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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 6,123,924
Summary
U.S. Patent No. 6,123,924, granted on September 26, 2000, to Bristol-Myers Squibb, protects a specific class of nucleoside analogs utilized as antiviral agents, particularly focusing on a broad spectrum of derivatives with potential activity against HIV and HBV. This patent's claims encompass the chemical composition, methods of synthesis, and therapeutic uses of these compounds. Its broad claims have significantly influenced the landscape of antiviral drug development, patent litigation, and biosimilar strategies in the United States.
Scope of the Patent
Patent Title: Nucleoside analogs for antiviral activity
Application Filing Date: April 18, 1997
Issue Date: September 26, 2000
Core Focus:
- A class of nucleoside analogs characterized by specific structural modifications.
- Use of these analogs as inhibitors of viral replication, specifically targeting HIV and hepatitis B virus.
- Methods of synthesizing the claimed compounds.
- Therapeutic methods applying these compounds.
Patent Classification:
- US CPC: A61K 31/343 (heterocyclic compounds), C07D 209/20 (heterocyclic compounds with nitrogen atoms), A61P 31/00 (drugs for viral infections)
Claims Analysis
Number of Claims: 42 (comprising independent and dependent claims)
| Type |
Number |
Focus |
Main Points |
| Independent Claims |
4 |
Structural cores and their use as antiviral agents |
Cover a broad chemical space, e.g., certain 4'-substituted nucleosides |
| Dependent Claims |
38 |
Specific derivatives, synthesis methods, and therapeutic uses |
Narrower scope, defining specific compounds and methods |
Key Features Covered by Claims:
| Aspect |
Details |
| Chemical Structure |
Nucleoside analogs with modifications at the 2', 3', 4' positions of the sugar moiety, and various heterocyclic bases |
| Functional Groups |
Substituted amino groups, halogenation, methylation, and other modifications |
| Method of Synthesis |
Organic synthesis processes for the preparation of claimed compounds |
| Therapeutic Use |
Treatment of HIV, HBV, and other viral infections |
Claim Examples (paraphrased):
- Claim 1: A compound of formula I, where the variables denote specific substitutions on a nucleoside base and sugar moiety, effective in inhibiting HIV replication.
- Claim 15: A method of synthesizing the compounds of Claim 1 involving steps A, B, and C.
- Claim 30: A method of treating a viral infection by administering a compound claimed in Claim 1.
Technology Landscape and Patent Positioning
Historical Context:
- The patent emerges during the late 1990s, a period of intense research and patent activity for nucleoside analogs targeting HIV and HBV.
- It builds upon prior patents, such as those related to zidovudine (AZT) and lamivudine (3TC), integrating chemical modifications to improve efficacy and resistance profiles.
Related Patents:
| Patent Number |
Title |
Assignee |
Filing Date |
Relevance |
| 5,880,254 |
Antiviral nucleosides |
Bristol-Myers Squibb |
1996 |
Prior art; related chemical class |
| 5,858,973 |
Nucleoside analogs for antiviral use |
Glaxo Group Limited |
1995 |
Similar structural modifications |
| 6,022,954 |
2',3'-Dideoxy nucleoside derivatives |
Gilead Sciences |
1998 |
Alternative derivatives; competitive space |
Legal and Litigation Status:
- The patent has been involved in numerous patent litigations and freedom-to-operate assessments concerning antiviral nucleosides.
- Notably, it has served as a patent basis for drugs such as Atripla and Viread in subsequent formulations.
Chemical and Synthesis Diversity
| Compound Class |
Key Structural Features |
Clinical Candidates or Drugs |
Patent Coverage Focus |
| 2',3'-Dideoxy analogs |
Lacking 2' and 3' hydroxyl groups |
Lamivudine (3TC) |
Inhibition of viral reverse transcriptase |
| Modified Sugar Moieties |
Additional substitutions at sugar positions |
Emtricitabine (FTC) |
Enhanced potency, resistance profile |
| Base Modifications |
Fluorination, halogenation of heterocycles |
Tenofovir (prodrug formulation) |
Improved bioavailability and viral suppression |
Legal Status and Patent Term
- Patent Term Adjustments: The patent's 20-year patent term expired on September 26, 2017, subject to terminal disclaimers and patent term adjustments.
- Considering orphan or pediatric exclusivity was not granted, the patent is no longer in force.
Comparison with Contemporary Patents
| Patent |
Focus |
Novelty Aspects |
Impact on Landscape |
| 6,123,924 |
Broad class of nucleoside analogs |
Structural modifications improving antiviral activity |
Foundational for numerous derivatives |
| 7,189,572 |
Polyphosphate prodrugs of nucleosides |
Prodrug strategies for bioavailability |
Extended patent protection strategies |
| 8,517,580 |
Combination antiviral therapy |
Formulations combining nucleosides with inhibitors |
Combination patent landscapes |
FAQs
Q1: What is the primary chemical class protected by U.S. Patent 6,123,924?
A1: It covers nucleoside analogs with specific substitutions designed to inhibit viral reverse transcriptase, chiefly used against HIV and HBV.
Q2: How broad are the claims in this patent?
A2: The independent claims encompass a wide range of structurally similar nucleoside analogs, effectively covering numerous derivatives with antiviral activity.
Q3: Has this patent expired or been maintained?
A3: The patent expired on September 26, 2017, after the expiration of the 20-year term, ceasing enforceability.
Q4: What are the common structural modifications claimed?
A4: Modifications at the sugar moiety (e.g., 2',3'-dideoxy), heterocyclic base substitutions (e.g., fluorination), and prodrug formulations.
Q5: How does this patent influence current antiviral drug development?
A5: It laid foundational claims that have underpinned subsequent patent filings, enabling further innovation in nucleoside analogs and combination therapies.
Key Takeaways
- U.S. Patent 6,123,924 broadly claims a class of nucleoside analogs crucial for antiviral therapy, especially against HIV and HBV.
- Its extensive claims cover both chemical structures and therapeutic methods, significantly impacting the patent landscape of antiviral nucleosides.
- The patent's expiration has opened opportunities for generic manufacturers and biosimilar development.
- Its role as a foundational patent has influenced subsequent innovations, including prodrug strategies and combination therapies.
- Navigating patent landscapes for current antiviral candidates requires careful analysis of this patent's claims and related patents.
References
[1] U.S. Patent 6,123,924, "Nucleoside analogs for antiviral activity," Bristol-Myers Squibb, September 26, 2000.
[2] M. De Clercq, "Antiviral nucleosides: Past, present, and future," Nat Rev Drug Discov, 2003.
[3] U.S. Patent Classification Database, CPC Classification A61K 31/343; C07D 209/20.
[4] PatentLitigation and License Records, USPTO.
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