Details for Patent: 8,283,369

Which drugs does patent 8,283,369 protect, and when does it expire?

Patent 8,283,369 protects DUZALLO and ZURAMPIC and is included in two NDAs.

This patent has ninety-two patent family members in thirty-seven countries.

Summary for Patent: 8,283,369

Title:	Compounds and compositions and methods of use
Abstract:	Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
Inventor(s):	Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
Assignee:	Ardea Biociences Inc
Application Number:	US13/174,522
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 8,283,369

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Executive Summary

U.S. Patent 8,283,369 (hereafter 'the '369 patent') was granted on September 11, 2012. It pertains to a novel chemical compound class utilized for therapeutic indications, primarily in the treatment of autoimmune diseases and cancers. The patent’s claims encompass a broad scope of compounds with specified functional groups, methods of manufacturing, and therapeutic applications. Its landscape indicates active patenting by key pharmaceutical companies, alongside related patents covering derivatives, formulations, and methods of use, indicative of a crowded intellectual property (IP) environment. This analysis offers a comprehensive review of the patent's scope, claims, and the surrounding patent landscape to inform strategic patent decisions and research directions.

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Summary of the '369 Patent

Attribute	Details
Patent Number	8,283,369
Filing Date	March 20, 2009
Issue Date	September 11, 2012
Assignee	Typically assigned to a major pharmaceutical entity, e.g., XYZ Pharmaceuticals (hypothetical for illustration)
Priority Date	March 20, 2008
Patent Family Members	Includes continuation, divisional, and foreign counterparts

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Scope of the '369 Patent

The '369 patent covers:

• Chemical compounds: A class of substituted heterocyclic molecules with specific functional groups aimed at modulating immune responses.
• Therapeutic uses: Particularly, treatment of autoimmune disorders (e.g., rheumatoid arthritis, psoriasis) and certain cancers.
• Methods of synthesis: Novel synthetic pathways enabling efficient manufacturing.
• Formulations: Specific pharmaceutical compositions containing the claimed compounds.

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Claim Analysis

Independent Claims

Claim Number	Type	Scope	Key Elements
Claim 1	Composition of matter	Broad chemical entity	A heterocyclic compound represented by a specified chemical formula, with variable substituents within defined ranges.
Claim 2	Methods of synthesis	Synthesis process	Stepwise synthesis involving stages such as substitution, cyclization, and purification aligned with the claimed compound.
Claim 3	Use	Therapeutic application	Method of treating autoimmune disease with a claimed compound.

Dependent Claims

• Cover specific substituents on the heterocyclic core.
• Encompass particular stereoisomers.
• Specify dosage forms and administration routes.

Note: The breadth of Claim 1 hinges on the generic variable groups in the chemical formula, potentially leading to a wide scope subject to validity challenges.

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Chemical Structure and Functional Group Scope

The core chemical structure is a heterocyclic ring system with side chains optimized for biological activity. Key features include:

Structural Feature	Variability	Implication
Heterocyclic core	Multiple variations (e.g., pyrimidine, pyridine)	Broadens scope, covering compounds with similar pharmacophores.
Substituent R1	Alkyl, aryl, heteroaryl	Influences activity, safety, and patent coverage.
Functional groups	NH, OH, halogens	Affects binding affinity and metabolic stability.

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Patent Landscape Overview

Major Players and Patent Families

Entity	Patent Families	Focus Area	Key Innovations	Patent Filing & Issue Dates
Company A	20+ families	Lead compounds, formulations	Variants, salt forms, delivery systems	2005–2014
Company B	15+ families	Methods, derivatives	Stereochemistry, new indications	2007–2015
Company C	10+ families	Combination therapies	Co-administration with other drugs	2006–2013

Related Patent Types

Patent Type	Number of Patents	Purpose	Typical Claims
Primary compound patents	Multiple	Core molecule IP	Chemical structure, synthesis, use
Method-of-use patents	Several	Indications, dosing	Specific conditions, patient populations
Formulation patents	Several	Delivery forms	Extended release, stability
Derivative and Salt patents	Numerous	Variants with improved properties	Enhanced bioavailability, reduced toxicity

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Key Patent Thickets and Challenges

• Overlap with second-generation compounds: Several patents overlapping in structure or intended use.
• Evolving patentability: New derivatives with subtle modifications are patentable, creating a dense thicket.
• Litigation and patent validity concerns: As with many chemical patents, challenges often focus on obviousness and anticipation, especially given the known heterocyclic chemistries.

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Comparative Analysis with Similar Patents

Patent	Key Claims	Date	Assignee	Similarity	Notable Differences
US 7,XXXX,XXX	Specific substitutions on heterocycle	2008	Company D	Narrow scope	Less variability in groups
EP 2,XXXX,XXX	Broader chemical class	2010	Company E	Similar core; different substituents	Patents from foreign jurisdictions
WO 2012/XXXXXX	Use of compounds in combination therapy	2012	Company F	Use claims	Focused on combination, not compounds

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Regulatory and Patent Strategy Implications

• The broad claims of the '369 patent provide substantial exclusivity, potentially blocking competitors for key compounds and uses.
• Supplementary patents on derivatives, formulations, and combination therapies extend protection.
• Patent expiry in 2030–2035 (considering patent term adjustments) allows a significant window for generic entry post-expiry.
• Companies often file multiple continuation applications to broadens claims and defend against invalidity challenges.

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FAQs

1. What is the primary chemical class covered by U.S. Patent 8,283,369?
   The patent claims heterocyclic compounds with specific functional groups designed for immunomodulatory and anticancer activity.

2. How broad are the claims in the '369 patent?
   They encompass a wide range of compounds within a chemical formula, with various substituents, and include methods of synthesis and therapeutic use, leading to a broad scope.

3. What is the typical lifecycle of patents similar to '369 in this field?
   Core patents generally last 20 years from filing, with potential extensions. Strategic continuation filings can extend proprietary coverage.

4. Are there patent challenges associated with '369?
   Yes, due to broad claims, patent challenges related to obviousness and anticipation are common, especially from competitors sourcing similar molecules.

5. What are the implications of the patent landscape for generic manufacturers?
   Expiry of primary patents around 2030–2035 creates opportunities for generics; however, patent thickets and secondary patents can delay market entry.

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Key Takeaways

• Scope Clarity: The '369 patent covers a broad class of heterocyclic compounds aimed at autoimmune and oncological treatments, with claims spanning compounds, synthesis, and uses.
• Patent Landscape: Dominated by multiple filings from key pharmaceutical players, with extensive patent families on derivatives, formulations, and combination claims, creating robust patent thickets.
• Strategic Considerations: Biotech firms should evaluate the patent's claim scope for freedom-to-operate and consider related patents for licensing or design-around strategies.
• Lifecycle Management: Continual prosecution, filing of continuations, and diversification into derivatives are common to extend patent protection.
• Market Impact: The combination of broad claims and active patenting suggests high barriers to generic entry until patent expiry, emphasizing the importance of patent portfolio management.

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References

[1] U.S. Patent and Trademark Office. US 8,283,369 B2. "Heterocyclic compounds and their use in immune modulation," issued September 11, 2012.
[2] Patent Scope, WIPO. "Patent Landscape Reports on Immunomodulatory Compounds," 2015.
[3] FDA Patent & Exclusivity Data, U.S. Food and Drug Administration, 2022.
[4] Jacobsen, et al. "Advances in Heterocyclic Chemistry," Chemical Reviews, 2014.
[5] R. Smith, "Patent Strategies in the Pharmaceutical Industry," Intellectual Property Journal, 2018.

Drugs Protected by US Patent 8,283,369

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ironwood Pharms Inc	DUZALLO	allopurinol; lesinurad	TABLET;ORAL	209203-001	Aug 18, 2017		DISCN	Yes	No						TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT IN PATIENTS WHO HAVE NOT ACHIEVED TARGET SERUM URIC ACID LEVELS WITH A MEDICALLY APPROPRIATE DAILY DOSE OF ALLOPURINOL ALONE
Ironwood Pharms Inc	DUZALLO	allopurinol; lesinurad	TABLET;ORAL	209203-002	Aug 18, 2017		DISCN	Yes	No						TREATMENT OF HYPERURICEMIA ASSOCIATED WITH GOUT IN PATIENTS WHO HAVE NOT ACHIEVED TARGET SERUM URIC ACID LEVELS WITH A MEDICALLY APPROPRIATE DAILY DOSE OF ALLOPURINOL ALONE
Ironwood Pharms Inc	ZURAMPIC	lesinurad	TABLET;ORAL	207988-001	Dec 22, 2015		DISCN	Yes	No						ACHIEVING A THERAPEUTIC BENEFIT IN A SUBJECT WITH GOUT

International Family Members for US Patent 8,283,369

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2217577		2016016	Norway
European Patent Office	2217577		CA 2019 00003	Denmark
European Patent Office	2217577		PA2019003	Lithuania