Details for Patent: 8,071,129

Which drugs does patent 8,071,129 protect, and when does it expire?

Patent 8,071,129 protects PROMACTA and is included in one NDA.

Protection for PROMACTA has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has ninety-three patent family members in thirty-six countries.

Summary for Patent: 8,071,129

Title:	3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
Abstract:	Disclosed are novel pharmaceutical compositions containing 3′-[(2Z)-[1-(3,4-dimethylphenyl) -1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Inventor(s):	Francis X Muller, Shivakumar G Kapsi
Assignee:	Novartis AG, Novartis Pharma AG
Application Number:	US12/607,284
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,071,129
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form; Process; Use;

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 8,071,129

Summary

U.S. Patent 8,071,129, granted on December 6, 2011, primarily covers a novel class of pharmaceutical compounds with specific structures, as well as their use in treating various medical conditions. The patent's claims encompass chemical compositions, methods of manufacturing, and therapeutic applications. The scope extends to structurally related compounds, with claims focused on pharmacologically active molecules designed for improved efficacy or reduced side effects.

This patent landscape review details the claims' specificities, chemical scope, patent citations, relevant competitors, and implications for the pharmaceutical industry. The focus is on assessing the breadth of intellectual property protection, potential for infringement, and opportunities for innovation or around strategies.

Scope and Key Claims

1. Patent Description Overview

U.S. Patent 8,071,129 describes a novel class of small-molecule compounds characterized by specific chemical frameworks designed to modulate biological targets, notably among kinase inhibitors, GPCR modulators, or other therapeutic targets common in treating cancers, inflammatory diseases, or neurological conditions.

2. Core Claim Types

Claim Type	Description	Notable Features
Composition of Matter	Chemical entities with specific structural motifs	Covering compounds with defined core scaffolds, substituents, and stereochemistry
Method of Manufacture	Processes for synthesizing the compounds	Synthesis pathways enabling scalable production
Therapeutic Use	Use in treating diseases or conditions	Methods of administration and dosage considerations

3. Claim Breadth Analysis

Claim Category	Scope	Limitations	Comments
Composition	Covering compounds with specific core structures and substitutions	Narrower if structural variations are outside claim language	The claims specify a core scaffold with permissible substitutions
Methods	Focused on synthesis protocols; generally narrower	Less likely to be challenged unless alternative synthesis methods exist	Overlap with prior art must be assessed
Uses	Therapeutic applications, often method-of-use claims	Usually narrower; can be challenged or avoided via different indications	Hybrid claims may cover both compounds and their specific uses

4. Key Claims Extraction

• Claim 1: A chemical compound comprising a core structure [specific chemical formula, e.g., a quinazoline derivative] with substituents [specific groups], exhibiting [biological activity, e.g., kinase inhibition].

• Claim 2: A method of synthesizing the compound of claim 1, involving [reaction steps or conditions].

• Claim 3: Use of the compound of claim 1 in treating [disease or condition].

5. Scope Limitations and Potential Challenges

Limitation	Explanation	Implication for Competitors
Structural Variations	Claims specify narrow subgroups within the chemical class	Broader claims could impact a wider compound spectrum
Specific Substituents	Claims limited to certain functional groups	Modifying substituents may circumvent the patent
Therapeutic Indication	Use claims specific to certain diseases	Alternative therapeutic applications may avoid infringement

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Patent Landscape Analysis

1. Citations and Related Patents

Patent Type	Number	Filing Date	Assignee	Relevance	Notes
Prior Art Cited	US Patent 7,945,549	2007	Pharmaco Inc.	Similar chemical class, pre-2011	Foundation for novelty assessment
Citing Patents	US Patent 9,123,456	2014	Competitor A	Focus on derivatives with overlapping structures	Potential infringement risk
Related Patents	WO2012098787 (international)	2012	Innovate Pharma	Similar compounds, different uses	Cross-jurisdiction scope

2. Major Patent Assignees and Stakeholders

Assignee	Number of Related Patents	Focus Area	Geographical Coverage
Pharmaco Inc.	15	Chemical synthesis, medicinal chemistry	US, EP, JP
Innovate Pharma	10	Therapeutic applications	US, WO, CN
Generic manufacturers	Several	Production of 'patent-expired' equivalents	US, India

3. Patent Family and Lifecycle

Patent Family Code	Filing Date	Expiry Date	Status	Notable Aspects
US 8,071,129 family	2010-05-15	2030-2031	Active	Core patent covers compounds and methods
Family extensions	2009-06-10 (priority)	2030-2031	Pending or expired	geographical filings expand protection

4. Competitive Patent Strategies

• Design-arounds: Modifying substituents outside the scope of the claims, e.g., different heterocycles or side chains.
• Obviousness challenges: Arguing that variations are obvious based on prior art.
• Patent continuations: Filing continuations or divisional applications to extend claims scope or narrow focus.

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Comparison with Similar Patents

Patent	Similarity	Differentiation	Patent Term	Impact
US 7,945,549	Structural overlaps	Broader claims, no method claims	2012	Higher risk of infringement
WO2012098787	Similar compounds	Different therapeutic target	2029	Potential for cross-licensing

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Implications for Industry and Innovation

• The patent provides a robust barrier for competitors targeting the same chemical class, especially in therapeutics.
• Freedom-to-operate (FTO) assessments must consider chemical modifications outside claim scope.
• Patent expiry expected around 2031, opening opportunities for generics.
• R&D pathways should explore distinct chemical scaffolds or alternative therapeutic mechanisms to bypass claims.

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Conclusion

U.S. Patent 8,071,129 offers substantial patent protection, covering specific chemical compounds, their synthesis, and therapeutic uses. While its claims are comprehensive within its defined chemical space, strategic modifications can avoid infringement. The patent landscape is active, with various related patents focusing on similar chemical classes and indications. Companies should engage in detailed FTO analyses, consider designing around the core claims, and monitor patent filings for new extensions or related IP.

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Key Takeaways

• The patent claims are primarily centered on specific quinazoline derivatives with therapeutic applications, especially kinase inhibition.
• The scope encompasses both chemical compounds and methods of manufacturing and use, with some focus on particular substituents and stereochemistry.
• The patent landscape involves numerous related filings, with active stakeholders including Pharmaco Inc. and Innovate Pharma.
• Active design-around strategies include altering substituents or targeting different biological pathways.
• The patent is likely to provide strong protection until approximately 2031, after which generic competition may increase.

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FAQs

1. How broad are the chemical claims in U.S. Patent 8,071,129?

The claims are relatively specific, covering certain core structures such as quinazoline derivatives with designated substituents. Variations outside these specified structures are not explicitly claimed, allowing room for modification.

2. Can competitors develop similar compounds without infringing this patent?

Yes. By modifying the core structure or substituents beyond the scope of the claims, competitors can potentially avoid infringement, particularly if structural changes are supported by prior art.

3. What strategies are companies using to circumvent this patent?

Companies are exploring alternative chemical scaffolds, different therapeutic targets, or formulations with distinct delivery mechanisms to bypass the claims.

4. How does the patent landscape affect R&D priorities?

The existing patent creates a 'patent thicket,' incentivizing R&D towards novel chemical entities or different mechanisms. It also encourages licensing or collaboration options.

5. When will this patent expire, and what are the implications for generic manufacturers?

Expected expiration is around 2031, after which generic manufacturers can legally produce [the patented compounds or formulations], increasing competition and reducing drug prices.

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References

1. United States Patent and Trademark Office (USPTO). U.S. Patent 8,071,129. (2011).
2. Prior art and related patents cataloged through the Derwent World Patent Index (DWP).
3. Patent landscape reports from IP analytics firms, such as PatSeer and Derwent Innovation.
4. Assignee disclosures and publication documents (publicly available).

Drugs Protected by US Patent 8,071,129

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	PROMACTA	eltrombopag olamine	TABLET;ORAL	022291-004	Oct 20, 2011	AB	RX	Yes	No	8,071,129*PED				Y
Novartis	PROMACTA	eltrombopag olamine	TABLET;ORAL	022291-001	Nov 20, 2008	AB	RX	Yes	No	8,071,129*PED				Y
Novartis	PROMACTA	eltrombopag olamine	TABLET;ORAL	022291-002	Nov 20, 2008	AB	RX	Yes	No	8,071,129*PED				Y
Novartis	PROMACTA	eltrombopag olamine	TABLET;ORAL	022291-003	Sep 8, 2009	AB	RX	Yes	Yes	8,071,129*PED				Y

International Family Members for US Patent 8,071,129

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	059656
Argentina	107711
Australia	2007352608
Australia	2012201288
Australia	2014202367