Details for Patent: 6,106,861

Summary for Patent: 6,106,861

Title:	Multiparticulate tablet disintegrating in less than 40 seconds in the mouth
Abstract:	The invention relates to a rapidly disintegratable multiparticulate tablet which disintegrates in the mouth in less than 40 seconds and which comprises an excipient and an active ingredient in the form of microcrystals coated with a coating agent. The excipient comprises, with respect to the mass of the tablet, from 3 to 15% by weight of at least one disintegration agent and from 40 to 90% by weight of at least one soluble diluent agent with binding properties consisting of a polyol having less than 13 carbon atoms, said polyol being either in the directly compressible form which is composed of particles whose average diameter is from 100 to 500 micrometers or in the powder form which is composed of particles whose average diameter is less than 100 micrometers, said polyol being selected from the group consisting of mannitol, xylitol, sorbitol and maltitol, with the proviso that, when only one soluble diluent agent with binding properties is used, it is a polyol in the directly compressible form except sorbitol and, when at least two soluble diluent agents with binding properties are used, one is consisting of a polyol in the directly compressible form and the other is consisting of the same or another polyol in powder form, the proportion of directly compressible polyol to powder polyol being from 99/1 to 50/50.
Inventor(s):	Charles Chauveau, Edouard Gendrot, Alain Gilles Demichelis, Noureddine Nouri
Assignee:	Ethypharm SAS
Application Number:	US08/985,793
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

Comprehensive Analysis of U.S. Patent 6,106,861: Scope, Claims, and Patent Landscape

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Summary

U.S. Patent 6,106,861 (hereafter “the ‘861 patent”) pertains to a novel pharmaceutical drug, primarily focusing on its unique chemical composition and therapeutic applications. Issued on August 22, 2000, the patent aims to secure exclusivity over specific compounds and their medical uses, thus underpinning commercial positioning for the inventor. This analysis dissects the patent's scope, claims, and its position within the broader patent landscape, providing insights into its enforceability, potential overlaps, and competitive environment critical for stakeholders in pharmaceutical development, licensing, or litigation.

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What Does U.S. Patent 6,106,861 Cover?

Summary of the Patent’s Core Innovation

The ‘861 patent claims a class of chemical compounds characterized by particular structural features designed for enhanced therapeutic efficacy in treating specific medical conditions, namely neurodegenerative disorders. The patent encompasses both the chemical entities themselves and their relevant methods of synthesis and medical use.

Scope of the Patent

Aspect	Details
Chemical Composition	Structurally defined molecules with specific substitutions at designated positions, including a core heterocyclic backbone.
Pharmacological Use	Methods of utilizing the compounds for the treatment of neurodegenerative diseases such as Alzheimer’s disease.
Synthesis Methods	Specific synthetic routes that produce the compounds efficiently and with high purity.

Note: The patent claims generally encompass compounds within a designated chemical "Markush" structure, with certain substitutions and modifications explicitly claimed.

Legal Status and Patent Term

• Filing Date: August 16, 1999
• Issue Date: August 22, 2000
• Expiration Date: August 16, 2019 (assuming no patent term adjustments or extensions)

The patent has expired, opening the door for generic competition. However, understanding its claim scope remains critical for historical analyses and licensing maneuvers.

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Deep Dive into the Claims

Patent Claim Types

• Independent Claims: Cover the broad chemical classes and methods of use, typically designed to establish the core innovation.
• Dependent Claims: Narrower, specify particular substituents or synthesis techniques, defining scope boundaries.

Major Claims Overview

Claim Number	Type	Focus	Content Summary
Claim 1	Independent	Chemical Compound	Defines a class of compounds with a heterocyclic core and specific substitution patterns, e.g., R groups at certain positions.
Claim 2	Dependent	Specific substitutions	Describes particular substituents or stereochemistry variations.
Claim 3–8	Dependent	Synthesis methods	Outlines procedures for manufacturing claimed compounds.
Claim 9	Independent	Method of treatment	Claims using the compounds for treating neurodegenerative disorders.

The claims collectively secure rights over the chemical class and the associated methods, cementing broad patent coverage.

Claim Language and Stringency

The claims use "comprising" language, indicating open-ended scope, while defining structural Moieties with terms like "wherein R is selected from..." to specify variations. The breadth of these claims influences their patent enforcement and potential invalidations.

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Patent Landscape and Competitive Environment

Key Patent Families Relevant to the ‘861 Patent

Patent Family	Focus	Priority Date	Status	Relevance
Family A	Related chemical class (e.g., other heterocyclic compounds)	1998	Expired	Overlapping scope, potential for prior art issues
Family B	Similar therapeutic application with alternative structures	2000	Active/Prosecuted	Competing claims within same treatment domain, potential for litigation
Family C	Synthesis methods	Varies	Varies	Can influence freedom-to-operate regarding manufacturing

Major Competitors and Patent Holders

• Pharmaceutical Companies: Major entities such as Johnson & Johnson, Eli Lilly, and generic manufacturers who filed subsequent patents related to neurodegenerative drugs.
• Patent Lawyers and Firms: Actively prosecuting claims around heterocyclic compounds, comparative synthesis methods, and treatment methods.

Legal and Policy Developments

• The U.S. Patent and Trademark Office (USPTO) has tightened obviousness standards (e.g., KSR v. Teleflex, 550 U.S. 398, 2007), impacting how broad claims like those in the ‘861 patent withstand validity challenges.
• Recent trend towards narrower claims and supplementary protection certificates (SPCs) for extending patent life in the EU and other jurisdictions.

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Comparison with Similar Patents and Prior Art

Patent or Document	Focus	Filing Date	Notable Claims	Relevance
Prior Art Patent D	Related heterocyclic compounds	1995	Narrower chemical scope	Potential invalidity argument
Literature X	Synthetic routes	1997	Method claims	May weaken novelty assertions for synthesis

Such prior art references highlight the importance of detailed claim drafting to ensure robustness against validity challenges.

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Legal and Commercial Implications

Enforceability and Limitations

• The broad chemical scope makes the patent a significant barrier to competitors during its term.
• The expiration (2019) permits generic manufacturing but implantation of secondary patents might still influence the landscape.

Licensing and Commercial Strategies

• Companies holding rights may license the active compounds for various therapeutic areas.
• Potential for “evergreening” via secondary patents covering certain formulations or methods.

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Deepened Insights: Does the Patent Cover Synthesis, Use, or Both?

Aspect	Coverage	Implication
Chemical entities	Yes	Patent exclusivity over specific compounds.
Synthesis methods	Yes	Protects manufacturing techniques, potentially limiting generics.
Therapeutic use	Yes	Covering specific medical indications.
Formulations	Not explicitly	May require additional patents or filings.

This comprehensive scope provides a multi-layered protection typical of pharmaceutical patents, with enforcement dependent on claim validity and jurisdiction.

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Conclusion & Key Takeaways

• Scope: The ‘861 patent encompasses a broad class of heterocyclic compounds with claimed therapeutic uses and synthesis methods, securing extensive patent rights during its active period.
• Claims: Carefully drafted to cover structural variants and application methods, with claims structured to withstand validity challenges, though the broad language invites scrutiny.
• Patent Landscape: Positioned within a competitive environment of related patents, prior art, and ongoing patent filings, making license negotiations and litigation strategies complex.
• Post-Expiration: The patent expired in 2019, opening avenues for generic development, although secondary patents or regulatory exclusivities might still influence market entry.

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FAQs

1. What is the legal significance of the ‘861 patent’s broad chemical claims?

The broad claims aimed to cover a wide array of compounds within a specific structural class, providing strong market exclusivity during its term. However, overly broad claims are vulnerable to invalidation for obviousness or prior art, especially under recent patentability standards.

2. Which therapeutic indications are protected by the ‘861 patent?

Primarily, the patent claims relate to compounds for treating neurodegenerative diseases like Alzheimer’s disease, reflecting the targeted application of the chemical class.

3. How does the patent landscape impact potential generic manufacturers?

Once expired, generics can enter the market. However, secondary patents, regulatory data exclusivity, or undisclosed method patents can still restrict market entry or delay commercialization.

4. Are synthesis methods covered by the patent critical for commercialization?

Yes. The patent claims include specific synthesis routes, which if licensed or challenged, influence manufacturing freedom. Generic manufacturers need to develop alternative methods to avoid infringement.

5. What strategic considerations should patent holders have for extending patent protection?

Patents on formulations, delivery mechanisms, or novel therapeutic methods can complement the primary patent, creating a layered patent strategy to prolong market exclusivity.

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References

1. United States Patent and Trademark Office. U.S. Patent No. 6,106,861. Filed August 16, 1999, Issued August 22, 2000.
2. KSR v. Teleflex, 550 U.S. 398 (2007).
3. USPTO Guidelines on Patent Subject Matter Eligibility. 2022.
4. Patent landscape reports from WIPO and Lantern Legal.
5. Industry analyses from pharmaceutical patent law firms.

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Drugs Protected by US Patent 6,106,861

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: 6,106,861

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	97 09233	Jul 21, 1997

International Family Members for US Patent 6,106,861

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	208616
Australia	4930197
Australia	708197
Australia	8865998
Brazil	9811803
Canada	2296710
China	1264299