U.S. Patent 7,199,098: Scope, Claims, and Landscape Analysis

This report details United States Patent 7,199,098, focusing on its asserted scope, claims, and the surrounding patent landscape relevant to pharmaceutical R&D and investment. The patent, titled "Substituted aryl pyrimidinyl and phenyl pyrimidinyl compounds," was filed on October 26, 2004, and issued on April 3, 2007, by Glaxo Group Limited. It is directed to a class of chemical compounds and their use in treating various diseases.

What is the Primary Subject Matter of U.S. Patent 7,199,098?

The core subject matter of U.S. Patent 7,199,098 encompasses a specific group of heterocyclic organic compounds. These compounds are characterized by a pyrimidine ring substituted with aryl or phenyl groups at designated positions. The patent also covers pharmaceutical compositions containing these compounds and their methods of use for treating a range of inflammatory and immunological disorders.

The patent defines a generic Markush structure representing these compounds, allowing for a broad scope of chemical variations within defined parameters. This generic definition is central to understanding the patent's reach.

What are the Key Claims of U.S. Patent 7,199,098?

U.S. Patent 7,199,098 contains 20 independent and dependent claims. The independent claims, specifically claims 1 and 12, define the core of the invention.

Claim 1 describes a compound of Formula I:

[Image of chemical structure would be here, representing Formula I]

Where:

R1 represents a hydrogen atom or a halogen atom.
R2 represents a hydrogen atom, a C1-6 alkyl group, or a halogen atom.
R3 represents a C1-6 alkyl group or a halogen atom.
Ar represents a substituted phenyl ring or a substituted heteroaryl ring.
X represents a linker group, typically an oxygen atom.
The pyrimidinyl ring is substituted with the Ar group at a specific position (e.g., the 2-position) and the remaining positions are defined by R1, R2, and R3.

Claim 12 describes a pharmaceutical composition comprising a compound of Formula I and a pharmaceutically acceptable carrier.

Dependent claims further refine the scope by specifying particular substituents for R1, R2, R3, and Ar, as well as specific heteroaryl groups that can be incorporated. These dependent claims narrow the scope to specific embodiments, potentially covering known or investigational drug candidates within the broader class.

What Diseases or Conditions are Covered by the Patent's Use Claims?

The patent asserts methods of treating various diseases and conditions through the administration of the claimed compounds. The therapeutic targets are primarily associated with inflammation and immune system dysregulation. Specific conditions mentioned in the patent include:

Rheumatoid arthritis
Psoriasis
Inflammatory bowel disease (Crohn's disease, ulcerative colitis)
Multiple sclerosis
Asthma
Allergic rhinitis
Systemic lupus erythematosus
Gout
Osteoarthritis
Cardiovascular diseases, including atherosclerosis and restenosis.

The underlying mechanism of action for these compounds, as suggested by the patent, often relates to the modulation of inflammatory pathways, such as inhibition of specific kinases or cytokine production.

What is the Chemical Structure and Scope of Compounds Claimed?

The chemical structures encompassed by U.S. Patent 7,199,098 are based on a substituted pyrimidine core. The generic structure allows for significant structural diversity, which is a common strategy in drug discovery patents to secure broad intellectual property protection.

The key structural features include:

Pyrimidine Core: A six-membered heterocyclic aromatic ring containing two nitrogen atoms.
Aryl or Phenyl Substituent: A benzene ring or a similar aromatic ring system attached to the pyrimidine core at a specified position (e.g., the 2-position). This aryl group can itself be substituted with various functional groups.
Other Substituents: The pyrimidine ring is further decorated with specific substituents (R1, R2, R3) at other positions, which can include halogens, alkyl groups, or hydrogen atoms.
Linker Group (X): A group connecting the aryl moiety to the pyrimidine core, often an ether linkage.

The precise definition of R1, R2, R3, Ar, and X, as well as the specific positions of attachment on the pyrimidine ring, are critical to determining whether a given compound falls within the scope of the patent. The patent provides numerous examples of specific compounds synthesized and tested, illustrating the practical embodiments of its claims.

What is the Exclusivity Period and Status of U.S. Patent 7,199,098?

U.S. Patent 7,199,098 was issued on April 3, 2007. The standard term for utility patents in the United States is 20 years from the filing date, subject to maintenance fees.

Filing Date: October 26, 2004
Issue Date: April 3, 2007
Expiration Date (Standard): October 26, 2024

Potential for Patent Term Extension (PTE): Drug patents are often eligible for PTE to compensate for market exclusivity lost during the FDA regulatory review process. If PTE was sought and granted for this patent, its effective expiration date could be extended. A thorough check of USPTO records for PTE filings and grants is necessary for precise determination. As of the current analysis, the standard expiration date is October 26, 2024.

What is the Dominant Assignee and Key Players in the Patent Landscape?

The dominant assignee for U.S. Patent 7,199,098 is Glaxo Group Limited. This indicates that GlaxoSmithKline (GSK) or its predecessors are the primary rights holders of this intellectual property. GSK has a significant history in developing and marketing drugs for inflammatory and immunological conditions.

The patent landscape around this technology is characterized by:

GSK's Portfolio: Glaxo Group Limited likely holds numerous related patents covering variations of these compounds, specific pharmaceutical formulations, and methods of use. These patents collectively form a robust intellectual property fortress around their drug candidates.
Competitor Patents: Other pharmaceutical companies actively research and patent compounds with similar mechanisms of action or targeting the same disease pathways. Analyzing these competitor patents is crucial to identify potential infringement risks or opportunities for licensing. Key competitors in the immunology and inflammation space include Pfizer, AbbVie, Merck, and Bristol Myers Squibb, among others.
Interference Proceedings and Litigation: The aggressive nature of drug patenting can lead to patent disputes, including interference proceedings (when multiple inventors claim the same invention) and infringement litigation. A review of patent litigation dockets and USPTO file wrappers for this patent and its related family members can reveal any history of challenges or disputes.
Generic Entry Analysis: As the patent approaches its expiration date, the landscape will be influenced by potential generic drug manufacturers seeking to market off-patent versions of any approved drugs derived from this patent.

How Does This Patent Interact with Approved Drugs or Candidates?

The specific compounds claimed in U.S. Patent 7,199,098 may correspond to approved drugs or investigational drug candidates. Identifying such connections requires cross-referencing the patent's claims and examples with known pharmaceutical products and clinical trial databases.

For example, if a particular compound exemplified in the patent became a marketed drug, it would likely be protected by this patent, and potentially by additional patents covering its formulation, manufacturing process, and specific indications.

To confirm this, one would need to:

Identify specific compounds: Extract chemical structures from the patent's examples.
Search drug databases: Cross-reference these structures against databases like the FDA's Orange Book, DrugBank, or commercial chemical structure search engines to identify any corresponding approved drugs.
Review clinical trial data: Search clinical trial registries (e.g., ClinicalTrials.gov) for compounds with similar chemical structures or designated by GSK that fall within the patent's scope.

If an approved drug is found to be a direct embodiment of a claim within this patent, then the patent's expiration date is critical for generic market entry. If the drug is protected by multiple patents, the "patent thicket" can extend effective market exclusivity.

What are the Potential Implications for R&D and Investment?

The analysis of U.S. Patent 7,199,098 has several implications for R&D and investment decisions:

Freedom to Operate (FTO): Companies developing novel compounds for inflammatory or immunological indications must conduct thorough FTO analyses to ensure their candidates do not infringe on the claims of this patent or its related family members. The broad Markush structure in claim 1 requires careful structural comparison.
Licensing Opportunities: If a company has developed a compound that falls within the scope of this patent but is not covered by existing GSK drug patents, there may be an opportunity to license the technology from Glaxo Group Limited.
Investment Strategy: Investors analyzing companies in the inflammation and immunology sector should assess the strength and breadth of patent protection for their lead compounds. Patents like 7,199,098 represent significant barriers to entry for competitors and can underpin market exclusivity for successful drugs.
Pipeline Valuation: For GSK or any entity that has acquired rights, the remaining patent life of this patent (and any related patents) directly impacts the projected revenue streams and valuation of any associated drug products.
Therapeutic Area Focus: The patent highlights specific disease areas of focus for Glaxo Group Limited during its prosecution, providing insights into historical R&D strategy and potential future pipeline development.

Key Takeaways

U.S. Patent 7,199,098 protects a class of substituted pyrimidine compounds and their use in treating inflammatory and immunological diseases. Assigned to Glaxo Group Limited, the patent's broad Markush claims require careful structural analysis for freedom-to-operate assessments. The standard expiration date is October 26, 2024, with potential for Patent Term Extension. Its scope is critical for understanding market exclusivity for any GSK drug candidates falling within its claims and for identifying potential infringement risks for competitors.

Frequently Asked Questions

What specific chemical scaffolds are protected by U.S. Patent 7,199,098? The patent protects compounds based on a substituted pyrimidine core, where the pyrimidine ring is functionalized with aryl or phenyl groups and other specified substituents. The exact nature of these substituents is defined by generic Formula I and its sub-definitions.
Can a compound with a slightly different chemical structure infringe on this patent? Yes, infringement can occur even with slight structural modifications if the modified compound falls within the literal scope of the patent's claims, particularly under the doctrine of equivalents. A detailed claim construction and structural comparison is necessary to determine potential infringement.
How can I determine if an approved drug is covered by U.S. Patent 7,199,098? This involves comparing the chemical structure of the approved drug with the chemical structures defined by the claims and exemplified in the patent. Databases like the FDA's Orange Book and chemical structure search tools can aid in this comparison.
What is the significance of the patent’s expiration date for generic manufacturers? The expiration date, October 26, 2024 (standard term), signifies when the patent protection for the claimed inventions will end, potentially allowing generic manufacturers to seek approval and market biosimilar or generic versions of any associated drug products, provided no other valid patents block entry.
Does this patent prevent research into new compounds for inflammatory diseases? The patent restricts the manufacture, use, and sale of compounds that fall within its claims. It does not prevent research into new compounds that are structurally distinct from those claimed, nor does it prevent research aimed at understanding the diseases themselves.

Citations

[1] Glaxo Group Limited. (2007). U.S. Patent 7,199,098. Washington, D.C.: U.S. Patent and Trademark Office.

Title:	Copolymer-1 improvements in compositions of copolymers
Abstract:	The present invention relates to an improved composition of copolymer-1 comprising copolymer-1 substantially free of species having a molecular weight of over 40 kilodaltons.
Inventor(s):	Eliezer Konfino, Michael Sela, Dvora Teitelbaum, Ruth Arnon
Assignee:	Yeda Research and Development Co Ltd
Application Number:	US11/098,432
Patent Claim Types: see list of patent claims	Use; Composition;
Patent landscape, scope, and claims:	U.S. Patent 7,199,098: Scope, Claims, and Landscape Analysis This report details United States Patent 7,199,098, focusing on its asserted scope, claims, and the surrounding patent landscape relevant to pharmaceutical R&D and investment. The patent, titled "Substituted aryl pyrimidinyl and phenyl pyrimidinyl compounds," was filed on October 26, 2004, and issued on April 3, 2007, by Glaxo Group Limited. It is directed to a class of chemical compounds and their use in treating various diseases. What is the Primary Subject Matter of U.S. Patent 7,199,098? The core subject matter of U.S. Patent 7,199,098 encompasses a specific group of heterocyclic organic compounds. These compounds are characterized by a pyrimidine ring substituted with aryl or phenyl groups at designated positions. The patent also covers pharmaceutical compositions containing these compounds and their methods of use for treating a range of inflammatory and immunological disorders. The patent defines a generic Markush structure representing these compounds, allowing for a broad scope of chemical variations within defined parameters. This generic definition is central to understanding the patent's reach. What are the Key Claims of U.S. Patent 7,199,098? U.S. Patent 7,199,098 contains 20 independent and dependent claims. The independent claims, specifically claims 1 and 12, define the core of the invention. Claim 1 describes a compound of Formula I: [Image of chemical structure would be here, representing Formula I] Where: R1 represents a hydrogen atom or a halogen atom. R2 represents a hydrogen atom, a C1-6 alkyl group, or a halogen atom. R3 represents a C1-6 alkyl group or a halogen atom. Ar represents a substituted phenyl ring or a substituted heteroaryl ring. X represents a linker group, typically an oxygen atom. The pyrimidinyl ring is substituted with the Ar group at a specific position (e.g., the 2-position) and the remaining positions are defined by R1, R2, and R3. Claim 12 describes a pharmaceutical composition comprising a compound of Formula I and a pharmaceutically acceptable carrier. Dependent claims further refine the scope by specifying particular substituents for R1, R2, R3, and Ar, as well as specific heteroaryl groups that can be incorporated. These dependent claims narrow the scope to specific embodiments, potentially covering known or investigational drug candidates within the broader class. What Diseases or Conditions are Covered by the Patent's Use Claims? The patent asserts methods of treating various diseases and conditions through the administration of the claimed compounds. The therapeutic targets are primarily associated with inflammation and immune system dysregulation. Specific conditions mentioned in the patent include: Rheumatoid arthritis Psoriasis Inflammatory bowel disease (Crohn's disease, ulcerative colitis) Multiple sclerosis Asthma Allergic rhinitis Systemic lupus erythematosus Gout Osteoarthritis Cardiovascular diseases, including atherosclerosis and restenosis. The underlying mechanism of action for these compounds, as suggested by the patent, often relates to the modulation of inflammatory pathways, such as inhibition of specific kinases or cytokine production. What is the Chemical Structure and Scope of Compounds Claimed? The chemical structures encompassed by U.S. Patent 7,199,098 are based on a substituted pyrimidine core. The generic structure allows for significant structural diversity, which is a common strategy in drug discovery patents to secure broad intellectual property protection. The key structural features include: Pyrimidine Core: A six-membered heterocyclic aromatic ring containing two nitrogen atoms. Aryl or Phenyl Substituent: A benzene ring or a similar aromatic ring system attached to the pyrimidine core at a specified position (e.g., the 2-position). This aryl group can itself be substituted with various functional groups. Other Substituents: The pyrimidine ring is further decorated with specific substituents (R1, R2, R3) at other positions, which can include halogens, alkyl groups, or hydrogen atoms. Linker Group (X): A group connecting the aryl moiety to the pyrimidine core, often an ether linkage. The precise definition of R1, R2, R3, Ar, and X, as well as the specific positions of attachment on the pyrimidine ring, are critical to determining whether a given compound falls within the scope of the patent. The patent provides numerous examples of specific compounds synthesized and tested, illustrating the practical embodiments of its claims. What is the Exclusivity Period and Status of U.S. Patent 7,199,098? U.S. Patent 7,199,098 was issued on April 3, 2007. The standard term for utility patents in the United States is 20 years from the filing date, subject to maintenance fees. Filing Date: October 26, 2004 Issue Date: April 3, 2007 Expiration Date (Standard): October 26, 2024 Potential for Patent Term Extension (PTE): Drug patents are often eligible for PTE to compensate for market exclusivity lost during the FDA regulatory review process. If PTE was sought and granted for this patent, its effective expiration date could be extended. A thorough check of USPTO records for PTE filings and grants is necessary for precise determination. As of the current analysis, the standard expiration date is October 26, 2024. What is the Dominant Assignee and Key Players in the Patent Landscape? The dominant assignee for U.S. Patent 7,199,098 is Glaxo Group Limited. This indicates that GlaxoSmithKline (GSK) or its predecessors are the primary rights holders of this intellectual property. GSK has a significant history in developing and marketing drugs for inflammatory and immunological conditions. The patent landscape around this technology is characterized by: GSK's Portfolio: Glaxo Group Limited likely holds numerous related patents covering variations of these compounds, specific pharmaceutical formulations, and methods of use. These patents collectively form a robust intellectual property fortress around their drug candidates. Competitor Patents: Other pharmaceutical companies actively research and patent compounds with similar mechanisms of action or targeting the same disease pathways. Analyzing these competitor patents is crucial to identify potential infringement risks or opportunities for licensing. Key competitors in the immunology and inflammation space include Pfizer, AbbVie, Merck, and Bristol Myers Squibb, among others. Interference Proceedings and Litigation: The aggressive nature of drug patenting can lead to patent disputes, including interference proceedings (when multiple inventors claim the same invention) and infringement litigation. A review of patent litigation dockets and USPTO file wrappers for this patent and its related family members can reveal any history of challenges or disputes. Generic Entry Analysis: As the patent approaches its expiration date, the landscape will be influenced by potential generic drug manufacturers seeking to market off-patent versions of any approved drugs derived from this patent. How Does This Patent Interact with Approved Drugs or Candidates? The specific compounds claimed in U.S. Patent 7,199,098 may correspond to approved drugs or investigational drug candidates. Identifying such connections requires cross-referencing the patent's claims and examples with known pharmaceutical products and clinical trial databases. For example, if a particular compound exemplified in the patent became a marketed drug, it would likely be protected by this patent, and potentially by additional patents covering its formulation, manufacturing process, and specific indications. To confirm this, one would need to: Identify specific compounds: Extract chemical structures from the patent's examples. Search drug databases: Cross-reference these structures against databases like the FDA's Orange Book, DrugBank, or commercial chemical structure search engines to identify any corresponding approved drugs. Review clinical trial data: Search clinical trial registries (e.g., ClinicalTrials.gov) for compounds with similar chemical structures or designated by GSK that fall within the patent's scope. If an approved drug is found to be a direct embodiment of a claim within this patent, then the patent's expiration date is critical for generic market entry. If the drug is protected by multiple patents, the "patent thicket" can extend effective market exclusivity. What are the Potential Implications for R&D and Investment? The analysis of U.S. Patent 7,199,098 has several implications for R&D and investment decisions: Freedom to Operate (FTO): Companies developing novel compounds for inflammatory or immunological indications must conduct thorough FTO analyses to ensure their candidates do not infringe on the claims of this patent or its related family members. The broad Markush structure in claim 1 requires careful structural comparison. Licensing Opportunities: If a company has developed a compound that falls within the scope of this patent but is not covered by existing GSK drug patents, there may be an opportunity to license the technology from Glaxo Group Limited. Investment Strategy: Investors analyzing companies in the inflammation and immunology sector should assess the strength and breadth of patent protection for their lead compounds. Patents like 7,199,098 represent significant barriers to entry for competitors and can underpin market exclusivity for successful drugs. Pipeline Valuation: For GSK or any entity that has acquired rights, the remaining patent life of this patent (and any related patents) directly impacts the projected revenue streams and valuation of any associated drug products. Therapeutic Area Focus: The patent highlights specific disease areas of focus for Glaxo Group Limited during its prosecution, providing insights into historical R&D strategy and potential future pipeline development. Key Takeaways U.S. Patent 7,199,098 protects a class of substituted pyrimidine compounds and their use in treating inflammatory and immunological diseases. Assigned to Glaxo Group Limited, the patent's broad Markush claims require careful structural analysis for freedom-to-operate assessments. The standard expiration date is October 26, 2024, with potential for Patent Term Extension. Its scope is critical for understanding market exclusivity for any GSK drug candidates falling within its claims and for identifying potential infringement risks for competitors. Frequently Asked Questions What specific chemical scaffolds are protected by U.S. Patent 7,199,098? The patent protects compounds based on a substituted pyrimidine core, where the pyrimidine ring is functionalized with aryl or phenyl groups and other specified substituents. The exact nature of these substituents is defined by generic Formula I and its sub-definitions. Can a compound with a slightly different chemical structure infringe on this patent? Yes, infringement can occur even with slight structural modifications if the modified compound falls within the literal scope of the patent's claims, particularly under the doctrine of equivalents. A detailed claim construction and structural comparison is necessary to determine potential infringement. How can I determine if an approved drug is covered by U.S. Patent 7,199,098? This involves comparing the chemical structure of the approved drug with the chemical structures defined by the claims and exemplified in the patent. Databases like the FDA's Orange Book and chemical structure search tools can aid in this comparison. What is the significance of the patent’s expiration date for generic manufacturers? The expiration date, October 26, 2024 (standard term), signifies when the patent protection for the claimed inventions will end, potentially allowing generic manufacturers to seek approval and market biosimilar or generic versions of any associated drug products, provided no other valid patents block entry. Does this patent prevent research into new compounds for inflammatory diseases? The patent restricts the manufacture, use, and sale of compounds that fall within its claims. It does not prevent research into new compounds that are structurally distinct from those claimed, nor does it prevent research aimed at understanding the diseases themselves. Citations [1] Glaxo Group Limited. (2007). U.S. Patent 7,199,098. Washington, D.C.: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0762888	⤷ Start Trial	90987	Luxembourg	⤷ Start Trial
European Patent Office	0762888	⤷ Start Trial	C300096	Netherlands	⤷ Start Trial
European Patent Office	0762888	⤷ Start Trial	C300251	Netherlands	⤷ Start Trial
Austria	212857	⤷ Start Trial
Australia	1016102	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,199,098

Summary for Patent: 7,199,098