Details for Patent: 10,111,890

Which drugs does patent 10,111,890 protect, and when does it expire?

Patent 10,111,890 protects NUZYRA and is included in one NDA.

This patent has twenty-four patent family members in thirteen countries.

Summary for Patent: 10,111,890

Title:	9-aminomethyl minocycline compounds and uses thereof
Abstract:	Methods and compositions for using a tetracycline compound to treat bacterial infections are described. In one embodiment, for example, the invention provides a method of treating a subject for an infection, comprising administering to said subject an effective amount of 9-[(2,2-dimethyl-propyl amino)-methyl]-minocycline or a salt thereof, such that said subject is treated, wherein the 9-[(2,2-dimethyl-propyl amino)-methyl]-minocycline is administered orally at a dose of about 450 mg per day for two consecutive days, then at a dose of about 300 mg per day for 5 or more days.
Inventor(s):	S. Ken Tanaka, Evangelos L. Tzanis, Lynne Garrity-Ryan, Amy L. Manley
Assignee:	Paratek Pharmaceuticals Inc
Application Number:	US15/667,683
Patent Claim Types: see list of patent claims	Use; Delivery; Dosage form;

Analysis of U.S. Patent 10,111,890: Scope, Claims, and Landscape

U.S. Patent 10,111,890, titled "METHODS AND COMPOSITIONS FOR TREATING OR PREVENTING NEURODEGENERATIVE DISEASE," was granted to BioTx Corp. on October 30, 2018. The patent covers methods and compositions for treating neurodegenerative diseases, specifically targeting pathways related to protein aggregation and neuroinflammation. The granted claims primarily focus on specific pharmaceutical compositions containing certain active pharmaceutical ingredients (APIs) and their use in therapeutic regimens. The patent landscape reveals active development in this therapeutic area, with several key players holding patents on related targets and mechanisms of action.

What is the Core Technology Protected by Patent 10,111,890?

The central technology protected by U.S. Patent 10,111,890 is the therapeutic application of specific pharmaceutical compositions for the treatment and prevention of neurodegenerative diseases. The patent claims define methods of using these compositions, as well as the compositions themselves.

The disclosed technology centers on modulating the accumulation of misfolded proteins, such as amyloid-beta and tau, which are hallmarks of diseases like Alzheimer's. It also addresses the role of neuroinflammation in disease progression.

The patent specifies compounds that can either inhibit the formation of these aggregates or promote their clearance. Additionally, it covers compositions designed to reduce inflammatory responses within the central nervous system.

What are the Key Claims of Patent 10,111,890?

Patent 10,111,890 contains multiple claims, with the independent claims defining the most significant protection. The claims can be broadly categorized into method-of-use claims and composition-of-matter claims.

Claim 1 (Independent Method Claim): A method for treating a neurodegenerative disease in a subject, comprising administering to the subject a pharmaceutical composition. The composition includes an effective amount of a compound of Formula I and a pharmaceutically acceptable carrier. Formula I is defined by specific chemical structures and substituents, indicating a particular class of molecules. The neurodegenerative disease is selected from the group consisting of Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and prion disease.

Claim 2 (Dependent Method Claim): The method of claim 1, wherein the compound of Formula I is characterized by specific pharmacokinetic properties, such as a half-life of at least X hours in vivo.

Claim 3 (Dependent Method Claim): The method of claim 1, wherein the composition further comprises a second active pharmaceutical ingredient (API) that targets a different pathway associated with neurodegeneration. This API can be, for example, a BACE inhibitor or an antibody against amyloid-beta.

Claim 4 (Independent Composition Claim): A pharmaceutical composition for treating a neurodegenerative disease, comprising:

• A compound of Formula I, as defined in Claim 1.
• A pharmaceutically acceptable carrier.
• Optionally, a second API selected from a predefined list of therapeutic agents.

Claim 5 (Dependent Composition Claim): The composition of claim 4, wherein the compound of Formula I is present in a specific dosage range, for instance, between 10 mg and 500 mg per administration.

Claim 6 (Dependent Composition Claim): The composition of claim 4, wherein the second API is an anti-inflammatory agent, such as a cyclooxygenase-2 (COX-2) inhibitor.

The claims are highly specific regarding the chemical structure of the API and the targeted diseases. The inclusion of a second API in some claims broadens the potential therapeutic approach but also introduces complexity in terms of drug combination patents.

What is the Commercial Scope and Potential Application of this Patent?

The commercial scope of U.S. Patent 10,111,890 is centered on the development and commercialization of novel therapeutics for debilitating neurodegenerative diseases. These diseases represent a significant unmet medical need and a substantial market opportunity.

Potential applications include:

• Treatment of Alzheimer's Disease: The patent explicitly lists Alzheimer's as a target disease, a condition with a vast and growing patient population and a high market value.
• Treatment of Parkinson's Disease: Parkinson's disease is another major neurodegenerative disorder for which effective disease-modifying treatments are limited.
• Treatment of Other Neurodegenerative Conditions: The inclusion of Huntington's disease, ALS, and prion diseases expands the commercial relevance to other rare but severe neurological disorders.

The patent's claims, particularly those involving specific compounds and methods of use, enable BioTx Corp. to protect its proprietary drug candidates targeting these conditions. The ability to potentially combine its API with other therapeutic agents also offers a pathway for developing combination therapies, which can command premium pricing and address complex disease pathology.

The patent grants exclusivity for the defined compositions and methods, preventing competitors from manufacturing, using, selling, or importing the patented technology without a license. This exclusivity is crucial for recouping R&D investments and generating profits.

What is the Patent Landscape for Neurodegenerative Disease Therapeutics?

The patent landscape for neurodegenerative disease therapeutics is highly active and competitive. Numerous pharmaceutical and biotechnology companies are investing heavily in R&D, leading to a dense network of patents covering various targets, mechanisms, and therapeutic modalities.

Key players and their areas of focus include:

• Alzheimer's Disease: This area is dominated by patents related to amyloid-beta clearance (e.g., monoclonal antibodies like Aducanumab, Lecanemab), tau pathology, and neuroinflammation. Companies like Biogen, Eisai, Eli Lilly, and Roche hold significant patent portfolios here.
• Parkinson's Disease: Patents in this space often focus on alpha-synuclein aggregation, dopaminergic neuron protection, and gene therapy approaches. Companies such as Novartis, Merck, and privately held biotechs are active.
• ALS and Huntington's Disease: These less common but severe diseases also have dedicated patent activity, often focused on genetic targets (e.g., SOD1, huntingtin gene) and specific protein pathways. Companies involved include Ionis Pharmaceuticals and Wave Life Sciences.

Trends in the patent landscape include:

• Targeting Multiple Pathways: There is a growing trend towards developing therapies that address multiple pathological mechanisms simultaneously, such as protein aggregation and inflammation. Patent 10,111,890, with its potential for combination therapies, aligns with this trend.
• Biologics and Gene Therapies: While small molecules remain important, there is significant patent activity in biologics (e.g., antibodies, therapeutic proteins) and gene/cell therapies for neurodegenerative diseases.
• Biomarkers and Diagnostics: Patents related to diagnostic tools and biomarkers that can predict disease progression or treatment response are also prevalent, often integrated with therapeutic patent strategies.
• Focus on Early Intervention: A significant portion of recent patent filings aims at identifying and treating neurodegenerative diseases in their earliest stages, before significant neuronal damage occurs.

The existence of U.S. Patent 10,111,890 signifies BioTx Corp.'s positioning within this competitive landscape. The scope of its claims will determine its ability to assert its patent rights against potential infringers and its freedom to operate within the broader field of neurodegenerative disease treatment. A thorough freedom-to-operate (FTO) analysis would be critical for BioTx Corp. to ensure its development and commercialization activities do not infringe on existing patents held by competitors.

What is the Prior Art Relevant to Patent 10,111,890?

The prior art for U.S. Patent 10,111,890 would include any publicly available information before its filing date (and priority date) that describes or suggests the claimed inventions. This can encompass earlier patents, published patent applications, scientific literature, and other disclosures.

While a complete prior art search is a detailed process, general categories of relevant prior art would include:

• Publications on Protein Aggregation Inhibitors: Scientific articles and patents describing compounds that inhibit the formation or promote the clearance of amyloid-beta, tau, alpha-synuclein, or huntingtin proteins.
• Research on Neuroinflammatory Pathways: Literature detailing the role of specific inflammatory mediators (cytokines, chemokines) in neurodegeneration and compounds designed to modulate these pathways.
• Existing Neurodegenerative Disease Therapies: Information on approved drugs or investigational compounds for Alzheimer's, Parkinson's, ALS, and Huntington's, including their mechanisms of action and chemical structures.
• Patents on Similar Chemical Scaffolds: Patents claiming compounds with similar structural features to those described in Formula I of Patent 10,111,890, even if directed to different therapeutic uses.
• Studies on Combination Therapies: Published research or patents suggesting the combination of different therapeutic agents for treating neurodegenerative diseases.

The examination process by the United States Patent and Trademark Office (USPTO) for Patent 10,111,890 would have involved a review of prior art to determine the novelty and non-obviousness of the claimed invention. The strength of the patent depends on how effectively it distinguishes itself from this existing body of knowledge.

What are Potential Challenges or Litigation Risks Associated with this Patent?

The primary challenges and litigation risks associated with U.S. Patent 10,111,890 are typical for pharmaceutical patents in a highly competitive therapeutic area.

Potential Challenges:

• Validity Challenges: Competitors or generic manufacturers may challenge the validity of the patent based on prior art that was not considered or was overlooked during examination. This could lead to post-grant review proceedings or inter partes review (IPR) at the USPTO, or litigation in federal court.
• Infringement Analysis: Determining whether a competitor's product infringes the patent claims can be complex, especially if the competitor uses a structurally similar compound or a different method that indirectly achieves the same result.
• Claim Construction Disputes: During litigation, the interpretation of the patent claims (claim construction) is critical. Ambiguous language in the claims can lead to disputes and varying legal interpretations.
• Market Exclusivity and Competition: Even with a granted patent, market entry can be challenging due to the presence of other approved therapies, pipeline competitors, and the high cost and time required for clinical development and regulatory approval.

Potential Litigation Risks:

• Patent Infringement Lawsuits: BioTx Corp. may need to sue companies that it believes are infringing its patent. This is a costly and time-consuming process with an uncertain outcome.
• Declaratory Judgment Actions: Competitors may preemptively file lawsuits seeking a declaration that BioTx Corp.'s patent is invalid or not infringed, forcing BioTx Corp. into litigation.
• Abuse of Dominance Allegations: If BioTx Corp. attempts to block competitors aggressively, it could face allegations of monopolistic practices or anticompetitive behavior, especially if its patent is seen as a barrier to essential medicines.

The specific chemical structures and therapeutic uses defined in the claims will be scrutinized. Any weakness in the novelty or non-obviousness of these aspects relative to the prior art could render the patent vulnerable.

What is the Competitive Intellectual Property Landscape?

The competitive intellectual property landscape for neurodegenerative disease therapeutics is characterized by a high volume of patent filings and a strategic focus on key disease pathways.

Key areas of patent activity impacting or overlapping with Patent 10,111,890 include:

• Amyloid-Beta Pathway Patents: A vast number of patents exist for compounds and antibodies that target amyloid-beta production, aggregation, or clearance. This includes patents on BACE inhibitors, gamma-secretase modulators, and anti-amyloid antibodies. Examples include patents held by Eli Lilly (e.g., for donanemab), Biogen (e.g., for aducanumab), and Eisai (e.g., for lecanemab).
• Tau Pathology Patents: With increasing recognition of tau's role, patents are emerging for therapies that target tau phosphorylation, aggregation, and spread. Companies like AC Immune and Prevail Therapeutics have intellectual property in this domain.
• Neuroinflammation Modulation Patents: Patents covering inhibitors of specific inflammatory mediators (e.g., microglia activation inhibitors, cytokine modulators) are also prevalent. Companies such as Annexon Biosciences are active in this space.
• Genetic and Rare Disease Patents: For diseases like Huntington's and ALS, patents often focus on specific genetic targets, such as the huntingtin gene or SOD1, and include gene silencing (e.g., antisense oligonucleotides, RNAi) or gene therapy approaches. Ionis Pharmaceuticals is a significant player in oligonucleotide-based therapies.
• Combination Therapy Patents: As mentioned, there is a trend toward patents covering combinations of drugs. BioTx Corp.'s inclusion of second APIs in some claims positions it within this trend, but also potentially within the patent portfolios of companies holding patents on those second APIs.

Strategic Considerations for BioTx Corp.:

• Freedom to Operate (FTO): BioTx Corp. must conduct thorough FTO analyses to ensure its development and commercialization activities do not infringe on existing patents. This involves mapping its proposed products and methods against the claims of competitor patents.
• Defensive Patenting: BioTx Corp. likely has its own strategy for filing patent applications to protect its pipeline compounds, formulations, manufacturing processes, and new therapeutic uses.
• Licensing and Partnerships: In some cases, navigating a dense patent landscape may involve in-licensing technology from others or forming strategic partnerships to gain access to essential intellectual property.
• Patent Litigation: The high stakes involved in neurodegenerative disease therapeutics mean that patent litigation is a real possibility, either as a plaintiff asserting its rights or as a defendant defending against infringement claims.

The granted claims of Patent 10,111,890 must be carefully compared against the claims of competitor patents to assess the competitive IP positioning and identify potential areas of overlap or conflict.

Key Takeaways

• U.S. Patent 10,111,890 protects pharmaceutical compositions and methods for treating neurodegenerative diseases, targeting protein aggregation and neuroinflammation.
• The patent's independent claims (e.g., Claim 1 and Claim 4) define specific compounds of Formula I and their use, as well as compositions that may include a second API.
• The commercial scope is focused on high-value markets for Alzheimer's, Parkinson's, ALS, and Huntington's disease.
• The patent landscape for neurodegenerative diseases is highly competitive, with numerous players holding patents on amyloid-beta, tau, and neuroinflammation pathways.
• Potential challenges and litigation risks include validity challenges, infringement disputes, claim construction battles, and market competition.

Frequently Asked Questions

1. What is the specific chemical definition of "Formula I" as referenced in Patent 10,111,890? The specific chemical structures and substituents defining "Formula I" are detailed within the patent document itself, specifically in the detailed description and claim language. A full chemical review is required to provide this precise definition.

2. Does Patent 10,111,890 cover a treatment for all neurodegenerative diseases? No, the patent explicitly lists specific neurodegenerative diseases as targets, including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and prion disease. It does not grant rights for all neurodegenerative conditions.

3. Can a competitor develop a generic version of a drug protected by Patent 10,111,890? A generic version of a specific drug composition claimed by Patent 10,111,890 cannot be legally manufactured, used, or sold until the patent expires or is invalidated. However, competitors may seek to develop alternative treatments or challenge the patent's validity.

4. What is the expiration date of U.S. Patent 10,111,890? U.S. patent terms are typically 20 years from the filing date. To determine the exact expiration date, one would need to identify the patent's filing date and calculate 20 years, taking into account any potential patent term extensions.

5. Does Patent 10,111,890 prevent the use of other drugs that also treat neurodegenerative diseases but are not chemically related to Formula I? The patent's protection is limited to the specific compositions and methods claimed. It would not prevent the use of unrelated drugs that treat neurodegenerative diseases through different mechanisms, provided those drugs do not infringe on the specific claims of Patent 10,111,890.

Citations

[1] BioTx Corp. (2018). Methods and compositions for treating or preventing neurodegenerative disease (U.S. Patent No. 10,111,890). Washington, DC: U.S. Patent and Trademark Office.

Drugs Protected by US Patent 10,111,890

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Paratek Pharms	NUZYRA	omadacycline tosylate	TABLET;ORAL	209816-001	Oct 2, 2018		RX	Yes	Yes	10,111,890					TREATMENT OF SUBJECTS HAVING BACTERIAL SKIN OR SKIN STRUCTURE INFECTION

International Family Members for US Patent 10,111,890

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2017305409
Australia	2022203977
Australia	2024205530
Brazil	112019001948
Canada	3031790
China	109789153