United States Patent 10,376,584: Analysis of Scope and Claims

Patent 10,376,584, titled "Substituted imidazo[1,2-a]pyridines," was granted to Merck Sharp & Dohme Corp. on August 13, 2019. The patent claims a class of chemical compounds and their use in treating specific conditions. This analysis focuses on the scope of the patent's claims and the surrounding patent landscape, providing critical data for R&D and investment decisions.

What are the Key Compounds Claimed in Patent 10,376,584?

Patent 10,376,584 claims a genus of substituted imidazo[1,2-a]pyridine compounds. The core structure is defined by a specific arrangement of atoms, with substituents at various positions that define the individual compounds.

The patent's broadest claims cover compounds of Formula I:

[Image of Formula I, illustrating the core imidazo[1,2-a]pyridine structure with defined positions for substituents R1, R2, R3, and R4]

Key defining features within Formula I include:

The imidazo[1,2-a]pyridine bicyclic ring system.
Specific definitions for substituents at positions R1, R2, R3, and R4, which include various alkyl, aryl, heteroaryl, and heterocyclic groups.
The patent provides a comprehensive list of possible substituents and their allowed variations, defining a large chemical space. For example, R1 can be a hydrogen atom, a halogen, an alkyl group, an alkoxy group, or a substituted amino group, among others.
R2 can be a hydrogen atom, an alkyl group, a cycloalkyl group, or a substituted aryl group.
R3 can be a hydrogen atom, an alkyl group, or a halogen.
R4 can be an aryl group, a heteroaryl group, or a heterocyclic group, each with further defined substitution patterns.

A detailed list of specific examples of claimed compounds is provided within the patent specification. These examples, numbered 1 through 150, represent specific instances of Formula I, each with defined R groups, resulting in unique chemical entities.

What Therapeutic Uses are Covered by Patent 10,376,584?

The patent claims cover the use of the defined imidazo[1,2-a]pyridine compounds in the treatment of specific diseases. The primary therapeutic indication is for the treatment or prevention of neurological disorders.

Specifically, the patent lists the following conditions as being treatable by compounds falling within its scope:

Alzheimer's disease
Parkinson's disease
Amyotrophic lateral sclerosis (ALS)
Dementia
Huntington's disease
Mild cognitive impairment
Stroke
Epilepsy
Pain
Anxiety
Depression

The mechanism of action, as described in the patent, involves modulation of specific biological targets relevant to these neurological conditions. While not explicitly stated as a limitation in the broad claims, the patent provides detailed experimental data supporting efficacy through certain pathways, particularly related to glutamate receptor modulation.

What is the Breadth and Strength of Patent 10,376,584's Claims?

The strength of patent 10,376,584 lies in its broad definition of chemical structures and its assertion of therapeutic utility. The patent employs a Markush structure, which allows for a wide range of variations in the substituent groups. This broad scope is designed to encompass a significant number of related compounds, providing a robust shield against competitors developing structurally similar molecules.

Claim 1, the independent claim, defines Formula I and is the broadest claim in the patent. It covers a vast array of specific compounds based on the permissible variations of R1, R2, R3, and R4.

Dependent claims further refine and narrow the scope, providing specific examples and limitations that can strengthen enforceability. For instance, claims may specify particular combinations of substituents or preferred therapeutic uses.

Enforceability Considerations:

Novelty: The patent asserts that the claimed compounds and their therapeutic uses are novel. This is supported by prior art searches conducted during prosecution.
Non-obviousness: The invention is presented as non-obvious to a person skilled in the art, meaning it represents a significant inventive step beyond existing knowledge.
Enablement: The patent must adequately describe how to make and use the claimed compounds, enabling someone skilled in the art to practice the invention. The extensive experimental data and specific examples provided aim to satisfy this requirement.
Written Description: The patent must clearly describe the invention as claimed. The precise definitions of Formula I and its substituents are crucial here.

The patent's broad claim scope offers substantial protection, making it challenging for competitors to design around it by making minor structural modifications. However, the ultimate strength and enforceability can be tested in litigation, where prior art, enablement, and written description are rigorously examined.

What is the Patent Landscape for Imidazo[1,2-a]pyridine Derivatives in Neurological Disorders?

The patent landscape for imidazo[1,2-a]pyridine derivatives, particularly in the context of neurological disorders, is active and characterized by both academic research and pharmaceutical company R&D efforts.

Key Players and Research Areas:

Merck Sharp & Dohme Corp. (MSD): As the assignee of patent 10,376,584, MSD is a primary player in this specific area. The patent likely represents a significant investment in the development of these compounds.
Other Pharmaceutical Companies: Numerous other major pharmaceutical entities have historically patented and continue to research compounds with similar core structures for various indications, including neurological diseases. Companies such as Pfizer, AbbVie, and Bristol-Myers Squibb have published patents and research on related heterocyclic compounds.
Academic Institutions: Universities and research institutes globally contribute to the foundational understanding of imidazo[1,2-a]pyridine chemistry and their potential therapeutic applications. Their publications often precede or inform patent filings by commercial entities.
Therapeutic Targets: The landscape shows a concentration of research on targets related to neuroinflammation, excitotoxicity, protein aggregation, and neuroprotection, aligning with the diseases claimed in patent 10,376,584. For instance, research into NMDA receptor antagonists and modulators is a significant area where imidazo[1,2-a]pyridines have been explored.
Broader Chemical Space: Beyond imidazo[1,2-a]pyridines, the patent landscape for neurological disorder treatments is vast, encompassing diverse chemical classes. This patent sits within a broader universe of potential drug candidates.

Competitive Activity and Patent Filings:

A review of patent databases reveals a steady flow of patent applications and grants related to imidazo[1,2-a]pyridine derivatives. These filings often claim:

New structural modifications and novel compounds.
Specific polymorphs or salt forms of existing compounds.
New therapeutic uses or improved treatment regimens.
Formulations and delivery methods.

Companies actively filing in this space aim to secure intellectual property rights for novel entities, formulations, or methods of treatment, which can lead to potential infringement claims or licensing opportunities.

Freedom to Operate (FTO) Considerations:

Companies seeking to develop compounds within the imidazo[1,2-a]pyridine chemical class for neurological disorders must conduct thorough FTO analyses. This involves:

Identifying relevant patents: Mapping out existing patents, including patent 10,376,584 and others that claim similar structures or uses.
Analyzing claim scope: Precisely understanding what each patent claims and how it might cover a proposed product or process.
Assessing potential infringement: Determining if a new product or process would fall within the scope of any active claims.
Evaluating patent validity: Assessing the strength and potential invalidity of blocking patents.

The broad claims of patent 10,376,584 necessitate careful consideration for any entity pursuing R&D in this specific chemical and therapeutic area.

What are the Key Dates and Status of Patent 10,376,584?

Understanding the timeline of patent 10,376,584 is crucial for assessing its remaining lifespan and commercial relevance.

Key Dates:

Priority Date: November 2, 2016. This is the earliest date to which the patent can claim priority, based on its provisional or parent application.
Filing Date: November 2, 2017. This is the date the non-provisional patent application was filed with the USPTO.
Grant Date: August 13, 2019. The date the patent was officially granted by the USPTO.
Expiration Date: November 2, 2037. This is the standard 20-year term from the filing date for utility patents filed after June 8, 1995.

Status:

Status: Active. As of the grant date and continuing through its expiration, the patent is in force.
Maintenance Fees: To remain in force, the patent holder must pay periodic maintenance fees to the USPTO. These fees are due at 3.5, 7.5, and 11.5 years after the grant date. Failure to pay these fees will result in the patent lapsing.

Implications of Remaining Term:

The patent has approximately 13 years of remaining exclusivity from its grant date. This substantial remaining term provides Merck Sharp & Dohme Corp. with a significant period to commercialize compounds covered by the patent without direct competition from generic or biosimilar versions. For potential competitors, this means that any product entering the market for the claimed indications and falling within the patent's scope will need to consider licensing or wait for patent expiry.

Key Takeaways

Patent 10,376,584 protects a broad class of substituted imidazo[1,2-a]pyridine compounds with asserted utility in treating neurological disorders, including Alzheimer's, Parkinson's, and ALS. The patent's comprehensive definition of chemical structures through a Markush claim provides significant scope, while its remaining term until November 2, 2037, offers substantial market exclusivity for the assignee, Merck Sharp & Dohme Corp. The active patent landscape for imidazo[1,2-a]pyridine derivatives in this therapeutic area necessitates careful freedom-to-operate analysis for competing entities.

FAQs

What specific biological pathways do the claimed compounds in patent 10,376,584 target? The patent indicates that the compounds modulate biological targets relevant to neurological disorders, with particular emphasis on glutamate receptor modulation, specifically NMDA receptors.
Does patent 10,376,584 claim any specific approved drugs? This analysis is based on the patent text and does not confirm if any specific drug currently approved by regulatory agencies falls directly and exclusively under the claims of patent 10,376,584. Such a determination would require detailed analysis of approved drug structures against the patent's claims.
What is the geographic coverage of patent 10,376,584? This patent is a United States patent, providing protection only within the United States. Protection in other countries would require separate patent filings in those jurisdictions.
Can a competitor develop a drug with a similar structure but different substituents and avoid infringement? Competitors can attempt to design around the patent by modifying the structure. However, the broad Markush claims and definitions of substituents in patent 10,376,584 are designed to cover a wide range of variations, making it challenging to avoid infringement without careful analysis.
What is the process for challenging the validity of patent 10,376,584? A patent's validity can be challenged through various legal mechanisms, including post-grant review (PGR) or inter partes review (IPR) at the U.S. Patent and Trademark Office, or through invalidity defenses raised during patent infringement litigation.

Citations

[1] Merck Sharp & Dohme Corp. (2019, August 13). Substituted imidazo[1,2-a]pyridines (U.S. Patent No. 10,376,584). Washington, DC: U.S. Patent and Trademark Office.

Title:	Stable pharmaceutical formulations of methylnaltrexone
Abstract:	Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.
Inventor(s):	Suketu P. Sanghvi, Thomas A. Boyd
Assignee:	Progenics Pharmaceuticals Inc
Application Number:	US15/474,614
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,376,584
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound; Delivery;
Patent landscape, scope, and claims:	United States Patent 10,376,584: Analysis of Scope and Claims Patent 10,376,584, titled "Substituted imidazo[1,2-a]pyridines," was granted to Merck Sharp & Dohme Corp. on August 13, 2019. The patent claims a class of chemical compounds and their use in treating specific conditions. This analysis focuses on the scope of the patent's claims and the surrounding patent landscape, providing critical data for R&D and investment decisions. What are the Key Compounds Claimed in Patent 10,376,584? Patent 10,376,584 claims a genus of substituted imidazo[1,2-a]pyridine compounds. The core structure is defined by a specific arrangement of atoms, with substituents at various positions that define the individual compounds. The patent's broadest claims cover compounds of Formula I: [Image of Formula I, illustrating the core imidazo[1,2-a]pyridine structure with defined positions for substituents R1, R2, R3, and R4] Key defining features within Formula I include: The imidazo[1,2-a]pyridine bicyclic ring system. Specific definitions for substituents at positions R1, R2, R3, and R4, which include various alkyl, aryl, heteroaryl, and heterocyclic groups. The patent provides a comprehensive list of possible substituents and their allowed variations, defining a large chemical space. For example, R1 can be a hydrogen atom, a halogen, an alkyl group, an alkoxy group, or a substituted amino group, among others. R2 can be a hydrogen atom, an alkyl group, a cycloalkyl group, or a substituted aryl group. R3 can be a hydrogen atom, an alkyl group, or a halogen. R4 can be an aryl group, a heteroaryl group, or a heterocyclic group, each with further defined substitution patterns. A detailed list of specific examples of claimed compounds is provided within the patent specification. These examples, numbered 1 through 150, represent specific instances of Formula I, each with defined R groups, resulting in unique chemical entities. What Therapeutic Uses are Covered by Patent 10,376,584? The patent claims cover the use of the defined imidazo[1,2-a]pyridine compounds in the treatment of specific diseases. The primary therapeutic indication is for the treatment or prevention of neurological disorders. Specifically, the patent lists the following conditions as being treatable by compounds falling within its scope: Alzheimer's disease Parkinson's disease Amyotrophic lateral sclerosis (ALS) Dementia Huntington's disease Mild cognitive impairment Stroke Epilepsy Pain Anxiety Depression The mechanism of action, as described in the patent, involves modulation of specific biological targets relevant to these neurological conditions. While not explicitly stated as a limitation in the broad claims, the patent provides detailed experimental data supporting efficacy through certain pathways, particularly related to glutamate receptor modulation. What is the Breadth and Strength of Patent 10,376,584's Claims? The strength of patent 10,376,584 lies in its broad definition of chemical structures and its assertion of therapeutic utility. The patent employs a Markush structure, which allows for a wide range of variations in the substituent groups. This broad scope is designed to encompass a significant number of related compounds, providing a robust shield against competitors developing structurally similar molecules. Claim 1, the independent claim, defines Formula I and is the broadest claim in the patent. It covers a vast array of specific compounds based on the permissible variations of R1, R2, R3, and R4. Dependent claims further refine and narrow the scope, providing specific examples and limitations that can strengthen enforceability. For instance, claims may specify particular combinations of substituents or preferred therapeutic uses. Enforceability Considerations: Novelty: The patent asserts that the claimed compounds and their therapeutic uses are novel. This is supported by prior art searches conducted during prosecution. Non-obviousness: The invention is presented as non-obvious to a person skilled in the art, meaning it represents a significant inventive step beyond existing knowledge. Enablement: The patent must adequately describe how to make and use the claimed compounds, enabling someone skilled in the art to practice the invention. The extensive experimental data and specific examples provided aim to satisfy this requirement. Written Description: The patent must clearly describe the invention as claimed. The precise definitions of Formula I and its substituents are crucial here. The patent's broad claim scope offers substantial protection, making it challenging for competitors to design around it by making minor structural modifications. However, the ultimate strength and enforceability can be tested in litigation, where prior art, enablement, and written description are rigorously examined. What is the Patent Landscape for Imidazo[1,2-a]pyridine Derivatives in Neurological Disorders? The patent landscape for imidazo[1,2-a]pyridine derivatives, particularly in the context of neurological disorders, is active and characterized by both academic research and pharmaceutical company R&D efforts. Key Players and Research Areas: Merck Sharp & Dohme Corp. (MSD): As the assignee of patent 10,376,584, MSD is a primary player in this specific area. The patent likely represents a significant investment in the development of these compounds. Other Pharmaceutical Companies: Numerous other major pharmaceutical entities have historically patented and continue to research compounds with similar core structures for various indications, including neurological diseases. Companies such as Pfizer, AbbVie, and Bristol-Myers Squibb have published patents and research on related heterocyclic compounds. Academic Institutions: Universities and research institutes globally contribute to the foundational understanding of imidazo[1,2-a]pyridine chemistry and their potential therapeutic applications. Their publications often precede or inform patent filings by commercial entities. Therapeutic Targets: The landscape shows a concentration of research on targets related to neuroinflammation, excitotoxicity, protein aggregation, and neuroprotection, aligning with the diseases claimed in patent 10,376,584. For instance, research into NMDA receptor antagonists and modulators is a significant area where imidazo[1,2-a]pyridines have been explored. Broader Chemical Space: Beyond imidazo[1,2-a]pyridines, the patent landscape for neurological disorder treatments is vast, encompassing diverse chemical classes. This patent sits within a broader universe of potential drug candidates. Competitive Activity and Patent Filings: A review of patent databases reveals a steady flow of patent applications and grants related to imidazo[1,2-a]pyridine derivatives. These filings often claim: New structural modifications and novel compounds. Specific polymorphs or salt forms of existing compounds. New therapeutic uses or improved treatment regimens. Formulations and delivery methods. Companies actively filing in this space aim to secure intellectual property rights for novel entities, formulations, or methods of treatment, which can lead to potential infringement claims or licensing opportunities. Freedom to Operate (FTO) Considerations: Companies seeking to develop compounds within the imidazo[1,2-a]pyridine chemical class for neurological disorders must conduct thorough FTO analyses. This involves: Identifying relevant patents: Mapping out existing patents, including patent 10,376,584 and others that claim similar structures or uses. Analyzing claim scope: Precisely understanding what each patent claims and how it might cover a proposed product or process. Assessing potential infringement: Determining if a new product or process would fall within the scope of any active claims. Evaluating patent validity: Assessing the strength and potential invalidity of blocking patents. The broad claims of patent 10,376,584 necessitate careful consideration for any entity pursuing R&D in this specific chemical and therapeutic area. What are the Key Dates and Status of Patent 10,376,584? Understanding the timeline of patent 10,376,584 is crucial for assessing its remaining lifespan and commercial relevance. Key Dates: Priority Date: November 2, 2016. This is the earliest date to which the patent can claim priority, based on its provisional or parent application. Filing Date: November 2, 2017. This is the date the non-provisional patent application was filed with the USPTO. Grant Date: August 13, 2019. The date the patent was officially granted by the USPTO. Expiration Date: November 2, 2037. This is the standard 20-year term from the filing date for utility patents filed after June 8, 1995. Status: Status: Active. As of the grant date and continuing through its expiration, the patent is in force. Maintenance Fees: To remain in force, the patent holder must pay periodic maintenance fees to the USPTO. These fees are due at 3.5, 7.5, and 11.5 years after the grant date. Failure to pay these fees will result in the patent lapsing. Implications of Remaining Term: The patent has approximately 13 years of remaining exclusivity from its grant date. This substantial remaining term provides Merck Sharp & Dohme Corp. with a significant period to commercialize compounds covered by the patent without direct competition from generic or biosimilar versions. For potential competitors, this means that any product entering the market for the claimed indications and falling within the patent's scope will need to consider licensing or wait for patent expiry. Key Takeaways Patent 10,376,584 protects a broad class of substituted imidazo[1,2-a]pyridine compounds with asserted utility in treating neurological disorders, including Alzheimer's, Parkinson's, and ALS. The patent's comprehensive definition of chemical structures through a Markush claim provides significant scope, while its remaining term until November 2, 2037, offers substantial market exclusivity for the assignee, Merck Sharp & Dohme Corp. The active patent landscape for imidazo[1,2-a]pyridine derivatives in this therapeutic area necessitates careful freedom-to-operate analysis for competing entities. FAQs What specific biological pathways do the claimed compounds in patent 10,376,584 target? The patent indicates that the compounds modulate biological targets relevant to neurological disorders, with particular emphasis on glutamate receptor modulation, specifically NMDA receptors. Does patent 10,376,584 claim any specific approved drugs? This analysis is based on the patent text and does not confirm if any specific drug currently approved by regulatory agencies falls directly and exclusively under the claims of patent 10,376,584. Such a determination would require detailed analysis of approved drug structures against the patent's claims. What is the geographic coverage of patent 10,376,584? This patent is a United States patent, providing protection only within the United States. Protection in other countries would require separate patent filings in those jurisdictions. Can a competitor develop a drug with a similar structure but different substituents and avoid infringement? Competitors can attempt to design around the patent by modifying the structure. However, the broad Markush claims and definitions of substituents in patent 10,376,584 are designed to cover a wide range of variations, making it challenging to avoid infringement without careful analysis. What is the process for challenging the validity of patent 10,376,584? A patent's validity can be challenged through various legal mechanisms, including post-grant review (PGR) or inter partes review (IPR) at the U.S. Patent and Trademark Office, or through invalidity defenses raised during patent infringement litigation. Citations [1] Merck Sharp & Dohme Corp. (2019, August 13). Substituted imidazo[1,2-a]pyridines (U.S. Patent No. 10,376,584). Washington, DC: U.S. Patent and Trademark Office. 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Details for Patent: 10,376,584

Summary for Patent: 10,376,584