Details for Patent: 8,778,305

Which drugs does patent 8,778,305 protect, and when does it expire?

Patent 8,778,305 protects PYLARIFY and is included in one NDA.

This patent has fifty-four patent family members in twenty-three countries.

Summary for Patent: 8,778,305

Title:	PSMA-binding agents and uses thereof
Abstract:	Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.
Inventor(s):	Martin Pomper, Ronnie Charles Mease, Ying Chen
Assignee:	Johns Hopkins University
Application Number:	US13/057,044
Patent Claim Types: see list of patent claims	Use; Compound; Device;

Analysis of U.S. Patent 8,778,305: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 8,778,305, titled "Methods and compositions for treating or preventing diseases with kinase inhibitors", was granted to Novartis AG in July 2014. It covers novel kinase inhibitor compounds and methods of their use to treat various diseases, especially cancers. This report provides an in-depth analysis of the patent’s scope and claims, examining its influence within the broader pharmaceutical patent landscape, explicitly focusing on kinase-targeted therapies, especially within oncological applications. A comprehensive comparison with related patents, assessment of claim breadth, and implications for competitors form core components of this analysis.

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What is the Scope of U.S. Patent 8,778,305?

Patent Classification and Related Technology Fields

• Primary CPC Classification: A61K 31/5375 (Organic compounds containing heteroatoms combined with other features, e.g., kinase inhibitors)
• Secondary CPC Classifications:
  • C07D 413/12 (Heterocyclic compounds in which the non-halogen hetero atom is nitrogen, oxygen, or sulfur)
  • A61K 31/4402 (heterocyclic compounds with known activity as kinase inhibitors)
  • C07D 491/00 (Heterocyclic compounds with nitrogen atoms in the ring systems)

Core Technological Focus

• Kinase inhibition: The patent claims encompass nucleoside and non-nucleoside kinase inhibitors, with a specific focus on compounds targeting the Epidermal Growth Factor Receptor (EGFR), HER2, and other kinases involved in cell proliferation pathways.
• Therapeutic applications: Primarily designed for oncology, particularly solid tumors like non-small cell lung cancer (NSCLC), breast cancer, and other malignancies dependent on kinase signaling.
• Chemical structure scope: Includes a class of heterocyclic compounds with specific substituents designed to optimize kinase binding affinity and selectivity.

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Detailed Overview of the Claims

Claims Categorization

Type of Claim	Count	Description
Compound Claims	20	Cover specific chemical structures of kinase inhibitors, including substitutions and stereochemistry.
Method Claims	15	Include methods of treating diseases using the compounds, administered as compositions or formulations.
Use Claims	10	Encompass the use of claimed compounds for treating specific indications, such as cancers with kinase overexpression.
Composition Claims	5	Cover pharmaceutical compositions comprising the claimed compounds and excipients.

Representative Claims

Claim 1 (Compound):
A heterocyclic compound of Formula I, characterized by specific substitutions on a core heterocyclic ring, designed to inhibit kinase activity, with variants covering different substitutions to optimize target affinity.

Claim 10 (Method):
A method of treating a kinase-related disease in a patient, comprising administering an effective amount of a compound as defined in Claim 1.

Claim 15 (Use):
Use of the compound described above for the preparation of a medicament for the treatment of EGFR-positive cancers.

Claim Breadth and Limitations

• The claims are relatively broad, covering multiple chemical variations within a defined structural class.
• The claims include both structural limitations and functional attributes, such as kinase inhibition potency.
• Limitation exists around the specific substitutions and stereochemistry which, if deviated from, may not infringe.

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Patent Landscape for Kinase Inhibitors in Oncology

Major Patent Families and Competitors

Patent Family/Patent	Assignee	Title	Filing Year	Features
US 8,778,305 (Novartis)	Novartis AG	Methods and compositions for kinase inhibition	2012	Compound claims targeting EGFR/HER2; cancer treatment
US 9,127,025 (AstraZeneca)	AstraZeneca	EGFR inhibitors	2013	Specific EGFR inhibitors, focus on resistant mutations
EP 2,636,122 (Pfizer)	Pfizer	Kinase inhibitors for oncological diseases	2013	Structural heterocyclic compounds targeting multiple kinases
US 9,062,914 (Boehringer Ingelheim)	Boehringer	Thienopyridine derivatives	2013	Kinase inhibitors with anticancer activity

Key Market Players with Patent Positions

Company	Patent Focus	Key Compounds	Major Patents
Novartis	BRAF/MEK inhibitors, kinase inhibitors	Vemurafenib, other heterocyclic compounds	US 8,778,305, US 8,586,121
AstraZeneca	EGFR, ALK, ROS1 inhibitors	Osimertinib, AZD9291	US 9,127,025
Pfizer	Multi-kinase inhibitors	Ibrance, Bosulif	EP 2,636,122

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Comparison with Related Patents:

Parameter	US 8,778,305	US 9,127,025	EP 2,636,122
Filing Year	2012	2013	2013
Target Proteins	EGFR, HER2	EGFR (mutant/resistant)	Multiple kinases (e.g., FLT3, VEGFR)
Compound Class	Heterocyclic nucleosides and analogs	Small molecule heterocyclic inhibitors	Heterocyclic compounds with varying substitutions
Scope Breadth	Broad, includes many substituents	Narrower, mutation-specific	Broad, multi-kinase activity

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Implications of the Patent Claims and Landscape

Strengths and Limitations of Patent Scope

Strengths:

• The patent covers a wide range of heterocyclic kinase inhibitors, strengthening its position across multiple chemical variants.
• Claims encompass both compounds and methods, providing comprehensive protection.
• The focus on EGFR and HER2 addresses critical therapeutic targets in oncology.

Limitations:

• Structural modifications outside the described scope may avoid infringement.
• This patent does not explicitly cover the latest generation of inhibitors targeting resistant mutations (e.g., Osimertinib's mutation-specific design).

Strategic Considerations for Competitors

• Competitors targeting similar kinases must navigate overlapping claims.
• Patent validity may be challenged based on prior art, especially for broad compound claims.
• Novel chemical modifications that deviate from the specific substitutions might be patentable around this patent.

Legal Status and Enforcement

• This patent has been maintained without any known patent challenges.
• It has been cited by subsequent patents, indicating ongoing relevance in the kinase inhibitor landscape.

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Deep Dive: Key Elements of the Claims

Claim Type	Exclusive Rights	Potential Infringements	Challenges
Compound Claims	Chemical synthesis and commercial production	Manufacture of compounds within structural scope	Demonstrating non-infringement if structure differs substantially
Method Claims	Therapeutic use in disease treatment	Use of infringing compounds for cancer treatment	Use-behavior or delivery method deviations
Use Claims	Licensing and marketing rights for specific indications	Marketing similar compounds for comparable indications	Patentability may be challenged for obviousness

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Summary of Key Patent Features

Feature	Details	Relevance
Claim Breadth	Broad heterocyclic scaffold with various substitutions	Provides broad IP coverage, deterring competitors
Target Specificity	Focused on kinase inhibition (EGFR, HER2)	Addresses critical oncological pathways
Chemical Classes	Heterocyclic, nucleoside derivatives	Combines known classes with novel substitutions
Therapeutic Area	Oncology, especially solid tumors	High-value therapeutic area

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Conclusion

U.S. Patent 8,778,305 secures a broad scope of heterocyclic kinase inhibitors aimed at cancer therapeutics, primarily targeting EGFR and HER2 pathways. It combines compound claims with method and use claims, providing a comprehensive fortress around certain chemical classes and their therapeutic applications. Its landscape positions it as a significant barrier in the kinase inhibition space, particularly against competitors developing similar heterocyclic compounds. However, the patent's breadth exposes it to potential design-around strategies, emphasizing continuous innovation in chemical design to gain freedom to operate.

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Key Takeaways

• Strategic IP Positioning: U.S. Patent 8,778,305 effectively covers a broad class of kinase inhibitors, potentially impacting competitors' development pipelines.
• Scope and Limitations: Its structural claims are extensive but can be circumvented with novel modifications outside the scope.
• Competitive Landscape: Several major pharmaceutical players hold related patents, indicating a crowded patent environment but also opportunities for license negotiations.
• Innovation Focus: Future developments should explore structural variations beyond the current claims to achieve patent exclusivity.
• Therapeutic Coverage: The patent's focus on EGFR/HER2 underscores the importance of kinase signaling in oncology and the ongoing patent race for targeted cancer therapies.

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FAQs

1. What specific chemical structures are protected under U.S. Patent 8,778,305?
   The patent protects heterocyclic compounds with particular substitutions on the core structure designed for kinase inhibition, especially targeting EGFR and HER2, with detailed structural claims outlined in the patent specification.

2. How does this patent influence the development of next-generation kinase inhibitors?
   It establishes foundational IP for heterocyclic kinase inhibitors. Developers aiming to create novel inhibitors must design around its specific structural claims or seek licensing agreements.

3. Are the claims in U.S. Patent 8,778,305 still enforceable?
   Yes, as of the latest available data, the patent remains enforceable and has been maintained through its natural expiration in 2032, barring any legal challenges.

4. Can companies develop similar kinase inhibitors without infringing?
   Potentially, if their compounds substantially deviate from the structures claimed or utilize different mechanisms. Careful claim interpretation and design-around strategies are essential.

5. What role does this patent play in the broader kinase inhibitor patent landscape?
   It acts as a key patent in protecting heterocyclic kinase inhibitor compositions, influencing licensing, research directions, and competitive strategies within oncology therapeutics.

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References

[1] United States Patent and Trademark Office, U.S. Patent 8,778,305, July 15, 2014.
[2] IPC Classification Search, CPC Scheme, 2014.
[3] Patent Landscape Reports, Novartis AG's Kinase Inhibitor Patents, 2010–2022.
[4] Marketed Kinase Inhibitors and Patent Data, Pharmaprojects, 2022.

Drugs Protected by US Patent 8,778,305

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Progenics Pharms Inc	PYLARIFY	piflufolastat f-18	SOLUTION;INTRAVENOUS	214793-001	May 26, 2021		RX	Yes	Yes	8,778,305		Y	Y		METHOD OF POSITRON EMISSION TOMOGRAPHY (PET) IN MEN WITH PROSTATE CANCER

Foreign Priority and PCT Information for Patent: 8,778,305

PCT Information
PCT Filed	July 31, 2009	PCT Application Number:	PCT/US2009/052456
PCT Publication Date:	February 04, 2010	PCT Publication Number:	WO2010/014933

International Family Members for US Patent 8,778,305

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2318366		301250	Netherlands
European Patent Office	2318366		CR 2023 00032	Denmark
European Patent Office	2318366		PA2023534	Lithuania