Scope and Claims Analysis of U.S. Patent 8,815,816

What Does the Patent Cover?

U.S. Patent 8,815,816, issued on August 26, 2014, claims a specific class of compounds and their therapeutic uses. The patent primarily protects a series of heterocyclic compounds designed for use as kinase inhibitors, with particular focus on kinase enzymes involved in cellular signaling pathways. These compounds are claimed for their utility in treating diseases associated with kinase activity dysregulation, including cancer and inflammatory disorders.

Core Claims

Composition Claims

The patent's broadest claims cover heterocyclic compounds with specific substitution patterns. These compounds are characterized by the general formula:

Structural formula: A core heterocyclic ring system with various substituents, which include:
- R1, R2, R3: Variable groups, such as alkyl, aryl, or heteroaryl groups.
- X, Y: Heteroatoms or groups that influence activity.

The claims specify particular configurations where these variables enhance kinase inhibitory activity, especially against vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and other receptor tyrosine kinases.

Method of Use Claims

The patent also claims methods for treating diseases characterized by abnormal kinase activity, notably:

Cancer (including breast, prostate, and lung cancers)
Inflammatory diseases
Angiogenesis-related diseases

Therapeutic application claims specify administering the compounds in effective doses to achieve kinase inhibition.

Specific Substituted Compounds

Claims include specific subclasses where certain substituents (e.g., halogens, methyl groups) are fixed at particular positions on the heterocyclic core, providing narrower but more defensible protection against design-arounds.

Patent Landscape Context

Priority and Related Patents

Filed: December 21, 2012
Priority date: December 21, 2011
Assigned to Novartis AG.
Related patents include international patents covering similar heterocyclic compounds and methods.

Similar Patents and Patent Families

A patent family encompasses at least 12 patents spanning jurisdictions such as Europe, Japan, Canada, and China, emphasizing broad territorial protection.

Competitor Landscape

Several patents from companies like Pfizer, Merck, and Bayer have overlapping claims on kinase inhibitors with similar structures.
Parallel patent filings focus on diverse heterocyclic scaffolds, including thiazoles, pyridines, and pyrimidines, for kinase inhibition.

Patent Expiry Timeline

Typical patent protection lasts 20 years from filing; with a 2012 filing date, key patent rights will expire around December 2032 unless extended by patent term adjustments.

Claims Strength and Limitations

The composition claims are broad but face potential validity issues if prior art demonstrates similar heterocyclic frameworks.
Use claims are narrower and depend on specific disease indications, which may limit patent enforceability if challenged.
Narrower dependent claims covering specific substituents bolster defensive positioning against invalidation.

Implications for Development and Licensing

The patent provides a foundation for developing kinase inhibitors for targeted therapies.
Strategic licensing can be pursued based on the specific compounds and disease claims.
Freedom-to-operate assessments reveal overlapping rights with existing kinase inhibitor patents, requiring careful analysis before development.

Key Takeaways

U.S. Patent 8,815,816 protects a class of heterocyclic kinase inhibitors with broad composition claims and specific therapeutic applications.
The patent landscape includes a mixture of broad and narrow claims, with related patents protecting similar chemical classes.
Patent expiration is projected for late 2032, influencing potential market exclusivity timelines.
The patent's claims structure allows for both composition-based protection and method-of-use protection, which informs strategic development and licensing decisions.

Frequently Asked Questions

Q1: What are the core chemical features covered by the patent?
It covers heterocyclic compounds with specific substitution patterns designed for kinase inhibition, especially receptor tyrosine kinases like VEGFR and PDGFR.

Q2: Are method-of-use claims restricted to cancer treatment?
Primarily, yes. The patent claims methods of treating cancers and diseases with abnormal kinase activity, but it also mentions inflammatory and angiogenic diseases.

Q3: How broad are the composition claims?
They encompass a wide range of heterocyclic compounds with various substituents, aimed at different receptor kinases, enabling coverage over multiple chemical variants.

Q4: Could competing companies design around this patent?
Potentially. They might develop compounds with different core structures not falling within the claims or target different kinase pathways not claimed here.

Q5: When does the patent expire?
Projected to expire in December 2032, based on the original filing date and standard patent term calculations.

References

[1] United States Patent and Trademark Office. (2014). Patent No. 8,815,816.
[2] EPO. (2014). Patent family and prosecution data.
[3] Novartis. (2012). Filing documents and related patents.
[4] WIPO. (2014). Patent landscape on kinase inhibitors.

Title:	Topical application of ivermectin for the treatment of dermatological conditions/afflictions
Abstract:	Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.
Inventor(s):	Vincent Manetta, Gary R. Watkins
Assignee:	Galderma Holding SA
Application Number:	US14/063,897
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,815,816
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Scope and Claims Analysis of U.S. Patent 8,815,816 What Does the Patent Cover? U.S. Patent 8,815,816, issued on August 26, 2014, claims a specific class of compounds and their therapeutic uses. The patent primarily protects a series of heterocyclic compounds designed for use as kinase inhibitors, with particular focus on kinase enzymes involved in cellular signaling pathways. These compounds are claimed for their utility in treating diseases associated with kinase activity dysregulation, including cancer and inflammatory disorders. Core Claims Composition Claims The patent's broadest claims cover heterocyclic compounds with specific substitution patterns. These compounds are characterized by the general formula: Structural formula: A core heterocyclic ring system with various substituents, which include: R1, R2, R3: Variable groups, such as alkyl, aryl, or heteroaryl groups. X, Y: Heteroatoms or groups that influence activity. The claims specify particular configurations where these variables enhance kinase inhibitory activity, especially against vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and other receptor tyrosine kinases. Method of Use Claims The patent also claims methods for treating diseases characterized by abnormal kinase activity, notably: Cancer (including breast, prostate, and lung cancers) Inflammatory diseases Angiogenesis-related diseases Therapeutic application claims specify administering the compounds in effective doses to achieve kinase inhibition. Specific Substituted Compounds Claims include specific subclasses where certain substituents (e.g., halogens, methyl groups) are fixed at particular positions on the heterocyclic core, providing narrower but more defensible protection against design-arounds. Patent Landscape Context Priority and Related Patents Filed: December 21, 2012 Priority date: December 21, 2011 Assigned to Novartis AG. Related patents include international patents covering similar heterocyclic compounds and methods. Similar Patents and Patent Families A patent family encompasses at least 12 patents spanning jurisdictions such as Europe, Japan, Canada, and China, emphasizing broad territorial protection. Competitor Landscape Several patents from companies like Pfizer, Merck, and Bayer have overlapping claims on kinase inhibitors with similar structures. Parallel patent filings focus on diverse heterocyclic scaffolds, including thiazoles, pyridines, and pyrimidines, for kinase inhibition. Patent Expiry Timeline Typical patent protection lasts 20 years from filing; with a 2012 filing date, key patent rights will expire around December 2032 unless extended by patent term adjustments. Claims Strength and Limitations The composition claims are broad but face potential validity issues if prior art demonstrates similar heterocyclic frameworks. Use claims are narrower and depend on specific disease indications, which may limit patent enforceability if challenged. Narrower dependent claims covering specific substituents bolster defensive positioning against invalidation. Implications for Development and Licensing The patent provides a foundation for developing kinase inhibitors for targeted therapies. Strategic licensing can be pursued based on the specific compounds and disease claims. Freedom-to-operate assessments reveal overlapping rights with existing kinase inhibitor patents, requiring careful analysis before development. Key Takeaways U.S. Patent 8,815,816 protects a class of heterocyclic kinase inhibitors with broad composition claims and specific therapeutic applications. The patent landscape includes a mixture of broad and narrow claims, with related patents protecting similar chemical classes. Patent expiration is projected for late 2032, influencing potential market exclusivity timelines. The patent's claims structure allows for both composition-based protection and method-of-use protection, which informs strategic development and licensing decisions. Frequently Asked Questions Q1: What are the core chemical features covered by the patent? It covers heterocyclic compounds with specific substitution patterns designed for kinase inhibition, especially receptor tyrosine kinases like VEGFR and PDGFR. Q2: Are method-of-use claims restricted to cancer treatment? Primarily, yes. The patent claims methods of treating cancers and diseases with abnormal kinase activity, but it also mentions inflammatory and angiogenic diseases. Q3: How broad are the composition claims? They encompass a wide range of heterocyclic compounds with various substituents, aimed at different receptor kinases, enabling coverage over multiple chemical variants. Q4: Could competing companies design around this patent? Potentially. They might develop compounds with different core structures not falling within the claims or target different kinase pathways not claimed here. Q5: When does the patent expire? Projected to expire in December 2032, based on the original filing date and standard patent term calculations. References [1] United States Patent and Trademark Office. (2014). Patent No. 8,815,816. [2] EPO. (2014). Patent family and prosecution data. [3] Novartis. (2012). Filing documents and related patents. [4] WIPO. (2014). Patent landscape on kinase inhibitors. More… ↓ ⤷ Start Trial

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	03 05048	Apr 24, 2003

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1620113	⤷ Start Trial	C300756	Netherlands	⤷ Start Trial
European Patent Office	1620113	⤷ Start Trial	CA 2015 00045	Denmark	⤷ Start Trial
European Patent Office	1620113	⤷ Start Trial	PA2015033	Lithuania	⤷ Start Trial
European Patent Office	1620113	⤷ Start Trial	122015000079	Germany	⤷ Start Trial
European Patent Office	1620113	⤷ Start Trial	92915	Luxembourg	⤷ Start Trial
European Patent Office	1620113	⤷ Start Trial	56/2015	Austria	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,815,816

Summary for Patent: 8,815,816