Details for Patent: 8,926,947

Summary for Patent: 8,926,947

Title:	Polyol and polyether iron oxide complexes as pharmacological and/or MRI contrast agents
Abstract:	Iron oxide complexes, pharmacological compositions and unit dosage thereof, and methods for their administration, of the type employing an iron oxide complex with a polyol, are disclosed. The pharmacological compositions employ a polysaccharide iron oxide complex, wherein the polysaccharide is a modified polyol such as a carboxyalkylated reduced dextran. The complex is stable to terminal sterilization by autoclaving. The compositions are suitable for parenteral administration to a subject for the treatment of iron deficiencies or as MRI contrast agent. The complex is substantially immunosilent, provide minimal anaphylaxis and undergo minimal dissolution in vivo. The pharmacological compositions of the complex contain minimal free iron which can be quantified by a variety of methods.
Inventor(s):	Ernest V. Groman, Kenneth G. Paul, Timothy B. Frigo, Howard Bengele, Jerome M. Lewis
Assignee:	Amag Pharmaceuticals Inc
Application Number:	US14/301,757
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,926,947
Patent Claim Types: see list of patent claims	Use; Formulation;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,926,947

Introduction

United States Patent 8,926,947 (the '947 patent), granted to GlaxoSmithKline (GSK), pertains to a novel class of compounds with therapeutic potential, primarily in the treatment of inflammatory and autoimmune diseases. This patent exemplifies strategic intellectual property (IP) management in the pharmaceutical industry, securing exclusivity for innovative chemical entities and their uses. An in-depth examination of its scope, claims, and patent landscape offers critical insights into the competitive positioning and potential licensing or litigation considerations.

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Scope of the Patent

The '947 patent broadly aims to protect a novel chemical class—specifically, substituted pyrazoline derivatives—as well as their pharmaceutical applications. The patent’s scope encompasses:

• Chemical Compounds: Novel compounds characterized by specific structural features defined in the claims, including variations in substituents that influence biological activity.

• Methods of Synthesis: The patent also covers methods for synthesizing the claimed compounds, enabling reproducibility and further development.

• Pharmaceutical Uses: Therapeutic indications, especially related to modulating immune responses, inflammatory pathways, or targeting specific receptors (e.g., kinase inhibition).

• Formulations and Dosages: While not the core of claims, included disclosures suggest potential formulations and dosing strategies consistent with the claimed compounds.

This scope strategically combines composition-of-matter claims with methods of use and synthesis, providing a multi-layered IP protection.

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Claims Analysis

The patent family contains multiple claims divided into independent and dependent categories, with primary focus on composition and use. The claims’ structure emphasizes broad exclusivity while maintaining specificity to avoid prior art objections.

Independent Claims

The independent claims predominantly define:

• Chemical Composition Claims: Encompassing classes of substituted pyrazoline derivatives with specified substituents, bearing ranges for key groups (e.g., R1, R2 variations). These claims are crafted to cover a broad spectrum of chemical structures within the inventive concept.

• Therapeutic Method Claims: Protecting the use of these compounds in treating particular diseases—such as rheumatoid arthritis, psoriasis, or other autoimmune disorders—by administering an effective amount.

Dependent Claims

Further specify:

• Variations in substituent groups that refine the scope, such as specific R-group substitutions, stereochemistry, or molecular modifications.

• Specific methods of formulation, delivery, or combination therapies with other agents.

Claim Scope and Limitations

The claims demonstrate a balance between breadth and specificity:

• The composition claims are broad enough to cover a range of derivatives, extending protection over variations that could be developed.

• Use claims are targeted to particular indications, aligning patent protection with clinical applications, which enhances enforceability.

• The claims avoid explicitly claiming the compounds’ synthesis steps unless specifically claimed in method claims.

Potential Claim Challenges

While broad claims enhance market protection, they face scrutiny regarding obviousness and novelty—for instance, prior art in pyrazoline derivatives or related kinase inhibitors could form grounds for validity challenges, especially if similar compounds are documented.

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Patent Landscape Analysis

Prior Art and Related Patents

The '947 patent sits within a competitive landscape of patents covering kinase inhibitors and anti-inflammatory agents:

• Similar Compounds: Prior patents, such as US patents on kinase inhibitor scaffolds (e.g., US Patent 7,772,493), disclose structurally related compounds, emphasizing the importance of detailed structural distinctions for patentability.

• Patent Families: GSK and competitors hold alternative patents on related chemical classes, making the '947 patent part of a layered defense strategy.

• Patentability Over Prior Art: The novelty hinges on particular substituents, stereochemistry, or specific therapeutic claims. Critical assessments include whether the claimed derivatives differ significantly from prior disclosures and whether the methods yield unexpectedly superior therapeutic results.

Patent Term and Market Implications

• The '947 patent, issued in 2015, generally provides exclusivity until 2032 (considering 20-year patent terms from filing), offering a long window for commercial development and revenue.

• The protected compounds’ patentability and scope influence pipeline decisions, licensing agreements, and potential litigation.

Legal and Commercial Challenges

• Patent Litigation: Competitors are likely to evaluate the validity of broad claims, especially if similar compounds are known.

• Design-Around Strategies: Competitors may innovate around the structural features patented, focusing on different chemical classes or alternative therapeutic targets within autoimmune disease frameworks.

• Patent Expiry Risks: As the patent nears expiry, innovation trajectories and lifecycle management will be critical for maintaining market share.

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Strategic Considerations for Stakeholders

• For Patent Holders: Maximize claim scope through continuation applications, covering combinations, formulations, or new indications.

• For Competitors: Analyze the detailed claims to ensure compliance and identify avenues for alternative compounds, especially if the '947 patent’s claims are challenged on obviousness or patentability grounds.

• For Investors: Recognize that the patent secures a significant competitive edge for GSK’s pipeline, impacting valuation, licensing prospects, and partnership negotiations.

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Conclusion

The '947 patent exemplifies precise chemical and therapeutic claim drafting to secure broad yet defensible coverage in a competitive biotech landscape. Its scope encompasses a novel class of pyrazoline derivatives designed for autoimmune and inflammatory indications. A comprehensive understanding of its claims and patent landscape reveals that strategic IP management—through broad composition claims, detailed method claims, and targeted indications—can safeguard market exclusivity. Future patent litigations and licensing strategies will likely hinge on the specific structural differences asserted against prior art and competitors’ innovations.

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Key Takeaways

• The '947 patent's claim structure strategically balances broad composition coverage with specific therapeutic applications, safeguarding core innovations.

• Its place within a complex patent landscape highlights the importance of detailed structural distinctions to sustain patent validity amid prior art challenges.

• The patent's longevity affords GSK an extended market exclusivity window, influencing development, licensing, and litigation strategies.

• Continuous portfolio management, including filings for secondary patents, is essential for maintaining competitive advantage post-expiry.

• Stakeholders must vigilantly monitor competitors' patent filings, potential infringement, and opportunities for licensing or design-around paths.

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FAQs

1. What is the primary chemical class protected by U.S. Patent 8,926,947?
The patent principally claims substituted pyrazoline derivatives designed for therapeutic use in inflammatory and autoimmune conditions.

2. How broad are the claims in the '947 patent?
The claims cover a wide range of derivatives with various substituents, as well as methods of using these compounds to treat specific diseases, offering substantial exclusivity.

3. What are potential challenges to the patent's validity?
Challenges include prior art disclosures of similar pyrazoline compounds and arguments of obviousness, especially if structural differences are minor or predictable based on existing literature.

4. How does the patent landscape influence future development?
It can both shield innovations and pose barriers; competitors will analyze the scope for design-around or challenge claims based on prior art. Strategic filings of secondary patents can extend protection.

5. When does the patent expire, and what implications does this have?
Assuming standard 20-year term from filing, the patent expires around 2035, after which generic or biosimilar development could increase. Licensing negotiations and R&D focus should plan accordingly.

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References

1. U.S. Patent 8,926,947. "Pyrazoline derivatives for treatment of inflammatory diseases."
2. Relevant prior art patents and literature in kinase inhibitors and anti-inflammatory agents.
3. Patent prosecution and legal analyses related to pyrazoline derivative patents.

Drugs Protected by US Patent 8,926,947

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 8,926,947

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1169062		C300558	Netherlands
European Patent Office	1169062		CA 2012 00050	Denmark
European Patent Office	1169062		92114	Luxembourg
European Patent Office	1169062		C01169062/01	Switzerland
European Patent Office	1169062		1290043-7	Sweden
European Patent Office	1169062		300558	Netherlands
European Patent Office	1169062		2012C/052	Belgium