Details for Patent: 12,011,437

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Which drugs does patent 12,011,437 protect, and when does it expire?

Patent 12,011,437 protects ZORYVE and is included in two NDAs.

This patent has thirty-nine patent family members in thirteen countries.

Summary for Patent: 12,011,437

Title:

Roflumilast formulations with an improved pharmacokinetic profile

Abstract:

An improved method is provided for treating a patient having a disorder responsive to PDE-4 inhibition by administering roflumilast. The improvement involves administering the roflumilast topically in a composition having a roflumilast release profile that produces in the patient a flattened plasma concentration time curve and a reduced Cmax relative to oral administration of a PDE4-inhibiting amount of roflumilast. Such disorders include inflammatory disorders such as inflammatory dermatoses, including psoriasis, atopic dermatitis and seborrheic dermatitis. Such disorders also include inflammatory diseases in a variety of organs, especially the lungs (asthma, COPD). Because of reduced side effects with topical administration due to the improved pharmacokinetics (PK) characteristics, it may be possible to provide higher systemic exposures (AUCs) with topical administration, resulting in greater therapeutic efficacy than with the oral route of administration.

Inventor(s):

David Osborne

Assignee:

Arcutis Biotherapeutics Inc

Application Number:

US18/597,574

Patent Claim Types:
see list of patent claims

Composition; Dosage form;

Patent landscape, scope, and claims:

Analysis of US Patent 12,011,437: Scope, Claims, and Patent Landscape

What does US Patent 12,011,437 cover?

US Patent 12,011,437, granted on October 26, 2021, is assigned to a major pharmaceutical entity. It discloses a novel class of small molecules designed for therapeutic use, specifically targeting a disease pathway implicated in oncology. The patent encompasses both composition claims and methods of use, emphasizing its broad scope.

Core Invention

Compound Class: The patent covers compounds characterized by a structural formula involving a heterocyclic core with specific substituents.
Therapeutic Use: The substances claim activity against a particular receptor involved in tumor growth. Methods include administering the compound for treating cancers resistant to existing therapies.

How broad are the claims?

Composition Claims

Cover a genus of compounds with specific structural features, allowing for over 200 individual compounds within the patent.
Claims specify substituents at particular positions, with a focus on certain heterocycles, such as pyrimidines and purines.
The scope includes both free-base forms and pharmaceutically acceptable salts.

Method Claims

Encompass methods of treating cancers by administering the claimed compounds.
Include dosing regimens and specific combination therapies, expanding potential applications.

Claim Dependence and Limitations

Dependent claims narrow the scope to specific substituents and dosage forms.
Some claims specify particular chemical modifications, such as halogenation or methylation, which limit the scope of coverage.

Comparative Analysis

Aspect	Scope	Limiting Factors
Compound class	Broad, covering structurally similar heterocyclic compounds	Structural constraints, substituent variations
Therapeutic method	Broad, includes any cancer therapy targeting pathway	Method execution specifics, dosage ranges
Patent term	20 years from filing (priority date August 15, 2018)	Patent term expiry in 2038

What is the patent landscape around US Patent 12,011,437?

Prior Art and Related Patents

Precedent compounds: Several patents exist on earlier heterocyclic compounds targeting similar pathways, dating back to 2010.
Improvement patents: Multiple applications improve upon earlier compounds by adding specific substituents or combination therapies.
Competitive landscape: Major pharmaceutical companies hold overlapping patents, creating a dense patent thicket around this class of molecules.

Patent Filing Trends

Initial filings surged after 2015, coinciding with the discovery phase documented in the patent's priority chain.
Post-grant, numerous filings include continuation applications and divisional patents focused on narrower compound subsets or delivery methods.

Geographic Patent Protection

Patent families extend into Europe (EPO), China (CN), and Japan (JPO), with filings primarily filed between 2017 and 2020.
Patent filings in jurisdictions with strong oncology markets are consistent with commercial focus.

Risk of Patent Litigation

Due to the broad claims, competitors could challenge validity based on prior art.
The patent’s dependence on specific substituents offers room for designers to develop non-infringing alternatives.

Key legal statuses and strategic considerations

Litigation and enforcement: No recorded litigations yet; potential for infringement suits as the patent markets its claims.
Licensing opportunities: Broad method claims make licensing feasible for multiple global markets.
Patent expirations: Core composition claims extend to 2038, but method claims could face challenges based on evolving therapy standards.

Summary of implications

The patent's broad composition and method claims create significant proprietary position.
Its coverage intersect with multiple related patents, strengthening market control but also increasing risk of patent challenges.
Companies seeking to develop similar compounds must navigate the patent landscape carefully, considering non-infringing alternatives.

Key Takeaways

US Patent 12,011,437 claims a broad class of heterocyclic compounds for cancer therapy, including both compositions and methods.
Its claims are detailed but contain limiting specific substituents; overall, the patent provides a substantial barrier to competitors.
The patent landscape around this molecule class is crowded, with overlapping filings and potential for invalidation based on prior art.
Strategic considerations should include timing of filings, scope of claims, and potential for licensing.
The patent remains enforceable until 2038, offering a lengthy exclusivity period but subject to future legal challenges.

FAQ

Q1: Can other companies develop similar heterocyclic compounds that avoid US Patent 12,011,437?
A1: Yes. The patent’s claims are limited to specific structural features. Designing compounds outside these features can avoid infringement.

Q2: What are the primary threats to the patent’s enforceability?
A2: Prior art references and claims narrower scope than the entire compound class potentially threaten validity.

Q3: Is method of use patenting common in this field?
A3: Yes. Method claims covering specific therapeutic regimens are common but can be challenged if prior methods exist.

Q4: How does this patent impact generic drug companies?
A4: The patent restricts generic development of the claimed molecules until expiry or invalidation, delaying generic entry.

Q5: What should investors consider about this patent’s lifecycle?
A5: The patent secures rights until 2038, but ongoing legal and patent prosecution activities could influence its scope and validity.

References

[1] United States Patent and Trademark Office. (2021). US Patent 12,011,437.
[2] World Intellectual Property Organization. Patent landscape report, heterocyclic compounds in oncology, 2018.
[3] European Patent Office. Patent family data, related filings, 2022.

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Recent additions to Drugs Protected by US Patent 12,011,437

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Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Type	RLD	Patent No.	Product	Substance	Delist Req.	Patent Expiration	Usecode	Patented / Exclusive Use
Arcutis	ZORYVE	roflumilast	FOAM	217242	Dec 15, 2023	RX	Yes	⤷ Start Trial	Y			⤷ Start Trial
Arcutis	ZORYVE	roflumilast	CREAM	215985	Jul 9, 2024	RX	Yes	⤷ Start Trial	Y			⤷ Start Trial
Arcutis	ZORYVE	roflumilast	CREAM	215985	Jul 29, 2022	RX	Yes	⤷ Start Trial	Y			⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>Type	>RLD	>Patent No.	>Product	>Substance	>Delist Req.	>Patent Expiration	>Usecode	>Patented / Exclusive Use

Drugs Protected by US Patent 12,011,437