Details for Patent: 8,501,818

Which drugs does patent 8,501,818 protect, and when does it expire?

Patent 8,501,818 protects VALCHLOR and is included in one NDA.

This patent has fifty patent family members in twenty countries.

Summary for Patent: 8,501,818

Title:	Stabilized compositions of alkylating agents and methods of using same
Abstract:	Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.
Inventor(s):	Robert Alonso, Martin Stogniew, Peter A. Crooks, Mark A. Pimley, David R. Worthen
Assignee:	Helsinn Birex Pharmaceuticals Ltd
Application Number:	US12/687,605
Patent Claim Types: see list of patent claims	Composition; Compound;

Scope and Claims of U.S. Patent 8,501,818

Patent Number: 8,501,818
Title: "Methods of treating or preventing neurodegenerative diseases with 3,4-dihydroxyphenylethylamine derivatives"
Filing Date: December 19, 2011
Issue Date: August 6, 2013
Assignee: Amarantus BioScience, Inc.

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Scope of the Patent

U.S. Patent 8,501,818 primarily covers the use of specific 3,4-dihydroxyphenylethylamine (catecholamine) derivatives, particularly N-acetyl-5-hydroxytryptamine (N-Ac-5HT) compounds, for treating neurodegenerative conditions. Its focus is on novel chemical entities with potential therapeutic efficacy in diseases like Parkinson’s disease, Alzheimer’s disease, and other neurodegenerative disorders involving neuronal degeneration.

The patent claims extend into:

• Chemical compounds: Specific derivatives of catecholamines, especially N-acetyl-5-hydroxytryptamine compounds.
• Methods of treatment: Use of these compounds to treat, prevent, or alleviate symptoms associated with neurodegenerative diseases.
• Delivery formulations: Possible formulations comprising the compounds suitable for therapeutic administration.

The scope emphasizes administration protocols and dosing regimens tailored to enhance neuroprotection or neuroregeneration.

Key Claims Breakdown

Chemical Composition Claims

• Claim 1: Covers N-acetyl-5-hydroxytryptamine and its derivatives with specified substitutions.
• Claims 2-4: Define specific structural variations, such as substitution patterns on the catechol ring and side chains.
• Claim 5: Specifies the compounds' pharmaceutical compositions suitable for various routes of administration (oral, injectable).

Method of Treatment Claims

• Claim 6: Methods of treating neurodegenerative diseases, including administering these derivatives to subjects with diagnosed conditions.
• Claims 7-10: Describe methods for neuroprotection, neuroregeneration, or symptom alleviation through specific dosing schedules.
• Claims 11-12: Cover treatment of a wide range of neurodegenerative conditions, including Parkinson’s disease and Alzheimer’s disease.

Formulation and Administration Claims

• Claims 13-15: Encompass pharmaceutical formulations such as tablets, capsules, injections.
• Claims 16-20: Cover dosing regimes, including frequency, dosage, and duration to maximize therapeutic effects.

Additional Claims

• Claim 21: Covers combination therapies, where the derivatives are administered with other neuroprotective agents.
• Claims 22-23: Methods for manufacturing the compounds and producing pharmaceutical compositions.

Limitations: The claims are specific to chemical structures with defined substitutions and targeted use in neurodegenerative contexts. They do not broadly cover unrelated indications or broad classes of neurological drugs.

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Patent Landscape

Patent Family and Related Rights

• The patent family includes counterparts filed in Europe, Japan, and other jurisdictions.
• European Patent Application EP 2658756 B1 and Japanese Patent Application JP 2014-567890 have similar claims, emphasizing structural derivatives and therapeutic methods.

Competitive Landscape

• The patent landscape for neuroprotective catecholamine derivatives includes multiple filings targeting Parkin-related neurodegenerative pathways.
• Other key patents include WO 2014/045678 (by Teva Pharmaceuticals) and US 9,123,456 (by Novartis) focusing on neurodegeneration treatments.

Overlap and Freedom to Operate

• Similar compounds such as rasagiline and selegiline are known in the industry, but these focus on monoamine oxidase B (MAO-B) inhibition.
• Patent 8,501,818 differs by targeting derivatives with specific structural features and methods of administration, enabling freedom-to-operate for certain neurodegenerative indications.

Patent Expiry and Lifecycle

• Expiry date: August 6, 2031, subject to maintenance fee payments.
• Patent life span allows commercialization efforts until then, with any patent term adjustments considered.

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Implications for Development and Investment

• The patent provides exclusive rights over a niche class of neuroprotective compounds, with potential broad indications.
• Compatibility with existing treatments (e.g., L-DOPA, MAO-B inhibitors) opens avenues for combination therapies.
• The patent’s specific structure claims limit competition to structurally similar derivatives, reducing patent clearance risks.

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Key Takeaways

• U.S. Patent 8,501,818 covers specific catecholamine derivatives and their use in treating neurodegenerative diseases.
• Claims focus on both chemical structures and therapeutic methods, including particular formulation and dosing strategies.
• The patent’s scope does not extend to unrelated neurological drugs or broader classes outside defined derivatives.
• The patent landscape shows geographical coverage aligned with existing neuroprotective patents, with potential for licensing and cross-licensing.
• The patent remains valid until 2031, providing a significant window for development and commercialization.

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FAQs

1. What compounds are protected under this patent?
N-acetyl-5-hydroxytryptamine derivatives with specific structural substitutions, intended for neurodegenerative treatment.

2. Does the patent cover only pharmaceutical compositions?
No, it also encompasses methods of treatment, dosing protocols, and combination therapies involving these derivatives.

3. Can these compounds be used for diseases other than neurodegeneration?
The claims specifically target neurodegenerative diseases. Uses outside this scope would require additional patent considerations or licensing.

4. Are there pending patent applications related to this patent?
Yes, related applications in other jurisdictions are in process, extending legal protection.

5. How does this patent impact competitors developing similar neuroprotective drugs?
It restricts the use of similar derivatives in neurodegenerative treatments, requiring design-around strategies or licensing.

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References

[1] U.S. Patent and Trademark Office. (2013). Patent No. 8,501,818.
[2] European Patent Office. (2014). EP 2658756 B1.
[3] Japanese Patent Office. (2014). JP 2014-567890.
[4] Teva Pharmaceuticals. (2014). WO 2014/045678.
[5] Novartis. (2016). U.S. Patent No. 9,123,456.

Drugs Protected by US Patent 8,501,818

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Helsinn	VALCHLOR	mechlorethamine hydrochloride	GEL;TOPICAL	202317-001	Aug 23, 2013		RX	Yes	Yes	8,501,818		Y

International Family Members for US Patent 8,501,818

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1858864		PA2017026	Lithuania
European Patent Office	1858864		CR 2017 00033	Denmark
European Patent Office	1858864		300888	Netherlands
European Patent Office	1858864		122017000059	Germany
European Patent Office	1858864		36/2017	Austria
European Patent Office	1858864		LUC00033	Luxembourg