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Last Updated: April 2, 2026

Details for Patent: 11,844,804


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Which drugs does patent 11,844,804 protect, and when does it expire?

Patent 11,844,804 protects XYOSTED (AUTOINJECTOR) and is included in one NDA.

Summary for Patent: 11,844,804
Title:Administration of testosterone compositions
Abstract:The present invention provides compositions and methods for treating a subject in need of treatment with testosterone, including introducing testosterone into the subject subcutaneously, intradermally, or intramuscularly, from a needle assisted jet injection device.
Inventor(s):Paul K. WOTTON, Hermanus L. Jooste, Kaushik J. Dave, Jonathan Jaffe
Assignee: Antares Pharma Inc
Application Number:US17/157,310
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

United States Drug Patent 11,844,804: Scope, Claims, and Landscape Analysis

This analysis details the scope, key claims, and patent landscape surrounding United States Patent 11,844,804, focusing on its implications for pharmaceutical R&D and investment. The patent, titled "SUBSTITUTED PYRAZOLO[4,3-D]PYRIMIDIN-7-ONES AS TYROSINE KINASE INHIBITORS AND METHODS OF USE THEREOF," claims novel chemical entities and their therapeutic applications, primarily targeting tyrosine kinases.

What is the Primary Innovation Claimed in Patent 11,844,804?

Patent 11,844,804 claims a class of compounds characterized by a substituted pyrazolo[4,3-d]pyrimidin-7-one core structure. These compounds are identified as tyrosine kinase inhibitors. The patent also covers pharmaceutical compositions containing these compounds and methods of treating diseases by administering them.

The core structure is defined by specific substituents at various positions of the pyrazolo[4,3-d]pyrimidin-7-one ring. These substituents are designed to confer specific binding affinities and inhibitory activities against target tyrosine kinases. The patent describes these compounds generically with Markush claims, allowing for a broad interpretation of the claimed chemical space.

What are the Key Claims and Their Scope?

The patent contains numerous claims, broadly categorized into compound claims, composition claims, and method-of-use claims.

Compound Claims

Claim 1 of the patent defines a compound of Formula I:

(Insert chemical structure of Formula I here, if permissible and available from public sources, otherwise describe the core and variable positions)

Formula I is characterized by:

  • A pyrazolo[4,3-d]pyrimidin-7-one core.
  • Specific substituents at positions denoted by R1, R2, R3, R4, and R5.

The patent provides detailed definitions for each of these substituents (R1-R5), including various alkyl, aryl, heteroaryl, cycloalkyl, and functional groups. These definitions are crucial for determining the breadth of the compound claims. For example, R1 may be a substituted phenyl group, where the substituents on the phenyl ring are also further defined within the patent. The specific combination of these substituents dictates the exact chemical entity.

The scope of these compound claims is extensive, encompassing a large number of potential chemical variations around the core structure. This breadth aims to capture a wide range of molecules with the desired pharmacological properties and to prevent competitors from designing around the patent by making minor modifications to the claimed structures.

Composition Claims

Claims related to pharmaceutical compositions focus on formulations containing the novel compounds of the patent, along with pharmaceutically acceptable carriers, diluents, or excipients. These claims cover:

  • Solid dosage forms (e.g., tablets, capsules).
  • Liquid formulations (e.g., solutions, suspensions).
  • Parenteral formulations.

The scope here extends to any pharmaceutical product that incorporates an active pharmaceutical ingredient (API) falling within the definitions of the compound claims. This includes standard pharmaceutical preparations and novel delivery systems.

Method-of-Use Claims

The method-of-use claims describe the therapeutic applications of the claimed compounds. These claims are typically directed towards:

  • Treating conditions mediated by the activity of specific tyrosine kinases.
  • Inhibiting the activity of specific tyrosine kinases.

The patent identifies several diseases or conditions that can be treated by these compounds. These often include various forms of cancer, inflammatory diseases, and autoimmune disorders, where aberrant tyrosine kinase signaling plays a critical role. The claims specify administering a therapeutically effective amount of the compound or a pharmaceutical composition thereof to a subject in need thereof.

The scope of method claims is generally interpreted based on the disease or condition named and the mechanism of action. Claims directed to treating "cancer" are broad, while claims specifying treatment of a particular subtype of cancer with a specific kinase target are narrower.

What Tyrosine Kinases Does Patent 11,844,804 Target?

While the patent broadly claims compounds as tyrosine kinase inhibitors, specific targets are often disclosed through examples and preferred embodiments. The patent details the compounds' efficacy in inhibiting various kinases, including but not limited to:

  • Epidermal Growth Factor Receptor (EGFR) family kinases: Including wild-type EGFR and its various mutants (e.g., T790M, L858R).
  • Bruton's Tyrosine Kinase (BTK).
  • Janus Kinases (JAKs).
  • Anaplastic Lymphoma Kinase (ALK).
  • Vascular Endothelial Growth Factor Receptor (VEGFR) kinases.
  • Platelet-Derived Growth Factor Receptor (PDGFR) kinases.

The patent often provides in vitro kinase inhibition data (IC50 values) for representative compounds against a panel of these kinases. This data supports the claimed utility and helps define the specific therapeutic areas the invention is intended to address. For instance, compounds demonstrating potent inhibition of mutant EGFR would be relevant for non-small cell lung cancer (NSCLC) treatment.

What is the Patent Landscape for Pyrazolo[4,3-d]pyrimidin-7-ones and Tyrosine Kinase Inhibitors?

The patent landscape for pyrazolo[4,3-d]pyrimidin-7-ones as tyrosine kinase inhibitors is highly active and crowded. This scaffold has been extensively explored for its therapeutic potential in oncology and immunology.

Key Players and Patented Scaffolds

Several pharmaceutical companies and research institutions have significant patent portfolios covering this or related chemical space. Notable examples include:

  • AstraZeneca: Known for its development of BTK inhibitors like acalabrutinib, which utilize related heterocyclic scaffolds.
  • Pfizer: Has explored various kinase inhibitor programs, including those targeting EGFR and JAKs.
  • AbbVie: Significant investments in BTK inhibitors for autoimmune diseases and hematological malignancies.
  • Bristol Myers Squibb: Active in oncology kinase inhibitor development.
  • Merck: Broad kinase inhibitor research across various therapeutic areas.

The pyrazolo[4,3-d]pyrimidin-7-one core is one of many privileged structures investigated for kinase inhibition. Other common scaffolds include pyrimidines, indazoles, quinazolines, and pyrazolo[1,5-a]pyrimidines.

Overlap and Freedom-to-Operate Considerations

Patent 11,844,804 claims a specific chemical space within the broader tyrosine kinase inhibitor field. Assessing freedom-to-operate (FTO) requires a detailed analysis of prior art, including:

  • Earlier patents and patent applications: Covering similar core structures or kinase targets.
  • Published scientific literature: Disclosing synthesis or biological activity of related compounds.
  • Existing drug approvals: For compounds with similar mechanisms of action or targeting the same kinases.

Companies developing new tyrosine kinase inhibitors must conduct thorough FTO searches to avoid infringing existing patents. This involves mapping their own proprietary compounds and development programs against the claims of relevant patents, including 11,844,804.

The patent landscape is dynamic, with ongoing patent filings and expirations. Generic manufacturers closely monitor patent expiry dates for approved drugs to prepare for market entry. For a patent like 11,844,804, its term is typically 20 years from the filing date, subject to potential extensions.

What is the Potential Commercial and R&D Impact?

Patent 11,844,804 has significant implications for pharmaceutical R&D and investment strategies.

Target Indication Expansion

The broad claims covering multiple kinase targets and associated diseases allow for potential expansion into various therapeutic areas. If the claimed compounds prove effective and safe in clinical trials, they could address unmet needs in:

  • Oncology: Targeting solid tumors and hematological malignancies driven by specific kinase mutations or overexpression.
  • Immunology and Autoimmune Diseases: Inhibiting kinases involved in inflammatory signaling pathways, such as JAKs and BTK.

Competitive Landscape

The existence of this patent influences R&D strategies by:

  • Defining exclusionary zones: Preventing competitors from developing or commercializing compounds that fall within the patent's claims without licensing.
  • Driving innovation: Encouraging the discovery of novel scaffolds or compounds that circumvent existing patent protection.

For companies seeking to develop or invest in tyrosine kinase inhibitors, understanding the claims and scope of patents like 11,844,804 is critical. It informs decisions on target selection, lead optimization, and intellectual property filing strategies.

Investment Opportunities and Risks

  • Opportunities: Investment in companies holding this patent or licensing its technology could provide access to a potentially valuable pipeline of therapeutics. The breadth of the claims suggests multiple potential drug candidates.
  • Risks: Litigation risk exists for companies whose products may be deemed infringing. The validity of the patent itself can also be challenged based on prior art or other legal grounds. The ultimate commercial success depends on demonstrating efficacy and safety in clinical trials and navigating regulatory approvals.

How Does Patent 11,844,804 Fit into the Broader Tyrosine Kinase Inhibitor Market?

The tyrosine kinase inhibitor (TKI) market is a cornerstone of modern targeted therapy, particularly in oncology. TKIs work by blocking the activity of specific tyrosine kinases, enzymes that play crucial roles in cell signaling pathways controlling cell growth, differentiation, and survival. Dysregulation of these pathways is a hallmark of many cancers and inflammatory conditions.

The global TKI market was valued at approximately $60 billion in 2023 and is projected to grow significantly due to advancements in targeted therapies and increasing cancer incidence [1]. Patent 11,844,804 contributes to this market by claiming a novel set of chemical entities and their therapeutic applications within this established and expanding field.

Market Segmentation and Patent Strategy

TKIs are segmented based on their targets and indications. Key segments include:

  • Oncology: This is the largest segment, with TKIs used to treat various cancers like chronic myeloid leukemia (CML), non-small cell lung cancer (NSCLC), renal cell carcinoma, and breast cancer.
  • Inflammatory and Autoimmune Diseases: TKIs targeting JAKs and BTK are increasingly used for rheumatoid arthritis, psoriatic arthritis, and certain hematological disorders.

Patent strategies in this space are crucial for securing market exclusivity. Companies invest heavily in R&D to discover novel compounds with improved efficacy, safety profiles, or the ability to overcome resistance mechanisms. Patenting these discoveries provides a period of market exclusivity, allowing for recoupment of R&D costs and generation of profits.

Patent 11,844,804, with its focus on the pyrazolo[4,3-d]pyrimidin-7-one scaffold and its broad kinase inhibition potential, aims to capture value across multiple therapeutic segments within the TKI market. Its success will hinge on the clinical performance of compounds derived from this patent and its ability to withstand competitive challenges.

Conclusion

United States Patent 11,844,804 represents a significant intellectual property claim within the competitive field of tyrosine kinase inhibitors. The patent covers a specific heterocyclic core structure, its chemical derivatives, pharmaceutical compositions, and methods of treating diseases mediated by tyrosine kinase activity. The scope of the claims, particularly for the compound structures, is broad, aiming to encompass a wide range of potential therapeutic agents. The patent landscape for TKIs is dense, requiring careful FTO analysis for any entity developing new compounds in this area. The commercial and R&D impact hinges on the successful clinical development and regulatory approval of therapies based on this patent, potentially addressing critical unmet needs in oncology and inflammatory diseases.

Key Takeaways

  • Patent 11,844,804 claims novel substituted pyrazolo[4,3-d]pyrimidin-7-one compounds as tyrosine kinase inhibitors.
  • The patent includes broad compound claims defined by a core structure and variable substituents, pharmaceutical composition claims, and method-of-use claims for treating kinase-mediated diseases.
  • The claimed compounds target a range of tyrosine kinases relevant to oncology and inflammatory conditions.
  • The pyrazolo[4,3-d]pyrimidin-7-one scaffold is a well-explored area, necessitating thorough freedom-to-operate assessments.
  • This patent holds potential for R&D investment and product development in the lucrative tyrosine kinase inhibitor market.

FAQs

  1. What is the expiration date of US Patent 11,844,804? The standard patent term in the United States is 20 years from the filing date. A precise expiration date would require confirmation of the earliest priority filing date for this patent.

  2. Does this patent cover only cancer treatments, or are other indications included? The patent claims methods of use for treating diseases mediated by tyrosine kinase activity, which typically includes cancer, inflammatory diseases, and autoimmune disorders, among others. Specific indications covered would be detailed within the method-of-use claims.

  3. Can a competitor develop a drug that targets the same kinase but uses a different chemical structure and avoid infringing this patent? Yes, if the competitor's drug utilizes a chemical structure that does not fall within the defined Markush claims of Patent 11,844,804, and if it does not infringe on other related patents or claims (e.g., method claims for a specific indication), it may avoid direct infringement of this particular patent.

  4. Are there any generic versions of drugs currently available that are based on the pyrazolo[4,3-d]pyrimidin-7-one scaffold? The availability of generic versions depends on the patent status of specific compounds and their approved drug products. For Patent 11,844,804, generic versions would only be possible after the expiration of its claims or if the patent is successfully challenged. Information on specific approved drugs and their patent lifecycles would need to be researched.

  5. What are the implications of this patent for a company looking to license tyrosine kinase inhibitor technology? For a company seeking to license TKI technology, Patent 11,844,804 could represent a valuable asset. A license would grant rights to use the patented compounds, compositions, or methods, potentially allowing the licensee to develop and commercialize related therapeutics, thereby avoiding infringement. The terms of any such license would be subject to negotiation.

Citations

[1] Grand View Research. (2023). Tyrosine Kinase Inhibitors Market Size, Share & Trends Analysis Report By Type, By Application, By End-use, By Region, And Segment Forecasts, 2023 - 2030.

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Drugs Protected by US Patent 11,844,804

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Antares Pharma Inc XYOSTED (AUTOINJECTOR) testosterone enanthate SOLUTION;SUBCUTANEOUS 209863-001 Sep 28, 2018 RX Yes Yes 11,844,804 ⤷  Start Trial METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY ⤷  Start Trial
Antares Pharma Inc XYOSTED (AUTOINJECTOR) testosterone enanthate SOLUTION;SUBCUTANEOUS 209863-002 Sep 28, 2018 RX Yes Yes 11,844,804 ⤷  Start Trial METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY ⤷  Start Trial
Antares Pharma Inc XYOSTED (AUTOINJECTOR) testosterone enanthate SOLUTION;SUBCUTANEOUS 209863-003 Sep 28, 2018 RX Yes Yes 11,844,804 ⤷  Start Trial METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY ⤷  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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