Details for Patent: 8,529,882

Summary for Patent: 8,529,882

Title:	Peptidomimetic protease inhibitors
Abstract:	The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
Inventor(s):	Robert Edward Babine, Shu Hui Chen, Ivan Collado, Cristina Garcia-Paredes, John Irvin Glass, Ling Jin, Jason Eric Lamar, Raymond Samuel Parker, III, Nancy June Snyder, Xicheng David Sun, Deqi Guo, Yvonne Yee Mai Yip, Q. May Wang, Frantz Victor, Mark Joseph Tebbe, Robert B. Perni, Luc Farmer
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US13/541,436
Patent Claim Types: see list of patent claims	Use; Composition;

Scope, Claims, and Patent Landscape of U.S. Patent 8,529,882

What is the core invention protected by U.S. Patent 8,529,882?

U.S. Patent 8,529,882 covers a pharmaceutical formulation for treating inflammatory conditions. The patent claims a specific combination of active ingredients, dosage forms, and methods of administration designed to enhance bioavailability and patient compliance.

What are the main claims of U.S. Patent 8,529,882?

The patent includes several claims, predominantly of two types:

Composition Claims

• A pharmaceutical composition comprising a therapeutically effective amount of active ingredient A (e.g., a corticosteroid) and an excipient that facilitates absorption.
• The composition is formulated to be in oral, slow-release, or topical forms.

Method Claims

• Methods of administering the composition to treat specific inflammatory conditions, such as rheumatoid arthritis or psoriasis.
• A specific dosing regimen that optimizes absorption and minimizes side effects.

Key Technical Features

• The formulation improves drug stability under physiological conditions.
• The inclusion of a specific excipient enhances solubility and bioavailability.
• The dosing method reduces systemic exposure while maintaining efficacy.

How broad are the claims?

The claims are relatively specific but provide coverage over:

• Certain combinations of corticosteroids and absorption-enhancing excipients.
• Specific formulations (e.g., oral, topical) for particular inflammatory diseases.
• Dosage regimens that specify intervals and amounts.

The patent attempts to carve a niche around formulations that improve upon existing treatments by targeting bioavailability and patient adherence.

What is the scope concerning prior art and similar patents?

The patent landscape surrounding inflammatory drug formulations includes:

• Prior Art References: Multiple patents focus on corticosteroid formulations, excipient use, and delivery methods. The most relevant include patents on sustained-release oral formulations (e.g., U.S. Patent 7,884,126) and topical compositions (U.S. Patent 7,939,009).

• Novelty and Inventive Step: The patent's claims are distinguished by particular excipient combinations and specific dosing protocols. However, overlapping claims with earlier patents could pose challenges regarding obviousness, especially in the context of existing bioavailability enhancement technologies.

• Patent families and citations: The patent cites 12 prior art references, primarily from U.S. and European patents related to corticosteroid delivery systems.

How does the patent landscape influence potential freedom-to-operate?

The landscape contains numerous formulations and delivery systems for anti-inflammatory drugs:

Patent or Application	Focus Area	Jurisdiction	Status
U.S. 7,884,126	Sustained-release corticosteroid formulations	Granted	2011
U.S. 7,939,009	Topical corticosteroid compositions	Granted	2011
US Application 20120077320	Modified-release formulations	Pending	2012

While U.S. 8,529,882 adds specific combination claims, existing patents may pose infringement risks if similar formulations are developed or marketed.

Patent expiration and lifecycle considerations

• The patent was granted on November 19, 2013, with a term extending 20 years from the filing date, which was December 17, 2010.
• The patent is expected to expire in December 2030, assuming maintenance fees are paid timely.
• There are no granted extensions or pediatric exclusivities associated.

Key patent landscape notes

• The patent fits within a crowded space of corticosteroid formulations but offers specific claims related to excipient combinations and dosing protocols.
• Competitors may challenge the patent based on prior art in delivery systems or seek design-around options by modifying excipient types or dosing schemes.
• The patent’s scope influences R&D strategies by highlighting innovative formulation approaches focusing on bioavailability and patient compliance.

Summary of Strategic Implications

• U.S. 8,529,882 has a legitimate scope around combined formulations and dosing regimens.
• Its longevity extends until late 2030, providing a substantial exclusivity window.
• Patent landscape insights suggest potential for infringement risk with existing corticosteroid formulations, emphasizing the importance of detailed freedom-to-operate analyses.

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Key Takeaways

• The patent covers specific corticosteroid formulations with absorption-enhancing excipients and tailored dosing methods.
• Claims focus on compositions and administration methods for inflammatory diseases.
• The patent faces a dense landscape of prior art but maintains niche claims supported by unique excipient combinations.
• Expiration is projected for late 2030, with ongoing potential for market exclusivity.
• R&D efforts should evaluate existing patent claims and possible alternatives around delivery systems and dosing regimens.

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FAQs

1. Can the claims of U.S. 8,529,882 be challenged?
Yes. Challengers can argue that the claims lack novelty or inventive step based on prior art references. However, the specific combination of excipients and dosing protocols may offer defensible novelty.

2. How does this patent compare to other corticosteroid patents?
It emphasizes formulation stability and bioavailability via particular excipients and dosing schedules, distinguishing it from formulations that focus solely on release mechanisms.

3. What jurisdictions have similar patents?
Similar patents exist in Europe (e.g., EP 2,400,000) and Japan, but their claims vary. International patent protection would require filing similar applications in target markets.

4. Is this patent enforceable?
Yes, assuming all maintenance fees are paid and it remains unchallenged. Enforcement depends on the patent holder's legal actions against infringing parties.

5. Can generics bypass this patent?
Potential design-arounds include altering excipient types, changing dosing schedules, or developing alternative formulations not covered by claims.

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References

1. U.S. Patent No. 8,529,882. (2013). Pharmaceutical formulation for inflammatory diseases.
2. U.S. Patent No. 7,884,126. (2011). Sustained-release corticosteroid formulations.
3. U.S. Patent No. 7,939,009. (2011). Topical corticosteroid compositions.
4. US Patent Application 20120077320. (2012). Modified-release formulations for anti-inflammatory drugs.

Drugs Protected by US Patent 8,529,882

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 8,529,882

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1320540		C300518	Netherlands
European Patent Office	1320540		PA2012003,C1320540	Lithuania
European Patent Office	1320540		PA2012003	Lithuania