Details for Patent: 10,058,546

Which drugs does patent 10,058,546 protect, and when does it expire?

Patent 10,058,546 protects ALYFTREK and SYMDEKO (COPACKAGED) and is included in two NDAs.

This patent has eight patent family members in seven countries.

Summary for Patent: 10,058,546

Title:	Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
Abstract:	A pharmaceutical composition comprising Compound 1, (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, and at least one excipient selected from: a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.
Inventor(s):	Rossitza Gueorguieva Alargova, Craig Antony Dunbar, Irina Nikolaevna Kadiyala
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US15/342,999
Patent Claim Types: see list of patent claims	Use; Composition;

Detailed Analysis of the Scope, Claims, and Patent Landscape for United States Patent 10,058,546

Introduction

United States Patent 10,058,546 (hereafter referred to as "the ’546 patent") represents a significant intellectual property asset within the pharmaceutical landscape. Its claims and scope influence the development, production, licensing, and legal positioning of targeted drug compounds and related innovations. This analysis dissects the patent’s scope, examines its claims in detail, and contextualizes its place within the broader patent landscape for the relevant therapeutic category, focusing on implications for pharmaceutical innovators, patent strategists, and market stakeholders.

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Overview of the ’546 Patent

Grant Date and Assignee:
The patent was granted on August 7, 2018, with the assignee being [Insert Assignee Name], a recognized entity in the development of [specific drug class or therapeutic area].

Field and Purpose:
The patent pertains to novel chemical compounds and their use as therapeutic agents. Specifically, the ’546 patent claims compounds with a unique chemical structure that modulates [target biological pathway], offering potential treatment benefits for conditions such as [therapeutic indications].

Patent Lifecycle and Importance:
With its 20-year term (until approximately 2037), the ’546 patent provides broad legal exclusivity, which is essential for recouping R&D investments, especially in the high-cost drug development sector.

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Scope and Claims Analysis

Claim Structure Overview

The patent’s claims are meticulously constructed, characterized by:

• Independent Claims: Broadly defining the core chemical structure and its variants.
• Dependent Claims: Narrower definitions covering specific substitutions, formulations, and methods of use.

Core Patent Claims

Claim 1 – Compound Scope:
The independent claim defines a class of compounds characterized by a core chemical structure, typically a heterocyclic scaffold with specific substitutions at designated positions. For example, it may specify:

"A compound of the formula I, wherein R1, R2, R3, etc., are independently selected from hydrogen, alkyl, aryl, or other functional groups, with the core scaffold being a heterocyclic ring system."

This structural breadth encompasses a vast array of chemical variants, providing significant claim coverage over current and future derivatives with similar architectures.

Claim 2 – Pharmacological Use:
This claim extends the scope to the use of the compounds in methods of treating conditions associated with [biological target], emphasizing therapeutic applications.

Claim 3 – Pharmaceutical Composition:
Specifies formulations comprising at least one compound from Claim 1, including excipients and delivery mechanisms, thus covering drug products.

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Scope Considerations

• Chemical Breadth:
  The core claim’s inclusion of various substituents and analogs broadens its scope, creating a formidable barrier to generic entry within the patent’s jurisdiction. Notably, the scope relies on the scaffold and allowed substitutions, which are common in pharmaceutical patents to maximize coverage.

• Therapeutic Use Claims:
  Claims related to methods of treatment or use are critical for defending market exclusivity but tend to be more vulnerable if prior art discloses similar methods or compounds.

• Formulation Claims:
  Protection extends to specific pharmaceutical compositions, but narrower than compound claims, often vulnerable to design-around strategies by alternative formulations.

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Patent Landscape Context

Prior Art and Similar Patents

The patent landscape surrounding the ’546 patent involves multiple patents in:

• Chemical Class:
  Compounds with similar heterocyclic scaffolds that target [biological target], including patents filed by competitors and related research entities.

• Therapeutic Area:
  Several patents have claimed related uses, such as treatment of [disease], signaling a crowded space but with innovation, the ’546 patent leverages specific structural differences to carve out a patent monopoly.

• Legal Status and Challenges:
  While the ’546 patent enjoys robust enforceability, prior art references, such as early-stage disclosures and previously known compounds, could threaten its scope if challenged in litigation or post-grant proceedings.

Patent Family and Continuations

The patent family includes several continuations and provisional applications, suggesting ongoing innovation and strategic patent positioning. These related patents expand protection to additional compounds and methods, forming a layered IP landscape.

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Implications for Stakeholders

• Generic Manufacturers:
  The broad claims—especially the compound claims—pose barriers to biosimilar or generic development unless those companies can design around specific claim limitations or challenge validity.

• Innovators and Licensees:
  The patent grants exclusivity but requires vigilant monitoring of patent extensions, competitor filings, and potential invalidity challenges.

• Legal and Regulatory:
  Careful analysis indicates that the patent’s scope is defensible based on current disclosures but might face challenges if prior art disclosures are uncovered or if new prior art emerges.

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Key Strategic Considerations

• Claim Enforcement:
  Aggressive patent enforcement could deter infringement but may invite inter partes reviews alleging obviousness or lack of novelty.

• Patent Lifecycle Management:
  Filing continuation applications or supplemental protection certificates could extend market exclusivity beyond initial terms.

• Navigating Competitor Patents:
  Analyzing overlapping claims within the landscape can inform licensing negotiations and potential cross-licensing arrangements.

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Key Takeaways

• The ’546 patent leverages broad chemical and therapeutic claims, presenting a significant barrier to competitors in the targeted drug space.
• Its claim scope encompasses a wide class of compounds with interchangeable substitutions, maximizing exclusivity but potentially increasing vulnerability to patent invalidity challenges if prior art is identified.
• The patent landscape is densely populated with related filings, necessitating ongoing analysis to avoid infringement and to optimize patent strategy.
• Formulation and method-of-use claims expand protection but are more susceptible to design-around strategies or prior art challenges.
• Stakeholders should monitor patent family continuations and licensing opportunities to maintain competitive advantage and maximize commercialization.

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FAQs

Q1: How does the broad chemical structure claimed in the ’546 patent impact generic drug development?
A1: The broad structure limits generic manufacturers' ability to produce similar compounds without risking infringement. Designing around the patent requires modifications that fall outside the scope of the claims, which can be legally and scientifically challenging.

Q2: What are the main vulnerabilities of the ’546 patent in legal challenges?
A2: The primary vulnerabilities include prior art disclosures related to similar structures or uses, and potential indefiniteness or obviousness arguments if the claims are deemed too broad or not sufficiently supported by the description.

Q3: Can the ’546 patent be extended beyond its 20-year term?
A3: Yes. Patent term extensions or supplemental protection certificates may be applicable, especially if regulatory delays or supplementary data submissions occur during the patent term.

Q4: How does the patent landscape influence strategic patent filing?
A4: Companies often file continuation or divisional applications to extend protection or target specific variations within the original claim scope, creating a layered and resilient patent family.

Q5: What implications does this patent have for licensing opportunities?
A5: Its broad scope potentially makes it an attractive licensing asset. Licensees can obtain rights to a wide range of compounds and uses, while licensors can generate revenue and block competitors.

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References

1. U.S. Patent and Trademark Office. Patent No. 10,058,546.
2. Patent document analysis reports, [Company/Patent Database], 2022.
3. Market and patent landscape studies in pharmaceutical innovation, [Industry Reports], 2022.

Drugs Protected by US Patent 10,058,546

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	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-002	Dec 20, 2024		RX	Yes	Yes						TREATMENT OF CF IN PATIENTS 6 YEARS AND OLDER WITH AT LEAST ONE F508DEL OR G551D AND AN R117H, A455E, 2789+5G->A, OR 3849+10KBC->T CFTR MUTATION, COMPRISING CONCURRENT COADMINISTRATION OF THE COMPOSITIONS OF US10058546 CLAIM 1 FURTHER COMPRISING VNZ
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No						TREATMENT OF CF IN PATIENTS 12 YEARS AND OLDER WHO HAVE A F508DEL OR G551D CFTR MUTATION AND A 2ND MUTATION SELECTED FROM R117H, A455E, 2789+5G->A, & 3849+10KBC->T, COMPRISING CONCURRENT COADMINISTRATION OF THE COMPOSITIONS OF CLAIM 1 OF US 10058546
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No						TREATMENT OF CF IN PATIENTS 6 YEARS AND OLDER WHO HAVE A F508DEL OR G551D CFTR MUTATION AND A 2ND MUTATION SELECTED FROM R117H, A455E, 2789+5G->A, AND 3849+10KBC->T, COMPRISING CONCURRENT COADMINISTRATION OF THE COMPOSITIONS OF CLAIM 1 OF US 10058546
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-001	Feb 12, 2018		RX	Yes	Yes						TREATMENT OF CF IN PATIENTS 6 YEARS AND OLDER WHO HAVE A F508DEL OR G551D CFTR MUTATION AND A 2ND MUTATION SELECTED FROM R117H, A455E, 2789+5G->A, AND 3849+10KBC->T, COMPRISING CONCURRENT COADMINISTRATION OF THE COMPOSITIONS OF CLAIM 1 OF US 10058546
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-001	Feb 12, 2018		RX	Yes	Yes						TREATMENT OF CF IN PATIENTS 12 YEARS AND OLDER WHO HAVE A F508DEL OR G551D CFTR MUTATION AND A 2ND MUTATION SELECTED FROM R117H, A455E, 2789+5G->A, & 3849+10KBC->T, COMPRISING CONCURRENT COADMINISTRATION OF THE COMPOSITIONS OF CLAIM 1 OF US 10058546

International Family Members for US Patent 10,058,546

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	092857
Australia	2013290444
Australia	2018208694
Canada	2878057
European Patent Office	2872122