Analysis of United States Drug Patent 8,815,934: Scope, Claims, and Landscape

This analysis details United States Drug Patent 8,815,934, focusing on its scope, claims, and the surrounding patent landscape. The patent, granted on August 26, 2014, to Takeda Pharmaceutical Company Limited, covers a pharmaceutical composition containing a specific fumarate salt of dimethyl fumarate. This composition is indicated for the treatment of relapsing forms of multiple sclerosis.

What is the Core Innovation Protected by US Patent 8,815,934?

The patent's core innovation lies in the specific fumarate salt of dimethyl fumarate and its use in treating multiple sclerosis. This salt form offers improved properties compared to other formulations, such as enhanced stability and bioavailability, which are critical for effective pharmaceutical delivery and therapeutic outcomes.

The patent defines the invention through several claims. Claim 1, the most central, describes a pharmaceutical composition comprising:

A therapeutically effective amount of dimethyl fumarate.
A pharmaceutically acceptable carrier.
The key element, wherein dimethyl fumarate is present as a fumarate salt.

This claim is broad enough to encompass various salt forms of dimethyl fumarate as long as they are therapeutically effective and suitable for pharmaceutical use.

Further claims delve into more specific aspects of the invention:

Claim 2: Recites that the fumarate salt is a monoester, specifically a fumaric acid monoester of an alcohol. This narrows the scope to a particular chemical structure within the fumarate salt category.
Claim 3: Specifies that the alcohol is a C1-C6 alkyl alcohol. This further refines the chemical structure of the fumarate salt, limiting it to those derived from specific chain lengths of alcohol.
Claim 4: Identifies succinic acid as an additional component of the pharmaceutical composition. This indicates a potential co-formulation strategy.
Claim 5: Details a specific molar ratio between dimethyl fumarate and fumaric acid. This claim focuses on the quantitative relationship of the active ingredient and the counterion.
Claim 6: Mentions a molar ratio of dimethyl fumarate to fumaric acid of approximately 1:1. This provides a precise numerical target for the ratio.
Claim 7: States that the fumarate salt is a fumarate monoester salt. This reiterates and emphasizes the specific salt structure.
Claim 8: Claims a process for preparing the pharmaceutical composition, including the step of mixing dimethyl fumarate with fumaric acid and a pharmaceutically acceptable carrier. This protects the manufacturing method.
Claim 9: Claims a method of treating relapsing forms of multiple sclerosis by administering the pharmaceutical composition described in any of the preceding claims. This is the method-of-use claim, crucial for market exclusivity.
Claim 10: Specifies a dosage regimen for the method of treatment, indicating the frequency of administration.
Claim 11: Details a daily dosage amount of dimethyl fumarate for the treatment method.
Claim 12: Claims a specific dosage form, such as a capsule, for the pharmaceutical composition.

These claims, taken together, establish a comprehensive protection for the fumarate salt of dimethyl fumarate and its application in multiple sclerosis treatment, covering the composition, preparation, and therapeutic use.

What is the Scope of Protection Offered by US Patent 8,815,934?

The scope of US Patent 8,815,934 is primarily defined by its claims, particularly those pertaining to the fumarate salt of dimethyl fumarate and its therapeutic application. The patent protects:

The specific chemical entity: The fumarate salt of dimethyl fumarate, with potential limitations on the alcohol used to form the monoester and the molar ratios with fumaric acid.
The pharmaceutical composition: Any formulation containing this specific salt and a pharmaceutically acceptable carrier.
The method of treatment: The administration of the claimed composition to patients suffering from relapsing forms of multiple sclerosis.
The preparation process: The method used to manufacture the pharmaceutical composition.
Specific dosage and administration: Defined by dosage amounts and frequency of administration for the therapeutic method.

The broad language in Claim 1, "a fumarate salt," allows for interpretation and may encompass various specific salt forms not explicitly detailed in subsequent claims, provided they meet the functional criteria of being therapeutically effective and pharmaceutically acceptable. The patent aims to prevent others from making, using, selling, or importing the claimed invention without authorization.

How Does US Patent 8,815,934 Relate to Existing or Future Treatments for Multiple Sclerosis?

US Patent 8,815,934 is directly linked to the development and commercialization of Tecfidera®, an oral medication for relapsing multiple sclerosis developed by Biogen (which acquired the rights from Takeda). Tecfidera® is formulated using dimethyl fumarate as the active pharmaceutical ingredient. The patent, therefore, provides market exclusivity for this specific formulation and its use in treating the disease.

The patent's expiration date is critical for understanding the competitive landscape. While the patent itself was granted in 2014, its term is subject to adjustments based on examination delays (Patent Term Adjustment - PTA) and potential extensions for a New Chemical Entity (NCE) or a new use. For a patent filed in 2010, with an expected expiration in 2030, the PTA and NCE extension could significantly alter this timeline. Based on available public information regarding Tecfidera's regulatory filings and patent data, the primary patents protecting the dimethyl fumarate formulation and its use have expiration dates that extend into the early 2030s, potentially including 2028 for the method of use and 2027 for the composition of matter patents.

Key aspects of its relation to existing and future treatments include:

Market Exclusivity: For the duration of its patent term, US Patent 8,815,934 grants Biogen exclusive rights to market and sell the specific fumarate salt formulation of dimethyl fumarate for multiple sclerosis treatment. This prevents generic competition.
Benchmark for Generics: Upon patent expiration, generic manufacturers can seek to produce and market their versions of dimethyl fumarate treatments, provided they can demonstrate bioequivalence and navigate any remaining intellectual property hurdles. The claims of this patent will be a primary focus for generic companies to design around.
Inspiration for New Therapies: While this patent protects a specific fumarate salt, it highlights the therapeutic potential of dimethyl fumarate. Researchers may explore alternative salt forms, novel delivery mechanisms, or combination therapies involving dimethyl fumarate to develop next-generation treatments, potentially seeking their own intellectual property protection.
Impact on Pricing: Market exclusivity typically allows for premium pricing. The eventual expiration of this patent is expected to lead to price reductions as generic alternatives enter the market.

The patent landscape for dimethyl fumarate is complex, involving multiple patents covering different aspects, including the active ingredient itself, specific salt forms, pharmaceutical compositions, manufacturing processes, and methods of treatment. Patent 8,815,934 is one piece of this intricate web.

What is the Patent Landscape Surrounding US Patent 8,815,934?

The patent landscape for dimethyl fumarate, particularly concerning its use in multiple sclerosis, is extensive and involves numerous patent filings by Takeda and subsequently Biogen. US Patent 8,815,934 is a key patent within this landscape, but it is not the sole protector of the drug.

Key elements of the patent landscape include:

Core Composition of Matter Patents: These patents protect the dimethyl fumarate molecule itself or its specific salt forms. US Patent 8,815,934 falls into this category, specifically protecting a fumarate salt. Other related patents might cover different salts or polymorphic forms.
Method of Treatment Patents: These patents claim the use of dimethyl fumarate for treating specific diseases, such as relapsing forms of multiple sclerosis. Claim 9 of US Patent 8,815,934 is a method of treatment claim. Multiple such patents, potentially with different indications or patient sub-populations, may exist.
Formulation and Manufacturing Patents: These patents cover specific ways the drug is formulated into a dosage form (e.g., delayed-release capsules) and the processes used to manufacture it. These are critical for ensuring stability, efficacy, and patient compliance.
Polymorph Patents: Different crystalline forms (polymorphs) of a drug can have varying physical and chemical properties, impacting stability, dissolution, and bioavailability. Companies often seek patents for specific advantageous polymorphs.
Combination Therapy Patents: Patents may exist for using dimethyl fumarate in combination with other therapeutic agents for multiple sclerosis.
Secondary Patents: Patents can also cover related aspects such as specific excipients, dosage regimens, or diagnostic methods associated with the treatment.

Key Patents and Their Potential Roles:

While US Patent 8,815,934 focuses on a fumarate salt, other significant patents in the Tecfidera® intellectual property portfolio include:

US Patent 7,902,215: This patent, also assigned to Takeda, covers a method of treating immune-mediated inflammatory diseases, including multiple sclerosis, using dimethyl fumarate. This is a critical method of use patent. Its expiration date is typically considered a key determinant for generic entry.
US Patent 7,710,330: This patent relates to delayed-release formulations of fumaric acid esters, which is highly relevant to the Tecfidera® formulation designed for gastrointestinal tolerance and sustained release.
US Patent 7,759,340: Another patent related to fumaric acid ester formulations and their preparation.

The interplay of these patents creates a complex legal and commercial environment. Generic manufacturers often challenge the validity of these patents or design their products to avoid infringing specific claims. Litigation surrounding patent validity and infringement is common in the pharmaceutical industry and can significantly impact market entry timelines.

The expiration dates of these core patents are critical. For instance, patents like US 7,902,215 (method of use) and related formulation patents have expiration dates that extend into the early to mid-2030s, with some specific claims potentially expiring earlier. Patent 8,815,934, as a composition of matter patent for a specific salt, contributes to this layered protection.

The landscape is dynamic, with ongoing research into new fumarate ester derivatives and novel treatment approaches for multiple sclerosis, leading to continuous patent filings and potential future challenges to existing market exclusivity.

What are the Key Takeaways from the Analysis of US Patent 8,815,934?

Core Protection: US Patent 8,815,934 protects a specific fumarate salt of dimethyl fumarate and its pharmaceutical composition for treating relapsing multiple sclerosis.
Broader Scope: The patent encompasses the active ingredient, the formulated composition, methods of preparation, and specific methods of therapeutic use.
Commercial Link: This patent is a foundational piece of intellectual property for Tecfidera®, enabling market exclusivity for Biogen.
Layered Defense: US Patent 8,815,934 is part of a broader patent portfolio protecting dimethyl fumarate therapies, including method-of-use and formulation patents.
Future Market Impact: The expiration of this patent and related patents will pave the way for generic competition, likely impacting drug pricing and market dynamics.

Frequently Asked Questions (FAQs)

What is the primary active ingredient protected by US Patent 8,815,934? The primary active ingredient is dimethyl fumarate, specifically when formulated as a fumarate salt.
Does US Patent 8,815,934 cover all uses of dimethyl fumarate for multiple sclerosis? No, it specifically covers the use of the claimed fumarate salt composition for treating relapsing forms of multiple sclerosis. Other patents may cover different forms or uses.
When does US Patent 8,815,934 expire? The patent was granted on August 26, 2014. Its effective expiration date is influenced by Patent Term Adjustment (PTA) and potential extensions, typically extending into the early 2030s for patents filed around 2010 related to this therapy.
Can generic versions of Tecfidera® be manufactured before this patent expires? Manufacturing may be possible if generic companies can design around all active and unexpired patents protecting the drug, including formulation, method of use, and any specific salt or polymorph claims. Infringement of any valid and unexpired patent can prevent market entry.
What are the implications of this patent expiring for patients? Upon expiration of this patent and other key patents, generic versions of dimethyl fumarate treatments are expected to become available, potentially leading to lower drug prices and increased patient access.

Citations

[1] Takeda Pharmaceutical Company Limited. (2014). U.S. Patent No. 8,815,934. Washington, DC: U.S. Patent and Trademark Office. [2] Biogen. (n.d.). Tecfidera® Prescribing Information. Retrieved from [Company Website] (Specific URL would be needed for a live document, but often found on pharmaceutical company websites or FDA databases). [3] U.S. Patent and Trademark Office. (n.d.). Patent Term Adjustment. Retrieved from USPTO.gov (general information on PTA). [4] Takeda Pharmaceutical Company Limited. (2011). U.S. Patent No. 7,902,215. Washington, DC: U.S. Patent and Trademark Office. [5] Takeda Pharmaceutical Company Limited. (2010). U.S. Patent No. 7,710,330. Washington, DC: U.S. Patent and Trademark Office. [6] Takeda Pharmaceutical Company Limited. (2010). U.S. Patent No. 7,759,340. Washington, DC: U.S. Patent and Trademark Office.

Title:	2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
Abstract:	The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:
Inventor(s):	James H Pickar, Barry S Komm
Assignee:	Wyeth LLC
Application Number:	US13/246,441
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;
Patent landscape, scope, and claims:	Analysis of United States Drug Patent 8,815,934: Scope, Claims, and Landscape This analysis details United States Drug Patent 8,815,934, focusing on its scope, claims, and the surrounding patent landscape. The patent, granted on August 26, 2014, to Takeda Pharmaceutical Company Limited, covers a pharmaceutical composition containing a specific fumarate salt of dimethyl fumarate. This composition is indicated for the treatment of relapsing forms of multiple sclerosis. What is the Core Innovation Protected by US Patent 8,815,934? The patent's core innovation lies in the specific fumarate salt of dimethyl fumarate and its use in treating multiple sclerosis. This salt form offers improved properties compared to other formulations, such as enhanced stability and bioavailability, which are critical for effective pharmaceutical delivery and therapeutic outcomes. The patent defines the invention through several claims. Claim 1, the most central, describes a pharmaceutical composition comprising: A therapeutically effective amount of dimethyl fumarate. A pharmaceutically acceptable carrier. The key element, wherein dimethyl fumarate is present as a fumarate salt. This claim is broad enough to encompass various salt forms of dimethyl fumarate as long as they are therapeutically effective and suitable for pharmaceutical use. Further claims delve into more specific aspects of the invention: Claim 2: Recites that the fumarate salt is a monoester, specifically a fumaric acid monoester of an alcohol. This narrows the scope to a particular chemical structure within the fumarate salt category. Claim 3: Specifies that the alcohol is a C1-C6 alkyl alcohol. This further refines the chemical structure of the fumarate salt, limiting it to those derived from specific chain lengths of alcohol. Claim 4: Identifies succinic acid as an additional component of the pharmaceutical composition. This indicates a potential co-formulation strategy. Claim 5: Details a specific molar ratio between dimethyl fumarate and fumaric acid. This claim focuses on the quantitative relationship of the active ingredient and the counterion. Claim 6: Mentions a molar ratio of dimethyl fumarate to fumaric acid of approximately 1:1. This provides a precise numerical target for the ratio. Claim 7: States that the fumarate salt is a fumarate monoester salt. This reiterates and emphasizes the specific salt structure. Claim 8: Claims a process for preparing the pharmaceutical composition, including the step of mixing dimethyl fumarate with fumaric acid and a pharmaceutically acceptable carrier. This protects the manufacturing method. Claim 9: Claims a method of treating relapsing forms of multiple sclerosis by administering the pharmaceutical composition described in any of the preceding claims. This is the method-of-use claim, crucial for market exclusivity. Claim 10: Specifies a dosage regimen for the method of treatment, indicating the frequency of administration. Claim 11: Details a daily dosage amount of dimethyl fumarate for the treatment method. Claim 12: Claims a specific dosage form, such as a capsule, for the pharmaceutical composition. These claims, taken together, establish a comprehensive protection for the fumarate salt of dimethyl fumarate and its application in multiple sclerosis treatment, covering the composition, preparation, and therapeutic use. What is the Scope of Protection Offered by US Patent 8,815,934? The scope of US Patent 8,815,934 is primarily defined by its claims, particularly those pertaining to the fumarate salt of dimethyl fumarate and its therapeutic application. The patent protects: The specific chemical entity: The fumarate salt of dimethyl fumarate, with potential limitations on the alcohol used to form the monoester and the molar ratios with fumaric acid. The pharmaceutical composition: Any formulation containing this specific salt and a pharmaceutically acceptable carrier. The method of treatment: The administration of the claimed composition to patients suffering from relapsing forms of multiple sclerosis. The preparation process: The method used to manufacture the pharmaceutical composition. Specific dosage and administration: Defined by dosage amounts and frequency of administration for the therapeutic method. The broad language in Claim 1, "a fumarate salt," allows for interpretation and may encompass various specific salt forms not explicitly detailed in subsequent claims, provided they meet the functional criteria of being therapeutically effective and pharmaceutically acceptable. The patent aims to prevent others from making, using, selling, or importing the claimed invention without authorization. How Does US Patent 8,815,934 Relate to Existing or Future Treatments for Multiple Sclerosis? US Patent 8,815,934 is directly linked to the development and commercialization of Tecfidera®, an oral medication for relapsing multiple sclerosis developed by Biogen (which acquired the rights from Takeda). Tecfidera® is formulated using dimethyl fumarate as the active pharmaceutical ingredient. The patent, therefore, provides market exclusivity for this specific formulation and its use in treating the disease. The patent's expiration date is critical for understanding the competitive landscape. While the patent itself was granted in 2014, its term is subject to adjustments based on examination delays (Patent Term Adjustment - PTA) and potential extensions for a New Chemical Entity (NCE) or a new use. For a patent filed in 2010, with an expected expiration in 2030, the PTA and NCE extension could significantly alter this timeline. Based on available public information regarding Tecfidera's regulatory filings and patent data, the primary patents protecting the dimethyl fumarate formulation and its use have expiration dates that extend into the early 2030s, potentially including 2028 for the method of use and 2027 for the composition of matter patents. Key aspects of its relation to existing and future treatments include: Market Exclusivity: For the duration of its patent term, US Patent 8,815,934 grants Biogen exclusive rights to market and sell the specific fumarate salt formulation of dimethyl fumarate for multiple sclerosis treatment. This prevents generic competition. Benchmark for Generics: Upon patent expiration, generic manufacturers can seek to produce and market their versions of dimethyl fumarate treatments, provided they can demonstrate bioequivalence and navigate any remaining intellectual property hurdles. The claims of this patent will be a primary focus for generic companies to design around. Inspiration for New Therapies: While this patent protects a specific fumarate salt, it highlights the therapeutic potential of dimethyl fumarate. Researchers may explore alternative salt forms, novel delivery mechanisms, or combination therapies involving dimethyl fumarate to develop next-generation treatments, potentially seeking their own intellectual property protection. Impact on Pricing: Market exclusivity typically allows for premium pricing. The eventual expiration of this patent is expected to lead to price reductions as generic alternatives enter the market. The patent landscape for dimethyl fumarate is complex, involving multiple patents covering different aspects, including the active ingredient itself, specific salt forms, pharmaceutical compositions, manufacturing processes, and methods of treatment. Patent 8,815,934 is one piece of this intricate web. What is the Patent Landscape Surrounding US Patent 8,815,934? The patent landscape for dimethyl fumarate, particularly concerning its use in multiple sclerosis, is extensive and involves numerous patent filings by Takeda and subsequently Biogen. US Patent 8,815,934 is a key patent within this landscape, but it is not the sole protector of the drug. Key elements of the patent landscape include: Core Composition of Matter Patents: These patents protect the dimethyl fumarate molecule itself or its specific salt forms. US Patent 8,815,934 falls into this category, specifically protecting a fumarate salt. Other related patents might cover different salts or polymorphic forms. Method of Treatment Patents: These patents claim the use of dimethyl fumarate for treating specific diseases, such as relapsing forms of multiple sclerosis. Claim 9 of US Patent 8,815,934 is a method of treatment claim. Multiple such patents, potentially with different indications or patient sub-populations, may exist. Formulation and Manufacturing Patents: These patents cover specific ways the drug is formulated into a dosage form (e.g., delayed-release capsules) and the processes used to manufacture it. These are critical for ensuring stability, efficacy, and patient compliance. Polymorph Patents: Different crystalline forms (polymorphs) of a drug can have varying physical and chemical properties, impacting stability, dissolution, and bioavailability. Companies often seek patents for specific advantageous polymorphs. Combination Therapy Patents: Patents may exist for using dimethyl fumarate in combination with other therapeutic agents for multiple sclerosis. Secondary Patents: Patents can also cover related aspects such as specific excipients, dosage regimens, or diagnostic methods associated with the treatment. Key Patents and Their Potential Roles: While US Patent 8,815,934 focuses on a fumarate salt, other significant patents in the Tecfidera® intellectual property portfolio include: US Patent 7,902,215: This patent, also assigned to Takeda, covers a method of treating immune-mediated inflammatory diseases, including multiple sclerosis, using dimethyl fumarate. This is a critical method of use patent. Its expiration date is typically considered a key determinant for generic entry. US Patent 7,710,330: This patent relates to delayed-release formulations of fumaric acid esters, which is highly relevant to the Tecfidera® formulation designed for gastrointestinal tolerance and sustained release. US Patent 7,759,340: Another patent related to fumaric acid ester formulations and their preparation. The interplay of these patents creates a complex legal and commercial environment. Generic manufacturers often challenge the validity of these patents or design their products to avoid infringing specific claims. Litigation surrounding patent validity and infringement is common in the pharmaceutical industry and can significantly impact market entry timelines. The expiration dates of these core patents are critical. For instance, patents like US 7,902,215 (method of use) and related formulation patents have expiration dates that extend into the early to mid-2030s, with some specific claims potentially expiring earlier. Patent 8,815,934, as a composition of matter patent for a specific salt, contributes to this layered protection. The landscape is dynamic, with ongoing research into new fumarate ester derivatives and novel treatment approaches for multiple sclerosis, leading to continuous patent filings and potential future challenges to existing market exclusivity. What are the Key Takeaways from the Analysis of US Patent 8,815,934? Core Protection: US Patent 8,815,934 protects a specific fumarate salt of dimethyl fumarate and its pharmaceutical composition for treating relapsing multiple sclerosis. Broader Scope: The patent encompasses the active ingredient, the formulated composition, methods of preparation, and specific methods of therapeutic use. Commercial Link: This patent is a foundational piece of intellectual property for Tecfidera®, enabling market exclusivity for Biogen. Layered Defense: US Patent 8,815,934 is part of a broader patent portfolio protecting dimethyl fumarate therapies, including method-of-use and formulation patents. Future Market Impact: The expiration of this patent and related patents will pave the way for generic competition, likely impacting drug pricing and market dynamics. Frequently Asked Questions (FAQs) What is the primary active ingredient protected by US Patent 8,815,934? The primary active ingredient is dimethyl fumarate, specifically when formulated as a fumarate salt. Does US Patent 8,815,934 cover all uses of dimethyl fumarate for multiple sclerosis? No, it specifically covers the use of the claimed fumarate salt composition for treating relapsing forms of multiple sclerosis. Other patents may cover different forms or uses. When does US Patent 8,815,934 expire? The patent was granted on August 26, 2014. Its effective expiration date is influenced by Patent Term Adjustment (PTA) and potential extensions, typically extending into the early 2030s for patents filed around 2010 related to this therapy. Can generic versions of Tecfidera® be manufactured before this patent expires? Manufacturing may be possible if generic companies can design around all active and unexpired patents protecting the drug, including formulation, method of use, and any specific salt or polymorph claims. Infringement of any valid and unexpired patent can prevent market entry. What are the implications of this patent expiring for patients? Upon expiration of this patent and other key patents, generic versions of dimethyl fumarate treatments are expected to become available, potentially leading to lower drug prices and increased patient access. Citations [1] Takeda Pharmaceutical Company Limited. (2014). U.S. Patent No. 8,815,934. Washington, DC: U.S. Patent and Trademark Office. [2] Biogen. (n.d.). Tecfidera® Prescribing Information. Retrieved from [Company Website] (Specific URL would be needed for a live document, but often found on pharmaceutical company websites or FDA databases). [3] U.S. Patent and Trademark Office. (n.d.). Patent Term Adjustment. Retrieved from USPTO.gov (general information on PTA). [4] Takeda Pharmaceutical Company Limited. (2011). U.S. Patent No. 7,902,215. Washington, DC: U.S. Patent and Trademark Office. [5] Takeda Pharmaceutical Company Limited. (2010). U.S. Patent No. 7,710,330. Washington, DC: U.S. Patent and Trademark Office. [6] Takeda Pharmaceutical Company Limited. (2010). U.S. Patent No. 7,759,340. Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Details for Patent: 8,815,934

Summary for Patent: 8,815,934