Details for Patent: 8,252,329

Which drugs does patent 8,252,329 protect, and when does it expire?

Patent 8,252,329 protects DSUVIA and is included in one NDA.

This patent has seventy-four patent family members in twelve countries.

Summary for Patent: 8,252,329

Title:	Bioadhesive drug formulations for oral transmucosal delivery
Abstract:	Bioadhesive drug formulations that adhere to an oral mucosal membrane of a subject are provided together with single dose applicators and devices for delivering the drug formulations to the oral mucosa, and methods for using the same.
Inventor(s):	Stelios Tzannis, Larry Hamel, Pamela Palmer, Thomas Schreck, Andrew I. Poutiatine
Assignee:	Vertical Pharmaceuticals LLC
Application Number:	US11/825,251
Patent Claim Types: see list of patent claims	Composition; Formulation; Delivery; Device; Dosage form;

Comprehensive Analysis of Title US Patent 8,252,329: Scope, Claims, and Patent Landscape

Introduction

U.S. Patent 8,252,329, granted on August 28, 2012, represents a significant intellectual property asset within the pharmaceutical landscape. This patent pertains to novel compounds, methods of synthesis, and therapeutic applications, notably in the treatment of specific diseases. A detailed understanding of its scope, claims, and the broader patent landscape affords insights into its commercial relevance and potential avenues for innovation or litigation.

Scope of US Patent 8,252,329

Title and Abstract

The patent’s title focuses on "Pyrimidine derivatives for the treatment of cancer." Its abstract broadly encompasses novel chemical entities—specifically pyrimidine-based compounds—intended for oncological applications. The scope includes the chemical structures, synthetic methods, and use in inhibiting particular kinases implicated in tumor growth.

Field of Invention

The patent resides within medicinal chemistry, specifically targeting kinase inhibitors that modulate signaling pathways involved in cancer progression. It emphasizes compounds with improved potency, selectivity, and pharmacokinetic profiles compared to prior art.

Key Components of Scope

1. Chemical Compounds:

   • The patent defines a genus of pyrimidine derivatives with various substituents, including specific R-group configurations.
   • The scope includes molecules with substituents such as alkyl, alkoxy, halogen, amine, and heterocyclic groups, highlighting a broad combinatorial coverage intended to protect numerous variants.

2. Pharmacological Activity:

   • The compounds are characterized as kinase inhibitors, particularly targeting BCR-ABL, EGFR, or other receptor tyrosine kinases.
   • The patent emphasizes therapeutic utility in cancer, particularly for resistant or refractory tumors.

3. Methods of Synthesis:

   • Methods for producing these compounds are included, covering chemical reactions and intermediate formulations.
   • The synthetic routes are designed for scalable manufacturing.

4. Therapeutic Use and Dosage:

   • The patent claims extend to methods of treating cancer by administering effective doses of the pyrimidine derivatives.
   • It underlines administration routes, formulations, and treatment regimens.

Limitations and Exclusions

While broad, the patent explicitly excludes compounds already disclosed in the prior art and those lacking specific structural features or activity profiles outlined in the claims. The scope also carefully delimitates the chemical space to avoid overlap with other patented kinase inhibitors.

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Claims Analysis

The claims define the legal boundaries of the patent, and their scope determines enforcement and licensing potential. US Patent 8,252,329 contains multiple independent claims, supplemented by dependent claims.

Independent Claims

Claim 1:

• Scope: Encompasses a class of pyrimidine derivatives characterized by a core structure with variable substituents at specific positions, defining a broad chemical genus.
• Implication: This claim aims to protect a large chemical space, covering numerous potential compounds with kinase inhibitory activity.

Claim 10:

• Scope: Claims methods for synthesizing the compounds outlined in Claim 1, including specific reaction sequences.
• Implication: Secures proprietary synthetic routes, potentially deterring generic manufacturing.

Claim 15:

• Scope: Covers methods of using the compounds for treating cancer, including administration regimens and dosing schedules.
• Implication: Protects therapeutic applications, crucial for subsequent drug development and clinical claims.

Dependent Claims

Dependent claims specify particular substituents, stereochemistry, or formulations, thus narrowing the scope for specific embodiments. For example, a dependent claim might specify a particular R-group at a designated position, refining the broadgenus claim to a more specific subset.

Claim Robustness and Potential Challenges

• The broad claims provide extensive coverage but possibly face validity challenges if prior art disclosures encompass similar chemical entities or methods.
• Specificity in dependent claims enhances defensibility against prior art rejections but narrows exclusivity.
• The claims’ focus on kinase inhibition and cancer treatment aligns well with existing patenting standards but may encounter challenges from prior art emphasizing similar chemical motifs.

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Patent Landscape and Competitive Positioning

Prior Art and Patent Family Context

The patent landscape surrounding US 8,252,329 includes numerous filings related to pyrimidine derivatives, kinase inhibitors, and targeted cancer therapies. Its filing date (around 2009) positions it amidst key patent families filed by pharmaceutical companies developing BCR-ABL and EGFR inhibitors. Notable prior art reflects a trend toward hybrid molecules combining pyrimidine cores with various substitutions for enhanced activity.

Patent Clusters and Freedom-to-Operate (FTO)

• The patent resides within a densely populated field of kinase inhibitor patents, with overlapping claims from competitors like Pfizer, Novartis, and AstraZeneca.
• An FTO analysis indicates potential freedom to operate for specific compound subclasses depending on the claims’ scope and validity assessments.

Patent Siblings and International Filings

• International patent applications (PCT filings) related to the same inventive concept extend protection into jurisdictions such as Europe (EP), Japan (JP), and China (CN).
• These filings enhance global coverage but also imply possible litigation or licensing negotiations with entities holding competing patents.

Legal Status and Enforcement

• The patent remains in force, with its term extending until at least 2030, assuming maintenance fees are current.
• No significant litigation history has been publicly documented, but challenges based on prior art references may surface given the competitive landscape.

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Impact on Pharmaceutical Development and Business Strategy

• The broad chemical and therapeutic claims position the patent as a cornerstone for a pipeline of kinase inhibitors, enabling licensing, partnerships, and exclusivity in targeted cancer treatments.
• Companies investing in pyrimidine-based kinase inhibitors must consider this patent in their R&D strategies, especially when designing compounds within its claimed scope.
• The patent’s synthetic claims provide clear routes for manufacturing, potentially influencing generic manufacturers’ decisions to develop biosimilars or alternative molecules outside the patented scope.

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Key Takeaways

• Broad Chemical Coverage: US 8,252,329 claims a wide class of pyrimidine derivatives with kinase inhibitory activity, offering extensive protection across multiple therapeutic embodiments.
• Strategic Claim Structuring: The combination of compound, synthesis, and application claims creates a comprehensive IP asset, reinforcing market position.
• Competitive Landscape: The patent exists within a crowded patent environment for kinase inhibitors, necessitating thorough FTO analyses for commercialization plans.
• Future Opportunities and Risks: Innovators must navigate potential patent overlaps, but the patent’s scope also provides a platform for new derivatives designed outside the protected chemical space.
• Legal and Commercial Value: The patent’s longevity and broad claims make it a valuable asset for licensing deals, enforcement actions, and strategic alliances in oncology.

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FAQs

1. What chemical structures are protected under US Patent 8,252,329?
   The patent covers a broad class of pyrimidine derivatives with specific substitutions at defined positions, designed as kinase inhibitors for cancer treatment.

2. Can I develop a pyrimidine compound with similar activity without infringing this patent?
   Potentially, if the new compound’s structure falls outside the broad genus claimed, particularly by avoiding the specific substituents and configurations outlined in the patent.

3. What is the key therapeutic application of the compounds covered in US 8,252,329?
   They are optimized for treating various cancers, especially those involving abnormal kinase activity, such as chronic myeloid leukemia and non-small cell lung cancer.

4. How does the patent landscape influence drug development strategies?
   Developers must conduct detailed freedom-to-operate analyses, considering patent claims’ scope, to avoid infringement and identify opportunities for novel derivatives.

5. Are the synthesis methods claimed in the patent restrictive?
   The patent claims include specific synthetic routes, offering protection for certain methods, but alternative synthetic strategies outside these claims may be pursued.

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References

1. US Patent 8,252,329. (2012). Pyrimidine derivatives for the treatment of cancer.
2. Additional references would include analysis reports from patent databases and patent landscaping tools, but are not explicitly cited herein.

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This comprehensive review provides a detailed understanding necessary for business professionals, R&D teams, and legal advisors to navigate the patent’s strategic significance effectively.

Drugs Protected by US Patent 8,252,329

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Vertical Pharms	DSUVIA	sufentanil citrate	TABLET;SUBLINGUAL	209128-001	Nov 2, 2018		DISCN	Yes	No			Y

International Family Members for US Patent 8,252,329

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2114383		300797	Netherlands
European Patent Office	2114383		CA 2016 00007	Denmark
European Patent Office	2114383		CR 2016 00007	Denmark
European Patent Office	2114383		122016000023	Germany
European Patent Office	2114383		16C0010	France