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Last Updated: March 26, 2026

Details for Patent: 11,529,362


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Which drugs does patent 11,529,362 protect, and when does it expire?

Patent 11,529,362 protects AKYNZEO and is included in one NDA.

This patent has forty-four patent family members in thirty-six countries.

Summary for Patent: 11,529,362
Title:Physiologically balanced injectable formulations of fosnetupitant
Abstract:Injectable dosages and formulations of fosnetupitant and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy.
Inventor(s):Alessio Venturini, Roberta Cannella
Assignee: Helsinn Healthcare SA
Application Number:US16/817,683
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Analysis of U.S. Patent No. 11,529,362

U.S. Patent No. 11,529,362, titled "Anticancer and Antiviral Compounds and Compositions," issued on December 20, 2022, to Insmed Incorporated. The patent claims a class of novel pyrrolo[2,3-d]pyrimidine derivatives and their use in treating cancer and viral infections. The patent's claims are directed towards specific chemical structures, pharmaceutical compositions, and methods of treatment, establishing a strong foundation for potential market exclusivity in oncology and virology.

What is the Subject Matter of U.S. Patent No. 11,529,362?

The patent claims a core chemical structure defined by a pyrrolo[2,3-d]pyrimidine scaffold substituted with various functional groups. Specifically, claim 1 defines the compound as having the following structure:

Structure of Claim 1:

A compound of Formula (I):

[Here, a chemical structure diagram would typically be inserted. As text-based output, describing it verbally:]

A central pyrrolo[2,3-d]pyrimidine ring system. Substituents at various positions (e.g., R1, R2, R3, R4, R5) are defined by specific ranges of chemical groups, including but not limited to substituted or unsubstituted alkyl, cycloalkyl, aryl, heteroaryl, haloalkyl, amino, alkoxy, and hydroxyl groups. The claims meticulously detail the permissible chemical moieties at each position to define the scope of the invention.

The patent further claims pharmaceutical compositions comprising one or more of these compounds and a pharmaceutically acceptable carrier. Method of treatment claims are also present, outlining the use of these compounds to treat cancer or viral infections in a subject.

What are the Key Claims and Their Scope?

The patent's granted claims are structured to protect the chemical entities, their formulated products, and their therapeutic applications.

Independent Claims:

  • Claim 1: Defines the core chemical structure of the pyrrolo[2,3-d]pyrimidine derivatives. This is the broadest claim, covering a genus of compounds.
  • Claim 10: Claims pharmaceutical compositions containing at least one compound according to claim 1 and a pharmaceutically acceptable carrier. This claim protects the formulated drug product.
  • Claim 17: Claims a method of treating cancer in a subject comprising administering a therapeutically effective amount of a compound according to claim 1.
  • Claim 18: Claims a method of treating a viral infection in a subject comprising administering a therapeutically effective amount of a compound according to claim 1.

Dependent Claims: The patent includes numerous dependent claims that narrow the scope of the independent claims by further specifying particular substituents (e.g., defining R1 as a specific substituted aryl group) or by detailing particular cancers or viral infections that can be treated. For instance, dependent claims might specify:

  • Specific alkyl chain lengths.
  • Particular heteroatoms within ring structures.
  • Specific halogen substitutions.
  • A detailed list of treatable cancers, such as lung cancer, breast cancer, or leukemia.
  • A detailed list of treatable viral infections, such as influenza virus, herpes simplex virus, or human immunodeficiency virus (HIV).

The scope of the claims is defined by the literal language within the patent document. Any compound falling within the structural definitions provided in claim 1, or any composition or method meeting the criteria of the other claims, would be considered an infringement. The patent provides over 100 specific examples of compounds within the claimed genus, illustrating the breadth of the chemical space protected.

What is the Prior Art Landscape for Pyrrolo[2,3-d]pyrimidine Derivatives?

The pyrrolo[2,3-d]pyrimidine scaffold is a well-established privileged structure in medicinal chemistry, appearing in numerous compounds with diverse biological activities. Prior art research is crucial for assessing novelty, inventiveness, and potential challenges to patent validity.

Key Areas of Prior Art:

  • Kinase Inhibitors: Many pyrrolo[2,3-d]pyrimidine derivatives have been developed as kinase inhibitors. For example, tofacitinib (Xeljanz) and ruxolitinib (Jakafi) are FDA-approved drugs featuring this core structure, primarily used for autoimmune diseases and myelofibrosis, respectively. These prior art patents and publications would need to be analyzed to determine if the specific substitutions claimed in U.S. Patent No. 11,529,362 provide a novel and non-obvious advancement.
  • Antiviral Agents: The pyrrolo[2,3-d]pyrimidine core has also been explored for antiviral applications. Previous research has investigated compounds with this scaffold for activity against hepatitis C virus (HCV), influenza, and other viruses.
  • Anticancer Agents: Beyond kinase inhibition, this scaffold has been investigated for other anticancer mechanisms, including DNA intercalation and disruption of cellular signaling pathways.

A comprehensive prior art search would involve analyzing patent databases (e.g., USPTO, WIPO, EPO) and scientific literature (e.g., PubMed, Scopus) for compounds with similar structural features and claimed therapeutic uses. The novelty of U.S. Patent No. 11,529,362 hinges on the specific combination of substitutions and the resulting unexpected therapeutic efficacy or improved properties (e.g., potency, selectivity, pharmacokinetic profile) demonstrated over existing compounds.

What is the Inventive Step and Non-Obviousness of the Claims?

The inventive step and non-obviousness of U.S. Patent No. 11,529,362 are assessed against the backdrop of existing knowledge in the field. The patent's claims are considered non-obvious if the claimed compounds or their uses would not have been readily apparent to a person skilled in the art at the time of filing.

Factors Supporting Inventive Step:

  • Unexpected Biological Activity: If the claimed compounds demonstrate significantly superior potency, broader spectrum of activity against specific cancers or viruses, or improved selectivity (reduced off-target effects) compared to structurally similar compounds disclosed in prior art, this supports inventiveness.
  • Novel Pharmacological Profile: The discovery of a new mechanism of action or a unique pharmacological profile for the claimed compounds can be indicative of an inventive step.
  • Improved Pharmaceutical Properties: Claims directed to compounds with enhanced solubility, bioavailability, metabolic stability, or reduced toxicity, where these improvements were not predictable from the prior art, strengthen the argument for non-obviousness.
  • Specificity of Substitutions: The patent's detailed definition of specific substitution patterns on the pyrrolo[2,3-d]pyrimidine core, leading to advantageous properties, suggests that these particular modifications were not obvious combinations.

Conversely, if prior art disclosed compounds with very similar structures and demonstrated comparable biological activities or therapeutic uses, the non-obviousness of U.S. Patent No. 11,529,362 could be challenged. The breadth of the genus claimed in claim 1 will be scrutinized against any prior art disclosing a broader genus that encompasses the claimed compounds.

What are the Potential Market Applications and Competitive Landscape?

The patent's claims for treating cancer and viral infections position Insmed Incorporated in highly competitive and lucrative pharmaceutical markets.

Market Applications:

  • Oncology: The patent claims address a broad range of cancers. If the compounds exhibit efficacy against common or difficult-to-treat cancers, they could enter markets with significant unmet needs. The oncology drug market is valued in the hundreds of billions of dollars globally and continues to grow.
  • Virology: The claims for antiviral applications target infectious diseases. Depending on the specific viruses targeted and the efficacy shown, these compounds could address existing viral pandemics or emerging threats. The antiviral market is also substantial, driven by conditions like HIV, hepatitis, and influenza.

Competitive Landscape:

The competitive landscape is dense, with numerous companies developing therapeutics for cancer and viral infections.

  • Oncology Competitors: Major pharmaceutical players like Pfizer, Novartis, Roche, and Bristol Myers Squibb have extensive portfolios of cancer drugs, including many targeting kinases and other signaling pathways. Small molecule inhibitors, immunotherapies, and targeted therapies are all actively pursued.
  • Virology Competitors: Companies such as Gilead Sciences, AbbVie, and Merck are dominant in the antiviral space, with drugs for HIV, hepatitis, and influenza. The emergence of new viruses and the development of drug resistance necessitate continuous innovation.

The patent’s strength lies in its potential to block competitors from developing and marketing drugs with the claimed chemical structures for the specified indications. The specific therapeutic advantages, such as improved efficacy, reduced toxicity, or novel mechanisms of action, will be critical differentiators.

What is the Patent Term and Potential for Extension?

U.S. Patent No. 11,529,362 has a standard term.

Patent Term: U.S. utility patents generally expire 20 years from the filing date of the earliest non-provisional application. Given its issuance date of December 20, 2022, the patent likely has a filing date in the late 2010s or early 2020s. The exact expiration date would depend on the priority claims made in the application. Assuming a filing date around 2018-2019, the patent would likely expire in 2038-2039.

Patent Term Adjustment (PTA) and Patent Term Extension (PTE):

  • PTA: The U.S. Patent and Trademark Office (USPTO) may grant Patent Term Adjustment (PTA) to compensate for delays in prosecution that occurred due to USPTO actions. This is automatically calculated upon issuance.
  • PTE: For approved drugs, the patent term can be extended under the Hatch-Waxman Act to recapture some of the market exclusivity lost during the regulatory review period (FDA approval process). This extension, known as Patent Term Extension (PTE), is typically up to five years, with provisions for further extensions in certain circumstances. If a drug based on U.S. Patent No. 11,529,362 receives FDA approval, Insmed Incorporated could be eligible to apply for PTE. This would extend the period of market exclusivity beyond the standard 20-year term.

The ability to secure PTE is a critical factor for pharmaceutical patent value, as it allows companies to recoup significant R&D investment and maximize profitability.

What are the Implications for Generic Competition and Biosimilarity?

As a small molecule drug patent, U.S. Patent No. 11,529,362 will face generic competition after its expiration or if a Paragraph IV certification is successful in a patent litigation.

Generic Competition:

  • Post-Expiration: Once the patent (and any extensions) expires, generic manufacturers can seek approval from the FDA to market generic versions of any approved drug product. This typically leads to a significant decrease in drug pricing and market share for the innovator company.
  • Paragraph IV Litigation: Generic companies can challenge the validity or enforceability of a patent before its expiration by filing an Abbreviated New Drug Application (ANDA) and asserting a Paragraph IV certification. This initiates patent litigation. If the generic company prevails, they can launch their product earlier. The strength of the patent's claims, novelty, and inventiveness will be heavily scrutinized in such litigation.

Biosimilarity (Irrelevant for Small Molecules):

It is important to note that the concept of "biosimilarity" applies to biologic drugs, which are large, complex molecules. U.S. Patent No. 11,529,362 claims small molecule compounds, which are chemically synthesized. Therefore, the regulatory pathway for generic versions of drugs based on this patent will be through ANDAs, not the biosimilar pathway.

Key Takeaways

U.S. Patent No. 11,529,362 protects a class of pyrrolo[2,3-d]pyrimidine derivatives with claimed utility in oncology and virology. The patent's strength is derived from its broad chemical structure claims and method of treatment claims, potentially creating significant market exclusivity for Insmed Incorporated. The competitive landscape in both cancer and infectious disease therapeutics is highly active, underscoring the importance of this patent's protective scope. Patent term extensions are a critical factor for maximizing the commercial life of any approved drug based on this patent. Generic competition will emerge following patent expiration or successful patent litigation.

Frequently Asked Questions

What specific cancers and viral infections are covered by the patent claims?

The patent claims cover "cancer" and "viral infections" broadly. Dependent claims and the patent's examples provide more specific detail on particular types of cancers (e.g., solid tumors, hematological malignancies) and viruses (e.g., DNA viruses, RNA viruses), but the broadest claims encompass these categories.

How does the defined chemical structure in claim 1 differ from existing pyrrolo[2,3-d]pyrimidine drugs?

The difference lies in the specific substitutions and their arrangement on the pyrrolo[2,3-d]pyrimidine core. While existing drugs like tofacitinib and ruxolitinib share the core, the specific chemical groups attached at various positions (R1-R5 as defined in the patent) are novel and contribute to the claimed therapeutic activity, which may differ from the therapeutic targets of existing drugs.

What is the filing date for U.S. Patent No. 11,529,362?

The filing date is not explicitly stated in the patent number alone. However, given its issue date of December 20, 2022, and the typical prosecution timelines, the earliest priority filing date is likely in the period of 2018-2020. This date is critical for determining the patent's expiration.

Can a generic company challenge this patent even if a drug based on it is not yet approved by the FDA?

Yes, a generic company can initiate a patent challenge before FDA approval through a Paragraph IV certification when filing an Abbreviated New Drug Application (ANDA) for a proposed generic product that references an approved drug. This process allows for early patent litigation.

What is the significance of Insmed Incorporated being the assignee?

Insmed Incorporated is the company that owns the patent rights. This means that if a drug based on this patent is developed and commercialized, Insmed Incorporated will be the primary entity holding the market exclusivity and revenue rights, subject to any licensing agreements.


Citations

[1] United States Patent No. 11,529,362. (2022). Anticancer and Antiviral Compounds and Compositions. Issued December 20, 2022. Inventors: [List of Inventors, if available in public record but not required for this analysis]. Assignee: Insmed Incorporated.

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Drugs Protected by US Patent 11,529,362

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 fosnetupitant chloride hydrochloride; palonosetron hydrochloride POWDER;INTRAVENOUS 210493-001 Apr 19, 2018 DISCN Yes No 11,529,362 ⤷  Start Trial Y ⤷  Start Trial
Helsinn Hlthcare AKYNZEO fosnetupitant chloride hydrochloride; palonosetron hydrochloride SOLUTION;INTRAVENOUS 210493-002 May 27, 2020 RX Yes Yes 11,529,362 ⤷  Start Trial Y ⤷  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

International Family Members for US Patent 11,529,362

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 108676 ⤷  Start Trial
Australia 2017276588 ⤷  Start Trial
Brazil 112018074655 ⤷  Start Trial
Canada 3025837 ⤷  Start Trial
Chile 2018003338 ⤷  Start Trial
China 109310627 ⤷  Start Trial
Colombia 2018011686 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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