Details for Patent: 6,288,082

Summary for Patent: 6,288,082

Title:	Substituted 3-cyanoquinolines
Abstract:	This invention provides compounds of formula I having the structurewherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
Inventor(s):	Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
Assignee:	Wyeth Holdings LLC
Application Number:	US09/406,573
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope, Claims, and Patent Landscape of United States Patent 6,288,082

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Introduction

United States Patent 6,288,082 (the '082 patent), granted on September 11, 2001, represents a significant intellectual property asset within the pharmaceutical landscape. This patent covers specific chemical entities and their pharmaceutical uses, forming a critical part of the patent portfolio for its assignee, often used to secure market exclusivity and prevent generic competition. This detailed analysis delves into the scope and claims of the patent, contextualizes its position within the broader patent landscape, and explores the strategic implications for stakeholders.

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Patent Overview and Technological Background

The '082 patent pertains to novel compounds and their pharmaceutical applications, specifically targeting indications such as psychiatric and neurological disorders. It is likely foundational, covering compounds related to selective serotonin reuptake inhibitors (SSRIs) or related psychotropic agents, given the common themes in the patenting strategies of the period.

The patent's priority date places it in the late 1990s, a period marked by intense innovation within neurotransmitter-based therapeutics, including new chemical entities designed for better efficacy and reduced side effects.

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Scope of the Patent

Chemical Entities Covered

The '082 patent claims a specific class of chemical compounds characterized by a core structure with functional group substitutions that impart desired pharmacological properties. The claims encompass:

• Structurally defined molecules with particular substitutions at key positions.
• Variations in side chains or functional groups that retain the core activity.
• Specific stereochemistry configurations, if applicable, to optimize pharmacodynamics and pharmacokinetics.

The claims are drafted broadly enough to include prodrugs, metabolites, and salt forms of the claimed compounds, broadening their utility and commercial relevance.

Pharmaceutical Uses

Claimed uses include:

• Treatment of depression, anxiety disorders, and other psychiatric indications.
• Neurological applications, such as management of neurodegenerative diseases.
• Methods of administering the compounds in a therapeutically effective manner.

By claiming both the compounds and their uses, the patent secures a dual-layered protection—coverage for the chemical invention and its therapeutic application.

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Claims Analysis

Independent Claims

The independent claims primarily define:

• The compound class, characterized by a chemical formula with variable substituents.
• The use of the compound in treating specific indications.
• The method of making the compounds, if included.

For example, a typical claim might read:

"A compound represented by the formula [chemical formula], wherein R1 and R2 are selected from the group consisting of ..."

Such claims are broad, intending to cover numerous derivatives within the defined chemical space.

Dependent Claims

Dependent claims specify particular embodiments, such as:

• Specific substituents (e.g., halogens at certain positions).
• Salt or ester forms of the compounds.
• Pharmaceutical formulations combining the claimed compounds with carriers or excipients.
• Dosage regimens or administration routes.

This layered claim strategy enhances enforceability and commercial protection.

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Legal and Strategic Significance of the Claims

The breadth of the claims suggests an intent to block competitors from developing chemically similar compounds with comparable therapeutic effects**. The inclusion of multiple formats (e.g., salts, prodrugs) further widens patent coverage.

The detailed stereochemical claims (if present) seek to protect specific isomers optimized for activity. Such claims can be crucial when competitors attempt to sidestep patent rights via minor structural modifications.

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Patent Landscape Context

Related Patents and Patent Families

The '082 patent is situated within a dense patent landscape comprising:

• Prior art references dating back to earlier serotonin-related compounds.
• Subsequent patents claiming improved formulations, dosing methods, or novel derivatives.

Patent families related to the '082 patent might include:

• Continuation or divisionals to extend protection beyond the original filing.
• Foreign counterparts protecting rights in key markets such as Europe, Japan, and China.

Literature and Market Dynamics

The patent's timeline aligns with the approval and commercialization of comparable drugs such as fluoxetine, paroxetine, and sertraline. Patents covering these drugs either predate or postdate the '082 patent, leading to complex rights and potential patent thickets.

In the context of generic drug entry, the '082 patent likely faced challenges or defenses based on obviousness, inventive step, or claim construction arguments, typical in patent litigations under ANDA (Abbreviated New Drug Application) processes.

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Patent Term and Lifecycle Considerations

Given its filing date (likely in the late 1990s) and grant date, the '082 patent likely expires around 2020-2021, considering patent term adjustments. This timeframe marks a critical inflection point for market exclusivity, opening the arena for generic competition, unless supplementary patents or exclusivities (e.g., pediatric extensions) are leveraged.

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Legal Status and Enforceability

As of recent years, the '082 patent may have faced litigation, patent challenges, or license agreements. Its enforceability depends on the validity of its claims and the absence of prior art or obviousness challenges. Maintenance fees, patent term adjustments, and potential patent term extensions would impact its commercial value.

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Implications for Stakeholders

• Innovators: Patent owners can enforce rights against generic entrants, securing revenue streams.
• Generic manufacturers: May seek around the claims or design-around strategies, such as designing structurally distinct but pharmacologically similar compounds.
• Investors: Evaluate the patent's remaining life to inform licensing or development strategies.
• Regulatory bodies: Must assess patent rights during drug approvals or patent litigations.

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Conclusion and Key Takeaways

The '082 patent’s scope centers on chemically defined compounds with specified therapeutic uses, employing broad claims to secure extensive protection. Its strategic positioning within the patent landscape underscores its role in shaping market exclusivity for its intended pharmaceutical class. Stakeholders should monitor its legal status and potential for patent expiration to guide development, licensing, or litigation strategies.

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Key Takeaways

• The '082 patent claims a broad chemical space of compounds for psychiatric and neurological indications, employing detailed structural and functional claims.
• Its strategic breadth aims to prevent competitors from developing similar therapeutics within the protected chemical and therapeutic scope.
• The patent landscape is dense, with related patents potentially influencing the scope and enforceability of the '082 patent.
• Patent expiration approaches, along with legal challenges, significantly influence its market relevance.
• Stakeholders must evaluate patent claims critically to navigate around protections or enforce rights effectively.

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FAQs

1. What types of compounds does the '082 patent cover?
   It primarily covers specific chemical structures related to psychotropic agents, including salts and prodrugs, designed for therapeutic use in psychiatric conditions.

2. Can generic companies develop similar drugs without infringing the '082 patent?
   They may attempt to design around the claims by modifying structures outside the scope of the patent or by developing different classes of compounds with similar activity, contingent on patent validity and scope.

3. How does the patent landscape influence drug development strategies?
   Companies analyze existing patents to identify freedom-to-operate, avoid infringement, or prepare for patent challenges, shaping R&D directions accordingly.

4. What role does the patent's expiration play in the market?
   Once expired, the patent allows generic manufacturers to produce similar drugs, increasing competition and reducing prices.

5. Are the claims of the '082 patent still enforceable today?
   Enforcement depends on factors like patent validity, possible legal challenges, and compliance with maintenance fees; actual enforceability should be assessed through legal review.

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References

1. U.S. Patent 6,288,082, "Chemical compounds for therapeutic use," 2001.
2. Patent family documents and terminal disclaimers related to the '082 patent.
3. Regulatory filings and patent status reports from USPTO and WIPO databases.
4. Market and legal analyses from pharmaceutical patent law literature.

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Note: This analysis is for informational purposes and should not substitute comprehensive legal or patent counsel review.

Drugs Protected by US Patent 6,288,082

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