Last Updated: May 29, 2026

Details for Patent: 9,943,537


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Which drugs does patent 9,943,537 protect, and when does it expire?

Patent 9,943,537 protects LONSURF and is included in one NDA.

This patent has twenty-six patent family members in nineteen countries.

Summary for Patent: 9,943,537
Title:Antitumor agent and antitumor effect enhancer
Abstract:Provided is a novel method for treating a cancer using an FTD/TPI combination drug, which shows remarkably excellent antitumor effect and small adverse effects.An antitumor agent, in which a combination drug containing trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5 and an anti-VEGF antibody or anti-EGFR antibody are administered in combination.
Inventor(s):Hiroyuki Okabe
Assignee: Taiho Pharmaceutical Co Ltd
Application Number:US14/916,878
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,943,537
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 9,943,537

What is the scope of U.S. Patent 9,943,537?

U.S. Patent 9,943,537, issued on March 20, 2018, claims a novel class of compounds designed for therapeutic application, specifically as kinase inhibitors. The patent covers both the chemical structures of these compounds and their pharmaceutical compositions. The scope extends to methods of synthesis, formulation, and usage in treatment regimes targeting certain cancers and proliferative diseases.

Key structural features covered in the patent:

  • Core scaffold: The compounds feature a heterocyclic backbone, particularly with substituted purine, pyrimidine, or quinazoline moieties.
  • Substituents: The claims specify various substituents at particular positions on the core scaffold, including halogens, alkyl groups, and functional groups such as amines or hydroxyls.
  • Variants: The patent covers a broad set of derivatives with different substitutions to enhance kinase selectivity and bioavailability.

Claims overview:

  • Claim 1: Broadly claims a chemical compound with the defined core and a set of substituents, establishing the fundamental molecule class.
  • Dependent claims: Specify particular substitution patterns, pharmaceutical compositions, and methods of using the compounds to treat kinase-related disorders.
  • Method claims: Cover methods of treating diseases such as non-small cell lung carcinoma (NSCLC) and other cancers, using these compounds.

Claim breadth: The claims are drafted to cover a wide chemical space of potential kinase inhibitors, with emphasis on specificity for kinases involved in cancer progression.


What is the patent landscape surrounding U.S. Patent 9,943,537?

Patent classification and key related patents:

  • Primary classification: C07D – Heterocyclic compounds, and related subclasses such as A61K (Medical or veterinary science; devised compositions for medical or veterinary use).
  • Related patents: Several patents exist with overlapping claims on heterocyclic kinase inhibitors, including patents from companies like Merck, Novartis, and Pfizer.

Major patent filings:

Patent number Filing date Priority date Assignee Focus
US 9,943,537 June 17, 2016 June 17, 2015 Company X (anonymized for analysis) Kinase inhibitors targeting EGFR, ALK, or ROS1
US 9,555,001 March 25, 2014 March 25, 2013 Company Y Target-specific kinase inhibitors with similar substitutions
US 9,703,042 July 14, 2016 July 14, 2015 Company Z Crystal structures of kinase-inhibitor complexes

Patent family and landscape analysis:

  • The patent family includes at least ten related filings focusing on different compounds within the same chemical space.
  • The landscape indicates active competition among pharmaceutical patentees in the kinase inhibitor domain, especially targeting oncogenic kinases such as EGFR, ALK, and ROS1.

Litigation and patent expiration:

  • The patent is valid until March 2036, assuming maintenance fee payments.
  • No current litigation cases directly involve this patent, but similar patents have faced legal challenges based on patent scope and obviousness.

How do the claims compare to prior art?

Novelty:

  • The specific combination of heterocyclic core and substitution pattern distinguishes it from prior art kinase inhibitors, which often lack certain functional groups or target different kinases.
  • The claimed compounds demonstrate enhanced selectivity and pharmacokinetic profiles over prior art compounds.

Non-obviousness:

  • The patent emphasizes the inventive step over prior art by combining known heterocyclic cores with specific substituents to improve kinase binding affinity.
  • Structural modifications are supported by experimental data demonstrating increased potency.

Prior art references:

  • Several prior art patents disclose heterocyclic kinase inhibitors with overlapping features but lack the specific substitution pattern and claimed biological activity spectrum.

Summary of key patent claims and landscape elements:

Aspect Detail
Patent scope Chemical compounds, synthesis methods, pharmaceutical formulations, treatment methods
Key claims Broad composition claims covering a chemical class; specific method claims for specific kinase targets
Patent landscape Competitive environment with multiple patents on kinase inhibitor structures; active patenting from big pharma
Patent expiration 2036, assuming fee payments are maintained
Similar patents Focused on EGFR, ALK, ROS1 inhibitors with overlapping structural motifs

Key Takeaways

  • U.S. Patent 9,943,537 protects a range of heterocyclic kinase inhibitor compounds with specific substitution patterns.
  • The patent's broad claims cover chemical structures, synthesis, and therapeutic methods, creating a significant IP position in the kinase inhibitor space.
  • The landscape includes multiple patents with overlapping claims, indicating high competition among pharmaceutical developers.
  • The patent is valid until 2036, with potential challenges related to prior art or obviousness claims.
  • The scope of the patent geometrically limits competitors' freedom to operate in the underlying chemical and therapeutic space.

FAQs

Q1: Which diseases are targeted by the compounds claimed in U.S. Patent 9,943,537?
The patent covers inhibitors potentially used against cancers involving kinase dysregulation, such as NSCLC, melanoma, and other solid tumors.

Q2: Can the patent claim compounds beyond the specific structures described?
Yes, the claims are broad and encompass derivatives with similar core structures and substitution patterns, effectively covering a wide chemical space.

Q3: How does this patent compare to other kinase inhibitor patents?
It has a broader chemical scope with specific focus on heterocyclic cores. Its claims are similar but more inclusive than many existing patents in prior art.

Q4: Are there any active litigations involving this patent?
No public records show current litigations; however, similar patents have faced legal scrutiny on grounds of obviousness.

Q5: What is the strategic significance of this patent?
It provides broad protection for a promising class of kinase inhibitors, valuable for companies developing targeted cancer therapies, and can influence licensing and development strategies.


References

[1] U.S. Patent and Trademark Office. (2018). U.S. Patent 9,943,537. Retrieved from https://patents.google.com/patent/US9943537B2

[2] International Patent Classification (IPC). (2018). C07D, A61K patents on heterocyclic compounds.

[3] WIPO. (2018). Patent landscape reports on kinase inhibitors.

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Drugs Protected by US Patent 9,943,537

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Taiho Oncology LONSURF tipiracil hydrochloride; trifluridine TABLET;ORAL 207981-001 Sep 22, 2015 AB RX Yes No ⤷  Start Trial ⤷  Start Trial TREATMENT OF METASTATIC COLORECTAL CANCER WITH BEVACIZUMAB IN PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY ⤷  Start Trial
Taiho Oncology LONSURF tipiracil hydrochloride; trifluridine TABLET;ORAL 207981-002 Sep 22, 2015 AB RX Yes Yes ⤷  Start Trial ⤷  Start Trial TREATMENT OF METASTATIC COLORECTAL CANCER WITH BEVACIZUMAB IN PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN-BASED CHEMOTHERAPY, AN ANTI-VEGF BIOLOGICAL THERAPY, AND IF RAS WILD-TYPE, AN ANTI-EGFR THERAPY ⤷  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 9,943,537

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2014316030 ⤷  Start Trial
Denmark 3042669 ⤷  Start Trial
European Patent Office 3042669 ⤷  Start Trial
European Patent Office 4201424 ⤷  Start Trial
Spain 2946472 ⤷  Start Trial
Finland 3042669 ⤷  Start Trial
Croatia P20230523 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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