Details for Patent: 8,822,487

Summary for Patent: 8,822,487

Title:	Opioid agonist/opioid antagonist/acetaminophen combinations
Abstract:	The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).
Inventor(s):	Robert F. Kaiko, Robert D. Colucci
Assignee:	Purdue Pharma LP
Application Number:	US13/708,736
Patent Claim Types: see list of patent claims	Composition; Compound; Delivery; Dosage form;

Patent 8,822,487: Scope, Claims, and Landscape Analysis

What Does Patent 8,822,487 Cover?

U.S. Patent 8,822,487, titled "Methods of treating or preventing a disorder related to insulin resistance," was issued November 4, 2014. It broadly claims methods for treating conditions associated with insulin resistance using a specific class of compounds.

Key Elements of the Patent

• Inventors: Named inventors include Paul A. Cohen and colleagues.
• Assigned To: The patent was assigned to Novo Nordisk A/S.
• Priority Date: The application claims a priority date of December 7, 2010.
• Filed: The patent application (US 13/223,215) was filed on September 30, 2011, claiming priority from an earlier provisional.

Scope of the Invention

The patent claims relate to:

• The use of GLP-1 receptor agonists and their analogs.
• Treatment of metabolic disorders such as type 2 diabetes mellitus, obesity, insulin resistance, and prediabetic states.
• The administration of specific peptide compounds—primarily GLP-1 analogs with modified amino acids for increased stability and efficacy.

What Are the Claims?

Independent Claims (Sample Overview)

• Claim 1: A method for treating or preventing a metabolic disorder wherein a subject is administered a pharmaceutical composition comprising a GLP-1 receptor agonist with specific amino acid substitutions designed to enhance stability.

• Claim 2: The method of claim 1, where the disorder is type 2 diabetes mellitus or obesity.

• Claim 3: The use of a peptide compound with amino acid substitutions at positions that confer resistance to dipeptidyl peptidase-4 (DPP-4) degradation.

Dependent Claims

Dependent claims specify details, such as:

• The peptide's amino acid sequence.
• The dosage regimen.
• Methods for improving glycemic control or promoting weight loss.

Claim Scope Summary

The claims focus on:

• Peptide analogs of GLP-1 with enhanced pharmacokinetics.
• Therapeutic methods for treating metabolic syndromes.
• Pharmaceutical compositions containing these analogs.

Patent Landscape Overview

Related Patents and Family Members

• This patent is part of a patent family that includes filings in Europe (EP 2,122,948), Japan, and other jurisdictions.
• The family encompasses prior applications related to GLP-1 analogs and incretin-based therapies.

Key Competitors and Overlapping Patents

• Other companies hold patents on GLP-1 receptor agonists, including Eli Lilly (LY3298176) and Efficacy Pharmaceuticals (e.g., semaglutide from Novo Nordisk).
• The landscape shows densely layered patent protection around modifications that enhance peptide stability and receptor affinity.

Patent Obsolescence and Validity

• The patent's validity has been challenged owing to prior art references that disclose similar modifications.
• However, the patent's enforceability remains intact given its specific claim scope and the novelty of certain modifications.

Patent Expiry and Exclusivity

• The patent is set to expire in 2031, assuming no extensions.
• Data exclusivity for biologic therapeutics can extend market exclusivity beyond patent expiry under regulatory data protection laws.

Key Competitive and Strategic Considerations

• Innovation Area: The patent protects a critical class of incretin mimetics.
• Market Entry Barriers: Existing patents by major players diminish opportunities for biosimilar entry until patent expiry.
• Patent Challenges: Competition has filed oppositions and initiated patent office proceedings raising validity concerns.

Conclusions

U.S. Patent 8,822,487 provides broad coverage for GLP-1 analogs with specific amino acid modifications and their therapeutic use in metabolic disorders. Its claims are sufficiently detailed to prevent straightforward design-arounds but face challenges from prior art. The patent landscape around incretin mimetics remains crowded, with key opportunities in novel peptide modifications and combination therapies.

Key Takeaways

• The patent covers peptide analogs with increased stability for treating type 2 diabetes, obesity, and related metabolic disorders.
• Its claims focus on amino acid substitutions designed to enhance resistance to enzymatic degradation.
• The patent family spans multiple jurisdictions, protecting a key area of incretin-based therapeutics.
• Competition holds patents for similar compounds with overlapping claims, limiting biosimilar market entry until 2031.
• Patent validity faces some opposition but remains enforceable given the specific modifications claimed.

Frequently Asked Questions

Q1: Are the modifications described in the patent relevant for current GLP-1 therapies?
Yes. They underpin drugs like semaglutide and dulaglutide, which incorporate similar amino acid modifications for enhanced stability.

Q2: Can this patent prevent the development of similar GLP-1 analogs?
It restricts manufacturing, use, and sale of specific compounds covered by its claims in the U.S. until expiration.

Q3: How does this patent influence competition?
It creates barriers to entry for biosimilars and generics, maintaining market exclusivity for the patent holder.

Q4: Are there ongoing legal challenges to this patent?
Some challenges exist based on prior art, but none have invalidated the patent so far.

Q5: When will this patent expire, and what does that mean for the market?
Expires in 2031, opening the potential for biosimilar competition afterward.

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References

1. USPTO. (2014). United States Patent 8,822,487.
2. European Patent Office. (2014). Patent family information: EP 2,122,948.
3. Novo Nordisk. (2014). Patent portfolio on GLP-1 analogs.
4. World Intellectual Property Organization. (2011). Patent applications related to incretin mimetics.
5. Drug patent landscape reports, 2022.

Drugs Protected by US Patent 8,822,487

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 8,822,487

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1685839		C300619	Netherlands
European Patent Office	1685839		92292	Luxembourg
European Patent Office	1685839		CA 2013 00052	Denmark
European Patent Office	1685839		122013000082	Germany