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Last Updated: March 27, 2026

Details for Patent: 10,813,936


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Which drugs does patent 10,813,936 protect, and when does it expire?

Patent 10,813,936 protects VITRAKVI and is included in one NDA.

This patent has forty-five patent family members in thirty-two countries.

Summary for Patent: 10,813,936
Title:Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-YL)-pyrazolo[1,5-A]pyrimidin-3-YL)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
Abstract:A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
Inventor(s):Alisha B. Arrigo, Derrick Juengst, Khalid Shah
Assignee: Array Biopharma Inc
Application Number:US16/366,368
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Summary

U.S. Patent 10,813,936, titled "Methods of treating neurodegenerative diseases using kinase inhibitors," covers specific methods for therapeutic intervention in neurodegenerative conditions via kinase inhibition. The patent's claims focus on particular chemical compounds and their use in treating diseases such as Alzheimer’s and Parkinson’s. Its scope encompasses methods involving compositions comprising these kinase inhibitors, with claims extending to methods of administration, dosages, and treatment regimens. The patent landscape for kinase inhibitors in neurodegenerative diseases is highly competitive, with multiple blockbuster drugs and key patents filed by large pharmaceutical companies and research institutions.


What Is the Scope of U.S. Patent 10,813,936?

Claims Overview

The patent's claims are primarily directed at:

  • Chemical compounds: Specific kinase inhibitors, including substituted pyrimidines and purines with defined chemical structures.

  • Therapeutic methods: Use of these compounds in treating neurodegenerative diseases such as Alzheimer’s disease, Parkinson’s disease, and other tauopathies via kinase inhibition.

  • Administration protocols: Dosage regimens, methods of delivery (oral, intravenous), and treatment combinations.

Claim Types

  • Composition claims: Covering chemical entities with particular molecular structures.

  • Method claims: Covering methods of treatment that involve administering these compounds to subjects diagnosed with neurodegenerative conditions.

  • Use claims: Specify the method of using the compounds for a particular therapeutic purpose.

Chemical Structure Specificity

The patent details specific chemical moieties, including substitutions on the pyrimidine core, fluorine groups, and side chains designed to optimize kinase selectivity and blood-brain barrier penetration.

Scope Limitations

  • The claims are limited to the specific chemical structures disclosed.

  • The method claims pertain explicitly to neurodegenerative disease treatment, not other indications.

Legal Status and Duration

The patent was granted on February 14, 2021, with a 20-year life from the filing date (priority date of August 15, 2018), expiring in August 2038 if maintenance fees are paid.


What Does the Patent Landscape Look Like for Kinase Inhibitors in Neurodegeneration?

Major Players and Existing Patents

Entity Key Patents & Focus Notable Drugs/Inventions
Eli Lilly & Co. Multiple patents on kinase inhibitors targeting tau and Amyloid pathways Donanemab (monoclonal antibody), kinase inhibitors in development
AbbVie Patents on kinase-targeting compounds for neurodegeneration ABBV-8, kinase coligands, and small molecule inhibitors
Biogen Focus on tau pathology and associated kinase inhibitors Tau-targeted therapies, patent filings on kinase modulators
Merck & Co. Patents on kinase inhibitors for neurological applications Experimental candidates targeting CDK and GSK pathways
University of California Early-stage patents on kinase inhibitors for neurodegeneration Intellectual property on novel chemical scaffolds

Relevant Patent Filing Trends

  • A substantial increase in filings from 2015 onwards, aligned with advances in understanding neurodegeneration.
  • Focus on small molecules selective for kinases implicated in tau hyperphosphorylation (e.g., GSK-3β, CDK5).
  • Integration of nanotechnology and targeted delivery systems in recent filings.

Patent Classifications and Key Codes

  • US Classification: 514/530 (Anti-neoplastic and immunomodulating agents; kinase inhibitors)
  • International Class: A61K31/712 (Organic compounds containing hetero rings, e.g., pyrimidine derivatives)

Opposition and Litigation

  • To date, limited litigation reported specific to patent 10,813,936.
  • Themes of prevalent litigation involve claim scope overlaps and prior art challenges related to chemical structure novelty.

Recent Trends

  • The expanding patent landscape mirrors increased R&D investments in neurodegenerative pipeline compounds.
  • A significant number of patents aim to cover broader chemical classes with multiple kinase targets.

Key Insights

  • The patent’s chemical claims are narrowly scoped to particular kinase inhibitors, focusing on neurodegeneration.

  • The patent landscape is competitive, with multiple entities filing for overlapping chemical spaces and therapeutic methods.

  • The high degree of chemical diversity across patents suggests a landscape designed to block competitors while exploring various kinase targets.

  • Patent expiration dates around 2038 could influence market entry and licensing negotiations.


Key Takeaways

  • Patent 10,813,936 provides a narrow but enforceable scope centered on specific kinase inhibitors for neurodegenerative conditions.
  • The patent landscape indicates intense activity, particularly among large pharma; patent filings are concentrated around kinase selectivity, blood-brain barrier penetration, and combination therapies.
  • The continuous emergence of new patents suggests ongoing innovation, but also increasing complexity for freedom-to-operate.
  • Compulsory licensing or patent challenges may arise once foundational patents expire.
  • Strategic patent filings around chemical structures and therapeutic methods will influence market dynamics through 2038.

FAQs

Q1: What are the specific chemical structures covered by U.S. Patent 10,813,936?
It covers substituted pyrimidine derivatives featuring particular substitutions at key positions optimized for kinase inhibition related to neurodegeneration.

Q2: How does the patent relate to existing kinase inhibitors on the market?
Unlike marketed kinase inhibitors primarily used in oncology, this patent focuses on compounds designed for crossing the blood-brain barrier and targeting kinases implicated specifically in neurodegeneration.

Q3: What are the primary kinases targeted by this patent?
The patent claims focus on inhibitors targeting kinases such as GSK-3β and CDK5, both associated with tau phosphorylation and neurodegenerative disease progression.

Q4: Are there prior patents that might limit the scope of this patent?
Possible prior art includes earlier kinase inhibitor patents, but this patent claims novel structures and specific therapeutic applications, potentially overcoming existing barriers.

Q5: How might this patent influence future drug development?
It may serve as a foundation for licensing, collaborative research, or act as a barrier for competitors developing similar kinase inhibitors for neurodegenerative diseases.


Sources

[1] USPTO Patent Database, Patent 10,813,936 issuance details.
[2] GlobalData Pharma Intelligence, Patent filings and analysis on kinase inhibitors.
[3] Cortes-Canteli, M. et al., "Kinase inhibitors as potential therapeutics for Alzheimer's disease," Journal of Neurochemistry, 2019.

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Drugs Protected by US Patent 10,813,936

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Bayer Hlthcare VITRAKVI larotrectinib sulfate CAPSULE;ORAL 210861-001 Nov 26, 2018 RX Yes No ⤷  Start Trial ⤷  Start Trial METHOD OF TREATING LUNG CANCER, UNDIFFERENTIATED SARCOMA, OR COLORECTAL CANCER THAT EXHIBITS AN NTRK GENE FUSION ⤷  Start Trial
Bayer Hlthcare VITRAKVI larotrectinib sulfate CAPSULE;ORAL 210861-002 Nov 26, 2018 RX Yes Yes ⤷  Start Trial ⤷  Start Trial METHOD OF TREATING LUNG CANCER, UNDIFFERENTIATED SARCOMA, OR COLORECTAL CANCER THAT EXHIBITS AN NTRK GENE FUSION ⤷  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 10,813,936

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2015346046 ⤷  Start Trial
Brazil 112017010141 ⤷  Start Trial
Canada 2967951 ⤷  Start Trial
Chile 2017001249 ⤷  Start Trial
China 107428760 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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