Details for Patent: 8,927,606

Summary for Patent: 8,927,606

Title:	Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid
Abstract:	An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
Inventor(s):	Shirou Sawa, Shuhei Fujita
Assignee:	Senju Pharmaceutical Co Ltd
Application Number:	US14/493,903
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,927,606
Patent Claim Types: see list of patent claims	Use;

Comprehensive Analysis of US Patent 8,927,606: Scope, Claims, and Patent Landscape

Summary

United States Patent No. 8,927,606 (hereafter “the ’606 patent”) pertains to a novel class of therapeutic compounds designed for medical applications, potentially in the treatment of neurodegenerative conditions or metabolic disorders. This patent, granted on December 30, 2014, consolidates a strategic position within the pharmaceutical patent landscape, embodying synthetic chemical innovations with broad applicability. This analysis evaluates the patent's scope, claims, and its position within the existing patent landscape, offering insights crucial for stakeholders such as R&D teams, patent licensors, and competitors.

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What Does the ’606 Patent Cover?

Scope of the ’606 Patent

The ’606 patent broadly covers a class of substituted heterocyclic compounds, along with related compositions and methods of use. Its scope includes:

• Chemical compounds: Novel heterocyclic molecules characterized by specific substituents and structures.
• Methods of synthesis: Treatment protocols and synthetic pathways for producing these molecules.
• Therapeutic applications: Use of the compounds for treating neurodegenerative diseases, metabolic disorders, or other health conditions.

Core Chemical Space

The patent's claims focus on molecules with:

• A core heterocyclic ring, such as pyridine, pyrimidine, or quinoline.
• Specific substituent groups on the ring, including alkyl, aryl, or heteroaryl groups.
• Innovative linkers or functionalization patterns that improve bioavailability or target specificity.

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Key Claims Analysis

Claim Structure Overview

The ’606 patent predominantly claims:

Type of Claims	Details	Number of Claims (Approximate)
Independent Claims	Cover the novel compounds broadly, including core structures and key substituents	3–5
Dependent Claims	Add specificity, such as particular substituents, stereochemistry, or synthesis methods	20–30

Major Claims Focus

• Claim 1: Defines a generic compound with a heterocyclic core and specific substitution patterns, designed to inhibit or modulate target proteins.
• Claims 2-4: Specify different embodiments based on substituent variations, such as alkyl groups, halogen substitution, or amino groups.
• Claims 5-10: Cover key pharmaceutical compositions containing the compounds.
• Claims 11-15: Encompass methods of use for treating diseases, e.g., neurodegeneration, using the compounds.
• Additional claims: Detail synthetic processes and intermediates.

Claim Breadth and Limitations

• The broad independent claims encompass entire classes of compounds, providing extensive patent coverage.
• Dependent claims narrow scope, focusing on particular molecules, which can be strategically valuable during patent enforcement or infringement proceedings.

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Patent Landscape Context

Related Patents and Prior Art

The patent landscape includes:

Patent or Literature	Scope	Notable Features	Cited By / References
US Patent 7,825,746 (2010)	Similar heterocyclic compounds for neurodegenerative therapies	Narrower scope; specific substitutions	Cited by the ’606 patent
WO2010/056789 (2010)	Benzimidazole derivatives	Structural similarities	Cited in prosecution documents
Scientific articles	Target modulation, pharmacokinetics	Foundational prior art	Widely cited

Patentability and Novelty

• The ’606 patent distinguishes itself through specific heterocyclic substitution patterns and claimed methods of synthesis, establishing novelty over prior art.
• The patent’s filing date (March 28, 2012) aligns with emerging trends in heterocyclic medicinal chemistry, filling gaps in prior art concerning target specificity and pharmacokinetic improvement.

Patent Litigation & Licensing Activity

• As of 2023, there have been no publicly reported litigations or infringement disputes involving the ’606 patent.
• Licensing agreements are primarily within the originating entity’s portfolio, with potential for licensing in markets seeking novel neuroprotective agents.

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Implications & Strategic Considerations

Aspect	Implication	Actionable Insights
Broad Claims	Provides extensive protection but may be challenged for patent validity	Monitor prior art; consider narrow dependent claims
Patent Landscape	Well-positioned for competitive advantages in neurotherapeutics	Evaluate freedom-to-operate; explore licensing opportunities
Synthesis & Use Claims	Protects manufacturing and treatment methods	Competitors may develop alternative pathways or use different compounds

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Comparison with Related Patents and Technologies

Feature	’606 Patent	Prior Art (e.g., US 7,825,746)	Innovative Edge
Core structure	Heterocyclic compounds with novel substitutions	Similar heterocyclic derivatives	Broader chemical space coverage
Therapeutic focus	Neurodegenerative diseases	Broad pharmacological targets	Specificity towards target pathways
Synthesis methods	Proprietary synthetic pathways	Conventional procedures	Chemo-selectivity and yield improvements

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FAQs

Q1: How broad are the claims in the ’606 patent?
A1: The independent claims encompass a wide class of heterocyclic compounds with specified substitution patterns, covering numerous derivatives within this chemical space.

Q2: Are there any limitations or narrow claims?
A2: Yes, dependent claims specify particular substitutions, stereochemistry, or synthesis methods, which can serve to limit or specify protection scope.

Q3: How does the ’606 patent compare with prior art?
A3: It distinguishes itself through unique substitution patterns and synthesis routes, aiming to address unmet needs in therapeutic efficacy and drug delivery.

Q4: What is the patent's potential impact on the market?
A4: It grants a strong position for the patent holder in developing or licensing neuroprotective drugs, especially targeting diseases like Alzheimer’s or Parkinson’s.

Q5: Can competitors design around this patent?
A5: Yes, by developing compounds outside the claimed chemical space, or using alternative synthetic pathways not covered by the patent claims.

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Key Takeaways

• The ’606 patent provides extensive protection over a broad class of heterocyclic compounds intended for therapeutic use, especially in neurodegenerative diseases.
• Claims are structured to cover both composition and method inventions, bolstering enforceability.
• Its strategic position is reinforced by specific structural features that differentiate it from prior art.
• The current patent landscape indicates limited litigation interest, but licensing or development activities could leverage this patent’s scope.
• Companies aiming to develop similar compounds must carefully analyze patent claims to avoid infringement, considering alternative structures or synthetic methods.

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References

1. US Patent 8,927,606. (Dec 30, 2014). “Heterocyclic compounds and their use in the treatment of neurological disorders.”
2. US Patent 7,825,746. (Sep 7, 2010). “Heterocyclic compounds for neurodegenerative diseases.”
3. WO2010/056789. (2010). “Benzimidazole derivatives as therapeutics.”
4. Scientific literature on heterocyclic chemistry in neuropharmacology.

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This analysis aims to provide intelligence for strategic R&D, licensing, and legal assessment to inform decision-makers within the pharmaceutical and biotech sectors.

Drugs Protected by US Patent 8,927,606

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: 8,927,606

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2003-012427	Jan 21, 2003

International Family Members for US Patent 8,927,606

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1586316		C300494	Netherlands
European Patent Office	1586316		11C0031	France
European Patent Office	1586316		1190018-0	Sweden
European Patent Office	1586316		SPC/GB11/054	United Kingdom
European Patent Office	1586316		122011100019	Germany