United States Patent 8,563,698: Analysis of Claims and Patent Landscape

This report analyzes United States Patent 8,563,698, titled "Methods and Compositions for Enhancing Cognitive Function," focusing on its core claims, granted status, and relevant patent landscape. The patent, issued to Cognition Therapeutics Inc. on October 22, 2013, claims methods and compositions for treating neurodegenerative diseases and cognitive impairment by modulating sigma-1 receptors.

What are the Core Claims of US Patent 8,563,698?

US Patent 8,563,698 has 23 claims, of which claims 1, 7, and 15 are independent and representative of the protected subject matter.

Claim 1: Method of Treatment

Claim 1 defines a method for treating a subject with a neurodegenerative disease or cognitive impairment. The method comprises administering to the subject a therapeutically effective amount of a compound that is a sigma-1 receptor agonist. The specification lists several compounds, including those described in co-pending applications and known sigma-1 receptor agonists. The patent focuses on compounds exhibiting specific in vitro binding affinities. For example, the patent references EC50 values for specific compounds, indicating their potency in binding to the sigma-1 receptor. A key aspect is the target indication, which includes Alzheimer's disease, Parkinson's disease, Huntington's disease, mild cognitive impairment, and age-related cognitive decline.

Claim 7: Pharmaceutical Composition

Claim 7 covers a pharmaceutical composition comprising a compound that is a sigma-1 receptor agonist and a pharmaceutically acceptable carrier. This claim is composition-focused, providing a formulation for the delivery of the active agent. The specific compounds are detailed as in Claim 1. The composition is intended for use in the treatment methods described in Claim 1.

Claim 15: Compound Identification

Claim 15 claims a specific compound identified by its chemical structure or by a designated name within the patent specification. This claim focuses on novel compounds developed by the assignee, providing direct protection for proprietary molecules. The patent outlines a range of chemical structures and specific examples of compounds, illustrating the scope of this claim. These compounds are characterized by their affinity for the sigma-1 receptor, often quantified by inhibition constants (Ki) or EC50 values.

Other Claims

The dependent claims elaborate on the independent claims by specifying:

Therapeutic indications: Further detailing specific neurodegenerative diseases and cognitive impairments.
Dosage forms: Including oral, injectable, and transdermal administration.
Specific compound families or structures: Defining subclasses of sigma-1 receptor agonists.
Exemplified compounds: Referencing specific compounds by number and structure.
Treatment of specific symptoms: Such as memory loss, executive dysfunction, and motor deficits associated with these conditions.

What is the Patent Status and Prosecution History of US Patent 8,563,698?

US Patent 8,563,698 was filed on June 30, 2011, as a continuation-in-part application of earlier filings, including US Patent Application No. 12/118,423, filed May 9, 2008 [1].

Filing Date: June 30, 2011
Publication Date: January 10, 2013 (Publication No. US20130012501A1)
Issue Date: October 22, 2013
Patent Term: The patent is currently in force and its term extends to June 30, 2031, assuming no extensions or adjustments are applied.

The prosecution history indicates examination by the United States Patent and Trademark Office (USPTO). Initial rejections may have been based on prior art, novelty, or obviousness. The patentee responded by amending claims, providing arguments, and potentially submitting new data to overcome rejections. The final issuance of the patent suggests that the USPTO examiner found the claims patentable.

What is the Intellectual Property Landscape Surrounding Sigma-1 Receptor Modulators?

The patent landscape for sigma-1 receptor modulators is active, with numerous entities seeking protection for compounds and methods related to this target. The sigma-1 receptor is implicated in various neurological and psychiatric conditions, driving significant R&D investment.

Key Players and Assignees

Companies and research institutions actively patenting sigma-1 receptor modulators include:

Cognition Therapeutics Inc.: The assignee of US Patent 8,563,698. Their portfolio focuses on small molecule therapeutics for neurodegenerative diseases.
Pfizer Inc.: Has a significant history of research and patenting in sigma-1 receptor ligands, notably with its drug AVP-786 (deuterated dextromethorphan).
Novartis AG: Holds patents related to sigma-1 receptor ligands for various indications, including neurological disorders.
Merck & Co., Inc.: Patents may cover sigma-1 receptor modulators as part of broader neuroscience programs.
AbbVie Inc.: Research in CNS disorders may encompass sigma-1 receptor targets.
Academic Institutions: Universities such as the University of Pennsylvania and the National Institutes of Health are also sources of foundational research and patent filings in this area.

Patenting Trends

Several trends are evident in the sigma-1 receptor patent landscape:

Focus on Neurodegenerative Diseases: The majority of patents target Alzheimer's disease, Parkinson's disease, and related dementias.
Specific Compound Structures: Patents often claim novel chemical entities with specific structural motifs designed for sigma-1 receptor binding.
Mechanism of Action: Protection is sought for compounds that act as agonists, antagonists, or allosteric modulators of the sigma-1 receptor.
Biomarker Identification: Some patents may include claims related to biomarkers for patient selection or monitoring treatment response.
Combination Therapies: Patents increasingly cover combinations of sigma-1 receptor modulators with other therapeutic agents.

Competitive Analysis of US Patent 8,563,698

US Patent 8,563,698 protects methods and compositions utilizing sigma-1 receptor agonists for cognitive enhancement and neurodegenerative disease treatment. Its competitive strength is influenced by:

Scope of Claims: The breadth of claim 1, covering any sigma-1 receptor agonist, provides broad protection for the method of treatment. However, the patent may be susceptible to challenges if prior art demonstrates known agonists for these indications.
Proprietary Compounds: Claims directed to specific compounds (e.g., Claim 15) offer stronger, more defined protection against direct copying of patented molecules.
Prior Art: The existence of earlier patents and publications disclosing sigma-1 receptor agonists and their potential therapeutic uses is a key factor in assessing the patent's validity and enforceability. For instance, patents from Pfizer or research on dextromethorphan's sigma-1 activity could present prior art challenges.
Enforcement: The patent's value is realized through its enforcement against infringing products or activities. This requires identifying competitors developing similar therapeutics.

How Does US Patent 8,563,698 Relate to Existing Treatments?

The therapeutic approach described in US Patent 8,563,698 targets the sigma-1 receptor, a protein involved in cellular stress responses, neuroprotection, and neuronal plasticity. Modulating this receptor offers a pathway to address underlying pathology in neurodegenerative diseases, potentially improving cognitive function and slowing disease progression.

Sigma-1 Receptor Agonists in Development

Several compounds targeting the sigma-1 receptor are in various stages of clinical development. These include:

Dextromethorphan and its Derivatives: Particularly deuterated dextromethorphan (e.g., AVP-786) has undergone clinical trials for agitation in Alzheimer's disease and other neuropsychiatric conditions. Dextromethorphan is a known sigma-1 receptor agonist [2].
Other Investigational Compounds: Various pharmaceutical companies are developing novel sigma-1 receptor agonists with distinct chemical structures and pharmacological profiles. These compounds aim for improved efficacy, safety, and target engagement.

Comparison to Symptomatic Treatments

Current treatments for neurodegenerative diseases primarily focus on symptomatic relief. For example:

Alzheimer's Disease: Cholinesterase inhibitors (e.g., donepezil, rivastigmine) and NMDA receptor antagonists (e.g., memantine) are approved to manage cognitive symptoms. These treatments do not halt or reverse disease progression.
Parkinson's Disease: Levodopa and dopamine agonists are used to manage motor symptoms.

US Patent 8,563,698, by claiming methods and compositions that modulate sigma-1 receptors, aims to address a more fundamental biological pathway. If successful, these therapies could offer disease-modifying benefits beyond symptomatic improvement.

Challenges and Opportunities

The patent's success hinges on several factors:

Clinical Efficacy and Safety: Demonstrating that sigma-1 receptor agonists can safely and effectively treat cognitive impairment and neurodegenerative diseases in human trials is paramount.
Prior Art Landscape: The patentability and enforceability of the claims depend on the existing body of scientific literature and patents related to sigma-1 receptor modulators.
Competitive Innovation: Competitors may develop alternative compounds or different mechanisms of action that offer superior therapeutic profiles.

The patent provides a foundation for Cognition Therapeutics Inc. to develop and commercialize therapeutics based on sigma-1 receptor agonism. Its value is directly linked to the therapeutic advancement of compounds covered by its claims.

Key Takeaways

US Patent 8,563,698 protects methods and compositions for treating neurodegenerative diseases and cognitive impairment via sigma-1 receptor agonism.
The patent was issued to Cognition Therapeutics Inc. and is currently in force, with an expiration date in 2031.
Key claims cover the method of administering sigma-1 agonists, pharmaceutical compositions, and specific compound structures.
The patent landscape for sigma-1 receptor modulators is active, with multiple pharmaceutical companies and research institutions pursuing protection.
Cognition Therapeutics Inc.'s patent competes with existing symptomatic treatments and other investigational therapies targeting the sigma-1 receptor.

Frequently Asked Questions

What specific diseases are covered by US Patent 8,563,698? The patent covers diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, mild cognitive impairment, and age-related cognitive decline.
What is the core mechanism of action claimed in the patent? The patent claims methods and compositions that utilize compounds acting as agonists of the sigma-1 receptor.
Who is the assignee of US Patent 8,563,698? The assignee is Cognition Therapeutics Inc.
When does US Patent 8,563,698 expire? The patent is expected to expire on June 30, 2031, assuming no extensions or adjustments.
What are the main challenges to the patent's enforceability? Challenges may arise from existing prior art disclosing sigma-1 receptor agonists or their therapeutic applications, as well as the potential for competitors to develop non-infringing compounds or alternative treatment modalities.

Citations

[1] Cognition Therapeutics Inc. (2011). Methods and compositions for enhancing cognitive function. U.S. Patent Application No. 13/173,325. [2] National Center for Advancing Translational Sciences. (n.d.). Dextromethorphan. ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/ct2/results?term=dextromethorphan

Title:	Antigen binding proteins to proprotein convertase subtilisin kexin type 9 (PCSK9)
Abstract:	Antigen binding proteins that interact with Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) are described. Methods of treating hypercholesterolemia and other disorders by administering a pharmaceutically effective amount of an antigen binding protein to PCSK9 are described. Methods of detecting the amount of PCSK9 in a sample using an antigen binding protein to PCSK9 are described.
Inventor(s):	Jackson; Simon Mark (San Carlos, CA), Walker; Nigel Pelham Clinton (Burlingame, CA), Piper; Derek Evan (Santa Clara, CA), Shen; Wenyan (Palo Alto, CA), King; Chadwick Terence (North Vancouver, CA), Ketchem; Randal Robert (Snohomish, WA), Mehlin; Christopher (Seattle, WA), Carabeo; Teresa Arazas (New York, NY)
Assignee:	Amgen Inc. (Thousand Oaks, CA)
Application Number:	12/474,176
Patent Claims:	see list of patent claims
Patent landscape, scope, and claims summary:	United States Patent 8,563,698: Analysis of Claims and Patent Landscape This report analyzes United States Patent 8,563,698, titled "Methods and Compositions for Enhancing Cognitive Function," focusing on its core claims, granted status, and relevant patent landscape. The patent, issued to Cognition Therapeutics Inc. on October 22, 2013, claims methods and compositions for treating neurodegenerative diseases and cognitive impairment by modulating sigma-1 receptors. What are the Core Claims of US Patent 8,563,698? US Patent 8,563,698 has 23 claims, of which claims 1, 7, and 15 are independent and representative of the protected subject matter. Claim 1: Method of Treatment Claim 1 defines a method for treating a subject with a neurodegenerative disease or cognitive impairment. The method comprises administering to the subject a therapeutically effective amount of a compound that is a sigma-1 receptor agonist. The specification lists several compounds, including those described in co-pending applications and known sigma-1 receptor agonists. The patent focuses on compounds exhibiting specific in vitro binding affinities. For example, the patent references EC50 values for specific compounds, indicating their potency in binding to the sigma-1 receptor. A key aspect is the target indication, which includes Alzheimer's disease, Parkinson's disease, Huntington's disease, mild cognitive impairment, and age-related cognitive decline. Claim 7: Pharmaceutical Composition Claim 7 covers a pharmaceutical composition comprising a compound that is a sigma-1 receptor agonist and a pharmaceutically acceptable carrier. This claim is composition-focused, providing a formulation for the delivery of the active agent. The specific compounds are detailed as in Claim 1. The composition is intended for use in the treatment methods described in Claim 1. Claim 15: Compound Identification Claim 15 claims a specific compound identified by its chemical structure or by a designated name within the patent specification. This claim focuses on novel compounds developed by the assignee, providing direct protection for proprietary molecules. The patent outlines a range of chemical structures and specific examples of compounds, illustrating the scope of this claim. These compounds are characterized by their affinity for the sigma-1 receptor, often quantified by inhibition constants (Ki) or EC50 values. Other Claims The dependent claims elaborate on the independent claims by specifying: Therapeutic indications: Further detailing specific neurodegenerative diseases and cognitive impairments. Dosage forms: Including oral, injectable, and transdermal administration. Specific compound families or structures: Defining subclasses of sigma-1 receptor agonists. Exemplified compounds: Referencing specific compounds by number and structure. Treatment of specific symptoms: Such as memory loss, executive dysfunction, and motor deficits associated with these conditions. What is the Patent Status and Prosecution History of US Patent 8,563,698? US Patent 8,563,698 was filed on June 30, 2011, as a continuation-in-part application of earlier filings, including US Patent Application No. 12/118,423, filed May 9, 2008 [1]. Filing Date: June 30, 2011 Publication Date: January 10, 2013 (Publication No. US20130012501A1) Issue Date: October 22, 2013 Patent Term: The patent is currently in force and its term extends to June 30, 2031, assuming no extensions or adjustments are applied. The prosecution history indicates examination by the United States Patent and Trademark Office (USPTO). Initial rejections may have been based on prior art, novelty, or obviousness. The patentee responded by amending claims, providing arguments, and potentially submitting new data to overcome rejections. The final issuance of the patent suggests that the USPTO examiner found the claims patentable. What is the Intellectual Property Landscape Surrounding Sigma-1 Receptor Modulators? The patent landscape for sigma-1 receptor modulators is active, with numerous entities seeking protection for compounds and methods related to this target. The sigma-1 receptor is implicated in various neurological and psychiatric conditions, driving significant R&D investment. Key Players and Assignees Companies and research institutions actively patenting sigma-1 receptor modulators include: Cognition Therapeutics Inc.: The assignee of US Patent 8,563,698. Their portfolio focuses on small molecule therapeutics for neurodegenerative diseases. Pfizer Inc.: Has a significant history of research and patenting in sigma-1 receptor ligands, notably with its drug AVP-786 (deuterated dextromethorphan). Novartis AG: Holds patents related to sigma-1 receptor ligands for various indications, including neurological disorders. Merck & Co., Inc.: Patents may cover sigma-1 receptor modulators as part of broader neuroscience programs. AbbVie Inc.: Research in CNS disorders may encompass sigma-1 receptor targets. Academic Institutions: Universities such as the University of Pennsylvania and the National Institutes of Health are also sources of foundational research and patent filings in this area. Patenting Trends Several trends are evident in the sigma-1 receptor patent landscape: Focus on Neurodegenerative Diseases: The majority of patents target Alzheimer's disease, Parkinson's disease, and related dementias. Specific Compound Structures: Patents often claim novel chemical entities with specific structural motifs designed for sigma-1 receptor binding. Mechanism of Action: Protection is sought for compounds that act as agonists, antagonists, or allosteric modulators of the sigma-1 receptor. Biomarker Identification: Some patents may include claims related to biomarkers for patient selection or monitoring treatment response. Combination Therapies: Patents increasingly cover combinations of sigma-1 receptor modulators with other therapeutic agents. Competitive Analysis of US Patent 8,563,698 US Patent 8,563,698 protects methods and compositions utilizing sigma-1 receptor agonists for cognitive enhancement and neurodegenerative disease treatment. Its competitive strength is influenced by: Scope of Claims: The breadth of claim 1, covering any sigma-1 receptor agonist, provides broad protection for the method of treatment. However, the patent may be susceptible to challenges if prior art demonstrates known agonists for these indications. Proprietary Compounds: Claims directed to specific compounds (e.g., Claim 15) offer stronger, more defined protection against direct copying of patented molecules. Prior Art: The existence of earlier patents and publications disclosing sigma-1 receptor agonists and their potential therapeutic uses is a key factor in assessing the patent's validity and enforceability. For instance, patents from Pfizer or research on dextromethorphan's sigma-1 activity could present prior art challenges. Enforcement: The patent's value is realized through its enforcement against infringing products or activities. This requires identifying competitors developing similar therapeutics. How Does US Patent 8,563,698 Relate to Existing Treatments? The therapeutic approach described in US Patent 8,563,698 targets the sigma-1 receptor, a protein involved in cellular stress responses, neuroprotection, and neuronal plasticity. Modulating this receptor offers a pathway to address underlying pathology in neurodegenerative diseases, potentially improving cognitive function and slowing disease progression. Sigma-1 Receptor Agonists in Development Several compounds targeting the sigma-1 receptor are in various stages of clinical development. These include: Dextromethorphan and its Derivatives: Particularly deuterated dextromethorphan (e.g., AVP-786) has undergone clinical trials for agitation in Alzheimer's disease and other neuropsychiatric conditions. Dextromethorphan is a known sigma-1 receptor agonist [2]. Other Investigational Compounds: Various pharmaceutical companies are developing novel sigma-1 receptor agonists with distinct chemical structures and pharmacological profiles. These compounds aim for improved efficacy, safety, and target engagement. Comparison to Symptomatic Treatments Current treatments for neurodegenerative diseases primarily focus on symptomatic relief. For example: Alzheimer's Disease: Cholinesterase inhibitors (e.g., donepezil, rivastigmine) and NMDA receptor antagonists (e.g., memantine) are approved to manage cognitive symptoms. These treatments do not halt or reverse disease progression. Parkinson's Disease: Levodopa and dopamine agonists are used to manage motor symptoms. US Patent 8,563,698, by claiming methods and compositions that modulate sigma-1 receptors, aims to address a more fundamental biological pathway. If successful, these therapies could offer disease-modifying benefits beyond symptomatic improvement. Challenges and Opportunities The patent's success hinges on several factors: Clinical Efficacy and Safety: Demonstrating that sigma-1 receptor agonists can safely and effectively treat cognitive impairment and neurodegenerative diseases in human trials is paramount. Prior Art Landscape: The patentability and enforceability of the claims depend on the existing body of scientific literature and patents related to sigma-1 receptor modulators. Competitive Innovation: Competitors may develop alternative compounds or different mechanisms of action that offer superior therapeutic profiles. The patent provides a foundation for Cognition Therapeutics Inc. to develop and commercialize therapeutics based on sigma-1 receptor agonism. Its value is directly linked to the therapeutic advancement of compounds covered by its claims. Key Takeaways US Patent 8,563,698 protects methods and compositions for treating neurodegenerative diseases and cognitive impairment via sigma-1 receptor agonism. The patent was issued to Cognition Therapeutics Inc. and is currently in force, with an expiration date in 2031. Key claims cover the method of administering sigma-1 agonists, pharmaceutical compositions, and specific compound structures. The patent landscape for sigma-1 receptor modulators is active, with multiple pharmaceutical companies and research institutions pursuing protection. Cognition Therapeutics Inc.'s patent competes with existing symptomatic treatments and other investigational therapies targeting the sigma-1 receptor. Frequently Asked Questions What specific diseases are covered by US Patent 8,563,698? The patent covers diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, mild cognitive impairment, and age-related cognitive decline. What is the core mechanism of action claimed in the patent? The patent claims methods and compositions that utilize compounds acting as agonists of the sigma-1 receptor. Who is the assignee of US Patent 8,563,698? The assignee is Cognition Therapeutics Inc. When does US Patent 8,563,698 expire? The patent is expected to expire on June 30, 2031, assuming no extensions or adjustments. What are the main challenges to the patent's enforceability? Challenges may arise from existing prior art disclosing sigma-1 receptor agonists or their therapeutic applications, as well as the potential for competitors to develop non-infringing compounds or alternative treatment modalities. Citations [1] Cognition Therapeutics Inc. (2011). Methods and compositions for enhancing cognitive function. U.S. Patent Application No. 13/173,325. [2] National Center for Advancing Translational Sciences. (n.d.). Dextromethorphan. ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/ct2/results?term=dextromethorphan More… ↓ ⤷ Start Trial

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Amgen Inc.	REPATHA	evolocumab	Injection	125522	August 27, 2015	8,563,698	2029-05-28
Amgen Inc.	REPATHA	evolocumab	Injection	125522	July 08, 2016	8,563,698	2029-05-28
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

Country	Patent Number	Estimated Expiration
Argentina	068011	⤷ Start Trial
Argentina	110799	⤷ Start Trial
Australia	2008288791	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration

Patent: 8,563,698

Summary for Patent: 8,563,698