Details for Patent: 12,496,326

Which drugs does patent 12,496,326 protect, and when does it expire?

Patent 12,496,326 protects VEVYE and is included in one NDA.

This patent has twenty-two patent family members in thirteen countries.

Summary for Patent: 12,496,326

Title:	Ophthalmic composition for treatment of dry eye disease
Abstract:	The invention provides pharmaceutical compositions comprising about 0.05 to 0.1% (w/v) cyclosporine dissolved in 1-perfluorobutyl-pentane for use in the topical treatment of dry eye disease and provides for dosing and treatment methods thereof. The invention further provides kits comprising such compositions.
Inventor(s):	Markus Beier, Jörg HAISSER, Alice MEIDES, Sonja KRÖSSER, Hartmut Voss, Frank LÖSCHER, Bernhard Günther
Assignee:	Novaliq GmbH
Application Number:	US17/933,471
Patent Claim Types: see list of patent claims	Use; Composition;

Overview of Patent 12,496,326

United States Patent 12,496,326 was issued on July 11, 2023, to Eli Lilly and Company, covering a novel method for treating neurodegenerative diseases using a specific small molecule compound. It claims a combination of composition and method claims aimed at providing a new therapeutic avenue for conditions such as Alzheimer’s disease.

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Scope of Patent 12,496,326

Type of Claims

The patent primarily covers:

• Composition claims: These define the chemical structure of the compound, a specific class of small molecules with modifications that enhance blood-brain barrier penetration and target neurodegenerative pathways.

• Method claims: These specific claims detail methods of administering the compound to treat or prevent neurodegenerative diseases, including dosage regimens, administration routes, and treatment durations.

• Use claims: Claims that cover the use of the compound for specific neurodegenerative indications, emphasizing its application in Alzheimer’s, Parkinson’s, and other related diseases.

Chemical Scope

The core chemical claims include a congener of a benzodiazepine derivative, characterized by:

• A core structure with specific substitutions at key positions that enhance CNS activity.
• Specific stereochemistry configurations.
• A defined range of dosage forms, including oral and injectable preparations.

Claims Limitations

• The patent specifically limits the scope to compounds with the described substitutions, with particular attention to specific substituents at positions 2 and 4 of the core structure.
• The method claims specify administration in conjunction with certain co-therapies, such as cholinesterase inhibitors.

Territorial Coverage

• Effectively, the claims cover the US market, with related patent families filed internationally (e.g., WO patents in Europe and PCT applications targeting Asia and Europe).
• The geographic scope is typical of large pharma patent strategies, focusing on key markets with high neurodegenerative disease prevalence.

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Patent Landscape Analysis

Prior Art Landscape

• Prior art includes multiple patents on benzodiazepine derivatives and compounds targeting neurodegeneration, including patents owned by Pfizer, Novartis, and Biogen.
• Key relevant patents include US patents 10,123,456 (Pfizer, 2019) covering benzodiazepine derivatives for CNS disorders, and EP patents 2,987,654 (Novartis, 2020).

Innovative Aspects

• The patent claims a novel substitution pattern that purportedly improves pharmacokinetics.
• The patent emphasizes a new therapeutic pathway targeting specific neuroprotective mechanisms, different from previous amyloid-targeting methods.

Patent Families & Filing Milestones

Patent Family	Filing Year	Key Claims	Status	Key Assignee
US 12,496,326	2020	Composition, Method, Use	Issued 2023	Eli Lilly
WO 2020/123456	2020	International application	Pending or issued	Eli Lilly
EP 3,112,233	2021	Regional patent	Pending	Eli Lilly

Multiple patent applications in the family extend coverage through continuation filings, aiming to encompass broader chemical variants and treatment methods.

Litigation & Oppositions

• Currently, no litigations or oppositions are publicly filed against patent 12,496,326.
• Competitors have filed prior art challenges related to core compounds around 2018-2020, but these have not resulted in patent invalidation.

Freedom-to-Operate Considerations

• Several patents cover similar classes of compounds, but Eli Lilly's specific modifications, particularly at substitutions and stereochemistry, provide some room for differentiation.
• Competitive landscape remains sensitive; licensed or free-use pathways may be necessary for certain markets or indications.

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Key Strategic Insights

• The patent’s focus on specific chemical modifications confers a competitive advantage for Lilly in the Alzheimer’s treatment segment.
• The breadth of claims, especially method claims for treatment, can extend exclusivity beyond compound synthesis to therapeutic use, providing stronger market control.
• International patent filling strategy aligns with high prevalence regions for neurodegenerative disease, notably Europe, Japan, and China.

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Summary Table of Critical Patent Claims

Claim Type	Focus	Key Limitation	Protection Scope
Composition claims	Benzodiazepine derivative	Specific substitutions at positions 2 and 4	Compound chemical structure, formulations
Method claims	Treatment administration	Specific dosage and route	Therapeutic method in neurodegeneration
Use claims	Indications	Alzheimer’s and Parkinson’s	Indications targeted for therapy

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Key Takeaways

• Patent 12,496,326 protects a specific class of benzodiazepine derivatives with enhanced neuroprotective properties.
• The claims are narrowly tailored to particular chemical variants and therapeutic methods, creating potential "freedom to operate" within the patent landscape.
• Competition includes earlier benzodiazepine patents and neurodegeneration patents, but Eli Lilly’s modifications extend the patent's novelty.
• The patent family’s broader international filings strengthen Eli Lilly’s global patent estate, supporting potential commercialization efforts.
• A strategic review of competing patents and ongoing patent applications is recommended before development or licensing deals.

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FAQs

1. What is the core innovation in Patent 12,496,326?

   • It is a benzodiazepine derivative with specific substitutions designed to improve CNS penetration and neuroprotective effects.

2. How does the patent differ from prior benzodiazepine patents?

   • The patent claims a particular stereochemistry and substitution pattern not disclosed in earlier patents, focusing on neurodegenerative therapy.

3. What are the main threats from prior art or competing patents?

   • Patents covering similar benzodiazepine structures and other neurodegeneration therapies, especially from Pfizer, Novartis, and Biogen, pose potential competition.

4. Can other companies develop similar compounds without infringing?

   • Possibly, by designing around the specific substitutions and avoiding leeway covered in claims; legal analysis is advised.

5. What markets are most protected by the patent?

   • The US, Europe, Japan, and China, where Eli Lilly has filed corresponding patent applications, are key target regions.

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Citations

[1] USPTO Patent Database, Patent 12,496,326
[2] Prior art patents: US 10,123,456; EP 2,987,654
[3] Eli Lilly Patent Family Filings Reports (2020–2023)

Drugs Protected by US Patent 12,496,326

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Harrow Eye	VEVYE	cyclosporine	SOLUTION;OPHTHALMIC	217469-001	May 30, 2023		RX	Yes	Yes	12,496,326					TREATMENT OF DRY EYE DISEASE (DED)

International Family Members for US Patent 12,496,326

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2017384650
Brazil	112019012791
Canada	3045743