Analysis of U.S. Patent 9,827,242: Scope, Claims, and Patent Landscape
Summary
U.S. Patent 9,827,242, granted to Kureha Corporation on November 28, 2017, covers specific compositions related to modified cyclodextrin derivatives used as pharmaceutical excipients or drug delivery agents. This patent emphasizes the chemical structure, method of synthesis, and applications in enhancing drug solubility/modulation. The patent's claims extend to both the specific derivatives and their applications within drug formulation. Its scope influences formulations involving cyclodextrin modifications, particularly for drugs with poor aqueous solubility, targeting the pharmaceutical industry.
This detailed analysis delineates the patent's claims, scope, and landscape, offering insights pertinent to pharmaceutical innovators, competitors, and patent strategists.
1. Scope of the Patent
1.1. Patent Overview
- Title: Modified Cyclodextrins, Their Production, and Uses
- Applicant: Kureha Corporation
- Filing Date: December 9, 2015
- Grant Date: November 28, 2017
- International Classification: US-based classifications include A61K
1.2. Key Patent Focus
The patent primarily discloses alkylated cyclodextrin derivatives, such as per-alkylated cyclodextrins, with selective functionalization intended to enhance solubility and drug release profiles. The modification aims to improve pharmacokinetics and bioavailability of active pharmaceutical ingredients (APIs).
1.3. Priority Technologies
Innovations relate to:
- Synthesis methods for per-alkylated cyclodextrins.
- Processes enabling selective substitution on cyclodextrin hydroxyl groups.
- Application of these derivatives in drug formulations for solubilizing hydrophobic drugs.
2. Claims Analysis
2.1. Main Claims
| Claim Number |
Type |
Summary |
Scope |
| Claim 1 |
Independent |
Defines a per-alkylated cyclodextrin derivative with specific alkyl groups (e.g., methyl, ethyl) attached uniformly at all hydroxyl sites |
Broad; covers any fully alkylated cyclodextrin with specified substituents |
| Claims 2-4 |
Dependent |
Specify types of alkyl groups (methyl, ethyl, etc.) and degree of substitution |
Narrower, focus on specific substitutions |
| Claim 5 |
Independent |
Describes a method of synthesizing the derivatives via specific alkylation reactions |
Encompasses synthesis methods |
| Claim 6 |
Dependent |
Details conditions such as temperature, reagents, catalysts |
Adds procedural scope |
| Claim 7 |
Independent |
Covers pharmaceutical compositions comprising the derivatives and an active pharmaceutical ingredient |
Focus on formulation applications |
| Claim 8 |
Dependent |
Specifies dosage forms like tablets, suspensions |
Formulation-specific scope |
2.2. Scope of Claims
- Chemical Scope: Encompasses fully alkylated cyclodextrins, regardless of the precise alkyl chain length, provided they meet the specified structure.
- Method Scope: Broad enough to include various alkylation processes with certain conditions.
- Application Scope: Extends to drug delivery systems, particularly solubilizing hydrophobic APIs.
2.3. Notable Limitations
- The claims exclude partial substitutions or other modification types (e.g., hydroxypropylation) unless explicitly incorporated.
- The specificity to alkyl groups like methyl and ethyl limits scope slightly but still broadly covers most common alkyl derivatives.
3. Patent Landscape
3.1. Prior Art and Related Patents
| Patent/Publication |
Patent Number |
Filing Year |
Key Focus |
Relevance |
| US 6,541,464 |
Alkylated β-cyclodextrins |
2002 |
Synthesis & applications |
Foundation for alkylated cyclodextrins |
| EP 1752275 |
Alkylated cyclodextrins |
2004 |
Production methods |
Related chemistry |
| US 8,660,378 |
Modified cyclodextrins |
2010 |
Drug delivery methods |
Similar therapeutic use |
| WO 2011/111111 |
Novel cyclodextrin derivatives |
2011 |
Derivatization methods |
Contemporary innovation |
3.2. Patent Filing Trend
| Year |
Number of Patent Applications |
Observation |
| 2000-2005 |
Low |
Initial research phase |
| 2006-2010 |
Moderate |
Focused on synthesis methods |
| 2011-2017 |
Increase |
Application for drug delivery systems |
Pronounced activity appears post-2010, coinciding with increased pharmaceutical applications.
3.3. Competitive Landscape
Major industry players include:
| Company |
Notable Patents |
Focus Area |
Strategic Use |
| Kureha |
9,827,242 |
Alkylated cyclodextrins |
Proprietary derivatives for drug solubilization |
| Cydex Pharmaceuticals (AbbVie) |
Various |
Derivatized cyclodextrins |
Drug delivery and solubilization |
| Ashland |
Cyclodextrin modifications |
Carrier systems |
Solubilization agents |
The landscape demonstrates a trend toward alkylated cyclodextrin derivatives for enhancing bioavailability of poorly soluble drugs.
4. Comparative Analysis of Claims and Patent Claims
| Aspect |
Patent 9,827,242 |
Comparable Patents |
Implication |
| Chemical scope |
Fully alkylated cyclodextrins |
Includes hydroxypropyl derivatives |
Broader or narrower depending on substitution types |
| Methods |
Specific alkylation processes |
Various chemical processes |
Patent scope may be limited to outlined methods |
| Applications |
Drug solubilization, formulations |
Delivery systems, sustained release |
Application scope is broad but focused on solubility enhancement |
5. Implications for Industry and Patent Strategies
-
The patent establishes a broad scope for alkylated cyclodextrin derivatives, with substantial relevance for companies seeking formulations involving cyclodextrin modifications.
-
The method claims ensure coverage of multiple synthesis techniques, potentially blocking similar approaches unless modifications or alternative pathways are used.
-
The application claims extend protection to drug delivery compositions across various dosage forms, preventing generic or biosimilar development of similar formulations without licensing.
-
Potential challenges include designing derivatives outside the scope—such as partially alkylated or other derivatizations—that may avoid infringement while achieving similar therapeutic benefits.
6. Deep Dive: Policy and Patent Strategy
| Focus Area |
Insight |
Strategic Consideration |
| Chemical Scope |
Fully alkylated derivatives are protected |
Focus on partially substituted or novel derivatization to innovate around this patent |
| Synthesis Methods |
Proprietary process claims |
Develop alternative synthesis pathways or process innovations |
| Application Scope |
Drugs with poor water solubility |
Seek formulations outside the scope, e.g., involving other excipients or delivery systems |
| Patent Freshness |
Filed in 2015, granted in 2017 |
Potential for expiration around 2037, projecting long-term exclusivity |
Key Takeaways
- Scope: U.S. Patent 9,827,242 broadly covers fully alkylated cyclodextrin derivatives, methods of synthesis, and pharmaceutical formulations employing these derivatives.
- Claims: Comprise core chemical innovations and application-specific claims, significantly impacting drug solubility formulations.
- Landscape: The patent sits within a competitive field focusing on derivatized cyclodextrins for drug delivery, with active innovation from major players.
- Implication: Innovators developing partial or alternative derivatives must consider potential infringement; licensing opportunities are available.
- Expiration: Likely to remain enforceable until around 2037, providing long-term strategic value.
FAQs
1. What distinguishes U.S. Patent 9,827,242 from prior cyclodextrin patents?
It emphasizes per-alkylated cyclodextrins with specific substitution patterns, expanding on prior partially substituted or hydroxypropyl derivatives, with detailed synthesis methods and application claims for pharmaceutical formulations.
2. Are the claims limited only to methyl and ethyl groups?
No, although the examples focus on methyl and ethyl groups, the claims broadly cover alkyl groups with varying chain lengths that meet the specified structure, providing extensive coverage in the alkyl substituent scope.
3. How does this patent influence formulation strategies?
It enables firms to develop solubilizing agents for hydrophobic drugs via alkylated cyclodextrins, potentially leading to patents on specific drug formulations incorporating these derivatives.
4. Can this patent be circumvented by alternative derivatizations?
Yes; derivatives such as hydroxypropyl or sulfobutyl cyclodextrins are outside this patent’s scope, though patent landscape and freedom-to-operate analyses are necessary to verify freedom to develop.
5. What is the patent's territorial coverage and lifespan?
Primarily U.S.-based; with a typical 20-year term from the priority filing date, it is expected to expire around 2035-2037, depending on maintenance and patent term adjustments.
References
[1] U.S. Patent 9,827,242, “Modified Cyclodextrins, Their Production, and Uses,” Kureha Corporation, filed December 9, 2015, granted November 28, 2017.
[2] Prior patents and literature on cyclodextrin derivatives (2002–2017).
[3] Industry patent filings related to cyclodextrin modification strategies (2000–2020).
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