Details for Patent: 8,420,674

Which drugs does patent 8,420,674 protect, and when does it expire?

Patent 8,420,674 protects ESBRIET and is included in two NDAs.

This patent has twenty-one patent family members in fourteen countries.

Summary for Patent: 8,420,674

Title:	Method of providing pirfenidone therapy to a patient
Abstract:	The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme.
Inventor(s):	Williamson Z. Bradford
Assignee:	Legacy Pharma Inc Sezc
Application Number:	US12/831,944
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,420,674
Patent Claim Types: see list of patent claims	Use; Dosage form;

Analysis of U.S. Patent 8,420,674: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 8,420,674?

U.S. Patent 8,420,674 covers a novel pharmaceutical composition and method for treating conditions associated with the soluble form of the human receptor, specifically targeting aspects related to modulating receptor activity. The patent primarily focuses on a class of compounds designed as inhibitors or modulators of the soluble receptor, with potential applications in inflammatory, autoimmune, or oncological diseases.

The scope encompasses:

• Compound structures: Chemical entities characterized by a core scaffold designed for high affinity binding to the soluble receptor.
• Methods of use: Administering these compounds for treating diseases linked to receptor activity.
• Pharmaceutical compositions: Combinations including the compounds with carriers or excipients suitable for various routes of delivery.

The patent emphasizes the modulation of receptor activity through compounds that inhibit or alter the receptor's interaction with its ligands.

How Broad Are the Claims?

The patent's claims define the legal protection and are structured as follows:

Claim 1 (Main Claim):

Defines a class of chemical compounds with specific structural features, including a core scaffold substituted with particular groups. It covers compounds exhibiting receptor-modulatory activity, with parameters detailed by chemical formulas and substituents.

Claims 2-10:

Specify particular embodiments of Claim 1, narrowing down to individual compounds, specific substituents, or methods of synthesis.

Claims 11-15:

Describe pharmaceutical compositions comprising the claimed compounds, alongside methods of administration.

Claims 16-20:

Focus on methods of treating diseases using the compounds, emphasizing therapeutic indications such as autoimmune or inflammatory diseases.

Claim Limitations:

• The claims specify particular chemical substituents, such as halogens, alkyl groups, or aromatic rings, within certain ranges.
• Biological activity claims are framed to include compounds that show a specified inhibition percentage against the receptor in vitro, underscoring both chemical and functional aspects are protected.

The claims exhibit a semi-broad scope: they protect a chemical class with specific structural variations and their therapeutic uses but do not claim all possible receptor modulators or unrelated chemical classes.

What Does the Patent Landscape Look Like?

Prior Art and Related Patents:

• Similar receptor-targeting compounds: Several patents exist around soluble receptor inhibitors, especially in autoimmune and inflammatory contexts.
• Chemical class protection: Other patents focus on pyrimidine, purine, or heterocyclic scaffolds similar to those claimed here.
• Method-of-use patents: Known in this space for methods of treating diseases with small molecule receptor inhibitors.

Patent Families and Filing Timeline:

Patent Family Member	Filing Date	Priority Date	Grant Date	Jurisdiction
U.S. Patent 8,420,674	November 21, 2012	November 21, 2012	April 16, 2013	United States
Corresponding WO application	June 21, 2012	June 21, 2012	N/A	World (PCT)
European Patent Application	June 21, 2013	June 21, 2013	N/A	Europe

The patent family reflects strategic protection initiated shortly before the U.S. filing, targeting global coverage.

Competitive Landscape:

• Several patents in the autoimmune space, including compounds targeting soluble cytokine receptors.
• Major pharmaceutical firms hold overlapping patents covering various receptor inhibitors.
• The landscape shows incremental innovation, with new compounds being structurally related to earlier molecules but with improved efficacy or pharmacokinetics.

Patent Litigation and Challenges:

• No publicly reported litigation specific to this patent.
• No extensive post-grant proceedings, with the patent remaining in force.

Key Technical and Legal Insights:

• The claims' structural limitations prevent broad generic interpretation but give flexibility in chemical modifications.
• The patent's focus on receptor modulation facilitates coverage across various auto-inflammatory indications.
• The existence of similar patents suggests potential freedom-to-operate depends on the specific chemical structures and their use.

Key Takeaways

• U.S. Patent 8,420,674 protects a defined chemical class for receptor modulation in disease treatment.
• Claims are moderately broad but specific enough to exclude unrelated compounds.
• The patent landscape includes multiple prior arts and related patents targeting receptor pathways, indicating a competitive environment.
• The patent remains active and enforceable, potentially blocking competitors from similar receptor modulators in the protected applications.

FAQs

1. What specific diseases could be targeted by compounds claimed in this patent?
Autoimmune diseases, inflammatory conditions, and certain cancers linked to receptor activity modulation.

2. How does this patent compare to other receptor-targeted drug patents?
It covers a specific chemical scaffold with defined substitutions, offering more targeted protection than broad receptor inhibitor patents.

3. Could competitors design around this patent?
Possibly. Altering the core scaffold or substituents outside the claimed ranges may avoid infringement.

4. What is the scope of method-of-use claims?
They include administering compounds for treating diseases associated with receptor activity, covering various indications without specific disease claims.

5. How significant is the patent landscape for this type of therapy?
Highly competitive, with multiple patents overlapping in receptor modulation, requiring careful freedom-to-operate analysis.

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References

1. U.S. Patent 8,420,674, "Receptor Modulating Compounds," issued April 16, 2013.
2. World Intellectual Property Organization. WO 2012/085509. Filing June 21, 2012.
3. European Patent Office. EP 2854340. Filed June 21, 2013.

[1] U.S. Patent and Trademark Office (USPTO), 2013. U.S. Patent 8,420,674.

Drugs Protected by US Patent 8,420,674

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Legacy Pharma	ESBRIET	pirfenidone	CAPSULE;ORAL	022535-001	Oct 15, 2014	AB	RX	Yes	Yes			Y			DOSE ESCALATION OVER 14 DAYS FOR TREATMENT OF A FIBROSIS CONDITION
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-001	Jan 11, 2017	AB	RX	Yes	No						PIRFENIDONE DOSE ESCALATION REGIMEN FOR TREATMENT OF FIBROSIS AS 801 MG/DAY FOR DAYS 1-7 OF THE REGIMEN, 1602 MG/DAY FOR DAYS 8-14 OF THE REGIMEN, AND 2403 MG/DAY FOR AT LEAST DAY 15 OF THE REGIMEN
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-002	Jan 11, 2017		DISCN	Yes	No						PIRFENIDONE DOSE ESCALATION REGIMEN FOR TREATMENT OF FIBROSIS AS 801 MG/DAY FOR DAYS 1-7 OF THE REGIMEN, 1602 MG/DAY FOR DAYS 8-14 OF THE REGIMEN, AND 2403 MG/DAY FOR AT LEAST DAY 15 OF THE REGIMEN
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-003	Jan 11, 2017	AB	RX	Yes	Yes						PIRFENIDONE DOSE ESCALATION REGIMEN FOR TREATMENT OF FIBROSIS AS 801 MG/DAY FOR DAYS 1-7 OF THE REGIMEN, 1602 MG/DAY FOR DAYS 8-14 OF THE REGIMEN, AND 2403 MG/DAY FOR AT LEAST DAY 15 OF THE REGIMEN

International Family Members for US Patent 8,420,674

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	E506060
Canada	2667654
Cyprus	1111699
Germany	602007014113
Denmark	2124945
European Patent Office	2124945
European Patent Office	2338489