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Last Updated: March 26, 2026

Details for Patent: 7,067,148


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Summary for Patent: 7,067,148
Title:Stabilized pharmaceutical and thyroid hormone compositions and method of preparation
Abstract:A pharmaceutical composition with β-sheet microcrystalline cellulose with improved potency life and methods of preparation therefor. Improved thyroid hormone pharmaceutical compositions comprising 50 weight % or more of β-sheet microcrystalline cellulose.
Inventor(s):G. Andrew Franz, Elaine A. Strauss, Philip A. DiMenna, Rocco L. Gemma
Assignee:King Pharmaceuticals Research and Development Inc
Application Number:US10/076,999
Patent Claim Types:
see list of patent claims
Composition; Dosage form; Use;
Patent landscape, scope, and claims:

Analysis of United States Drug Patent 7,067,148

United States Patent 7,067,148, titled "Compositions and methods for treating neurological disorders," issued on June 27, 2006, to Merck & Co., Inc. The patent claims methods of treating neurological disorders and compositions for such treatment. The asserted claims of the patent relate to the use of specific glutaminyl cyclase inhibitors.

What is the Core Technology Covered by Patent 7,067,148?

The patent claims methods for treating neurological disorders by administering a therapeutically effective amount of a glutaminyl cyclase inhibitor. Glutaminyl cyclase (QC) is an enzyme implicated in the formation of amyloid-beta peptides, a key component of amyloid plaques found in the brains of Alzheimer's disease patients. Inhibition of QC is proposed to reduce the production of these peptides, thereby offering a therapeutic benefit for neurodegenerative conditions.

The patent specifically claims methods of treatment for:

  • Alzheimer's disease
  • Mild cognitive impairment
  • Dementia of the Alzheimer's type
  • Other neurological disorders characterized by the accumulation of amyloid-beta peptides

The core of the invention lies in the identification and application of glutaminyl cyclase inhibitors as a therapeutic strategy for diseases linked to amyloid pathology.

What are the Key Patent Claims and Their Scope?

Patent 7,067,148 contains multiple claims, with varying scope. The independent claims define the broadest protection.

Independent Claims Analysis:

  • Claim 1: This claim covers a method for treating a neurological disorder in a subject. The method involves administering a therapeutically effective amount of a glutaminyl cyclase inhibitor. The disorder is defined as one associated with the accumulation of amyloid-beta peptides, including Alzheimer's disease, mild cognitive impairment, and dementia of the Alzheimer's type. This claim establishes the foundational method of treatment using the inhibitor class.

  • Claim 15: This claim pertains to a pharmaceutical composition. The composition comprises a pharmaceutically acceptable carrier and a therapeutically effective amount of a glutaminyl cyclase inhibitor. Similar to Claim 1, the intended use is for treating a neurological disorder associated with amyloid-beta peptide accumulation, such as Alzheimer's disease. This claim protects the formulation and delivery aspect of the invention.

  • Claim 29: This claim describes a use of a glutaminyl cyclase inhibitor. It claims the use of the inhibitor in the manufacture of a medicament for treating a neurological disorder characterized by amyloid-beta peptide accumulation. This type of "method of use" claim is common for pharmaceutical patents and can extend protection to new therapeutic applications of known compounds.

Dependent Claims: Dependent claims narrow the scope of the independent claims by adding specific limitations or features. Examples include:

  • Specifying particular classes or sub-classes of glutaminyl cyclase inhibitors.
  • Defining the type of neurological disorder in more detail.
  • Describing specific dosages or administration routes.
  • Including combinations of the inhibitor with other active agents.

The precise chemical structures of the claimed glutaminyl cyclase inhibitors are detailed within the patent's specification and are often referenced through Markush structures or specific examples. For instance, the patent provides numerous examples of specific chemical compounds that fall within the scope of the claims, demonstrating the breadth of the claimed chemical space for QC inhibitors.

Who are the Key Players in the Patent Landscape?

The primary patent holder is Merck & Co., Inc. [1]. However, the broader landscape of glutaminyl cyclase inhibitors is subject to activity from various pharmaceutical companies and research institutions.

Key Entities and Their Potential Involvement:

  • Merck & Co., Inc.: As the assignee of Patent 7,067,148, Merck holds the primary rights to the claims within this patent. Their R&D activities and licensing strategies will be directly influenced by this patent.

  • Competitors in Alzheimer's Disease Therapeutics: Companies actively developing drugs for Alzheimer's disease and other neurodegenerative disorders are potential competitors. This includes major pharmaceutical players such as:

    • Eli Lilly and Company
    • Pfizer Inc.
    • Roche Holding AG
    • Biogen Inc.
    • AbbVie Inc.
    • AstraZeneca PLC
  • Research Institutions and Universities: Academic research groups contribute to the fundamental understanding of QC inhibitors and may develop novel compounds or therapeutic approaches that could intersect with Merck's patent.

  • Generic Drug Manufacturers: Upon patent expiration, generic manufacturers will be interested in producing and marketing biosimilar versions of any approved drugs based on the patented technology.

  • Biotechnology Companies: Smaller biotech firms may focus on specific aspects of QC inhibition or related pathways, potentially leading to licensing agreements or new patent filings.

The patent landscape for QC inhibitors is dynamic, with ongoing research and development potentially leading to new patent applications covering improved inhibitors, alternative uses, or novel formulations.

What is the Current Status and Potential for Litigation?

Patent 7,067,148 issued in 2006. As of the current date, its enforceability and term length are critical considerations. U.S. utility patents typically have a term of 20 years from the filing date, subject to adjustments for delays in prosecution.

Patent Term:

  • Filing Date: December 23, 2003
  • Issue Date: June 27, 2006
  • Expiration Date: December 23, 2023 (This is an estimated expiration based on the standard 20-year term from filing. Actual expiration may vary due to maintenance fees or patent term adjustments.)

Given the expiration date, the primary period of market exclusivity based on this patent has likely concluded or is nearing its end.

Litigation Potential: While the patent is nearing or has reached its expiration, past or potential future litigation remains relevant for any compounds or methods developed under its protection during its active term. Litigation risk is generally higher when a patent is in force and covers commercially valuable products.

  • Past Litigation: A review of USPTO and court databases would reveal any prior infringement lawsuits filed by Merck concerning this patent. Such records can indicate enforcement strategies and the patent's perceived strength.
  • Future Considerations: Post-expiration, the focus shifts from infringement litigation to the potential for challenges to the patent's validity (though this is less common after expiration) or continued freedom to operate for competitors based on their own innovations that may build upon the knowledge disclosed in the patent.

Companies developing QC inhibitors or similar therapies should conduct thorough freedom-to-operate analyses to ensure their products do not infringe any valid, in-force patents, including those that may have issued from continuing applications or divisions of the original patent family.

What are the Key Therapeutic Areas and Diseases Addressed?

Patent 7,067,148 specifically targets neurological disorders characterized by the accumulation of amyloid-beta peptides.

Primary Therapeutic Areas:

  • Neurodegenerative Diseases: The central focus is on diseases where amyloid-beta deposition is a hallmark pathology.

Specific Diseases Covered:

  • Alzheimer's Disease (AD): This is the primary disease indication explicitly mentioned. AD is characterized by progressive cognitive decline and the presence of amyloid plaques and neurofibrillary tangles in the brain.
  • Mild Cognitive Impairment (MCI): MCI is a state between normal age-related cognitive decline and the more severe decline of dementia. Amyloid pathology can be present in individuals with MCI who may progress to AD.
  • Dementia of the Alzheimer's Type: This classification refers to the cognitive decline consistent with Alzheimer's disease.

The patent's claims broadly cover "neurological disorders" associated with amyloid-beta accumulation. This phrasing suggests that the invention may also be applicable to other conditions exhibiting similar pathological features, even if not explicitly named.

The rationale behind targeting QC inhibition is to reduce the generation of amyloid-beta, thereby potentially slowing or halting disease progression and alleviating symptoms.

What are the Key Chemical Structures or Classes of Compounds Claimed?

While Patent 7,067,148 claims a method of treatment using a class of compounds (glutaminyl cyclase inhibitors), the specification provides detailed examples of specific chemical entities. The exact chemical structures are complex and often represented by broad generic formulas (Markush structures) that encompass a wide range of variations.

General Characteristics of Claimed Inhibitors:

  • Mechanism of Action: These compounds are designed to inhibit the enzymatic activity of glutaminyl cyclase.
  • Structural Diversity: The patent discloses numerous specific examples, indicating a broad exploration of chemical space around the QC inhibitor scaffold. These examples would detail specific atom arrangements, functional groups, and stereochemistry.
  • Therapeutic Efficacy: The compounds are claimed for their ability to reduce amyloid-beta peptide levels or associated neurological pathologies.

To understand the precise chemical structures, one would need to examine the detailed chemical drawings and formula disclosures within the patent document itself. These typically involve heterocyclic ring systems, specific substituent patterns, and chiral centers, all designed to fit into the active site of the glutaminyl cyclase enzyme and block its function. For instance, specific examples might include compounds with imidazopyridine cores or related heterocyclic structures.

Accessing and analyzing the full patent document is necessary to visualize the specific chemical structures claimed.

What is the Competitive Landscape and Potential for Future Innovation?

The competitive landscape for Alzheimer's disease therapeutics is intense, with numerous approaches being investigated beyond QC inhibition. However, QC inhibitors represent a specific pathway with ongoing research interest.

Competitive Approaches to Alzheimer's Disease:

  • Amyloid-Beta Targeting (Monoclonal Antibodies): Drugs like Aducanumab (Aduhelm), Lecanemab (Leqembi), and Donanemab aim to clear existing amyloid plaques.
  • Tau Protein Targeting: Research into therapies that prevent the aggregation of tau tangles.
  • Neuroinflammation Modulation: Strategies to reduce chronic inflammation in the brain.
  • Synaptic Function Enhancement: Therapies aimed at improving communication between neurons.
  • Metabolic and Vascular Interventions: Addressing underlying vascular or metabolic issues that can contribute to cognitive decline.

Future Innovation Related to QC Inhibitors:

  • Next-Generation Inhibitors: Development of QC inhibitors with improved potency, selectivity, pharmacokinetic profiles (e.g., better brain penetration), or reduced side effects.
  • Combination Therapies: Investigating the use of QC inhibitors in conjunction with other therapeutic agents targeting different aspects of Alzheimer's pathology.
  • Biomarker Development: Identifying biomarkers that can predict patient response to QC inhibition or monitor treatment efficacy.
  • Expanded Indications: Exploring the potential use of QC inhibitors for other neurological or non-neurological conditions where QC activity may play a role.
  • Formulation and Delivery Systems: Novel methods for delivering QC inhibitors to the brain, potentially bypassing the blood-brain barrier more effectively.

Merck's patent has established a foundational claim on the method of using QC inhibitors for specific neurological disorders. Future innovations will likely aim to design novel compounds that are either structurally distinct enough to avoid infringement of existing patents (especially those that have expired) or represent significant improvements over existing technologies.

Key Takeaways

  • Core Technology: United States Patent 7,067,148 protects methods of treating neurological disorders, specifically those involving amyloid-beta peptide accumulation (e.g., Alzheimer's disease), by administering glutaminyl cyclase (QC) inhibitors.
  • Claim Scope: Key claims cover methods of treatment and pharmaceutical compositions utilizing QC inhibitors.
  • Patent Holder: Merck & Co., Inc. is the assignee of the patent.
  • Patent Term: The patent, filed in 2003 and issued in 2006, is nearing or has reached its expiration date (estimated December 23, 2023).
  • Therapeutic Focus: The primary diseases addressed are Alzheimer's disease, mild cognitive impairment, and related dementias.
  • Chemical Scope: The patent covers a class of QC inhibitors, with detailed examples of specific chemical structures provided within the patent specification.
  • Competitive Environment: The field of Alzheimer's therapeutics is highly competitive, with multiple drug modalities under development. Future innovation in QC inhibitors will likely focus on next-generation compounds, combination therapies, and expanded indications.

FAQs

1. What is the expiration date of United States Patent 7,067,148? The patent was filed on December 23, 2003, and issued on June 27, 2006. Based on a standard 20-year term from the filing date, its expiration is estimated to be December 23, 2023.

2. What specific neurological disorders are covered by the patent? The patent explicitly covers Alzheimer's disease, mild cognitive impairment, and dementia of the Alzheimer's type, as well as other neurological disorders characterized by the accumulation of amyloid-beta peptides.

3. Who is the owner of United States Patent 7,067,148? The assignee of United States Patent 7,067,148 is Merck & Co., Inc.

4. What is the mechanism of action for the compounds claimed in the patent? The compounds claimed in the patent are glutaminyl cyclase (QC) inhibitors, designed to reduce the production of amyloid-beta peptides, which are implicated in neurodegenerative diseases like Alzheimer's.

5. Does this patent prevent the development of all Alzheimer's disease treatments? No, this patent specifically covers methods and compositions related to glutaminyl cyclase inhibitors for treating amyloid-beta-related neurological disorders. It does not cover other therapeutic approaches to Alzheimer's disease, such as those targeting tau proteins, neuroinflammation, or utilizing different mechanisms of action, nor does it affect treatments for neurological disorders not characterized by amyloid-beta accumulation.

Citations

[1] Merck & Co., Inc. (2006). Compositions and methods for treating neurological disorders (U.S. Patent No. 7,067,148). Washington, DC: U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 7,067,148

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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