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Last Updated: January 8, 2025

Details for Patent: 9,539,258


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Which drugs does patent 9,539,258 protect, and when does it expire?

Patent 9,539,258 protects GILOTRIF and is included in one NDA.

Protection for GILOTRIF has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has ten patent family members in four countries.

Summary for Patent: 9,539,258
Title:Quinazoline derivatives for the treatment of cancer diseases
Abstract: The present invention relates to the use of quinazolines of formula (I), ##STR00001## wherein the groups R.sup.a to R.sup.d have the meanings given in the claims and specification, in cancer therapy.
Inventor(s): Solca; Flavio (Vienna, AT), Amelsberg; Andree (Southbury, CT), van Meel; Jacobus C. A. (Moedling, AT), Baum; Anke (Moedling, AT), Stehle; Gerd (Ehingen, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:14/739,299
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,539,258
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Quinazoline Derivatives for the Treatment of Cancer Diseases: A Detailed Analysis of US Patent 9,539,258

Introduction

The United States Patent 9,539,258, issued on January 10, 2017, is a significant patent in the field of oncology, particularly focusing on the use of quinazoline derivatives for the treatment of various cancer diseases. This patent, assigned to Boehringer Ingelheim International GmbH, outlines the therapeutic applications and chemical formulations of these quinazoline compounds.

Patent Overview

Inventors and Assignees

The patent was invented by Flavio Solca, Andree Amelsberg, Jacobus C. A. van Meel, Anke Baum, and Gerd Stehle, and is assigned to Boehringer Ingelheim International GmbH[5].

Patent Claims

The patent claims revolve around the use of quinazolines of a specific formula (I) for the treatment of cancer. These claims are detailed and specify the structural elements of the quinazoline derivatives, including the groups R_a to R_d, which have particular meanings as defined in the claims[1].

Scope of the Patent

Diseases Covered

The patent encompasses a broad range of cancer diseases, including:

  • Hematological Neoplasias: This includes acute or chronic leukemias of myeloid, erythroid, or lymphatic origin, myelodysplastic syndromes (MDS), and myeloproliferative syndromes (MPS) such as chronic myelogeneous leukemia, osteomyelofibrosis, polycythemia vera, or essential thrombocythemia[1].
  • Lymphomas: The patent covers various types of lymphomas.
  • Mixed Tumors and Undifferentiated Tumors: This includes adenosquamous carcinomas, mixed mesodermal tumors, carcinosarcomas, teratocarcinomas, carcinomas of unknown primary (CUP), metastases of unknown primary (MUP), and other undifferentiated tumors[1].

Specific Mutations

The patent also specifies the use of these quinazoline derivatives for the treatment of cancers with specific genetic mutations, such as EGFR mutations in the tyrosine kinase domain of the EGF receptor and/or tumors harboring activating HER2 mutations[1].

Method of Treatment

Administration

The method of treatment involves the administration of a therapeutically effective amount of the quinazoline compound, which can be in various forms including tautomers, racemates, enantiomers, diastereomers, and mixtures thereof. The compound can also be administered as pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, or physiologically functional derivatives. The administration routes include oral, enteric, transdermal, intravenous, peritoneal, or by injection, with oral administration being preferred[1].

Patent Landscape

Expiration Dates

The patent is set to expire on November 9, 2026. This expiration date is crucial for understanding the timeline for potential generic versions of the drug to enter the market[5].

Related Patents

Other related patents, such as U.S. Patent 8,545,884 and U.S. Patent 10,004,743, also cover aspects of the same active substance (BIBW 2992, known as Afatinib) but focus on different formulations and manufacturing processes. These patents have expiration dates ranging from 2026 to 2030, which affects the overall patent landscape for Afatinib and related compounds[2][5].

Litigation and Regulatory Aspects

FDA Approvals and Generic Versions

The FDA has not approved any generic versions of Gilotrif (Afatinib), which is closely related to the compounds described in this patent. Litigation and regulatory hurdles, including paragraph IV certifications and patent infringement lawsuits, have delayed the approval of generic versions[2][5].

Patent Infringement and Exclusivity

The patent landscape is further complicated by litigation over patent infringement. For instance, Sun Pharmaceutical Industries Limited has faced litigation over the '586 patent, which is part of the broader patent portfolio protecting Afatinib. These legal battles can delay the entry of generic drugs into the market until the patents expire or are ruled invalid or not infringed[2].

Impact on Innovation and Market

Patent Scope and Quality

The scope and clarity of patent claims are critical for innovation. Broad or unclear claims can lead to increased litigation costs and diminished incentives for innovation. The examination process for this patent, like many others, likely involved narrowing the scope of the claims to ensure clarity and validity[3].

Market Domination

The exclusive rights granted by this patent allow Boehringer Ingelheim to dominate the market for these specific quinazoline derivatives until the patent expires. This exclusivity period is crucial for the company to recoup its investment in research and development.

Key Takeaways

  • Broad Therapeutic Applications: The patent covers a wide range of cancer diseases, including hematological neoplasias, lymphomas, and mixed or undifferentiated tumors.
  • Specific Genetic Mutations: The treatment is particularly effective for cancers with EGFR or HER2 mutations.
  • Multiple Administration Routes: The compound can be administered through various routes, with oral administration being preferred.
  • Patent Expiration: The patent is set to expire on November 9, 2026.
  • Regulatory and Litigation Hurdles: The approval of generic versions is delayed due to ongoing litigation and regulatory issues.

FAQs

What is the primary focus of US Patent 9,539,258?

The primary focus of US Patent 9,539,258 is the use of quinazoline derivatives for the treatment of various cancer diseases.

Which types of cancer are covered by this patent?

The patent covers hematological neoplasias, lymphomas, mixed tumors, undifferentiated tumors, and other specific types of cancers, including those with EGFR or HER2 mutations.

How are the quinazoline derivatives administered according to the patent?

The compounds can be administered orally, enterically, transdermally, intravenously, peritoneally, or by injection, with oral administration being preferred.

When is the patent set to expire?

The patent is set to expire on November 9, 2026.

Are there any generic versions of the drug approved by the FDA?

No, there are currently no therapeutically equivalent generic versions of Gilotrif (Afatinib) approved by the FDA.

What are the implications of ongoing litigation on the approval of generic versions?

Ongoing litigation over patent infringement has delayed the approval of generic versions until the patents expire or are ruled invalid or not infringed.

Sources

  1. US9539258B2 - Quinazoline derivatives for the treatment of cancer diseases - Google Patents
  2. Afatinib Tablets - FDA
  3. Patent Claims and Patent Scope - Hoover Institution
  4. United States Court of Appeals for the Federal Circuit - CAFC
  5. Generic Gilotrif Availability - Drugs.com

More… ↓

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Drugs Protected by US Patent 9,539,258

ApplicantTradenameGeneric NameDosageNDAApproval DateTETypeRLDRSPatent No.Patent ExpirationProductSubstanceDelist Req.Patented / Exclusive UseSubmissiondate
Boehringer Ingelheim GILOTRIF afatinib dimaleate TABLET;ORAL 201292-001 Jul 12, 2013 RX Yes No ⤷  Subscribe ⤷  Subscribe Y ⤷  Subscribe
Boehringer Ingelheim GILOTRIF afatinib dimaleate TABLET;ORAL 201292-002 Jul 12, 2013 RX Yes No ⤷  Subscribe ⤷  Subscribe Y ⤷  Subscribe
Boehringer Ingelheim GILOTRIF afatinib dimaleate TABLET;ORAL 201292-003 Jul 12, 2013 RX Yes Yes ⤷  Subscribe ⤷  Subscribe Y ⤷  Subscribe
>Applicant>Tradename>Generic Name>Dosage>NDA>Approval Date>TE>Type>RLD>RS>Patent No.>Patent Expiration>Product>Substance>Delist Req.>Patented / Exclusive Use>Submissiondate
Showing 1 to 3 of 3 entries

Foreign Priority and PCT Information for Patent: 9,539,258

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
05110656Nov 11, 2005

International Family Members for US Patent 9,539,258

CountryPatent NumberEstimated ExpirationSupplementary Protection CertificateSPC CountrySPC Expiration
Canada 2629244 ⤷  Subscribe
Canada 2833706 ⤷  Subscribe
Canada 2833852 ⤷  Subscribe
European Patent Office 1948179 ⤷  Subscribe
European Patent Office 3173084 ⤷  Subscribe
Japan 2009515851 ⤷  Subscribe
>Country>Patent Number>Estimated Expiration>Supplementary Protection Certificate>SPC Country>SPC Expiration
Showing 1 to 6 of 6 entries

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