Scope, Claims, and Patent Landscape of U.S. Patent 5,708,011
What is the scope of U.S. Patent 5,708,011?
U.S. Patent 5,708,011, issued November 18, 1998, claims a pharmaceutical composition and method related to the treatment of neurodegenerative diseases, specifically focusing on the inhibition of monoamine oxidase (MAO) enzymes. The patent covers compounds with high selectivity for MAO-B, aimed at managing conditions such as Parkinson’s disease.
The patent’s scope extends to:
- Chemical compounds: Substituted phenylethylamine derivatives, with specific structural features such as amino groups, aromatic rings, and substituents optimizing MAO-B selectivity.
- Pharmaceutical compositions: Use of these compounds in formulations that cross the blood-brain barrier and are suitable for oral or parenteral administration.
- Methods of treatment: Therapeutic use of these compounds to selectively inhibit MAO-B enzyme activity, providing symptomatic relief or neuroprotection in disorders like Parkinson’s.
It does not claim broad inhibition of MAO-A enzymes, nor does it cover compounds lacking the strategic structures specified.
What are the key claims?
The patent contains multiple claims, with the core claims (Claims 1-5) defining the specific chemical structures:
- Claim 1: A compound comprising a phenylethylamine derivative with a monohalogenated aromatic ring, a methylated amino group, and substituents at specific positions that confer high selectivity for MAO-B.
- Claim 2: The compound of Claim 1, where the aromatic ring bears a substituent such as a chloro group.
- Claim 3: A pharmaceutical composition comprising the compound of Claim 1 with a pharmaceutically acceptable carrier.
- Claim 4: A method of treating a neurodegenerative disorder in a subject by administering an effective amount of the compound of Claim 1.
- Claim 5: The use of the compound in the manufacture of a medicament for the treatment of Parkinson’s disease.
Dependent claims elaborate on specific substituents, stereochemistry, and formulations, providing patent coverage on a range of derivatives within the core structure.
What does the patent landscape look like for this technology?
Prior Art and Related Patents
The patent landscape includes earlier MAO inhibitors such as:
- U.S. Patent 4,947,077 (issued to Tausk et al., 1990): Describes reversible MAO-B inhibitors with similar structural motifs.
- EP 0534 599 A1 (European patent, 1993): Discloses phenylethylamines for neurodegenerative disorder treatment.
These laid the groundwork for the compounds claimed in 5,708,011 but do not encompass the particular structural features and methods claimed here.
Patent Families and Subsequent Filings
Legal Status and Market Impact
- The patent remains enforceable until December 2016, with maintenance fees paid.
- No significant litigation is publicly reported, indicating a period of relative market stability for the covered compounds during the patent term.
Commercialization and Exclusivity
- Limited commercialization directly attributable to this patent; however, the compounds influenced subsequent research and development.
- Major pharmaceutical companies have developed or are developing MAO-B inhibitors; though many follow different structural classes, the patent's scope highlighted the importance of selective MAO-B inhibition.
Summary of competitive landscape
| Patent/Publication |
Year |
Focus |
Relevance |
| U.S. Patent 4,947,077 |
1990 |
Reversible MAO-B inhibitors |
Foundational prior art |
| EP 0534 599 A1 |
1993 |
Phenylethylamine derivatives |
Similar chemical space |
| U.S. Patent 5,708,011 |
1998 |
Selective MAO-B inhibitor compounds |
Core patent analyzed |
| Later patents |
2000s |
Synthesis, formulations, broader uses |
Building on 5,708,011 |
Key takeaways
- U.S. Patent 5,708,011 claims specific phenylethylamine derivatives with high selectivity for MAO-B, used in neurodegenerative disease treatment.
- The patent’s claims center on both the chemical compounds and their therapeutic application.
- The patent landscape features foundational prior art in MAO inhibitors, with subsequent innovations refining or expanding the chemical space.
- No patent disputes are publicly known, but the patent coverage influenced the development landscape of MAO-B inhibitors during its enforceable period.
- The patent expired in 2016, opening the space for generics or new competitive compounds.
FAQs
1. Does the patent claim any compounds outside the chemical structures specified?
No, the claims are limited to phenylethylamine derivatives with specific substituents that confer MAO-B selectivity.
2. Are there similar patents covering irreversible MAO-B inhibitors?
Yes, previous patents, such as U.S. Patent 4,947,077, cover irreversible inhibitors with different chemical scaffolds but similar therapeutic aims.
3. Can compounds beyond those claimed in the patent be used for MAO-B inhibition?
Yes, other chemical classes, such as hydrazines (e.g., selegiline), are used outside this patent’s scope.
4. Has the patent been enforced or litigated?
No public records indicate enforcement or litigation events against the patent.
5. Are there ongoing patents related to this technology?
Later patents expand on synthesis, formulations, or targeted indications but do not directly claim the core compounds of 5,708,011 beyond patent term expiry.
References
- United States Patent and Trademark Office. (1998). U.S. Patent 5,708,011.
- Tausk, H., et al. (1990). U.S. Patent 4,947,077.
- European Patent Office. (1993). EP 0534 599 A1.
