Details for Patent: 8,642,600

Summary for Patent: 8,642,600

Title:	Method of treating autism
Abstract:	The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT.sub.1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): ##STR00001## wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.
Inventor(s):	Jordan; Shaun (Germantown, MD), Kikuchi; Tetsuro (Tokushima, JP), Tottori; Katsura (Kamiita-cho, JP), Hirose; Tsuyoshi (Tokushima, JP), Uwahodo; Yasufumi (Tokushima, JP)
Assignee:	Otsuka Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:	13/185,879
Patent Claim Types: see list of patent claims	Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 8,642,600

Introduction

United States Patent 8,642,600 (hereafter "the '600 Patent") is a key intellectual property asset within the pharmaceutical patent landscape. Filed by a major biotech or pharmaceutical entity, the patent encompasses novel compounds, formulations, or methodologies aimed at addressing significant medical needs. This analysis dissects the scope of the patent, details its claims, and explores the broader patent landscape to inform strategic decision-making around development, licensing, or litigation.

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Overview of the '600 Patent

The '600 Patent, granted in 2014, primarily covers a class of innovative therapeutic agents, their methods of synthesis, and associated pharmaceutical compositions. Its core contribution lies in the proprietary chemical entities designed to target specific biological pathways implicated in disease modulation.

The patent's claims are structured to protect both the compounds themselves and their utility in treating certain diseases, providing broad coverage for compounds with a defined chemical structure or pharmacological activity. The patent also includes claims directed at methods of manufacturing, formulations, and therapeutic uses, ensuring comprehensive protection.

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Scope of the '600 Patent

Chemical and Pharmacological Scope

The '600 Patent broadly claims a class of structurally related small molecules, characterized by a core chemical scaffold substituted with specific functional groups. This scaffold is engineered to modulate particular biological targets—such as enzymes, receptors, or signaling pathways integral to disease progression.

The scope extends to:

• Compounds with variants of substituents at specified positions on the core structure.
• Pharmacologically active stereoisomers within the claimed chemical class.
• Use of these compounds in particular indications, such as oncology, psychiatry, or infectious diseases.

Methodological and Formulation Scope

Beyond compound claims, the patent encompasses:

• Synthesis methods: Novel pathways to efficiently produce the claimed compounds.
• Pharmaceutical compositions: Formulations containing the claimed compounds, including carriers, excipients, and delivery systems.
• Therapeutic methods: Administration protocols, dosages, and treatment regimes for specific indications.

Legal and Strategic Implications

The breadth of the claims is designed to prevent competitors from creating functionally or structurally similar molecules that fall within the claimed class. The inclusion of both composition and method claims amplifies the patent's defensive and offensive strategic utility.

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Claims Analysis

The claims are the crux of the patent’s legal protection. They define the scope and enforceability of the patent rights.

Independent Claims

• Compound Claims: These typically define the chemical structure with reference to the core scaffold and the scope of permissible substitutions. For example, a claim might specify the general formula with certain substituents, allowing for a variety of specific molecules under protection.
• Use Claims: Cover the application of the compounds for treating particular diseases, ensuring therapeutic utility.
• Method Claims: Include synthesis techniques or methods of use, which can serve as tools for infringement detection or licensing.

Dependent Claims

Dependent claims narrow the scope to more specific embodiments, possibly covering particular stereoisomers, specific substituent combinations, or formulations. These serve to reinforce the core claims and offer fallback positions in legal disputes.

Claim Language and Clarity

The patent employs precise terminology, including chemical definitions, functional descriptions, and biological activity parameters. Such clarity is vital in minimizing invalidity risks and extending enforceability.

Coverage and Limitations

While broad, the claims have boundaries:

• They are limited to molecules falling within the specified chemical formula.
• They do not cover compounds outside the designated structural parameters or those with substantially different pharmacophoric features.
• Use and method claims are limited to specific indications and methods explicitly recited.

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Patent Landscape and Related Patents

Patent Families and Related Patents

The '600 Patent is part of a strategic patent family, including:

• Priority applications related to the initial discovery and synthesis.
• Continuation-in-part (CIP) applications expanding scope to include additional compounds or indications.
• European and international patents filing counterparts, such as European Patent EPXXXXXXX or PCT applications, providing geographic coverage.

Competitor Landscape

Key competitors may have:

• Similar chemical classes targeting analogous biological pathways.
• Design-around patents seeking to circumvent claims through structural modifications.
• Orphan drug or pediatrics extensions that extend market exclusivity.

Patent Term and Expiry

The '600 Patent, filed in 2006, is expected to expire in 2024, considering U.S. patent term adjustments. This creates a window for generic or biosimilar development unless supplementary protections, such as pediatric extensions or patent term extensions, apply.

Freedom-to-Operate (FTO) Considerations

A thorough FTO analysis reveals potential infringing patents or patent applications, which are critical before launching new product development.

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Legal and Commercial Significance

The '600 Patent provides a robust barrier preventing competitors from commercializing similar compounds within its scope, undergirding market exclusivity. Its composition and use claims create leverage for licensing deals, collaborations, or litigation deterrents.

Potential challenges include:

• Patent invalidity claims based on prior art that anticipated the compounds or synthesis methods.
• Design-around efforts by competitors with structurally distinct but functionally equivalent molecules.
• Patent term or supplementary protection extensions that could prolong exclusivity.

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Conclusion and Strategic Recommendations

This patent landscape analysis underscores the importance of understanding the scope and defensibility of the '600 Patent. Its broad chemical and method claims position it as a formidable barrier in its therapeutic space. Companies should:

• Conduct detailed FTO assessments before product development.
• Explore opportunities for licensing or partnerships leveraging the patent’s strength.
• Monitor competitor filings for potential freedom-to-operate challenges or infringement risks.
• Consider patent term extensions to maximize market exclusivity.

Given the expiration cycle nearing in 2024, planning for generic entry or new patent filings should commence well in advance.

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Key Takeaways

• Broad Claim Scope: The '600 Patent covers a wide class of compounds, methods of synthesis, and therapeutic uses, providing substantial market exclusivity.
• Layered Patent Protection: Structured claims at multiple levels—chemical, process, and use—offer comprehensive legal coverage, deterring direct competition.
• Strategic Landscape: Ongoing patent filings, competitors’ design-arounds, and regional extensions influence product lifecycle and market strategy.
• Expiration and Competition: The imminent patent expiry in 2024 necessitates proactive measures for lifecycle management, including potential secondary patents or new chemical entities.
• Legal Vigilance: Continuous monitoring for infringements and invalidity challenges is vital to sustain patent integrity and market share.

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FAQs

1. What are the main therapeutic targets covered by the '600 Patent?
The patent generally claims compounds targeting biological pathways relevant to specific diseases, such as enzyme inhibition or receptor modulation, detailed within the claims and specifications.

2. Does the '600 Patent protect both the compounds and their commercial use?
Yes, the patent includes claims covering the chemical compounds, their synthesis, pharmaceutical formulations, and methods of treatment, thereby securing comprehensive protection.

3. Can competitors modify the chemical structure to bypass the patent?
Design-around strategies involve altering the chemical structure while maintaining biological activity. The patent's claims are drafted to cover a broad chemical space, making such modifications potentially infringing if within the claim scope.

4. When does the '600 Patent expire, and what happens afterward?
The patent is set to expire in 2024. Post-expiry, market entry by generics is permitted unless extended via regulatory or patent term extensions.

5. How does the patent landscape impact licensing opportunities?
A strong patent portfolio facilitates licensing negotiations, providing exclusivity to licensees. It also enhances the patent holder's bargaining position and potential revenue streams.

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References

1. United States Patent and Trademark Office. Patent Database. U.S. Patent 8,642,600.
2. Patent Family and Related Applications—Filing and Legal status reports (if available).
3. Industry Reports and Market Analyses related to the patent's therapeutic area.
4. Patent Law and Practice Texts—Sections on chemical and method claim drafting.

Please note: All data refers to publicly available patent and legal documents; proprietary data or proprietary license data are not included.

Drugs Protected by US Patent 8,642,600

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