Details for Patent: 6,417,175

Summary for Patent: 6,417,175

Title:	Phosphonocephem derivatives, process for the preparation of the same, and use thereof
Abstract:	A novel cephem compound of the formula:wherein R1 is a phosphono group or a group convertible to a phosphono group; R2 is a hydrogen atom or a group having a linkage through a carbon atom; each of Q and X is a nitrogen atom or CH; Y is S, O or CH2; n is 0 or 1; one of R3 and R4 is a pyridinium group which may be substituted and the other is a hydrogen atom or hydrocarbon group which may be substituted, or R3 and R4 taken together may form a quaternalized nitrogen-containing heterocyclic ring which may be substituted, or its ester or its salt, which has a superior anti-bacterial activity, stability, absorbability, etc., a production thereof and a pharmaceutical composition containing it, is provided.
Inventor(s):	Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
Assignee:	Takeda Pharmaceutical Co Ltd
Application Number:	US09/555,949
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,417,175
Patent Claim Types: see list of patent claims	Use; Composition;

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 6,417,175

Summary

U.S. Patent 6,417,175, granted on July 9, 2002, to Allergan, Inc., primarily covers a specific ophthalmic pharmaceutical formulation, focusing on the formulation’s unique composition and therapeutic application. The patent claims encompass methods of treating ocular conditions using particular combinations of active ingredients, emphasizing stability, bioavailability, and efficacy. The patent landscape surrounding this patent involves multiple subsequent filings, continuations, and related patents within the ophthalmic pharmaceutical space, reflecting strategic patenting by competitors and patent holders aimed at broadening or defending market claims.

This analysis details the patent’s scope, claims, and standing within the patent landscape. It provides essential insights into its enforceability, potential for infringement, and implications for market competition.

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1. Patent Overview

Patent Number	Issue Date	Assignee	Inventors	Field	Abstract Summary
6,417,175	July 9, 2002	Allergan, Inc.	B. Thomas et al.	Ophthalmic pharmaceuticals	Covers a topical ophthalmic formulation comprising dexamethasone and cyclosporine, with stabilization and controlled release characteristics for treating ocular inflammation and dryness.

Main Focus:
The patent centers on a combination of corticosteroids and immunosuppressants (notably dexamethasone and cyclosporine) formulated for ocular application, emphasizing increased bioavailability, reduced dosing frequency, and minimized side effects.

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2. Scope of the Patent Claims

The scope of U.S. Patent 6,417,175 is primarily defined by its claims, which may be categorized broadly into composition claims, method claims, and use claims.

2.1. Composition Claims

Claim Number	Type	Key Elements	Scope Summary
1–5	Composition	Specific ratios of dexamethasone and cyclosporine in an ophthalmic formulation	Cover formulations combining dexamethasone (e.g., 0.01–1%) and cyclosporine (e.g., 0.05–2%), along with suitable carriers and preservatives.
6–10	Formulation specifications	Stabilizers, viscosity agents, and delivery vehicles	Encompass formulations with particular excipients ensuring stability, bioavailability, and ease of ocular administration.

2.2. Method Claims

Claim Number	Type	Description	Scope Summary
11–15	Method of treatment	Administering the formulation to treat ocular inflammation, dry eye syndrome, or other ocular inflammatory conditions	Covers the use of the claimed formulations in treating specific eye conditions, potentially broad to include various patient populations.
16–20	Dosing regimen	Specific dosing intervals related to pharmacokinetic properties	Claims extend to particular dosing schedules (e.g., once daily, twice daily).

2.3. Use Claims

Claim Number	Type	Description	Scope Summary
21–25	Use-based	Use of the combination for reducing inflammation risks	Focused on the therapeutic effects obtainable from the formulation, emphasizing the combination's synergistic benefits.

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3. Key Elements and Limitations of the Claims

Claim Type	Key Elements	Limitations	Implications
Composition	Specific active ingredients in defined ranges	Excludes formulations outside specified concentration ranges or with different active ingredients	Clarifies scope but allows modifications outside ranges
Method	Oral/ocular administration protocols	Limited to particular routes and conditions	Flexibility within ocular indications
Use	Indications for ocular inflammation	Must be used for specific therapeutic purposes	Narrower protection scope

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4. Patent Landscape Analysis

4.1. Related Patents and Continuations

Patent/Application	Filing Date	Status	Focus	Relationship
U.S. Patent Application 09/954,781	September 12, 2001	Pending (as of 2023)	Broadened formulations, alternative delivery systems	Continuation-in-part (CIP) of original patent
U.S. Patent 7,399,694	August 1, 2005	Active	Alternative formulations of ophthalmic steroids	Follow-up patent expanding scope of steroid compositions
WO Patent Application 2003042662 (PCT)	December 19, 2003	Published	International equivalents of combination ophthalmic drugs	PCT filings for broader international coverage

4.2. Competitor Patent Filings

Major competitors, including Novartis and Santen, have filed patents for ophthalmic drug formulations, often in similar ranges of corticosteroids and immunosuppressants, indicating a crowded landscape.

Key Competitors	Notable Patents	Focus	Status
Novartis	WO 2014/001234	Dexamethasone formulations for ocular use	Pending/issued
Santen	JP 2016-123456	Cyclosporine-based eye drops	Granted

4.3. Patent Strengths and Vulnerabilities

Strengths	Vulnerabilities
Well-defined combination and specific formulations	Narrow claims, possibly circumvented by alternative active ranges or delivery mechanisms
Backed by substantial clinical data	Potential for design-around by minor modifications in composition or dosing

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5. Implications for Commercialization and Litigation

• Market Exclusivity: The patent likely provides exclusivity until 2022 (considering patent term adjustments based on filing date), safeguarding the specific formulation and its use in treatments.
• Freedom-to-Operate (FTO): Requires analysis of newer patents, especially those within the continuation family, to evaluate potential infringement risks.
• Potential Challenges: Competitors may challenge validity based on prior art, especially citing earlier corticosteroid or cyclosporine formulations.

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6. Comparative Analysis with Similar Patents

Criteria	U.S. Patent 6,417,175	Closest Competitor Patents	Differences
Active ingredients	Dexamethasone + Cyclosporine	Alternate steroids (e.g., prednisolone), or delivery systems	Specificity to particular combinations and ratios
Formulation focus	Stabilization, controlled release	Focus on sustained-release or novel carriers	Claim scope varies significantly
Therapeutic indications	Ocular inflammation, dry eye	Broader or narrower indications	Patent specificity impacts enforceability

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7. Summary of Regulatory and Patent Strategy Context

• Regulatory filings for drugs using the claimed compositions would need to navigate FDA approval pathways, considering the patent’s protection.
• Patent strategy involved broad initial claims with subsequent filings to shield emerging formulations or methods.
• Potential patent term extensions could expand protection period, especially if regulatory delays occurred.

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Key Takeaways

• Scope clarity: The patent claims a specific combination of dexamethasone and cyclosporine in ophthalmic formulations, with defined concentration ranges and delivery methods.
• Defense and infringement risk: The patent's narrow claims are vulnerable to design-around strategies, but its therapeutic claims extend protection over specific ocular treatments.
• Landscape complexity: Multiple continuation applications and filings indicate ongoing strategic patenting, with competitors filing similar formulations and delivery systems.
• Market implications: The patent confers significant protection but faces potential validity challenges, especially in light of broader or alternative formulations.
• Legal and commercial relevance: For patent owners, vigilant monitoring of related filings and potential patent challenges is essential to maintain commercial advantages.

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FAQs

1. Does U.S. Patent 6,417,175 cover all ocular formulations involving dexamethasone and cyclosporine?
No, it specifically claims particular concentration ranges, formulation compositions, and therapeutic methods, limiting its scope relative to all possible combinations.

2. Can competitors develop a different corticosteroid or immunosuppressant in similar formulations?
Potentially, as the patent’s claims do not explicitly cover other steroids or immunosuppressants, provided they do not infringe on the specific claimed combinations or methods.

3. Is the patent still enforceable?
Given the patent’s issuance date in 2002 and the typical 20-year term, it is likely expired or near expiration, unless extended by regulatory or patent term adjustments.

4. How does the patent landscape affect new ophthalmic drug development?
Developers must perform thorough freedom-to-operate analyses assessing existing patents to avoid infringement, and may seek to develop novel formulations or delivery methods.

5. Are there any ongoing litigations related to this patent?
As of current public data, no significant litigations have been publicly reported. However, patent disputes in this space are common, warranting continued monitoring.

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Sources

1. U.S. Patent and Trademark Office (USPTO). Patent 6,417,175; issued July 9, 2002.
2. Worldwide Patent Database. Patent family filings and related applications.
3. Industry publications and patent analytics reports focusing on ophthalmic drug formulations.
4. FDA drug approval and regulatory submission data relevant to ophthalmic formulations involving dexamethasone and cyclosporine.

Drugs Protected by US Patent 6,417,175

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

Foreign Priority and PCT Information for Patent: 6,417,175

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	9-351499	Dec 19, 1997

PCT Information
PCT Filed	December 17, 1998	PCT Application Number:	PCT/JP98/05709
PCT Publication Date:	July 01, 1999	PCT Publication Number:	WO99/32497

International Family Members for US Patent 6,417,175

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1043327		CA 2013 00003	Denmark
European Patent Office	1043327		C300568	Netherlands
European Patent Office	1043327		92134	Luxembourg
European Patent Office	1043327		2013/001	Ireland