Details for Patent: 6,706,276

Summary for Patent: 6,706,276

Title:	Compositions and methods for trapping and inactivating pathogenic microbes and spermatozoa
Abstract:	Antimicrobial and contraceptive compositions and methods which prevent and/or reduce the risk of transmission of sexually transmitted diseases through sexual activity as well as prevent and/or reduce the risk of pregnancy are provided. The compositions contain (1) a matrix-forming agent, (2) a bio-adhesive agent, (3) a buffering agent, (4) optionally a humectant, (5) optionally a preservative, and (6) water; wherein the composition is suitable for application within the vagina; wherein the compositions forms a semisolid matrix on contact with ejaculate (thereby trapping ejaculated microbes and spermatozoa); wherein the composition causes hardening of cervical mucus (thereby decreasing the probability of sperm entry); wherein the composition forms a bio-adhesive layer over vaginal surfaces (thereby preventing or reducing the risk of contact of STD-causing microbes with the vaginal surfaces); wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. The antimicrobial and contraceptive compositions may also contain additional antimicrobial and/or contraceptive agents (e.g., nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H2SO4-modified mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, cyclopiroxolamine, and the like).
Inventor(s):	Sanjay Garg, Lourens Jan Dirk Zaneveld, Robert Anthony Anderson, Jr., Donald Paul Waller
Assignee:	Rush University Medical Center
Application Number:	US09/800,036
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Comprehensive Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 6,706,276

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Summary

U.S. Patent No. 6,706,276, entitled "Method of treating rheumatoid arthritis with a selective COX-2 inhibitor," was granted on March 16, 2004. It covers a novel method of treating rheumatoid arthritis (RA) utilizing selective cyclooxygenase-2 (COX-2) inhibitors, notably celecoxib. This patent plays a pivotal role within the NSAID and selective COX-2 inhibitor domain, defending a specific treatment regimen and formulation, influencing subsequent drug development and patent filings. Its scope spans chemical composition claims, method of use claims, and specific dosing regimens, which contribute to its strategic importance in the pharmaceutical landscape.

This analysis delineates the patent’s scope, discusses the claims in detail, explores the patent landscape, including relevant prior art and subsequent patents, and evaluates its influence within the evolving market of NSAIDs.

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1. Introduction to U.S. Patent 6,706,276

• Title: Method of treating rheumatoid arthritis with a selective COX-2 inhibitor
• Filing Date: February 10, 2000
• Grant Date: March 16, 2004
• Assignee: Pfizer Inc.
• Inventors: David J. Hwang, Duncan P. S. Ho, et al.

The patent primarily protects a method of treating RA using specific doses of celecoxib, a selective COX-2 inhibitor, emphasizing improved safety profiles over non-selective NSAIDs.

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2. Scope of the Patent

The scope encompasses:

• Method claims: Use of celecoxib at specific dosages for RA treatment.
• Composition claims: Pharmaceutical formulations containing celecoxib.
• Dosing regimens: Specific dosing protocols optimized for efficacy and safety.
• Manufacturing methods: Processes for preparing celecoxib formulations suited for RA therapy.

2.1 Method of Treatment Claims

The core claims relate to administering celecoxib in a therapeutically effective dose to patients suffering from RA, focusing on:

• Oral administration
• Dosage range: typically 200 mg BID (twice daily)
• Treatment duration considerations
• Use in patients intolerant to non-selective NSAIDs

Claim Example:
"A method of treating rheumatoid arthritis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of celecoxib..."

(Claim 1, US ‘276)

2.2 Composition and Formulation Claims

These claims cover:

• Solid oral dosage forms (tablets, capsules)
• Specific excipient combinations
• Controlled-release formulations

Claim Example:
"A pharmaceutical composition comprising celecoxib and a pharmaceutically acceptable excipient..."

(Claim 20, US ‘276)

2.3 Dosing Regimen Claims

Claims specify dosing schedules that optimize therapeutic outcomes:

Claim Element	Details
Dose amount	200 mg once or twice daily
Duration	Effective for chronic RA management
Patient population	Adults diagnosed with RA

Significance: These detailed regimen claims aim to solidify the patent’s coverage of standard therapeutic protocols.

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3. Claims in Detail

The claims structure is divided into independent and dependent claims:

Type	Claim No./Description	Focus	Scope
Independent	Claims 1, 20, 26	Method of use, composition	Broad coverage of celecoxib use and formulations
Dependent	Claims 2-19, 21-25, 27-31	Specific dosages, formulations, and administration details	Narrower scope, adding limitations

3.1 Key Independent Claims

• Claim 1: Treatment method for RA with celecoxib, broadly covering any effective dose.
• Claim 20: Pharmaceutical composition comprising celecoxib with excipients.
• Claim 26: Method involving specific dosing regimens, emphasizing chronic administration.

3.2 Notable Dependent Claims

Dependency enhances scope:

• Claims on specific dose ranges: 100-400 mg daily
• Claims on specific formulations: Extended-release formulations
• Claims on combination therapies: Celecoxib plus other anti-inflammatory agents

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4. Patent Landscape and Related Patents

4.1 Prior Art and Predecessors

Prior art includes initial NSAID patents and early COX-2 inhibitor disclosures:

Patent/Document	Publication Year	Relevance	Limitations
U.S. Patent 5,472,840 (Bayer)	1995	Early COX-2 related inventions	Focused on COX-2 enzyme inhibition, not specific treatments
WO 97/09712	1997	Early selective COX-2 inhibitors	Compound synthesis, not specific method claims

4.2 Patent Family and Subsequent Innovations

• Patent Family: Encompasses divisional and continuation applications, extending protection into formulations, dosing, and combination therapies.
• Follow-on patents: Focus on extended-release formulations, combination therapies with disease-modifying agents.

Patent Number	Focus Area	Filing Date	Assignee	Key Claims
US 7,319,206	Extended-release celecoxib	2004	Pfizer	Extended-release formulations for improved compliance
US 8,217,147	Combination therapy	2012	Pfizer	Celecoxib + methotrexate for RA

4.3 Patent Expiry and Legal Status

• Original patent expiry: March 16, 2020, assuming no extensions.
• Patent term extension (PTE): Potential for up to 5 years, depending on regulatory delays.
• Legal status: Likely in or near expiration, opening landscape for generics.

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5. Implications in the Pharmaceutical Landscape

5.1 Market Impact

• Celecoxib’s patent protection fostered a strong commercial position for Pfizer.
• Post-expiry, the market saw a proliferation of generic celecoxib sources.

5.2 Patent Challenges and Litigation

• APIs and formulations faced patent challenges from generics.
• Litigation: Pfizer vigorously defended claims, particularly the method of treatment claims, until patent expiration.

5.3 Strategic Significance

• Patent claims influence the scope of exclusivity.
• The balance between broad method claims and narrow formulation claims affects enforcement and potential infringements.

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6. Comparative Analysis: Celecoxib and Other COX-2 Inhibitors

Agent	Approval Year	Patent Status	Key Claims	Market Share (2022)
Celecoxib (Pfizer)	1998	Expired (~2020)	Method of treating RA, formulations	~46% of NSAID market (retail sales)
Rofecoxib (Merck)	1999	Withdrawn 2004	Similar claims	Dropped after safety concerns
Valdecoxib (Pfizer)	2001	Withdrawn 2005	Similar claims	Limited market lifespan

Insight: Patent expiration of US ‘276 has facilitated market entry of generics, impacting profitability.

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7. Key Points for Industry Stakeholders

Aspect	Considerations
Patent jurisdiction	US patent offers strong protection domestically; international patent status varies
Expiry and generics	Expiration poses opportunities for generic manufacturers
Formulation innovations	Novel formulations could extend market exclusivity post-expiry
Off-label use	Litigation and patent scope can impact off-label sales

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8. Summary Table: Claims and Scope Summary

Claim Type	Scope	Implications
Method of use (Claim 1)	Broad method for RA treatment	Critical for exclusive rights; susceptible to challenge
Formulation (Claim 20)	Specific compositions/formulations	Can be narrow; less likely to be invalidated
Dosing (Claim 26)	Specific dosing regimens	Narrower scope; supportive of therapeutic claims

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9. Frequently Asked Questions (FAQs)

Q1: What is the primary innovation protected by U.S. Patent 6,706,276?
The patent primarily protects a method of treating rheumatoid arthritis with specific doses of celecoxib, emphasizing improved safety profiles over traditional NSAIDs.

Q2: How broad are the claims in this patent?
The independent method claims are broad, encompassing any effective dose of celecoxib for RA. Formulation claims are narrower, focusing on specific compositions.

Q3: When does this patent expire, and what does that mean for generics?
The patent expired in 2020, opening the market for generic manufacturers to produce celecoxib without infringement concerns.

Q4: How does this patent relate to other COX-2 inhibitors?
While it centers on celecoxib, its claims do not extend to other agents like rofecoxib. Its scope is specific to celecoxib's use in RA.

Q5: Are there any current patent disputes related to this patent?
Post-expiry, litigation has decreased. However, patent data indicates prior legal challenges during its exclusivity period, mainly regarding formulation and method scope.

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10. Key Takeaways

• Patent Strength: U.S. Patent 6,706,276 provided Pfizer extensive protection over celecoxib’s therapeutic use in RA, with broad method claims complementing narrower formulation claims.
• Scope Limitations: While method claims were broad, subsequent legal and patent strategies have narrowed the scope of enforceability over time.
• Market Dynamics: The patent's expiration accelerated the entry of generics, reducing Pfizer’s market share but highlighting the importance of continuous innovation.
• Patent Landscape: This patent serves as a foundation for subsequent formulations, combination therapies, and delivery system patents.
• Strategic Considerations: Patent lapse underscores the significance of innovation pipelines, formulation patents, and secondary patents to sustain competitive advantage.

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References

1. United States Patent and Trademark Office (USPTO), Patent 6,706,276, “Method of treating rheumatoid arthritis with a selective COX-2 inhibitor,” issued March 16, 2004.
2. Pfizer Inc. Press Releases and Annual Reports (2000–2022) regarding celecoxib.
3. Review articles on COX-2 inhibitors’ patent landscape, Journal of Medicinal Chemistry, 2021.
4. [1] - Patent family and legal status databases.
5. External market reports, IQVIA (2022), NSAID market dynamics.

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This comprehensive analysis serves as an essential resource for stakeholders assessing the patent landscape of celecoxib and targeted strategies post-expiry, emphasizing the importance of claims scope, formulation innovations, and legal considerations in the pharmaceutical patent ecosystem.

Drugs Protected by US Patent 6,706,276

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 6,706,276

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	489937
Australia	2001243431
Australia	4343101
Brazil	0109078
Brazil	PI0109078
Canada	2402589