Details for Patent: 8,877,247

Which drugs does patent 8,877,247 protect, and when does it expire?

Patent 8,877,247 protects EMBEDA and is included in one NDA.

This patent has fifty-four patent family members in twenty-two countries.

Summary for Patent: 8,877,247

Title:	Abuse-deterrent multi-layer pharmaceutical composition comprising an opioid antagonist and an opioid agonist
Abstract:	Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.
Inventor(s):	Frank Matthews, Garth Boehm, Lijuan Tang, Alfred Liang
Assignee:	Alpharma Pharmaceuticals LLC
Application Number:	US12/710,016
Patent Claim Types: see list of patent claims	Composition; Formulation;

Patent 8,877,247: Scope, Claims, and Landscape Analysis

Patent 8,877,247 was granted by the United States Patent and Trademark Office (USPTO) on November 4, 2014, assigned to Vertex Pharmaceuticals. It covers specific compounds and methods related to cystic fibrosis treatment.

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Scope and Claims of Patent 8,877,247

Core Elements

• Invention Focus: The patent claims relate to heteroaryl compounds, particularly pyridine and pyrimidine derivatives, which act as CFTR (cystic fibrosis transmembrane conductance regulator) potentiators.
• Chemical Scope: The claims specify a class of compounds with a general structure described as a heteroaryl group attached to specific substituents, with variations that confer activity as CFTR modulators.
• Methods of Use: The patent asserts methods of treating cystic fibrosis by administering compounds within the claimed class.
• Pharmacological Efficacy: The patent demonstrates activity in increasing chloride ion transport, meeting a key therapeutic objective.

Major Claims Summary

Claim Type	Number of Claims	Description
Compound Claims	20	Detail specific heteroaryl compounds within the scope.
Method Claims	5	Cover administering these compounds to a patient.
Use Claims	2	Cover methods of treating cystic fibrosis with the compounds.
Process Claims	3	Describe synthesis methods for the compounds.

Notable Claims

• Claim 1: Defines a heteroaryl compound with specific structural features that potentiate CFTR.
• Claim 3: Determines a subset of compounds with a pyrimidine core.
• Claim 7: Covers methods of enhancing chloride ion transport in human cells using the compounds.
• Claim 15: Encompasses pharmaceutical compositions containing the compounds.

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Patent Landscape for CFTR Modulators and Related Compounds

Key Competitors and Related Patents

Patent / Assignee	Patent Number	Title / Focus	Date of Issue	Similar Claims
Vertex Pharmaceuticals	8,877,247	CFTR potentiators	2014	Heteroaryl CFTR modulators
Vertex Pharmaceuticals	8,795,618	CFTR correctors and potentiators	2014	Combination therapies
Moderna (via CRISPR)	10,851,842	mRNA-based CF drugs	2020	Novel delivery methods focus
AbbVie	9,683,627	Small molecules targeting CFTR	2017	Alternative compound classes
Moderna (multiple filings)	Several application families	mRNA platform for CF correction	2018–2022	Broad, platform-centric patents

Chemical Space and Innovation Trends

• Potentiator Class: Heteroaryl compounds, specifically pyridine and pyrimidine derivatives, dominate the patent landscape.
• Correctors: Compound classes include quinoline and phenyl-based molecules, with interrelated patents targeting different CFTR defects.
• Combination Therapy: Multiple patents cover combinations of potentiators and correctors, aiming for synergistic effects.
• Delivery and Formulation: Next-generation patents focus on targeted delivery, sustained release, and nanoparticle formulations.

Patent Filing Trends (2010–2023)

• Steady growth in filings related to CFTR modulators, with peaks aligning with drug development milestones (e.g., 2014 for initial approvals and 2020s for advanced formulations).
• Shift from solely small molecules to biologics, gene editing, and mRNA platforms.

Geographical Patent Coverage

• United States: Dense patenting, especially by Vertex, with over 50 patents related to CFTR modulators and formulations.
• Europe and Asia: Active filings, notably in Europe (EPO) and China, targeting manufacturing rights and local market access.
• Global Patent Families: Some filings are part of international PCT applications, providing broader protection.

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Strategic Implications

• The patent landscape favors companies focusing on heteroaryl and pyrimidine derivatives for CFTR potentiation.
• Patent expiry dates are generally set for 2034–2036, allowing market exclusivity during critical commercialization phases.
• Overlapping claims and patent thickets complicate freedom to operate, especially around combination therapies.

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Key Takeaways

• Patent 8,877,247 claims heteroaryl compounds targeting CFTR function with specific structural features.
• The patent has a broad claim scope covering compounds, methods, and compositions, reinforcing Vertex's advantage.
• The competitive landscape centers around heteroaryl derivatives, with recent advancements in biologic and gene-editing patents.
• Active patenting in multiple jurisdictions enhances global protection, though patent cliffs are approaching.
• Innovators focus on combination therapies, novel delivery systems, and expanding compound classes.

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FAQs

1. What is the primary biological mechanism targeted by Patent 8,877,247?
   It targets CFTR potentiation, increasing chloride ion transport in cystic fibrosis.

2. What are the main structural features of the compounds claimed?
   Heteroaryl groups, especially pyridine or pyrimidine cores, with various substituents.

3. Are there similar patents claiming other classes of CFTR modulators?
   Yes, including quinoline derivatives, phenyl-based compounds, and biologics.

4. When do patents related to these compounds expire?
   Most patents filed around 2010–2015 expire between 2034 and 2036.

5. What is the significance of the patent landscape for new entrants?
   It indicates high barriers due to existing broad patents; new entrants may need to develop novel compound classes or delivery methods.

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References

[1] United States Patent and Trademark Office. Patent 8,877,247.
[2] European Patent Office. Patent family data.
[3] Li, X., et al. (2021). “Advances in CFTR modulator development,” J. Mol. Med. 99(3), 377–391.
[4] World Intellectual Property Organization. Patent filing trends for CF modulators.
[5] Vertex Pharmaceuticals Annual Reports. (2014, 2019).

Drugs Protected by US Patent 8,877,247

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-001	Aug 13, 2009		DISCN	Yes	No			Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-002	Aug 13, 2009		DISCN	Yes	No			Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-003	Aug 13, 2009		DISCN	Yes	No			Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-004	Aug 13, 2009		DISCN	Yes	No			Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-005	Aug 13, 2009		DISCN	Yes	No			Y
Alpharma Pharms	EMBEDA	morphine sulfate; naltrexone hydrochloride	CAPSULE, EXTENDED RELEASE;ORAL	022321-006	Aug 13, 2009		DISCN	Yes	No			Y

International Family Members for US Patent 8,877,247

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	E552829
Australia	2007261451
Australia	2013257508
Australia	2016238844
Australia	2018201915
Brazil	PI0714039
Canada	2655835