United States Patent 4,526,892: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,526,892, titled "Dimethylaminoalkyl-3-(ergoline-8'βcarbonyl)-ureas," is a significant patent in the field of pharmaceuticals, particularly focusing on ergoline derivatives. This patent, granted on July 2, 1985, outlines novel compounds with potential therapeutic applications.
Background and Context
The patent was filed on December 9, 1982, and is a continuation of an earlier application filed on March 3, 1981. The invention pertains to the field of organic chemistry and pharmaceuticals, specifically targeting the development of ergoline derivatives with hypotensive and antiprolactinic activities[1].
Scope of the Patent
General Formula and Structure
The patent describes ergoline derivatives with a general formula that includes various substituents. The formula involves an 8-carboxy ergoline reacted with a carbodiimide to form ureas. The substituents include:
- ( R_1 ): Hydrogen or methyl group
- ( R_2 ): Hydrogen, halogen (preferably chlorine or bromine), methyl, formyl, or specific alkyl or phenyl groups
- ( R_3 ): Hydrogen or methoxy group
- ( R_4 ): Hydrocarbon group with 1 to 4 carbon atoms, benzyl, or phenethyl
- ( R_5 ) and ( R_6 ): Alkyl groups with 1 to 4 carbon atoms, cyclohexyl, or substituted/unsubstituted phenyl groups, with specific constraints[1].
Therapeutic Applications
The compounds described in the patent have potential therapeutic uses, particularly in treating conditions related to hypertension and hyperprolactinemia. The antiprolactinic activity makes these compounds relevant for managing disorders associated with prolactin imbalance.
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover the specific chemical structures of the ergoline derivatives, the process for preparing these compounds, and pharmaceutical compositions containing these compounds.
Dependent Claims
Dependent claims further specify the substituents and conditions under which the compounds are prepared and used. These claims provide detailed descriptions of the preferred embodiments of the invention, including the types of alkyl groups, halogens, and other substituents[1].
Preparation Process
The patent outlines a process for preparing the ergoline derivatives, which involves reacting an acid of a specific formula with a carbodiimide. This reaction is crucial for forming the urea linkage that characterizes these compounds. The process details the conditions and reagents necessary for the synthesis[1].
Pharmaceutical Compositions
The patent also describes pharmaceutical compositions that contain therapeutically effective amounts of the ergoline derivatives. These compositions can be formulated in various ways, such as tablets, capsules, or injectable solutions, to facilitate administration and efficacy[2].
Patent Landscape
Related Applications and Family
The patent is part of a family of applications that include both U.S. and international filings. The U.S. application (US06/448,364) is linked to a Bulgarian application (BG098515A), indicating a global strategy for patent protection[1].
Global Dossier and International Harmonization
The patent is part of the Global Dossier system, which provides access to the file histories of related applications from participating IP offices. This system facilitates the management and analysis of patent families across different jurisdictions[4].
Public Search and Resource Centers
The U.S. Patent and Trademark Office (USPTO) provides various resources, including the Public Search Facility and Patent and Trademark Resource Centers (PTRCs), which assist in searching and analyzing patent information. These resources are crucial for understanding the broader patent landscape and identifying prior art[4].
Patent Term and Extension
The patent term for U.S. Patent 4,526,892 has expired, as it was granted in 1985 and the standard patent term is 20 years from the filing date. However, there was a determination for a patent term extension related to the human drug product DOSTINEX® (cabergoline), which is a different compound but may be relevant in the context of related pharmaceuticals[5].
Impact and Relevance
Therapeutic Impact
The ergoline derivatives described in this patent have significant therapeutic potential, particularly in managing conditions related to hypertension and hyperprolactinemia. These compounds represent a class of drugs that can be tailored to specific medical needs.
Industry and Research
The patent's focus on novel chemical structures and synthesis processes contributes to the advancement of pharmaceutical research. It sets a precedent for further innovation in the field of ergoline derivatives and related therapeutic agents.
Key Takeaways
- Novel Compounds: The patent introduces new ergoline derivatives with hypotensive and antiprolactinic activities.
- Therapeutic Applications: These compounds have potential uses in treating hypertension and hyperprolactinemia.
- Synthesis Process: The patent details a specific process for preparing these compounds using carbodiimides.
- Pharmaceutical Compositions: The patent covers various formulations for administering these compounds.
- Patent Landscape: The patent is part of a global strategy for patent protection and is linked to international filings.
- Public Resources: The USPTO provides resources for searching and analyzing patent information related to this patent.
FAQs
What are the primary therapeutic applications of the compounds described in U.S. Patent 4,526,892?
The primary therapeutic applications are in treating conditions related to hypertension and hyperprolactinemia.
How are the ergoline derivatives prepared according to the patent?
The preparation involves reacting an acid with a carbodiimide to form the urea linkage.
What is the significance of the Global Dossier system in relation to this patent?
The Global Dossier system provides access to the file histories of related applications from participating IP offices, facilitating global patent management.
Has the patent term for U.S. Patent 4,526,892 expired?
Yes, the patent term has expired as it was granted in 1985 and the standard patent term is 20 years from the filing date.
Are there any related patents or applications associated with this patent?
Yes, the patent is part of a family of applications that include both U.S. and international filings.
Sources
- US4526892A - Dimethylaminoalkyl-3-(ergoline-8'βcarbonyl)-ureas - Google Patents
- United States Patent (19) - googleapis.com
- Patent Claims and Patent Scope - SSRN
- Search for patents - USPTO
- Patent Term Extension - USPTO
