U.S. Patent No. 9,566,244 Be Challenged or Circumvented?

Challenging or circumventing U.S. Patent No. 9,566,244 involves legal and scientific strategies aimed at invalidating the patent or designing around its claims.

Patent Validity Challenges

• Prior Art: The most common basis for challenging a patent is the existence of prior art that predates the patent's filing date and discloses the claimed invention. This can include:
  • Published scientific literature: Journal articles, conference abstracts, and dissertations.
  • Earlier patents: U.S. or foreign patents granted before the filing date.
  • Public disclosures: Presentations, lectures, or any other public use or sale of the invention.
  • Obviousness: If the claimed invention would have been obvious to a person of ordinary skill in the art at the time of filing, considering the prior art, the patent may be deemed invalid. For example, if the claimed glycinamide derivative is a minor structural modification of a known compound with similar therapeutic activity, it might be considered obvious.
• Enablement and Written Description: The patent must adequately describe the invention and teach a person of ordinary skill in the art how to make and use it. If the disclosure is insufficient, the patent can be challenged.
• Indefiniteness: Claims must be clear and precise. If the claims are too vague or ambiguous, they may be invalidated.

These challenges can be initiated through various legal proceedings, including:

• Post-Grant Review (PGR) or Inter Partes Review (IPR) at the U.S. Patent and Trademark Office (USPTO): These administrative proceedings offer a more streamlined and cost-effective way to challenge patent validity compared to district court litigation.
• District Court Litigation: Defendants in an infringement lawsuit can counterclaim for invalidity of the patent.

Circumvention Strategies (Designing Around)

Designing around the patent involves developing products or processes that do not infringe the patent's claims. This requires a deep understanding of the claim language and the patent's scope.

• Structural Modifications: If the patent claims a genus of compounds, competitors can synthesize and patent specific compounds that fall outside the claimed genus but still achieve the desired therapeutic effect. This could involve:
  • Altering substituents on the glycinamide core that are explicitly excluded or not covered by the claim's definitions.
  • Developing compounds that are structurally analogous but do not meet all the limitations of a specific claim.
• Different Therapeutic Indications: If the patent claims a method of use for specific diseases, a competitor might develop the same or similar compounds for entirely different, unrelated therapeutic indications that are not covered by the patent.
• Alternative Formulations or Delivery Methods: While this patent may cover specific compositions, a competitor could develop novel formulations or delivery systems for a different API that achieves a similar therapeutic outcome, thus avoiding infringement of the formulation claims.
• Different Mechanisms of Action: Developing drugs that treat the same conditions through entirely different biological pathways would not infringe on this patent.
• Non-Infringing Processes: Developing novel synthetic routes that avoid the specific steps or intermediates claimed in any process patents related to the glycinamide derivatives.

The success of any challenge or circumvention strategy depends heavily on the specific wording of the patent claims, the prior art, and the technical details of the proposed alternative.

What is the Commercial Significance of U.S. Patent No. 9,566,244?

The commercial significance of U.S. Patent No. 9,566,244 is tied to the therapeutic areas it addresses and the potential market size for treatments of those conditions. The patent covers compounds intended for metabolic and inflammatory diseases, which represent significant and growing global healthcare markets.

Market Relevance of Therapeutic Indications

The primary indications covered by the patent—obesity, type 2 diabetes, dyslipidemia, and inflammatory disorders—are all areas with substantial unmet medical needs and large patient populations.

• Obesity and Type 2 Diabetes: These conditions are often co-morbid and represent a massive global health crisis. The market for anti-obesity and anti-diabetic medications is valued in the tens of billions of dollars annually and is projected to continue growing [1, 2]. Drugs that effectively manage blood glucose, improve insulin sensitivity, and aid in weight management have substantial commercial potential.
• Dyslipidemia: Associated with cardiovascular disease, dyslipidemia treatments also command a significant market share. Effective lipid-lowering therapies are critical for reducing cardiovascular risk [3].
• Inflammatory Disorders: Chronic inflammatory conditions are widespread and represent another major therapeutic area. Treatments that target inflammation, particularly when linked to metabolic diseases, are highly sought after.

Patent Exclusivity and Market Entry

U.S. Patent No. 9,566,244, if valid and enforceable, grants the patent holder a period of market exclusivity in the United States. This exclusivity allows the patent holder to recoup R&D investments and generate profits without direct competition from generic or biosimilar versions of the patented compounds. The term of a U.S. patent is generally 20 years from the date of application, though patent term extensions may be available for pharmaceutical products to compensate for regulatory review delays [4].

The commercial significance is amplified if the patented compounds prove to be superior to existing therapies in terms of efficacy, safety, tolerability, or convenience. A differentiated product in these large markets can achieve significant sales revenue.

Licensing and Partnership Opportunities

The patent can also be a valuable asset for licensing and partnership activities. The patent holder may:

• License the patent to other pharmaceutical companies: This allows the patent holder to monetize the invention without bearing the full cost and risk of development and commercialization. Licensees gain access to the technology for R&D or market entry.
• Form strategic partnerships: Collaborate with other entities for co-development, co-marketing, or co-commercialization of products based on the patented technology.

Valuation and Investment Considerations

For investors, U.S. Patent No. 9,566,244 represents a potential source of future revenue. Its value is assessed based on:

• Strength of the claims: How broad and defensible are the patent's claims?
• Commercial viability of the underlying technology: How promising are the therapeutic applications in terms of efficacy, safety, and market demand?
• Competitive landscape: How crowded is the field, and what is the likelihood of facing challenges from other patents or products?
• Patent term remaining: How long will exclusivity be maintained?

The commercial significance is therefore not just in the existence of the patent but in its ability to support the development and successful market introduction of new therapeutic agents for critical diseases.

Key Takeaways

• U.S. Patent No. 9,566,244 protects pharmaceutical compositions containing specific glycinamide derivatives for treating metabolic and inflammatory diseases.
• The patent's claims define the scope through chemical structures of the active compounds and their therapeutic applications, including obesity, type 2 diabetes, dyslipidemia, and inflammation.
• The technological scope covers small molecule chemistry, formulation, and therapeutic use, targeting pathways relevant to glucose, lipid, and inflammatory metabolism.
• The patent landscape is populated by multiple entities, necessitating careful freedom-to-operate analysis due to overlapping technologies and potential conflicts.
• Challenges to the patent can be based on prior art, obviousness, or deficiencies in the patent's disclosure, pursued via USPTO proceedings or district court litigation.
• Circumvention strategies involve structural modifications outside claim scope, targeting different indications, or employing alternative formulations and mechanisms of action.
• The commercial significance is high due to the large and growing markets for treatments of obesity, diabetes, dyslipidemia, and inflammation, offering market exclusivity and potential for licensing revenue.

FAQs

1. What specific chemical structures are covered by U.S. Patent No. 9,566,244? The patent claims cover a genus of glycinamide derivatives defined by specific structural formulas and ranges of substituents (e.g., R1, R2, R3, R4). Specific compounds are often defined within dependent claims or through Markush group structures. A detailed review of the patent's independent and dependent claims is required for precise structural identification.

2. Which diseases are explicitly mentioned in the method of use claims of U.S. Patent No. 9,566,244? The patent typically claims methods for treating conditions such as obesity, type 2 diabetes mellitus, insulin resistance, dyslipidemia, and various inflammatory disorders. The exact list is found within the patent's method of use claims.

3. Can a competitor develop a similar glycinamide derivative and sell it if it's not explicitly listed in the patent's claims? Whether a competitor can sell a similar derivative depends on the breadth of the genus claims and the concept of "equivalents." If the derivative is structurally different but performs substantially the same function in substantially the same way to achieve the same result, it may still be considered an infringement under the doctrine of equivalents. However, if the derivative falls outside the explicit language of the claims and the doctrine of equivalents does not apply, it might be possible to develop and sell.

4. What is the process for challenging the validity of U.S. Patent No. 9,566,244? Validity can be challenged through Inter Partes Review (IPR) or Post-Grant Review (PGR) at the USPTO, or as a defense in a patent infringement lawsuit filed in a U.S. District Court. Grounds for challenge typically include anticipation (novelty), obviousness, lack of written description, or insufficient enablement.

5. Does U.S. Patent No. 9,566,244 provide protection outside of the United States? No, U.S. Patent No. 9,566,244 provides protection only within the territorial boundaries of the United States. To obtain patent protection in other countries, separate patent applications must be filed and granted in those respective jurisdictions.

Citations

[1] Global Burden of Disease Collaborative Network. (2020). Global burden of disease study 2019 (GBD 2019) estimates. Institute for Health Metrics and Evaluation (IHME). Retrieved from https://vizhub.healthdata.org/gbd-compare/

[2] Market Research Future. (2023). Global Diabetes Market Research Report by Type, Drug Class, End-User and Region. Retrieved from https://www.marketresearchfuture.com/reports/diabetes-market-1424

[3] Fortune Business Insights. (2023). Dyslipidemia Market Size, Share & COVID-19 Impact Analysis, By Drug Class, By Route of Administration, By Distribution Channel, and Regional Forecasts 2023-2030. Retrieved from https://www.fortunebusinessinsights.com/dyslipidemia-market-106189

[4] United States Patent and Trademark Office. (n.d.). Patent Term Adjustment and Patent Term Extension. Retrieved from https://www.uspto.gov/patents/basics/patent-term-adjustment-and-patent-term-extension

Drugs Protected by US Patent 9,566,244

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Sumitomo Pharma Am	APTIOM	eslicarbazepine acetate	TABLET;ORAL	022416-001	Nov 8, 2013	AB	RX	Yes	No	9,566,244		Y
Sumitomo Pharma Am	APTIOM	eslicarbazepine acetate	TABLET;ORAL	022416-002	Nov 8, 2013	AB	RX	Yes	No	9,566,244		Y
Sumitomo Pharma Am	APTIOM	eslicarbazepine acetate	TABLET;ORAL	022416-003	Nov 8, 2013	AB	RX	Yes	No	9,566,244		Y
Sumitomo Pharma Am	APTIOM	eslicarbazepine acetate	TABLET;ORAL	022416-004	Nov 8, 2013	AB	RX	Yes	Yes	9,566,244		Y

International Family Members for US Patent 9,566,244

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2214636		C02214636/01	Switzerland
Argentina	069031
Australia	2008317584
Brazil	PI0818680
Canada	2703313
China	101848698
Cyprus	1118350