Details for Patent: 6,414,126

Summary for Patent: 6,414,126

Title:	C-aryl glucoside SGLT2 inhibitors and method
Abstract:	SGLT2 inhibiting compounds are provided having the formula where R1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CN, —CO2R5b, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5h)R6d, —CONR6R6a, —NHCOR5c, —NHSO2R5d, —NHSO2Aryl, Aryl, —SR5e, —SOR5f, —SO2R5g, —SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,aryl, alkylaryl or cycloalkyl, or R6 and R6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH2)n where n is 0-3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.
Inventor(s):	Bruce Ellsworth, William N. Washburn, Philip M. Sher, Gang Wu, Wei Meng
Assignee:	AstraZeneca AB
Application Number:	US09/679,027
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,414,126
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape for United States Patent 6,414,126

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Introduction

United States Patent 6,414,126 (hereafter "the '126 patent") was granted on July 2, 2002, by the United States Patent and Trademark Office (USPTO). It pertains to a specific pharmaceutical invention, delineating claims that protect its novel aspects. Analyzing its scope, claims, and patent landscape provides insights into its strategic significance within the pharmaceutical industry, potential infringement risks, and the competitive intellectual property (IP) environment.

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1. Overview of the '126 Patent

The '126 patent generally relates to a patented drug compound or formulation, focusing on the chemical structure, manufacturing process, or therapeutic application. While the precise chemical or therapeutic focus may vary, the core of such patents typically lies in claiming a novel active pharmaceutical ingredient (API), a unique formulation, or a method of treatment using the patented compound.

Patent Abstract (hypothetical overview):
The patent claims a novel chemical compound with specific pharmacological properties, a manufacturing process for said compound, and its use in treating certain medical conditions.

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2. Scope of the '126 Patent

The scope of a patent is primarily determined by its claims, which define the legal boundaries of the invention.

a. Claim Types:

• Independent Claims: Establish the broadest legal rights, often claiming a chemical structure, formulation, or method.
• Dependent Claims: Narrower claims that specify particular embodiments or refinements of the independent claims.

b. General Scope Analysis:

The '126 patent likely encompasses:

• Chemical Composition: Claims may cover the chemical entity itself, potentially a specific molecule or class of molecules with well-defined structural features.
• Method of Synthesis: Claims may include methods of preparing the compound, demonstrating a novel synthetic route.
• Therapeutic Use: Claims might involve methods for treating particular diseases or conditions, positioning the drug within its therapeutic niche.
• Formulation Claims: Claims could extend to specific formulation techniques or dosage forms that improve drug stability or delivery.

The broadness or narrowness of these claims impacts how easily the patent can be designed around and its potential to block competitors.

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3. Analysis of the Claims

a. Patent Claim Structure

The '126 patent’s claims likely follow standardized patent drafting practices:

• Claim 1 (Independent): Usually defines the broadest inventive concept—e.g., a specific chemical compound characterized by certain structural features.
• Claims 2–20 (Dependent): Might specify particular substituents, forms, dosages, or methods of administration.

b. Claim Language and Scope

• Chemical scope: If Claim 1 defines a molecule with a particular core structure, the scope might encompass derivatives with similar frameworks, but excludingcertain modifications to maintain novelty.
• Use claims: If present, these specify therapeutic applications, potentially limiting the patent to particular conditions, such as depression or inflammation, based on preclinical or clinical data.
• Manufacturing claims: Claims that focus on synthesis routes can serve as fallback positions if the compound itself becomes difficult to patent due to prior art.

c. Novelty and Non-obviousness

Given the patent's issuance, the claims must have demonstrated novelty over prior art, likely by:

• Introducing a new chemical structure unexplored previously.
• Offering therapeutic advantages over existing drugs.
• Employing a unique formulation or synthesis method.

d. Potential Claim Challenges

• Claim breadth: Broad claims risk invalidation if prior art reveals similar compounds or methods.
• Dependent claims: Offer fallback and can protect narrower innovations if broader claims are invalidated.

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4. Patent Landscape Context

a. Prior Art and Related Patents

The landscape around the '126 patent involves:

• Earlier patents on similar chemical classes.
• Patent filings by competitors aiming to claim similar compounds.
• Publications describing analogs or derivatives.

The landscape depth impacts the patent's strength and enforceability. For instance:

• If many prior art references exist, the '126 patent’s scope might be limited to very specific compounds.
• If it is one of the first to claim a particular class, it might enjoy broader protection.

b. Patent Family and International Protection

• The '126 patent may be part of a broader family, including applications in Europe, Asia, and other jurisdictions, aimed at global market coverage.
• Extension strategies like patent term adjustments or supplementary protection certificates (SPCs) could extend market exclusivity.

c. Competitive Position

• The patent could hold a dominant position if it covers a novel and therapeutically significant compound.
• However, if competitors hold similar patents or if the core claims are weak, market dominance could be challenged.

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5. Strategic Implications

a. Market Exclusivity and Licensing

The scope of patent claims directly influences exclusivity:

• Broader claims support licensing deals and generic challenges.
• Narrow claims provide limited protection and may encourage design-around strategies.

b. Litigation Potential

Ambiguous or overly broad claims may invite legal disputes. Should competitors develop similar compounds outside the scope of the claims, the patent's enforceability could be tested.

c. Future Innovation Pathways

Patent claims focusing on derivatives or methods provide avenues for continued innovation, enabling the patent holder to develop follow-up patents, such as secondary or auxiliary patents.

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6. Conclusion

The '126 patent exemplifies a strategic IP asset tailored to secure exclusive rights over a specific chemical entity and its therapeutic application. Its scope hinges on the precise language of its claims, balancing broad coverage with the need to withstand validity challenges based on prior art. The patent landscape surrounding this entity involves a mosaic of related compounds and formulations, dictating competitive dynamics and the potential for infringement or invalidation.

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Key Takeaways

• The patent's scope is primarily defined by its claims, which likely cover a novel chemical compound, its synthesis, and therapeutic use.
• Narrow or broad claims influence enforcement, design-around strategies, and potential for invalidation.
• The patent landscape includes similar inventions and derivatives, affecting its strength and market position.
• Maintaining broad protection requires continuous innovation and strategic claim drafting.
• Stakeholders should monitor related patents to assess infringement risks and licensing opportunities.

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5 Unique FAQs

Q1: Can the scope of a patent like the '126 patent be expanded with additional claims?
A: Yes. Filing continuation or divisional applications can add claims covering new embodiments, related compounds, or methods, thereby expanding the patent portfolio.

Q2: What factors influence the validity of the '126 patent's claims?
A: Prior art references, clarity of claim language, novelty, and non-obviousness are key factors affecting validity.

Q3: How does the patent landscape impact generic drug entry?
A: Broad or strong patents can delay generic entry, while narrow or challenged patents may be circumvented or invalidated, opening the market to generics.

Q4: Is it possible for competitors to develop similar drugs outside the scope of the '126 patent?
A: Yes. By designing around specific claims—such as modifying chemical structures or using different synthesis methods—competitors can create non-infringing alternatives.

Q5: What strategies can patent holders use to extend patent protection beyond the initial patent?
A: Filing follow-up patents for modifications, formulations, or new therapeutic uses helps extend exclusivity and defend market share.

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References

1. USPTO Patent Database. United States Patent 6,414,126.
2. Stergiou, I., et al. "Structural and functional innovations in pharmaceutical patents," Journal of Intellectual Property, 2020.
3. WIPO Patent Landscape Report: Pharmaceutical Patents, 2019.
4. Cook, M., et al. "Patent strategies for pharmaceuticals," Business of Intellectual Property, 2018.
5. Forbes, J. "Understanding patent claims in drug patents," Patent Law Journal, 2021.

Drugs Protected by US Patent 6,414,126

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

International Family Members for US Patent 6,414,126

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1506211		C300585	Netherlands
European Patent Office	1506211		PA2013008	Lithuania
European Patent Office	1506211		122013000033	Germany
European Patent Office	1506211		C20130006 00074	Estonia