United States Patent 5,980,864: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 5,980,864, titled "1,4,7,10-tetraazacyclododecane butyltriols, processes for their production and pharmaceutical agents containing them," is a significant patent in the field of pharmaceuticals and diagnostic imaging. This patent, assigned to Bayer Schering Pharma Aktiengesellschaft, covers a range of compounds, their production processes, and their applications in medical diagnostics and therapy.
Background
The patent was granted on November 9, 1999, and has since expired, but its impact on the pharmaceutical and diagnostic imaging industries remains substantial. The patent focuses on 1,4,7,10-tetraazacyclododecane butyltriols, which are complex compounds used in various medical applications.
Scope of the Patent
Compounds and Their Production
The patent describes the synthesis and purification of 1,4,7,10-tetraazacyclododecane butyltriols. These compounds are produced through specific chemical reactions involving the reaction of 1,4,7,10-tetraazacyclododecane with butyltriols. The process ensures the production of high-purity compounds suitable for pharmaceutical use[1][4].
Pharmaceutical Agents
The patent covers pharmaceutical agents containing these compounds, which are designed for various medical applications. These agents are formulated to meet the stringent requirements for pharmaceutical use, ensuring stability, efficacy, and safety[1].
Claims of the Patent
Key Claims
The patent includes several key claims that define its scope:
- Claim 1: This claim covers the 1,4,7,10-tetraazacyclododecane butyltriols themselves, including their chemical structure and synthesis process.
- Claim 2: This claim pertains to the pharmaceutical compositions containing these compounds, including their formulation and preparation.
- Claim 3: This claim addresses the use of these compounds as susceptibility reagents and shift reagents for in vivo NMR spectroscopy.
- Claim 4: This claim covers the use of these compounds as radiodiagnostic media, including their application in positron emission tomography (PET)[1].
Specific Applications
- NMR Diagnostic Media: The patent specifies the use of these compounds in amounts of 0.0001-5 mmol/kg, preferably 0.005-0.5 mmol/kg, for NMR diagnostic purposes[1].
- Radiodiagnostic Media: The compounds are also suitable for use in radiodiagnostic applications, including PET, using positron-emitting isotopes such as 43Sc, 44Sc, 52Fe, 55Co, and 68Ga[1].
Patent Landscape
Related Patents
The patent landscape surrounding US 5,980,864 includes several related patents that build upon or intersect with its claims:
- US20210284662A1: This patent application describes a process for the preparation of 2,2',2''-(10-((2R,3S)-1,3,4-trihydroxybutan-2-yl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid and its complexes, which are related to the compounds described in US 5,980,864[4].
Litigation and Enforcement
While the patent itself is no longer in force, the principles and compounds described in it have been involved in various legal disputes. For instance, the complexities of patent claims and their enforcement are highlighted in cases such as the one involving United Therapeutics Corporation and Liquidia Technologies, Inc., where the focus was on the infringement and validity of related pharmaceutical patents[2].
Impact on Medical Diagnostics and Therapy
Diagnostic Imaging
The compounds described in this patent have been crucial in the development of diagnostic imaging techniques, particularly in NMR spectroscopy and PET. These techniques rely on the unique properties of these compounds to enhance image quality and provide detailed diagnostic information[1].
Pharmaceutical Applications
The pharmaceutical agents formulated from these compounds have been used in various therapeutic applications. For example, gadobutrol, a compound related to those described in the patent, is used as a contrast agent in MRI scans to improve the visibility of internal body structures[4].
Challenges and Criticisms
Patent Scope and Clarity
The patent landscape has seen debates over patent scope and clarity, particularly in the context of pharmaceutical and diagnostic patents. Critics argue that overly broad or unclear claims can hinder innovation by increasing licensing and litigation costs[3].
Regulatory Considerations
Regulatory bodies have to navigate complex patent claims to ensure that new products do not infringe existing patents. This is evident in the strict statutory provisions governing the approval of new drug applications (NDAs) and the need for precise claim construction to determine infringement[2].
Key Takeaways
- Compound Synthesis: The patent details the synthesis and purification of 1,4,7,10-tetraazacyclododecane butyltriols.
- Pharmaceutical Applications: These compounds are used in various pharmaceutical agents for diagnostic and therapeutic purposes.
- Diagnostic Imaging: The compounds are essential in NMR spectroscopy and PET.
- Patent Landscape: The patent is part of a broader landscape involving related patents and legal disputes.
- Regulatory Impact: The patent's claims have implications for regulatory approvals and infringement determinations.
FAQs
Q: What are the primary compounds described in US Patent 5,980,864?
A: The primary compounds are 1,4,7,10-tetraazacyclododecane butyltriols.
Q: What are the main applications of these compounds?
A: They are used as susceptibility reagents and shift reagents for in vivo NMR spectroscopy and as radiodiagnostic media, including in PET scans.
Q: How are these compounds synthesized?
A: They are synthesized through specific chemical reactions involving the reaction of 1,4,7,10-tetraazacyclododecane with butyltriols.
Q: What is the significance of this patent in medical diagnostics?
A: It has been crucial in the development of diagnostic imaging techniques, particularly in NMR spectroscopy and PET.
Q: Is the patent still in force?
A: No, the patent has expired.
Sources
- US5980864A - 1,4,7,10-tetraazacyclododecane butyltriols, processes for their production and pharmaceutical agents containing them - Google Patents
- Civil Action No. 20-755-RGA - District of Delaware
- Patent Claims and Patent Scope - Hoover Institution
- US20210284662A1 - Process for the preparation of 2,2',2''-(10-((2R,3S)-1,3,4-trihydroxybutan-2-yl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid and its complexes - Google Patents
- Federal Register, Volume 79 Issue 15 - Federal Register
