Detailed Analysis of the Scope and Claims of United States Patent 4,824,860
Introduction
United States Patent 4,824,860, titled "1,3-Dihydro-2H-indol-2-one compounds and their use in treating Parkinson's disease," is a significant patent in the field of neuropharmacology. This patent, granted to various inventors and assigned to pharmaceutical companies, outlines the synthesis, pharmacological properties, and therapeutic applications of specific indolone compounds.
Background
The patent builds on earlier research and patents related to dopamine receptor agonists, particularly those targeting the D2/D3 receptors. These compounds have been explored for their potential in treating neurological disorders such as Parkinson's disease and fibromyalgia[1][4][5].
Scope of the Patent
Chemical Compounds
The patent focuses on a class of compounds known as 1,3-dihydro-2H-indol-2-ones. Specifically, it describes the synthesis and pharmacological properties of compounds like 4-[2-(dipropylamino)-ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole[5].
Synthesis
The patent details two primary methods for synthesizing these indolone compounds. These methods involve starting from either 4-aminoalkyl-7-hydroxy-2(3H)-indolones or 2-methyl-3-nitro-benzene acetic acid. The processes are described in multiple steps, highlighting the chemical intermediates and conditions necessary for the synthesis[5].
Claims
Therapeutic Use
The primary claim of the patent is the use of these indolone compounds as therapeutic agents for treating Parkinson's disease. The patent asserts that these compounds, particularly Ropinirole, are effective dopamine D2/D3 receptor agonists with minimal liability to cause dyskinesia, a common side effect associated with other dopamine agonists[1][4].
Pharmacological Properties
The patent highlights the pharmacological advantages of these compounds, including their ability to produce minimal central behavioral effects compared to other dopamine agonists. This makes them safer and more tolerable for patients[1].
Formulations
The patent also covers various formulations of these compounds, including their pharmacologically acceptable salts and acid addition salts. These formulations can be administered alone or in combination with a pharmaceutically acceptable carrier[4].
Patent Landscape
Related Patents
This patent is part of a broader landscape of patents related to dopamine receptor agonists. Other patents, such as CA2414774C and US6277875B1, also describe the use of similar compounds for treating conditions like fibromyalgia and Parkinson's disease[1][4].
Inventors and Assignees
The patent was granted to inventors who have contributed significantly to the field of neuropharmacology. The assignees include pharmaceutical companies that have further developed and commercialized these compounds, such as SmithKline Beecham (now part of GlaxoSmithKline)[4].
Expiration and Current Status
The patent has expired, as is typical for patents that were granted several decades ago. The expiration allows other companies to manufacture and market generic versions of the drug, increasing accessibility and reducing costs for patients.
Impact on Treatment
Parkinson's Disease
The compounds described in this patent, particularly Ropinirole, have become standard treatments for Parkinson's disease. They offer an alternative to older ergot-derived dopamine agonists, which can have more severe side effects[1][4].
Fibromyalgia
While the primary focus is on Parkinson's disease, similar compounds have also been explored for treating fibromyalgia, highlighting the broader therapeutic potential of these indolone compounds[4].
Conclusion
United States Patent 4,824,860 has played a crucial role in the development of treatments for Parkinson's disease and other neurological disorders. The patent's detailed descriptions of synthesis methods, pharmacological properties, and therapeutic applications have contributed significantly to the field of neuropharmacology.
Key Takeaways
- Compounds: The patent focuses on 1,3-dihydro-2H-indol-2-one compounds, particularly Ropinirole.
- Synthesis: Describes two methods for synthesizing these compounds.
- Therapeutic Use: Primarily for treating Parkinson's disease.
- Pharmacological Properties: Minimal central behavioral effects and low risk of dyskinesia.
- Formulations: Includes various pharmacologically acceptable salts and carriers.
- Patent Landscape: Part of a broader landscape of patents on dopamine receptor agonists.
- Impact: Significant in treating Parkinson's disease and potentially other neurological disorders.
Frequently Asked Questions (FAQs)
What is the primary compound described in US Patent 4,824,860?
The primary compound is 4-[2-(dipropylamino)-ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole.
What is the therapeutic use of the compounds described in this patent?
The compounds are primarily used for treating Parkinson's disease.
What are the pharmacological advantages of these compounds?
They produce minimal central behavioral effects and have a low risk of causing dyskinesia compared to other dopamine agonists.
How are these compounds synthesized?
The patent describes two methods for synthesizing these compounds, starting from either 4-aminoalkyl-7-hydroxy-2(3H)-indolones or 2-methyl-3-nitro-benzene acetic acid.
Is the patent still in effect?
No, the patent has expired, allowing for the manufacture and marketing of generic versions of the drug.
Cited Sources
- CA2414774C - Use of dopamine d2/d3 receptor ... - Google Patents
- Patent 2498735 Summary - Canadian Patents Database
- Patent Claims and Patent Scope - Search eLibrary :: SSRN
- US6277875B1 - USE OF DOPAMINE D/D, RECEPTOR AGONSTS TO TREAT FIBROMYALGIA - Google Patents
- US20050159605A1 - Process for the preparation of 4-(2-dipropylaminoethyl)-1,3-dihydro-2H-indol-2-one hydrochloride - Google Patents
