Detailed Analysis of the Scope and Claims of United States Patent 8,486,947
Introduction
United States Patent 8,486,947, titled "Treatment of Parkinson's disease, obstructive sleep apnea, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamines histamine H3-receptor ligands," is a significant patent in the field of neuropharmacology. This patent, assigned to Bioprojet, outlines novel therapeutic applications of specific chemical compounds for treating various neurological and sleep disorders.
Background and Context
The patent focuses on the therapeutic use of non-imidazole alkylamine derivatives as antagonists of the histamine H3-receptor. Histamine H3-receptors play a crucial role in regulating various physiological processes, including wakefulness, cognitive functions, food intake, and vestibular reflexes[1].
Scope of the Patent
Diseases and Conditions Treated
The patent covers the treatment of several conditions, including:
- Parkinson's Disease (PD): A neurodegenerative disorder characterized by motor symptoms such as tremors and rigidity.
- Obstructive Sleep Apnea (OSA): A sleep disorder marked by repeated interruptions in breathing during sleep.
- Dementia with Lewy Bodies (DLB): A neurodegenerative disorder characterized by cognitive decline and the presence of Lewy bodies in the brain.
- Vascular Dementia (VD): A condition resulting from reduced blood flow to the brain, often due to a series of small strokes[1].
Mechanism of Action
The compounds described in the patent act as antagonists of the histamine H3-receptor. This mechanism increases the synthesis and release of cerebral histamine, leading to extended wakefulness, improved cognitive processes, reduced food intake, and normalized vestibular reflexes[1].
Claims of the Patent
Chemical Compounds
The patent specifies a class of non-imidazole alkylamine derivatives with a general formula (I). These compounds are characterized by:
- General Formula: The compounds have a specific structural formula, with variations in the substituents and the length of the alkyl chain.
- Preferred Compounds: The patent highlights preferred groups of compounds, including those with an oxygen atom in the X position and those with a linear chain of 3 to 5 carbon atoms[1].
Substituents and Modifications
The patent details various substituents and modifications that can be made to the core structure, including:
- Substituted Phenyl Moiety: Compounds with an unsubstituted or substituted phenyl group.
- Polycyclic Radicals: Compounds containing benzothiazolyl, quinolinyl, or isoquinolinyl radicals.
- Nitrogen-Containing Rings: Compounds with piperidyl or pyrrolidinyl rings, which can be mono- or di-substituted with alkyl groups[1].
Patent Landscape
Patent Expiration Dates
The patent is set to expire on September 26, 2029. This expiration date is crucial for understanding the timeline for generic versions of the drug to enter the market[2].
Related Patents and Exclusivities
- Generic Availability: As of the current date, there is no generic version of Wakix, a drug related to this patent, available in the United States[2].
- Exclusivity Periods: The FDA has granted exclusivity periods for Wakix, including new chemical entity exclusivity and exclusivity for specific indications, which run concurrently with the patent but may extend beyond its expiration[2].
Litigation and Validity
There have been legal challenges to the validity of the claims in this patent. For instance, some litigation has questioned the compliance of the claims with patent requirements, although the patent remains active[5].
Impact on Pharmaceutical Industry
Innovation and Competition
The patent's scope and claims influence the development of new drugs and the competitive landscape in the pharmaceutical industry. The expiration of this patent could open up opportunities for generic drug manufacturers, potentially increasing market competition and reducing drug prices[2].
Clinical Utility and Market Acceptance
The clinical utility and market acceptance of drugs developed under this patent are critical factors. Companies like Bioprojet invest heavily in commercialization efforts and face risks related to market acceptance and potential off-label use penalties[4].
Key Takeaways
- Therapeutic Applications: The patent covers the treatment of Parkinson's disease, obstructive sleep apnea, dementia with Lewy bodies, and vascular dementia using non-imidazole alkylamine derivatives.
- Mechanism of Action: The compounds act as histamine H3-receptor antagonists, enhancing wakefulness and cognitive functions.
- Chemical Structure: The patent specifies a general formula and preferred compounds with specific substituents and modifications.
- Patent Expiration: The patent is set to expire on September 26, 2029.
- Impact on Industry: The patent influences innovation, competition, and the development of generic drugs in the pharmaceutical industry.
FAQs
What conditions are treated by the compounds described in US Patent 8,486,947?
The compounds described in the patent are used to treat Parkinson's disease, obstructive sleep apnea, dementia with Lewy bodies, and vascular dementia.
How do the compounds in this patent work?
The compounds act as antagonists of the histamine H3-receptor, increasing the synthesis and release of cerebral histamine, which leads to extended wakefulness, improved cognitive processes, and other therapeutic effects.
When is the patent set to expire?
The patent is set to expire on September 26, 2029.
Are there any generic versions of the drugs related to this patent available?
As of the current date, there are no generic versions of Wakix, a related drug, available in the United States.
What are the potential impacts of this patent on the pharmaceutical industry?
The patent influences innovation, competition, and the development of generic drugs. Its expiration could lead to increased market competition and potentially lower drug prices.
Cited Sources:
- US8486947B2 - Google Patents
- Generic Wakix Availability - Drugs.com
- Patent Claims and Patent Scope - SSRN
- FORM 10-K - Annual Reports
- in the united states district court - Insight.RPXcorp.com
