United States Patent 6,962,940: A Comprehensive Analysis
Introduction
United States Patent 6,962,940, issued on November 8, 2005, is a significant patent in the pharmaceutical sector, particularly in the area of inflammatory disease treatment. This patent, assigned to Celgene Corporation, revolves around the compound (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, hereafter referred to as "Compound A."
Background and Context
Compound A is a stereomerically pure enantiomer that has shown promise in treating various inflammatory diseases by inhibiting the activity of tumor necrosis factor-alpha (TNF-α)[4].
Scope of the Patent
The patent encompasses several key aspects:
Compound and Its Forms
The patent describes various solid forms of Compound A, including single-component crystal forms, multiple-component crystal forms (such as co-crystals and solvates, including hydrates), single-component amorphous forms, and multiple-component amorphous forms. These forms are designed to have advantageous physical and chemical properties, enhancing their utility in manufacturing, processing, formulation, and storage[1][4].
Pharmaceutical Applications
The patent covers the use of Compound A and its various forms for treating diseases and disorders, particularly those implicated by TNF-α. This includes conditions such as chronic obstructive pulmonary disease (COPD), allergic rhinitis, and other inflammatory diseases[4].
Biological Properties
The solid forms of Compound A are noted for their improved bioavailability and biological activity. This is crucial for ensuring the efficacy of the compound in therapeutic applications[1].
Claims of the Patent
The patent includes several claims that define the scope of protection:
Compound A and Its Enantiomer
The primary claim is for the stereomerically pure (+)-enantiomer of Compound A, substantially free of its (−) isomer[4].
Solid Forms
Claims cover various solid forms, including crystal forms, co-crystals, solvates (including hydrates), and amorphous forms. These forms are specified to have particular physical and chemical properties beneficial for pharmaceutical use[1].
Pharmaceutically Acceptable Salts and Prodrugs
The patent also claims pharmaceutically acceptable salts, solvates, hydrates, co-crystals, prodrugs, and polymorphs of Compound A. These are important for enhancing the compound's stability, solubility, and bioavailability[1][4].
Methods of Treatment
Claims include methods for treating diseases and disorders by reducing the level of cytokines and their precursors in mammals using Compound A and its various forms[4].
Patent Landscape and Related Patents
The patent landscape surrounding U.S. Patent 6,962,940 is complex and involves several related patents:
Patent Expiration and Generic Competition
The patent has expired as of March 19, 2023, which opens the door for generic competition. Other related patents, such as U.S. Patents 7,208,516, 7,427,638, and others, also have expiration dates ranging from 2023 to 2034[2].
Litigation and Patent Challenges
The patent has been part of various legal proceedings, including challenges to its validity and infringement cases. These proceedings can affect the patent's enforceability and the timing of generic entry into the market[3].
Industry Impact
The expiration of U.S. Patent 6,962,940 and related patents has significant implications for the pharmaceutical industry:
Generic Entry
Generic versions of the drug can now be approved and marketed, potentially reducing costs for patients and increasing competition in the market[2].
Research and Development
The expiration of these patents may also spur further research and development in the area of inflammatory disease treatments, as companies may now build upon or modify the existing compounds without patent restrictions.
Key Takeaways
- Compound A: The patent revolves around the stereomerically pure (+)-enantiomer of Compound A.
- Solid Forms: Various solid forms of Compound A are covered, including crystal, co-crystal, solvate, and amorphous forms.
- Therapeutic Applications: The compound is used for treating inflammatory diseases implicated by TNF-α.
- Patent Expiration: The patent has expired, allowing for generic competition.
- Related Patents: Several related patents have different expiration dates, influencing the overall patent landscape.
FAQs
What is the primary compound covered by U.S. Patent 6,962,940?
The primary compound is (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, known as Compound A.
What are the various solid forms of Compound A covered by the patent?
The patent covers single-component crystal forms, multiple-component crystal forms (including co-crystals and solvates), single-component amorphous forms, and multiple-component amorphous forms.
What diseases are treated using Compound A?
Compound A is used to treat diseases and disorders implicated by TNF-α, such as chronic obstructive pulmonary disease (COPD) and allergic rhinitis.
Has U.S. Patent 6,962,940 expired?
Yes, the patent expired on March 19, 2023.
What is the impact of the patent's expiration on the pharmaceutical industry?
The expiration allows for generic versions of the drug to be approved and marketed, potentially reducing costs and increasing competition.
Cited Sources
- European Patent Application EP 2 695 616 A1 - Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione[1].
- FDA Approval Letter for Apremilast Tablets - Bioequivalence and therapeutic equivalence determination[2].
- The BioLoquitur Bulletin - Overview of patent litigation and generic competition[3].
- U.S. Patent 6,962,940 B2 - Stereomerically pure (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione[4].
- U.S. Patent 8,629,173 B2 - Related patent covering various aspects of Compound A[5].
