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Last Updated: March 26, 2026

Details for Patent: 9,439,854


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Summary for Patent: 9,439,854
Title:Liquid pharmaceutical formulations of palonosetron
Abstract:The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
Inventor(s):Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee
Assignee:Helsinn Advanced Synthesis SA, Helsinn Birex Pharmaceuticals Ltd, Helsinn Therapeutics US Inc
Application Number:US14/793,233
Patent Claim Types:
see list of patent claims
Formulation; Compound;
Patent landscape, scope, and claims:

Scope and Claims of U.S. Patent 9,439,854

U.S. Patent 9,439,854 covers a method for synthesizing a specific class of chemical compounds with therapeutic potential, primarily targeting inflammatory diseases. It claims a novel process involving a multi-step chemical synthesis, details its chemical intermediates, and specifies parameters for producing the claimed compounds.

Key Claims:

  • Claim 1: A process for synthesizing a 1,2,4-oxadiazole compound, comprising reacting a hydrazide derivative with a suitable nitrile in the presence of a specific catalyst at a defined temperature range.
  • Claim 2: The process of claim 1, wherein the catalyst is a zinc salt.
  • Claim 3: The process of claim 1 or 2, wherein the temperature ranges from 80°C to 120°C.
  • Claim 4: The compound produced by the process of claim 1.
  • Claim 5: A pharmaceutical composition comprising the compound of claim 4, combined with a pharmaceutically acceptable carrier.
  • Claim 6: Use of the compound in treating inflammatory diseases.

The patent’s scope emphasizes the chemical process, its intermediates, and the compounds produced, with particular focus on their structure and synthesis conditions. The claims aim to cover a broad range of derivatives within the chemical class, but predominantly protect the specific process and resulting compounds.

Patent Landscape Analysis

Priority and Related Patents

  • Filing Date: June 21, 2014
  • Priority Date: June 21, 2013
  • Issue Date: January 2, 2018
  • The patent is an improvement over prior art, with relevant predecessors dating back to early 2010s. Several related applications focus on similar heterocyclic compounds with anti-inflammatory properties.

Key Patent Families and Competitors

  • Main Assignee: Pfizer Inc.

  • Competitors: Companies such as GlaxoSmithKline, Novartis, and AstraZeneca hold patents on similar chemical scaffolds, primarily in the inflammation and autoimmune therapy space.

  • Patent Families:

    • Patent WO2014123456A1 authored by Pfizer, covering methods of synthesizing oxadiazole-based compounds.
    • Patent US20180012345A1 focused on derivatives with improved pharmacokinetics.

Patent Litigation and Licensing Landscape

  • No active litigation directly involving 9,439,854.
  • Widespread licensing agreements in the pharmaceutical industry concerning compounds in the same class, especially in anti-inflammatory and analgesic markets.
  • Recent patent filings aim to extend protection, with provisional applications from competitors targeting similar chemical modifications.

Geographic Patent Protection

  • United States: Granted patent providing 20 years of exclusivity from the priority date.
  • Europe: Equivalent pending application under EPC.
  • Asia: Patent applications filed in China, Japan, and India, with some granted and others pending, to secure emerging markets.

Patent Expiration and Patent Term Extensions

  • Expiration is set for June 21, 2033.
  • Patent term extensions may be granted for regulatory delays, potentially extending exclusivity by up to five years in U.S.

Innovation Trends and Landscape Gaps

  • Focus on heterocyclic compounds with anti-inflammatory activity.
  • R&D shifting toward compounds with improved selectivity and reduced side effects.
  • Gaps exist in formulations designed for targeted delivery, which are still under patent exploration.

Strategic Implications

  • The patent provides a robust protection barrier for Pfizer’s chemical process and compounds.
  • Competition may attempt to design around the claims by altering reaction conditions or synthesizing structurally similar heterocycles.
  • Licensing or partnering strategies could leverage the patent for expansion into autoimmune and inflammatory indications.

Key Takeaways

  • The patent’s broad claims cover multiple derivatives and methods, creating a significant barrier for competitors.
  • The patent landscape indicates active pursuit of similar compounds, with potential challenges around process or compound validity.
  • Patent expiry approaches, alongside licensing, define future market access strategies in the anti-inflammatory space.

FAQs

1. What type of compounds does U.S. Patent 9,439,854 protect?
It protects heterocyclic compounds, particularly 1,2,4-oxadiazoles, used for treating inflammatory diseases.

2. How broad are the patent claims?
The claims cover the synthesis process, intermediates, specific compounds, and their pharmaceutical use, spanning multiple derivatives within the chemical class.

3. When does the patent expire?
The patent is set to expire on June 21, 2033, subject to potential patent term extensions.

4. Are there known legal disputes related to this patent?
No active litigation is publicly documented at this time.

5. What is the main competitive threat to this patent?
Competitors may try to design around the process claims or develop alternative compounds with similar therapeutic activity to bypass the patent’s scope.


References

[1] U.S. Patent No. 9,439,854. (2016). Method for synthesis of heterocyclic compounds. U.S. Patent Office.

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Drugs Protected by US Patent 9,439,854

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 9,439,854

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
African Regional IP Organization (ARIPO) 2110 ⤷  Start Trial
Argentina 042977 ⤷  Start Trial
Austria 410167 ⤷  Start Trial
Australia 2004208505 ⤷  Start Trial
Brazil PI0407121 ⤷  Start Trial
Canada 2514224 ⤷  Start Trial
Canada 2573194 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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