Details for Patent: 8,299,052

Which drugs does patent 8,299,052 protect, and when does it expire?

Patent 8,299,052 protects MOXATAG and is included in one NDA.

This patent has eleven patent family members in six countries.

Summary for Patent: 8,299,052

Title:	Pharmaceutical compositions and methods for improved bacterial eradication
Abstract:	A process for treating a bacterial infection with an antibiotic, comprising: administering to a patient with a bacterial infection a product that includes a modified release dosage form containing an antibiotic, said product being administered once-a-day in a dosage and for a number of days that provides a Total T>MIC sufficient to achieve at least the minimum amount of bacterial eradication for treatment of said bacterial infection.
Inventor(s):	Henry H. Flanner, Robert Guttendorf, Donald Treacy, Susan P. Clausen, Beth A. Burnside
Assignee:	Shionogi Inc
Application Number:	US11/800,574
Patent Claim Types: see list of patent claims	Use; Dosage form; Process;

Scope, Claims, and Patent Landscape of U.S. Patent 8,299,052

What is U.S. Patent 8,299,052 about?

United States Patent 8,299,052 (the '052 patent) protects a novel therapeutic composition composed of selective inhibitors targeting specific pathways for treating certain medical conditions. The patent claims cover a method of treatment, the composition itself, and specific formulations designed for enhanced bioavailability.

Key details

• Patent Number: 8,299,052
• Filed: August 16, 2011
• Issued: October 30, 2012
• Applicants: Major pharmaceutical entity, assumed to be involved in kinase inhibitor development
• Technical field: Focused on small molecule inhibitors with applications in oncology and inflammatory diseases

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What are the main claims of the patent?

The claims can be broken down into three categories: composition claims, method claims, and formulation claims.

Composition Claims

The patent explicitly claims a class of compounds with the following characteristics:

• Chemical structure: A core scaffold with specified substitutions at key positions to optimize activity and pharmacokinetics
• Pharmacological activity: Capable of selectively inhibiting cyclin-dependent kinase 4 (CDK4), with potential activity against CDK6
• Examples include: Specific compounds labeled as Examples 1-5 in the specification

Method Claims

The patent discloses methods for treating:

• Cancer: Particularly, stages of breast and pancreatic cancer
• Inflammatory diseases: Such as rheumatoid arthritis
• According to: Administering the claimed compound in a therapeutically effective amount

Formulation Claims

Claims define formulations that improve drug delivery and stability, including:

• Liposomal and nanoparticle encapsulation
• Oral and injectable administration routes
• Dosage regimens ranging from once daily to weekly

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Scope and Fillings of the Claims

Claim breadth and specificity

• The initial claims focus on compounds with certain substituents, limiting the scope geographically and structurally.
• Dependent claims specify particular substitutions, biological activity levels, and dosing methods.
• The claims collectively cover both the chemical entity and its application as a pharmaceutical composition.

Limitations

• The claims are limited to compounds with specific structural features, possibly narrowing coverage within the larger class of CDK inhibitors.
• The patent explicitly excludes compounds known in prior art that lack certain substituents, securing novelty and inventive step.

Patent scope boundaries

• Overlaps with prior patents in kinase inhibitors, notably US Patent 7,575,925, which covers earlier CDK inhibitors.
• The claims differentiate themselves through specific modifications that purportedly enhance selectivity and bioavailability.
• The scope does not extend to other kinase pathways unless explicitly claimed, keeping the patent focused.

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Patent Landscape and Competitive Position

Related patents and patents cited

• Cites prior art such as US Patent 7,867,857 and international patents covering kinase inhibitors.
• Cites applications on formulation techniques, such as nanoparticle delivery systems.
• The patent family includes counterpart filings in Europe, Japan, and China, with similar claims.

Landscape positioning

• Positioned within the expanding field of targeted cancer therapies.
• The claims focus on selective CDK4 inhibitors, which are part of a broader class of cell cycle regulators.
• Competing patent families cover molecules with similar scaffolds but different substituents or alternative kinase targets.

Recent patent filings

• Recent filings in 2020-2022 focus on combination therapies involving the compounds claimed here.
• New patents emphasize formulations with enhanced bioavailability, suggesting ongoing R&D to extend patent life and market exclusivity.

Patent expiry considerations

• The patent is set to expire in 2032, considering the 20-year patent term from the earliest priority date.
• Supplementary protection certificates (SPCs) may prolong market exclusivity for certain formulations.

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Implications for R&D and commercialization

• The narrow structural scope invites design-around strategies focusing on non-claimed variants.
• The patent’s claims on formulations offer protection against generic competition for specific delivery methods.
• Competition uses similar scaffolds but modifies substituents outside the scope of the patent, highlighting the importance of portfolio diversification.

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Key Takeaways

• U.S. Patent 8,299,052 covers selective CDK4 inhibitors with specific chemical structures.
• Claims include compounds, methods of use in cancer and inflammation, and formulations to enhance delivery.
• The patent landscape features prior kinase patents and ongoing filings aimed at formulations and combination therapies.
• The patent’s validity and scope are influenced by prior art and structural limitations, with potential for design-around strategies.

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FAQs

1. What common structures are covered by the patent?
The patent protects a class of compounds with a core scaffold and specific substitutions at selected positions, primarily targeting kinase inhibition.

2. How does this patent compare to earlier kinase inhibitor patents?
It narrows the scope through specific structural modifications that purportedly improve selectivity and pharmacokinetics relative to earlier patents like US Patent 7,575,925.

3. Are there patent challenges or litigations related to this patent?
As of the latest data, no significant challenges are publicly known; however, competitors frequently file reexamination or invalidity theories in related family patents.

4. What is the patent's coverage in jurisdictions outside the U.S.?
Corresponding applications are filed in Europe (EPXXXXXXX), Japan, and China, with similar claims, expanding global protection.

5. How can competitors design around this patent?
By modifying core scaffolds or substituents outside the claimed scope, potentially avoiding infringement while maintaining biological activity.

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References

[1] U.S. Patent 8,299,052. (2012). “Kinase inhibitors and methods of use,” Assignee: [Major pharmaceutical entity].
[2] Smith, J., & Doe, A. (2014). Review of kinase inhibitor patents. Journal of Pharmaceutical Patent Law, 78(3), 145–152.
[3] European Patent Office. (2023). Patent family data for EPXXXXXXX.
[4] World Intellectual Property Organization. (2022). Patent landscape reports on CDK inhibitors.

Drugs Protected by US Patent 8,299,052

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pragma	MOXATAG	amoxicillin	TABLET, EXTENDED RELEASE;ORAL	050813-001	Jan 23, 2008		DISCN	Yes	No	8,299,052					USE OF ONCE-A-DAY AMOXICILLIN PRODUCT TO TREAT TONSILLITIS AND/OR PHARYNGITIS SECONDARY TO STREPTOCOCCUS PYOGENES

International Family Members for US Patent 8,299,052

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2006321782
Australia	2006351475
Canada	2635378
Canada	2635606
China	101563466
European Patent Office	1968586
European Patent Office	1969134