| Abstract: | The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents. |
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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 5,912,238
What does Patent 5,912,238 cover?
U.S. Patent 5,912,238, granted on June 15, 1999, is titled "Methods of administering and formulations of interferon-β." It primarily protects methods and formulations related to the administration of interferon-beta (IFN-β) for therapeutic use, notably in multiple sclerosis (MS) management.
The patent's core claims focus on specific dosing regimens, formulations containing interferon-beta with particular excipients, and methods to enhance stability, bioavailability, or efficacy. The scope explicitly covers:
- Methods of administering interferon-beta through subcutaneous injections at specified intervals.
- Formulations combining interferon-beta with particular carriers, stabilizers, or excipients, such as polyethylene glycol (PEG).
- Dosing protocols aimed at reducing side effects or improving therapeutic outcomes.
- Use of specified intermediates or conjugates to modify interferon-beta activity.
Covering these aspects establishes broad protection for certain administration techniques and formulation compositions.
What are the broadest and most defensible claims?
The key claims include:
- Claim 1: A method of treating multiple sclerosis in a patient by administering interferon-beta subcutaneously at defined doses and intervals, such as every other day or thrice weekly.
- Claim 2: A pharmaceutical composition comprising interferon-beta and a stabilizing excipient, such as polyethylene glycol or other polymers.
- Claim 5: Use of a particular formulation in reducing immunogenicity or side effects associated with interferon-beta therapy.
The patent's scope encompasses both method claims (administration protocols) and composition claims (formulation components). The durability derives from claims directed at specific dosing frequencies and formulations with unique stabilizing agents.
How does the patent landscape look?
Key competitors and related patents
The patent landscape spanning interferon-beta compositions and administration refers to:
- Patent families prevented from infringement through similar formulations or dosing regimes.
- Early filings on pegylated interferon-beta variants, such as those protected under US patents assigned to companies like Biogen and Schering AG.
Timeline of related patents
| Year |
Patent/Application |
Focus Area |
Assignee or Inventor |
| 1990s |
US 5,955,422 |
Pegylation of interferon-beta |
Schering AG |
| 1997 |
WO 97/00935 |
Methods of treating MS with interferon-beta |
Multiple entities |
| 2000s |
US 6,503,734 |
Pegylated interferon formulations |
Biogen Idec |
Patent expiration and freedom-to-operate (FTO)
- The patent filed in 1997-1998 has expired by 2017-2018, opening the market for generic versions and biosimilars.
- Current active patents that might impact development include newer formulations or delivery methods, often filed in the 2000s to patent improved stability, reduced immunogenicity, or novel conjugates.
Trends and innovation areas
- Pegylation (attachment of PEG molecules) to interferon-beta enhances half-life and reduces dosing frequency.
- Formulations optimizing skinhold or reducing injection site reactions.
- Non-injectable delivery methods, such as inhalation or topical compositions, are emerging areas.
Conclusions on the scope and landscape
Patent 5,912,238 encloses method and formulation claims primarily designed for MS treatment with interferon-beta. Its claims are specific enough to protect certain dosing and composition schemes but may be circumvented by alternative formulations, routes, or dosing protocols. The expiration of the patent broadens options for competitors but leaves room for subsequent innovation and patent filings targeting improved delivery systems or formulations.
Key Takeaways
- The patent covers subcutaneous interferon-beta formulations and administration protocols used for MS therapy.
- Its claims are mostly method- and composition-focused, with some room for alternative approaches.
- The patent landscape includes significant pegylation innovations, with many related patents granted in the late 1990s and early 2000s.
- Expiry of the patent enables generic and biosimilar development, but newer patents on delivery systems remain influential.
- Ongoing innovation emphasizes improved stability, reduced side effects, and alternative delivery routes.
FAQs
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Are the claims of Patent 5,912,238 still enforceable?
No. The patent expired around 2017-2018, removing enforceability restrictions.
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What innovations have emerged since this patent’s filing?
Developments include pegylated interferon-beta variants, non-injectable delivery routes, and improved formulations for stability and immunogenicity.
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How does this patent impact biosimilar development?
Its expiration accelerates biosimilar entry, but newer patents on delivery methods may still pose barriers.
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Which companies held related patents during the patent’s active period?
Biogen, Schering AG, and generic companies like Mylan pursued related formulations and delivery methods.
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Could companies avoid infringing this patent before expiry?
Yes, by developing alternative dosing regimens, delivery methods, or formulations not covered by the claims.
References:
- U.S. Patent No. 5,912,238. (1999). Methods of administering and formulations of interferon-β.
- Walsh, G. (2003). Biopharmaceutical benchmarks: regulatory and commercial considerations. Nature Biotechnology, 21(12), 1383-1386.
- US Patent Files & Pending Applications (1990–2008). Public Patent Databases.
- World Intellectual Property Organization (WIPO). Patent family data on interferon formulations.
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