United States Patent 6,017,927: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 6,017,927, titled "Quinuclidine derivatives and medicinal composition thereof," is a significant patent in the pharmaceutical industry, particularly in the treatment of various medical conditions. This patent, held by Astellas Pharma Inc., has been a focal point in several legal and pharmaceutical discussions.
Background of the Patent
The patent was granted for quinuclidine derivatives and their salts, or quaternary ammonium salts, which exhibit muscarinic receptor antagonistic activities. These compounds are particularly useful in treating urologic diseases, respiratory diseases, and other conditions associated with muscarinic receptors[1].
Muscarinic Receptors and Their Subtypes
Muscarinic receptors are part of the cholinergic system and are divided into several subtypes, including M1, M2, and M3. The M1 receptor is primarily found in the brain, the M2 receptor in the heart, and the M3 receptor in smooth muscles and gland tissues. The selective antagonism of these receptors is crucial for targeted therapeutic effects without the broad side effects associated with non-selective antagonists like atropine[1].
Key Claims of the Patent
The patent claims cover specific quinuclidine derivatives and their pharmaceutical compositions. Here are some key aspects:
- Compound Specificity: The patent specifies quinuclidine derivatives with selective antagonistic activities against muscarinic receptors, particularly the M3 receptor, which is involved in smooth muscle and gland tissue functions[1].
- Pharmaceutical Compositions: The patent includes claims for pharmaceutical compositions containing these quinuclidine derivatives, which are formulated for various administration routes[1].
Patent Scope and Claims Analysis
The scope of the patent is defined by its claims, which outline the specific compounds, their structures, and the pharmaceutical compositions that contain them.
- Independent Claim Length and Count: Research on patent scope metrics suggests that the length and count of independent claims can indicate the breadth and clarity of the patent. Narrower claims are often associated with a higher probability of grant and a shorter examination process[3].
- Claim Construction: The construction of claims is critical in determining the patent's scope. For instance, preambles in claims can be limiting if they provide essential elements of the invention or describe the intended use of the claimed methods or compositions[4].
Patent Landscape and Litigation
The patent landscape surrounding US 6,017,927 is marked by significant litigation and enforcement efforts by Astellas Pharma Inc.
- Patent Infringement Lawsuit: Astellas filed a patent infringement lawsuit against Teva Pharmaceutical Industries Ltd. regarding Teva's submission of an abbreviated new drug application (ANDA) for a generic version of solifenacin succinate, marketed under the brand name VESIcare®. Astellas sought to prevent the approval of Teva's ANDA until the expiration of the patent or any later date of exclusivity[2].
- Global Marketing and Exclusivity: Solifenacin succinate, the active ingredient protected by this patent, has been marketed in approximately 50 countries since its launch in Europe in 2004. In the US, it has been co-promoted by Astellas and GlaxoSmithKline since 2005[2].
Pharmaceutical Impact
The patent has significant implications for the treatment of overactive bladder and other conditions.
- Solifenacin Succinate: This compound, protected by the patent, is a selective M3 receptor antagonist used primarily for the treatment of overactive bladder. Its selective action reduces the side effects associated with non-selective muscarinic antagonists[1][2].
Legal and Regulatory Aspects
The enforcement of this patent highlights the importance of intellectual property protection in the pharmaceutical industry.
- Patent Validity and Enforcement: Astellas has vigorously defended the validity of the patent against generic challenges, emphasizing the importance of maintaining exclusivity to protect innovation and investment in drug development[2].
- PTO and Court Decisions: The patent has been subject to various legal proceedings, including those at the U.S. Patent and Trademark Office (PTO) and federal courts, which have scrutinized the claims and scope of the patent[4].
Economic and Market Implications
The patent's impact extends beyond legal and regulatory realms to economic and market considerations.
- Market Exclusivity: The patent's exclusivity period allows Astellas to maintain a monopoly on the market for solifenacin succinate, which is crucial for recouping the significant investment in research and development[2].
- Generic Competition: The expiration of the patent or successful generic challenges can lead to increased competition, potentially reducing prices and expanding access to the medication but also affecting the innovator company's revenue[2].
Conclusion
United States Patent 6,017,927 is a pivotal patent in the pharmaceutical industry, particularly in the treatment of overactive bladder and other muscarinic receptor-related conditions. The patent's scope, claims, and the surrounding legal landscape underscore the importance of intellectual property protection in drug development and the significant economic and market implications of such patents.
Key Takeaways
- Selective Muscarinic Antagonism: The patent covers quinuclidine derivatives with selective antagonistic activities against muscarinic receptors, particularly the M3 receptor.
- Pharmaceutical Compositions: The patent includes claims for pharmaceutical compositions containing these derivatives.
- Litigation and Enforcement: Astellas has actively defended the patent against generic challenges to maintain market exclusivity.
- Global Marketing: Solifenacin succinate, protected by this patent, is marketed globally under the brand name VESIcare®.
- Economic Implications: The patent's exclusivity period is crucial for Astellas to recoup its investment in research and development.
FAQs
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What is the primary use of the compounds protected by US Patent 6,017,927?
- The compounds are primarily used for the treatment of overactive bladder and other conditions associated with muscarinic receptors.
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Which muscarinic receptor subtype is targeted by the compounds in this patent?
- The compounds selectively target the M3 receptor subtype.
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Who is the holder of US Patent 6,017,927?
- The patent is held by Astellas Pharma Inc.
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What is the brand name under which solifenacin succinate is marketed?
- Solifenacin succinate is marketed under the brand name VESIcare®.
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Why did Astellas file a patent infringement lawsuit against Teva?
- Astellas filed the lawsuit to prevent Teva from obtaining approval for a generic version of solifenacin succinate until the expiration of the patent or any later date of exclusivity.
Sources
- US6017927A - Quinuclidine derivatives and medicinal composition thereof - Google Patents
- Astellas filed lawsuit against Vesicare ® generic for patent infringement - Astellas
- Patent Claims and Patent Scope - Hoover Institution
- ELI LILLY AND COMPANY v. TEVA PHARMACEUTICALS - U.S. Court of Appeals for the Federal Circuit
- Details for Patent: 6017927 - DrugPatentWatch
