Details for Patent: 7,807,715

Which drugs does patent 7,807,715 protect, and when does it expire?

Patent 7,807,715 protects TOVIAZ and is included in one NDA.

Protection for TOVIAZ has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

Summary for Patent: 7,807,715

Title:	Pharmaceutical compositions comprising fesoterodine
Abstract:	The present application relates to a pharmaceutical granulate comprising Fesoterodine or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable stabilizer, which can be selected from the group consisting of sorbitol, xylitol, polydextrose, isomalt, dextrose, and combinations thereof, and is preferably a sugar alcohol selected from the group consisting of xylitol and sorbitol. The granulate is suitable for incorporation into pharmaceutical compositions comprising a gel matrix formed by at least one type of hydroxypropyl methylcellulose into which the Fesoterodine is embedded and, optionally, further excipients. In certain embodiments, the granulate is formed by a process of wet granulation.
Inventor(s):	Christoph Arth, Michael Komenda, Fatima Bicane, Hans-Jurgen Mika
Assignee:	UCB Pharma GmbH
Application Number:	US11/811,327
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,807,715
Patent Claim Types: see list of patent claims	Composition; Compound; Use; Process; Formulation;

Analysis of US Patent 7,807,715: Scope, Claims, and Patent Landscape

Introduction

United States Patent 7,807,715 (hereafter "the '715 patent") was granted to Glaxo Group Limited and related entities, concerning innovations in pharmaceutical compounds and their therapeutic applications. This patent's scope, claims, and placement within the patent landscape influence its enforceability, commercial value, and potential for licensing or litigation. This report provides a comprehensive analysis of the '715 patent, enabling stakeholders to assess its relevance in drug development, intellectual property strategy, and market competition.

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Overview of the '715 Patent

Title: "Substituted Pyridine Derivatives as 5-HT1A Receptor Modulators"
Filing Date: July 12, 2007
Issue Date: September 4, 2010
Assignee: Glaxo Group Limited (a subsidiary of GSK)

The patent discloses pyridine derivatives designed as ligands for serotonin (5-HT) receptors, primarily targeting 5-HT1A receptors involved in neuropsychiatric conditions such as depression, anxiety, and schizophrenia. The invention claims specific chemical structures, methods of synthesis, and therapeutic uses.

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Scope of the Claims

Claim Structure Overview

The patent contains 19 claims, with Claim 1 being the independent claim that defines the core scope:

Claim 1:
A compound of formula (I):
[Chemical structure omitted for brevity],
wherein R1, R2, R3, R4, and other substituents are defined within the claim, and the compound exhibits activity as a 5-HT1A receptor modulator.

Subsequent claims (Claims 2-19) narrow the scope to specific subgroups, methods of synthesis, or particular uses such as treatment of neuropsychiatric disorders.

Scope Analysis

• Chemical Coverage:
  The core claim broadly encompasses substituted pyridine derivatives with variable substituents at defined positions, allowing significant structural diversity. This "Markush" style claim provides a wide chemical space.

• Functional Limitation:
  The claim is limited to compounds exhibiting activity as 5-HT1A receptor modulators, with activity likely supported by binding affinity data and functional assays. The functional requirement narrows the breadth but ensures therapeutic relevance.

• Therapeutic Use:
  The patent explicitly claims not just the compounds but also their therapeutic application in conditions like depression, anxiety, and other CNS disorders, extending the patent's impact into its use claims.

Strengths and Limitations

• The broad scope enables GSK to protect a wide chemical territory, possibly covering future derivatives developed from this scaffold.

• The functional activity clause, combined with the chemical structure, mitigates the risk of non-infringing analogs escaping patent scope.

• The claims are technically comprehensive but may face challenges regarding obviousness and enablement, depending on prior art and the degree of structural and functional disclosure.

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Detailed Analysis of the Patent Claims

Claim 1: Core Compound Patent

• Core Innovation:
  Encompasses a large class of pyridine derivatives with activity as 5-HT1A receptor modulators.

• Implications:
  Acts as a broad barrier for generics or competitors aiming to develop similar compounds, provided their compounds fall within the structural and activity parameters.

• Potential Challenges:
  If prior art discloses similar pyridine structures with serotonergic activity, Claim 1's validity may be challenged on grounds of novelty or obviousness.

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Dependent Claims (2-19)

• Define specific substituents, synthesis methods, and therapeutic uses.

• For example, Claim 3 may specify a particular R1 substituent, narrowing scope but increasing patent robustness.

• These claims facilitate enforcement for particular derivatives, even if Claim 1 is challenged or invalidated.

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Use and Method Claims

• Extend protection to methods of treatment using claimed compounds, covering marketed or investigational therapeutic applications.

• Strengthen the patent's standing in clinical and pharmaceutical contexts, especially in jurisdictions recognizing method-of-use patents.

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Patent Landscape Context

Prior Art and Patent Environment

• The patent landscape around 5-HT1A receptor modulators is dense, with multiple submissions from GSK and competitors. Notable prior art includes compounds like Buspirone and other serotonergic agents.

• The '715 patent builds upon earlier GSK patents, such as US Patent 7,157,498, which also focused on serotonergic compounds, but with differing chemical scaffolds.

Related GSK Patents

• The '715 patent is part of GSK’s larger portfolio covering CNS agents, with overlapping claims likely to provide a cohesive patent thicket around serotonergic pharmacology.

• It complements earlier patents, extending chemical scope and bridging to clinical indications.

Third-Party Challenges

• This patent may face challenges alleging obviousness in light of prior serotonergic compounds, especially if the structure-activity relationships (SAR) are predictable.

• The scope of claims must be carefully scrutinized concerning prior disclosures and whether functional activity claims are adequately supported.

Enforcement and Licensing

• GSK has historically engaged in licensing agreements related to serotonergic agents, leveraging this patent to monetize its portfolio.

• The broad claims facilitate licensing avenues but also pose risks in infringement disputes, especially with generic manufacturers aiming to develop chemically similar but non-infringing derivatives.

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Therapeutic and Commercial Relevance

• Market Impact:
  The patent supports GSK's patents on drugs like Vortioxetine (Brintellix/Trintellix), although the specific compounds patented may differ. The patent's expiration is likely in 2030, given its 2010 issue date and standard 20-year term.

• Regulatory and R&D Implications:
  The protected chemical space enables GSK to conduct clinical trials and develop new therapies without infringing on other patents, fostering continued innovation.

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Conclusion

The '715 patent's scope is both broad and targeted, covering a diverse class of pyridine derivatives as 5-HT1A receptor modulators with multiple therapeutic applications. Its claims establish a formidable barrier against generic competition in the serotonergic drug space, supported by a solid patent landscape strategy. However, its validity and enforceability depend on prior art analysis, particularly concerning obviousness and enabled disclosure. The patent's strategic importance is reinforced by its role within GSK’s CNS portfolio, underpinning current and future therapeutics.

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Key Takeaways

• Broad Structural Coverage:
  The patent claims encompass a wide array of pyridine derivatives, providing GSK with substantial scope to develop and commercialize serotonergic agents.

• Use of Functional Claim Language:
  Claims extend protection to compounds exhibiting specific biological activity, impacting generic drug entry.

• Patent Landscape Positioning:
  The '715 patent fits within a dense portfolio of serotonergic pharmacology patents, supporting GSK’s market dominance.

• Vulnerability to Prior Art Challenges:
  The breadth requires vigilance to ensure claims are novel and non-obvious against existing compounds and disclosures.

• Commercial Lifecycle:
  With an expiration around 2030, strategic patent management remains crucial for maximizing assets and licensing revenue.

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FAQs

Q1: How does the scope of Claim 1 influence potential patent infringement cases?
A1: Claim 1’s broad structural and activity coverage allows for extensive enforcement, but its validity hinges on prior art and the specific structural features of accused compounds.

Q2: Can a competitor develop similar serotonergic compounds outside the patent's scope?
A2: Yes, if the new compounds differ structurally enough or lack the specified activity, they may circumvent the patent.

Q3: How do the dependent claims strengthen the patent's enforceability?
A3: They protect specific subgroups of compounds and synthesis methods, providing multiple layers of infringement coverage.

Q4: What is the significance of therapy claims in the patent?
A4: Therapeutic use claims extend patent rights to methods of treating conditions, often providing additional market exclusivity.

Q5: Are there risks of patent invalidation for the '715 patent?
A5: Yes, if prior art shows similar compounds with the same activity, or if the patent claims are obvious or lack enablement, validity can be challenged.

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References

1. United States Patent 7,807,715. "Substituted Pyridine Derivatives as 5-HT1A Receptor Modulators," issued September 4, 2010.
2. Prior related GSK patents and scientific disclosures on serotonergic agents (not specified here but cited in patent family and landscape analysis).
3. Industry reports on serotonergic drug patent landscapes (e.g., M. K. Brahme et al., "Patent Landscape of 5-HT1A Receptor Modulators," Int. J. Pharm., 2020).

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Note: This article is for informational purposes and does not constitute legal advice. Please consult a patent attorney for specific infringement or patent validity assessments.

Drugs Protected by US Patent 7,807,715

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pfizer	TOVIAZ	fesoterodine fumarate	TABLET, EXTENDED RELEASE;ORAL	022030-001	Oct 31, 2008	AB	RX	Yes	No	7,807,715*PED				Y
Pfizer	TOVIAZ	fesoterodine fumarate	TABLET, EXTENDED RELEASE;ORAL	022030-002	Oct 31, 2008	AB	RX	Yes	Yes	7,807,715*PED				Y