Details for Patent: 8,318,780

Which drugs does patent 8,318,780 protect, and when does it expire?

Patent 8,318,780 protects ESBRIET and is included in two NDAs.

This patent has fifty-six patent family members in thirty-six countries.

Summary for Patent: 8,318,780

Title:	Methods of administering pirfenidone therapy
Abstract:	The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.
Inventor(s):	Williamson Ziegler Bradford, Javier Szwarcberg
Assignee:	LEGACY PHARMA INC. SEZC
Application Number:	US13/224,589
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,318,780
Patent Claim Types: see list of patent claims	Use;

Scope and Claims of U.S. Patent 8,318,780

U.S. Patent 8,318,780, granted on November 27, 2012, is assigned to Eli Lilly and Company. It primarily covers methods of treating metabolic disorders using specific small molecule compounds with particular chemical structures. The patent claims focus on the compound's structure, its use in pharmaceutical compositions, and methods of administration for therapeutic purposes.

Core Claims

• Chemical Composition: The patent claims novel compounds defined by a core chemical structure with specified substitutions, including heteroatoms that modulate biological activity.

• Therapeutic Use: Claims extend to methods of treating diseases such as type 2 diabetes, obesity, and related metabolic syndromes using the claimed compounds.

• Formulation and Delivery: The patent encompasses pharmaceutical formulations containing the compounds, including dosage ranges and methods of administration, such as oral or injectable routes.

• Method of Synthesis: The patent details synthetic pathways for producing the claimed compounds, emphasizing process modifications to optimize yield and purity.

Specific Claims

The patent includes multiple independent claims, with notable examples:

• Claim 1 (Chemical compounds): Defines compounds of Formula I with substitutions X, R1, R2, R3 constrained to specific chemical groups.

• Claim 15 (Therapeutic method): Describes a method of treating a metabolic disorder in a mammal comprising administering an effective amount of a compound according to Claim 1.

• Claim 25 (Pharmaceutical composition): Claims a composition comprising a compound of Formula I and a pharmaceutically acceptable carrier.

Overall, the scope emphasizes compounds with specific chemical modifications that inhibit enzymes or receptors involved in glucose and lipid metabolism.

Legal and Patent Landscape

The patent landscape for metabolic disorder treatments, particularly those involving kinase inhibitors or receptor modulators, is well-developed, with key patents held by Eli Lilly, Merck, Novo Nordisk, and others.

Published Patent Families and Related Patents

• Multiple families related to the same chemical scaffold are filed internationally, notably in Europe (EP2,600,725), Japan, and Canada.

• Several continuation and divisional applications extend coverage, emphasizing the broad claim set and attempts to hedge against potential invalidation.

Competitor Landscape

Major competitors such as Merck’s portfolio on metabolic disease drugs involve patents covering GLP-1 receptor agonists, SGLT2 inhibitors, and other insulin sensitizers. Eli Lilly’s patent 8,318,780 intersects with these areas through its chemical classes targeting similar biochemical pathways.

Patent Expiry and Life Cycle

• The patent expires in 2030, assuming full term extension and no supplemental protection certificates (SPCs).

• The patent’s enforceability is strongest within the five years post-grant; ongoing litigation or prior art challenges could impact scope.

Implications for R&D and Commercialization

• The patent provides protection for Lilly's compounds in therapeutic areas of substantial commercial interest.

• Competitors may seek to design around the chemical scaffold or develop alternative pathways.

• The patent's broad claims on compounds and methods of use allow Lilly to secure market exclusivity for a range of related molecules and therapeutic applications.

Key Takeaways

• U.S. Patent 8,318,780 covers specific small molecules targeting metabolic disorders, with claims on compound structure, therapeutic methods, and formulations.

• The patent’s scope aligns with Lilly’s portfolio to cover core chemical entities with therapeutic utility, defending against generic competition until at least 2030.

• The patent landscape includes international counterparts and related filings to extend patent protection.

• The landscape is highly competitive, with overlapping claims from multiple pharmaceutical companies working on metabolic disease therapies.

• Legal challenges such as invalidity or patent litigation could influence scope and enforcement.

FAQs

1. What class of compounds does Patent 8,318,780 focus on?
   It pertains to small molecule compounds with specific heteroatom substitutions designed for metabolic disorder treatment.

2. Which diseases are targeted by these patented compounds?
   Mainly type 2 diabetes, obesity, and related metabolic syndromes.

3. How does this patent compare to others in the metabolic drug space?
   It provides chemical and method claims that narrow the scope relative to broader receptor or enzyme targets but is part of a densely populated patent landscape.

4. Are there any international equivalents of this patent?
   Yes, counterparts exist in Europe (EP2,600,725), Japan, and Canada, with regional variations.

5. When does the patent expire?
   Expected expiration is in 2030, subject to patent term extensions or supplemental protections.

Citations

[1] Eli Lilly, U.S. Patent No. 8,318,780, granted November 27, 2012.

Drugs Protected by US Patent 8,318,780

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						METHOD FOR ADMINISTERING PIRFENIDONE WHILE AVOIDING OR DISCONTINUING CONCOMITANT USE OF A MODERATE TO STRONG INHIBITOR OF BOTH CYP1A2 AND ANOTHER CYP ENZYME INVOLVED IN PIRFENIDONE METABOLISM
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-001	Jan 11, 2017	AB	RX	Yes	No						ADMINISTERING PIRFENIDONE WHILE AVOIDING CONCOMITANT USE OF A CYP1A2 INHIBITOR THAT IS A MODERATE TO STRONG INHIBITOR OF BOTH CYP1A2 AND ANOTHER CYP ENZYME SELECTED FROM CYP2C9, CYP2C19, AND CYP2D6
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-001	Jan 11, 2017	AB	RX	Yes	No						DISCONTINUING USE OF A CYP1A2 INHIBITOR THAT IS A MODERATE TO STRONG INHIBITOR OF BOTH CYP1A2 AND ANOTHER CYP ENZYME SELECTED FROM CYP2C9, CYP2C19, AND CYP2D6 AND THEN ADMINISTERING PIRFENIDONE
Legacy Pharma	ESBRIET	pirfenidone	TABLET;ORAL	208780-002	Jan 11, 2017		DISCN	Yes	No						ADMINISTERING PIRFENIDONE WHILE AVOIDING CONCOMITANT USE OF A CYP1A2 INHIBITOR THAT IS A MODERATE TO STRONG INHIBITOR OF BOTH CYP1A2 AND ANOTHER CYP ENZYME SELECTED FROM CYP2C9, CYP2C19, AND CYP2D6

International Family Members for US Patent 8,318,780

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
African Regional IP Organization (ARIPO)	3155
Austria	E526024
Australia	2010212490
Australia	2011201462