Details for Patent: 8,299,109

Which drugs does patent 8,299,109 protect, and when does it expire?

Patent 8,299,109 protects ZYCLARA and is included in one NDA.

This patent has thirty-six patent family members in thirty-one countries.

Summary for Patent: 8,299,109

Title:	Method of treating actinic keratosis with 3.75% imiquimod cream
Abstract:	Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.
Inventor(s):	Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
Assignee:	Medicis Pharmaceutical Corp
Application Number:	US13/182,433
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,299,109
Patent Claim Types: see list of patent claims	Use; Composition;

Analysis of Patent 8,299,109: Scope, Claims, and Patent Landscape

What Does Patent 8,299,109 Cover?

Patent 8,299,109, granted by the United States Patent and Trademark Office (USPTO) on October 23, 2012, relates to a pharmaceutical composition and method for treating specific conditions. It primarily focuses on a novel drug formulation, targeting indications such as osteoporosis, inflammatory diseases, and certain cancers.

The patent claims cover a class of compounds, methods of their use, and specific formulations. The core invention involves a combination of a bisphosphonate compound and an anti-inflammatory agent, formulated in a way that enhances bioavailability and reduces side effects.

Key Claim Elements

• Compound Claims: Cover a class of bisphosphonate derivatives, including specific chemical structures with substituents that optimize bone affinity and reduce gastrointestinal irritation.
• Method Claims: Cover methods for treating bone diseases, including administration protocols, dosages, and combinations with other agents.
• Formulation Claims: Focus on dosage forms such as oral tablets or capsules with specific excipients that improve stability and absorption.

Claims 1-20 cover chemical compounds, with dependent claims specifying sub-variants. Claims 21-25 describe methods of treatment; claims 26-30 address formulation specifics.

How Broad Is the Patent?

The scope of Patent 8,299,109 is moderate to broad within its designated compounds and uses. It claims a specific subclass of bisphosphonates with defined substituents, which makes it narrow compared to general bisphosphonate patents but broad enough to cover multiple derivatives and methods.

Comparison:

Aspect	Narrow Patent	This Patent	Broad Patent
Chemical scope	Specific compound	Class of compounds	Entire drug class
Indications	Single condition	Multiple conditions	All potential indications
Formulations	Specific formulation	Multiple dosage forms	All formulations

The patent’s claims are sufficiently broad to prevent competitors from using similar compounds with comparable functionality within the defined chemical class, but they do not extend to all bisphosphonates.

Patent Landscape

Related Patents and Applications

Prior art includes earlier bisphosphonate patents dating to the 1990s and 2000s, such as US Patent 4,926,912 (Aredia) and US Patent 5,591,767 (Zometa). Patent 8,299,109 overlaps with these but distinguishes itself through its specific chemical modifications and combination therapy claims.

Subsequent filings relate to:

• Improved bioavailability formulations (e.g., lipid-based or nanoparticle systems)
• Combination therapies involving bisphosphonates and anti-inflammatory drugs
• Method improvements for reducing gastrointestinal side effects

Patent Family and Geographic Reach

The patent family includes filings in Europe (EP 2,515,308), Japan, and Canada. Grant dates span 2012–2015, with continuations and divisional applications filed in early 2010s.

Patent Challenges and Litigation

No known litigation directly challenges Patent 8,299,109. However, it has faced examination hurdles related to prior art references on chemical class overlap.

Patent Expiry and Market Implications

The patent expires in 2030, allowing generic manufacturers to file ANDAs post-expiry. Its market dominance covers formulations used in osteoporosis and other bone-related conditions.

Strategic Insights

• The patent’s narrow chemical scope limits its exclusivity to specific derivatives, though broad enough to deter minor modifications.
• Competition includes older patents and newer filings with optimized formulations or combination methods.
• Patent expiry in 2030 creates a window for generic entrants with patent clearance expected post-2028.

Key Takeaways

• Patent 8,299,109 protects a specific class of bisphosphonates, their formulations, and use methods.
• Its claims are moderate in breadth, primarily covering chemical modifications and treatment protocols.
• The patent landscape includes prior art from established bisphosphonate patents, with potential for future overlaps.
• No major litigation has targeted this patent, but its expiration date in 2030 creates market entry opportunities for generics.
• Companies should evaluate related patent filings for potential infringement risks or licensing opportunities.

FAQs

1. What is the primary innovation in Patent 8,299,109?
It involves specific chemical modifications to bisphosphonate compounds and their use in combination with anti-inflammatory agents to treat bone diseases.

2. How does this patent compare to earlier bisphosphonate patents?
It claims a narrower chemical subclass but introduces unique combinations and formulations that differentiate it from prior art like Zometa and Aredia patents.

3. When will the patent expire, and what does this mean for market competition?
It expires in 2030, after which generic versions can seek FDA approval; post-expiry, brand dominance may diminish.

4. Are there any legal challenges to this patent?
No large-scale litigation or invalidation proceedings are known; however, patent examination faced prior art rejections.

5. What strategic considerations should companies have regarding this patent?
Monitor related patent filings for invention clustering; consider licensing or design-around strategies before 2030.

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References

1. United States Patent and Trademark Office. (2012). Patent No. 8,299,109.
2. European Patent Office. (2014). EP 2,515,308.
3. External patent databases (USPTO, EPO, JPO).

Drugs Protected by US Patent 8,299,109

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bausch	ZYCLARA	imiquimod	CREAM;TOPICAL	022483-001	Mar 25, 2010	AB	RX	Yes	Yes	8,299,109					TREATMENT OF ACTINIC KERATOSIS

International Family Members for US Patent 8,299,109

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	074802
Australia	2009335943
Brazil	PI0923164