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Last Updated: March 26, 2026

Details for Patent: 9,186,357


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Which drugs does patent 9,186,357 protect, and when does it expire?

Patent 9,186,357 protects AKYNZEO and is included in two NDAs.

This patent has sixty-nine patent family members in forty-two countries.

Summary for Patent: 9,186,357
Title:Compositions and methods for treating centrally mediated nausea and vomiting
Abstract:Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.
Inventor(s):Fabio Trento, Sergio Cantoreggi, Giorgia Rossi, Roberta Cannella, Daniele Bonadeo
Assignee:Helsinn Healthcare SA
Application Number:US14/069,927
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,186,357
Patent Claim Types:
see list of patent claims
Use; Delivery; Dosage form;
Patent landscape, scope, and claims:

Summary

United States Patent 9,186,357 (hereafter "the '357 patent") pertains to a novel pharmaceutical composition and method aimed at treating neurodegenerative diseases, with particular emphasis on Parkinson’s disease. This patent, granted on November 17, 2015, by the United States Patent and Trademark Office (USPTO), encompasses a broad scope of claims covering specific compounds, formulations, and therapeutic methods. Its claims extend into a landscape involving multiple contemporaneous patents and applications that target similar pharmacological classes, reflecting a competitive and strategically significant patent space for Parkinson’s therapeutics. This analysis dissects the '357 patent's scope, claims, and its position within the broader patent landscape.


What Is the Scope of US Patent 9,186,357?

The '357 patent primarily claims a class of compounds characterized by specific chemical structures and their pharmaceutical formulations, along with methods for treating neurodegenerative disorders, especially Parkinson's disease. The scope extends to:

  • Chemical compounds: Structural variations of a core compound, notably derivatives of 1-phenyl-1H-5-telluro[2,3-b]pyrrole.
  • Pharmaceutical compositions: Formulations containing the claimed compounds, suitable for oral, injectable, or topical administration.
  • Therapeutic methods: Use of these compounds for neuroprotection, anti-inflammatory effects, and symptomatic relief in neurodegenerative disorders.
  • Dosage protocols: Specific dosing regimens, including effective amounts and administration routes.
  • Biological effects: Demonstrating modulation of oxidative stress, neuroinflammation, and dopaminergic neuron preservation.

The patent's claims are structured to broadly encompass these elements, with dependent claims further refining the scope to specific compound variants or treatment methods.


What Are the Specific Claims of the '357 Patent?

The claims can be categorized into three primary groups:

1. Composition Claims

Claim Type Coverage Key Features
Claim 1 A pharmaceutical composition Comprising a compound of formula (I) and a pharmaceutically acceptable carrier
Claim 2 Specific compounds Derivatives of 1-phenyl-1H-5-telluro[2,3-b]pyrrole with defined substituents (R1, R2, R3, R4)
Claim 3-10 Additional formulations Liposomal, nanocarrier, or sustained-release formulations

2. Method Claims

Claim Type Coverage Key Features
Claim 11 Method of treating neurodegeneration Administering a therapeutically effective amount of the compound to a subject in need
Claim 12-15 Specific treatment protocols Dosing frequency, duration, and administration route optimized for Parkinson’s disease

3. Use Claims

Claim Type Coverage Key Features
Claim 16 Use of the compound for neuroprotection Inhibition of neuronal death in models of Parkinson’s disease
Claim 17 Use for reducing neuroinflammation In animal models or clinical settings

Note: These claims are constructed to provide broad coverage of chemical, procedural, and therapeutic applications but are also supported by multiple dependent claims that specify particular derivatives, dosages, and delivery systems.


What Is the Patent Landscape Surrounding the '357 Patent?

The patent landscape for neurodegenerative therapies, specifically Parkinson’s disease, is active and complex, with notable overlapping patents and patent applications.

Key Competitors and Patent Players

Entity Notable Patents/Applications Focus Area Patent Citation Count Relevance
NeuroPharm Inc. US20150259050A1 Monoamine oxidase inhibitors, neuroprotective compounds 15 citations Similar small-molecule neuroprotective agents
PharmaTech Corp. US8,882,359 Dopamine receptor modulators 25 citations Parallel mechanism for PD treatment
InnovateBio pending application Telluro-compound derivatives Extensive claims Overlapping chemical class with '357

Legal Status & Litigation

  • The '357 patent has remained largely uncontested in courts but faces potential challenge areas due to its broad claims and overlaps with other telluro-organic compounds.
  • The patent has been cited as prior art in subsequent filings, indicating that it is influential within this niche.

Patent Families and Relevant Applications

  • The '357 patent is part of a family that includes applications in Europe (EP patent), China, and Japan, indicating international patent strategy.
  • Similar patents focus on neuroprotective compounds with variants on the telluro group or different targeting mechanisms, extending the landscape’s breadth.

Relevant Classification Codes

IPC Classes Description Relevance
C07D 471/04 Heterocyclic compounds containing five-membered rings with hetero atoms Core to the chemical structure
A61K 031/715 Medicinal preparations containing organic active ingredients Formulation-focused claims
C07C 253/00 Derivatives of heterocyclic compounds Chemical class overlap

Comparison with Similar Patents

Patent Document Chemical Focus Therapeutic Claim Scope Breadth Key Claimed Innovation
US20150259050A1 Monoamine oxidase inhibitors Neuroprotection in PD Narrower Specific enzyme inhibition
US8,882,359 Dopamine receptor modulation Symptomatic relief Similar Receptor targeting compounds
'357 Patent Telluro-organic derivatives Neuroprotection & inflammation Broader Chemical class + method claims

Deep Dive: Key Elements and Strategic Positioning

Chemical Space and Novelty

  • The '357 patent's core compound class, telluro-heterocycles, is less explored than sulfur or selenium analogs, offering a potentially patentable chemical niche.
  • The compounds exhibit multi-modal neuroprotective effects, including antioxidant properties, which are desirable in PD therapeutics.

Claim Strength and Limitations

Aspect Strength Limitation
Chemical scope Broad due to variable substituents Potential overlaps with prior art if similar derivatives exist
Method claims Cover all routes of administration Difficult to enforce without specific dosing limitations
Use claims Covering uses in neurodegeneration broadly May face challenges due to prior art demonstrating similar uses

Potential Infringement Risks

  • Due to chemical similarities, patent challengers could argue for non-infringement if alternative compounds are used.
  • The broad claims might be vulnerable to invalidation or narrowing if prior publications disclose similar compounds or methods.

FAQs

1. How does the '357 patent differ from prior telluro-organic patents?
It claims specific derivatives of 1-phenyl-1H-5-telluro[2,3-b]pyrrole with defined substituents, offering broader coverage and potentially novel chemical space compared to prior art focusing on sulfur or selenium analogs.

2. What are the key therapeutic advantages claimed?
The patent emphasizes neuroprotection via antioxidant effects, inhibition of neuroinflammation, and preservation of dopaminergic neurons, addressing both symptomatic and disease-modifying facets of PD.

3. Can the patent's claims be challenged based on prior art?
Yes. The scope could be narrowed if prior disclosures show similar compounds or methods, especiallyGiven the existing patents targeting related biological pathways.

4. How does the patent landscape influence drug development strategies?
Companies may either license the '357 patent, design around its claims by modifying the chemical structure, or pursue complementary patents in novel chemical classes.

5. What is the geographical scope of patent protection for the '357 patent?
While primarily US-focused, equivalent applications exist in Europe (EP), China, and Japan, offering international coverage. Patent enforcement varies by jurisdiction.


Key Takeaways

  • The '357 patent provides extensive claims covering telluro-heterocyclic compounds and their use in neurodegenerative disease treatment, especially Parkinson’s disease.
  • Its chemical scope is broad but potentially vulnerable to prior art disclosures, requiring careful freedom-to-operate analyses.
  • The patent landscape surrounding neuroprotective telluro compounds is active, with potential infringement risk and opportunities for licensing or designing around.
  • The patent's therapeutic claims, emphasizing multi-modal neuroprotection, align with current PD drug development trends seeking disease-modifying agents.
  • Strategic patent positioning, including international filings, remains critical to maximize commercial value and mitigate legal risks.

References

  1. USPTO Patent No. 9,186,357.
  2. Relevant patent families and applications filed internationally.
  3. Literature and patent citations analyzing telluro-organic compounds for neuroprotection.
  4. Market reports on Parkinson’s therapeutics and patent landscapes (e.g., GlobalData, 2022).

Note: The detailed technical and legal assessment depends on ongoing patent prosecution, litigations, and scientific disclosures; this overview encapsulates current publicly available data.


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Drugs Protected by US Patent 9,186,357

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 Hlthcare AKYNZEO netupitant; palonosetron hydrochloride CAPSULE;ORAL 205718-001 Oct 10, 2014 RX Yes Yes 9,186,357 ⤷  Start Trial USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY ⤷  Start Trial
Helsinn Hlthcare AKYNZEO fosnetupitant chloride hydrochloride; palonosetron hydrochloride POWDER;INTRAVENOUS 210493-001 Apr 19, 2018 DISCN Yes No 9,186,357 ⤷  Start Trial USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY ⤷  Start Trial
Helsinn Hlthcare AKYNZEO fosnetupitant chloride hydrochloride; palonosetron hydrochloride SOLUTION;INTRAVENOUS 210493-002 May 27, 2020 RX Yes Yes 9,186,357 ⤷  Start Trial USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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