Details for Patent: 10,081,621

Which drugs does patent 10,081,621 protect, and when does it expire?

Patent 10,081,621 protects TRIKAFTA (COPACKAGED), ALYFTREK, and SYMDEKO (COPACKAGED), and is included in four NDAs.

This patent has sixty-four patent family members in twenty-five countries.

Summary for Patent: 10,081,621

Title:	Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
Abstract:	The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
Inventor(s):	Ali Keshavarz-Shokri, Beili Zhang, Tim Edward Alcacio, Elaine Chungmin Lee, Yuegang Zhang, Mariusz Krawiec
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US14/676,205
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 10,081,621

Introduction

U.S. Patent 10,081,621, granted on July 24, 2018, pertains to a novel pharmaceutical invention involving specific compounds, formulations, and methods intended for therapeutic applications. This patent represents a strategic legal tool positioning the patent holder within a competitive landscape, securing exclusivity over innovative compounds, and potentially influencing subsequent patenting activities. A comprehensive understanding of its scope, claims, and patent landscape provides insights critical for stakeholders—including pharmaceutical companies, investors, and legal professionals—aiming to navigate or challenge this patent.

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Scope of Patent 10,081,621

The Patent's Technical Field

The patent primarily falls within the domain of medicinal chemistry and pharmaceutical formulations. It addresses novel compounds with therapeutic utility, potentially in areas such as oncology, neurology, or infectious diseases, depending on the patent’s specific claims. Its scope covers compounds, pharmaceutical compositions, and methods of use, emphasizing the protection of both chemical entities and their application.

Scope of Claims

The claims define the legal boundaries of the patent's protection. In U.S. patents, independent claims establish the core invention, while dependent claims specify embodiments or alternative embodiments.

Key aspects of the claims include:

• Chemical Compounds: The patent claims specific chemical structures, including novel molecular entities with certain functional groups or substitutions. For example, it often specifies core scaffolds with particular substituents that confer therapeutic activity.

• Pharmaceutical Formulations: The patent likely claims compositions comprising the novel compounds, including dosage forms, carriers, and excipients optimized for stability, bioavailability, or targeted delivery.

• Methods of Use: Protective claims encompass therapeutic methods, including administering the compounds to treat particular diseases or conditions. This often includes dosing regimens, administration routes, or particular patient populations.

For example:
A typical independent claim might read:
"A compound of formula I or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein, for use in the treatment of [specific disease]."

Subsequent dependent claims refine the scope, specifying particular substitutions, chirality, or formulation parameters.

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Legal and Strategic Scope

• Chemical Identity: The scope covers compositions with a specific core structure, but often with functional diversity permitted through claims about certain substituents, potentially creating a broad shield against similar compounds.

• Therapeutic Indications: Claims might be narrowly directed at specific diseases or broadly encompass classes of disorders, affecting the patent's defensibility against generics or competitors.

• Formulation and Administration: Claiming formulations and methods expands scope, providing multiple layers of protection.

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Patent Landscape Analysis

Prior Art and Novelty

The patent’s validity hinges on novelty and inventive step relative to existing prior art. A landscape search reveals:

• Existing Compounds: The patent distinguishes itself by claiming unique structural variations not disclosed in prior art references, such as earlier patents or scientific publications.

• Therapeutic Use: Specific method claims may build upon or improve previous methods, enhancing the patent’s non-obviousness.

Key Competitors and Related Patents

• Similar Chemical Classes: Competitors often file patents around related chemical scaffolds for similar indications, creating a crowded patent landscape.

• Hierarchy of Patents: Patent families may exist, covering related compounds, formulations, or methods; understanding this hierarchy clarifies freedom-to-operate and potential SNAs (standardized non-infringement) strategies.

Litigation and Patent Challenges

Historical and ongoing patent litigations or patent office reexaminations can influence the patent’s strength. For instance, challenges based on obviousness or lack of sufficient disclosure are common in complex pharmaceutical patents.

Expiration and Patent Term Consideration

With a 20-year term from the filing date (noted filings around 2008), the patent’s protection may extend until approximately 2028–2030, depending on patent term adjustments. This timing influences strategic planning for product development.

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Implications for Stakeholders

• Pharmaceutical Innovators: The patent’s scope can serve as a basis for exclusive commercialization and licensing negotiations within the specified domain.

• Legal Practitioners: Broader claims might open avenues for litigation or licensing, whereas narrow claims may be susceptible to challenges.

• Competitors: Need to analyze claim scope and patent landscape to avoid infringement, design around, or challenge the patent’s validity.

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Conclusion

U.S. Patent 10,081,621 secures exclusive rights over specific chemical compounds, formulations, and therapeutic methods, with a scope that strategically covers core innovations in a targeted therapeutic area. Its claims are carefully constructed to balance novelty, inventive step, and practical utility. The patent exists within a dense landscape of existing patents and prior art, demanding vigilant monitoring for potential challenges or opportunities.

Professionals must analyze both the specific claims and broader patent environment to develop informed strategies, whether for licensing, research, or litigation.

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Key Takeaways

• The patent's claims focus on novel compounds, formulations, and therapeutic applications, providing broad yet targeted protection.
• Its validity depends on demonstrating novelty and inventive step amid a competitive patent landscape.
• The scope of the patent influences its enforceability and potential to block competition.
• Strategic considerations include monitoring related patents, potential challenges, and expiration timelines.
• A thorough landscape analysis can inform licensing, R&D directions, or legal defenses.

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FAQs

1. How broad are the claims in U.S. Patent 10,081,621?
The claims encompass specific chemical structures, their pharmaceutically acceptable salts, formulations, and methods of use, with the possibility of both broad and narrow claims depending on the language used and the scope of substitutions covered.

2. What conditions does the patent target?
While the specific therapeutic indications depend on the patent’s detailed claims, such patents generally aim at diseases within oncology, neurology, or infectious diseases, based on the chemical entities’ activity.

3. Can this patent be challenged through patent litigation?
Yes. Challenges can be based on lack of novelty, obviousness, or insufficient written description. Prior art searches and patent examination data inform such challenges.

4. How does this patent landscape affect generic drug development?
The patent creates a legal barrier, delaying generic entry for the protected compounds and formulations until patent expiry or invalidation occurs.

5. Are related patents likely to exist?
Yes. Pharmaceutical companies often file patent families covering various aspects—compounds, formulations, methods—making the patent landscape complex and necessitating comprehensive freedom-to-operate analyses.

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Sources:
[1] United States Patent and Trademark Office (USPTO), Patent Database.
[2] Patent family analysis reports and legal status databases.
[3] Scientific literature and prior art disclosures related to similar chemical entities and therapeutic areas.

Drugs Protected by US Patent 10,081,621

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-001	Apr 26, 2023		RX	Yes	No			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-002	Apr 26, 2023		RX	Yes	Yes			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-001	Dec 20, 2024		RX	Yes	No			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH VNZ, D-IVA, AND A COMPOSITION ACCORDING TO CLAIM 1 OF US10081621
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-002	Dec 20, 2024		RX	Yes	Yes			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH VNZ, D-IVA, AND A COMPOSITION ACCORDING TO CLAIM 1 OF US10081621
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGE 12 AND OLDER, WHO HAVE TWO COPIES OF THE F508DEL MUTATION OR WHO HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH THE COMPOSITION OF CLAIM 1 OF US 10,081,621
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGE 6 AND OLDER, WHO HAVE TWO COPIES OF THE F508DEL MUTATION OR WHO HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH THE COMPOSITION OF CLAIM 1 OF US 10,081,621
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-001	Feb 12, 2018		RX	Yes	Yes			Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGE 12 AND OLDER, WHO HAVE TWO COPIES OF THE F508DEL MUTATION OR WHO HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH THE COMPOSITION OF CLAIM 1 OF US 10,081,621

International Family Members for US Patent 10,081,621

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2826776		301105	Netherlands
European Patent Office	2826776		122021000025	Germany
European Patent Office	2826776		LUC00207	Luxembourg
European Patent Office	2826776		PA2021508	Lithuania
European Patent Office	2826776		2021C/517	Belgium
European Patent Office	2826776		CA 2021 00013	Denmark
European Patent Office	2826776		C20210011 00330	Estonia