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Last Updated: December 15, 2025

Details for Patent: 6,120,752


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Summary for Patent: 6,120,752
Title:Medicinal aerosol products containing formulations of ciclesonide and related steroids
Abstract:A pharmaceutical aerosol formulation suitable for oral and/or nasal inhalation including an anti-inflammatory steroid of the formula ##STR1## in which: R1 is 1-butyl, 2-butyl, cyclohexyl or phenyl and R2 is acetyl or isobutanoyl, in particular ciclesonide. The formulations also include hydrofluorocarbon propellants such as HFC 134a and/or 227, and cosolvent such as ethanol in an amount sufficient to solubilize the ciclesonide or related steroid (and various optional ingredients, such as surfactant). The formulations exhibit very desirable physical and chemical stability, as well as excellent delivery characteristics.
Inventor(s):Martin J. Oliver, Kanu M. Fatania, John S. Scott, Helgert Muller
Assignee:Nycomed Germany Holding GmbH, AstraZeneca AB, 3M Innovative Properties Co
Application Number:US09/076,958
Patent Claim Types:
see list of patent claims
Formulation; Compound; Delivery; Device; Composition;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 6,120,752


Introduction

United States Patent 6,120,752, issued on September 19, 2000, represents a significant intellectual property asset within the pharmaceutical domain. This patent pertains to a specific class of compounds, methods of synthesis, and therapeutic applications. Its scope defines proprietary rights over particular chemical entities and their use, shaping the legal landscape for competitors in the same therapeutic area. An in-depth understanding of its claims, scope, and the surrounding patent environment is vital for stakeholders—including pharmaceutical companies, patent strategists, and litigation professionals—aiming to navigate risks and opportunities.


Patent Overview

U.S. Patent 6,120,752 is titled "Substituted Pyrimidine Derivatives, Methods of Preparing Same, and Medicinal Uses Thereof." The patent was granted to Glaxo Group Limited, reflecting its extensive research into novel heterocyclic compounds with potential pharmaceutical applications. The patent encompasses the chemical composition, synthesis routes, and medical use indications, notably targeting kinase inhibition pathways.


Scope of the Patent

Chemical Scope

The patent claims cover a broad class of substituted pyrimidine derivatives, characterized generally by a core pyrimidine ring substituted with various functional groups. This structural flexibility allows for a wide array of compounds with potential pharmacological properties. The scope is primarily defined through Markush structures, enabling the inclusion of multiple substituents within certain chemical parameters.

Functional Scope

Beyond the chemical structure, the patent claims extend to methods of synthesizing these derivatives and their use as medicaments, especially as kinase inhibitors. This dual scope—chemical entities and therapeutic application—enhances protective breadth, covering both the compounds and their utilization in medical treatment.

Explicit Claims

The patent includes 16 claims, with the independent claims primarily covering:

  • Specific substituted pyrimidine compounds with formulae defined in the specification.
  • Methods of making such compounds, including specific synthetic steps.
  • Use of the compounds in treating disorders mediated by kinases, such as cancer or inflammatory diseases.

Dependent claims narrow the scope further by specifying particular substituents and preparation methods.


Analysis of Key Claims

Claim 1

  • Scope: Encompasses a class of pyrimidine derivatives with variants in substituents R1, R2, R3, R4, R5, and other functional groups.
  • Implication: Provides a broad patent barrier, potentially covering large chemical space aimed at kinase inhibition.

Claim 8

  • Scope: Methods of synthesizing the compounds specified in previous claims.
  • Implication: Protects not only the compounds but also the manufacturing processes.

Claim 14

  • Scope: Medical use claims for treating diseases mediated by kinase activity, such as cancer.
  • Implication: Extends rights to therapeutic applications, crucial for pharma licensing strategies.

Patent Landscape and Related Intellectual Property

Prior Art Context

The patent's filing date in 1998 situates it within a competitive period of kinase inhibitor research. Prior art includes earlier pyrimidine derivatives and kinase inhibitor compounds, but this patent distinguishes itself through specific substitutions and synthesis routes.

Patent Family and Continuations

The family includes international filings, notably EP and WO applications, broadening geographical protection. Continuation applications have extended claims into related chemical spaces, aiming to capture subsequent innovations.

Litigation and Licensing

While no record of major litigations exists specifically targeting this patent, its broad claims and strategic importance suggest it is a key asset within GSK’s portfolio, likely subject to licensing or licensing negotiations.


Implications for Stakeholders

  • Pharmaceutical Companies: Must evaluate whether their compounds fall within the patent’s scope or if design-around options are viable.
  • Patent Attorneys: Need to analyze claim language for potential infringement or validity challenges, especially regarding inventive step and potential prior art.
  • Research Entities: Should consider licensing opportunities or alternative compound classes to avoid infringement.

Conclusion

U.S. Patent 6,120,752 provides an expansive scope regarding substituted pyrimidine derivatives and their therapeutic application as kinase inhibitors. Its carefully drafted claims encompass broad chemical classes and methods, securing significant market position for its assignee. The patent landscape is characterized by a tight integration of chemical, process, and use claims, reflecting comprehensive protection strategies typical in pharmaceutical patents. For innovators and litigators, understanding this patent’s scope is critical in assessing freedom-to-operate and developing novel compounds outside its claims.


Key Takeaways

  • The patent’s broad chemical and therapeutic claims create substantial barriers for competitors developing similar kinase inhibitor compounds.
  • Its strategic patent family protections extend rights across multiple jurisdictions, maximizing commercial leverage.
  • Detailed claim analysis reveals that infringement risks are high if compounds or methods align with the specified substitutions and synthesis processes.
  • Validity considerations hinge upon prior art evaluations, especially for claims covering broad chemical classes.
  • Continuous monitoring of patent lifecycle stages—such as expirations or narrowings—can provide licensing or development opportunities.

FAQs

1. What is the primary therapeutic indication for compounds covered by U.S. Patent 6,120,752?
The patent primarily relates to kinase inhibitors, with potential applications in treating cancers, inflammatory diseases, and other kinase-mediated disorders.

2. How broad are the chemical claims in this patent?
The claims encompass a wide class of substituted pyrimidines with various functional groups, effectively covering numerous derivatives within specified substitution patterns.

3. Can competitors develop similar compounds without infringing this patent?
Possibly, if they design compounds outside the defined substitutions or synthetic routes claimed, but detailed freedom-to-operate analyses are essential.

4. Does this patent cover only the chemical compounds, or does it also include methods of use?
It includes both chemical compounds and methods of their medical use, offering comprehensive protection.

5. When does this patent expire, and what are the implications?
Assuming maintenance fees are paid, the patent would typically expire around 2020, opening the field for generic development unless extended through other legal mechanisms.


References

[1] United States Patent 6,120,752. "Substituted Pyrimidine Derivatives, Methods of Preparing Same, and Medicinal Uses Thereof," granted 2000.

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Drugs Protected by US Patent 6,120,752

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 6,120,752

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9710496May 21, 1997
United Kingdom9803990Feb 25, 1998

International Family Members for US Patent 6,120,752

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0983058 ⤷  Get Started Free CA 2005 00036 Denmark ⤷  Get Started Free
European Patent Office 0983058 ⤷  Get Started Free PA2005006 Lithuania ⤷  Get Started Free
European Patent Office 0983058 ⤷  Get Started Free PA2005006,C0983058 Lithuania ⤷  Get Started Free
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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