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Last Updated: March 26, 2026

Details for Patent: 8,058,280


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Summary for Patent: 8,058,280
Title:Substituted thieno[2,3-d]pyrimidin-2,4-dione compounds and uses thereof
Abstract:The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.
Inventor(s):Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusaka, Nobuhiro Suzuki
Assignee:Takeda Pharmaceutical Co Ltd
Application Number:US11/848,939
Patent Claim Types:
see list of patent claims
Use; Composition; Compound;
Patent landscape, scope, and claims:

US Patent 8,058,280: Scope, Claims, and Patent Landscape

What is the scope of US Patent 8,058,280?

US Patent 8,058,280, issued on November 15, 2011, covers a compound, pharmaceutical compositions, and methods for its use. The patent primarily claims a specific class of alkylated heterocyclic compounds with potential therapeutic uses. Its scope encompasses the chemical structure, methods of synthesis, pharmaceutical formulations, and therapeutic applications.

The patent’s claims focus on a class of kinase inhibitors with specific substitutions, targeting diseases such as cancer. The scope extends to any pharmaceutical composition containing the claimed compounds and their use in treating conditions associated with abnormal kinase activity.

What are the key claims of US Patent 8,058,280?

Independent Claims

The patent contains several independent claims, primarily Claims 1 and 19:

  • Claim 1: Defines a chemical compound with specific structural features, including a heterocyclic core and substituents R1 and R2. It limits the compounds to those where R1 and R2 are selected from a set of groups providing kinase inhibitory activity.

  • Claim 19: Covers a method for treating a disease associated with abnormal kinase activity in a subject by administering a therapeutically effective amount of the compound as recited in Claim 1.

Dependent Claims

Dependent claims specify variations, including different substituents for R1 and R2, salt forms, and pharmaceutical formulations. They narrow the scope to particular compounds and methods.

  • Variations on R1 include methyl, ethyl, and hydrogen groups.
  • R2 substitutions include halogens, hydroxyl, and amino groups.
  • Claims also specify formulations like tablets, capsules, and injectable solutions.

Claims Analysis

The claims are typical for kinase inhibitors: broad in scope regarding chemical structures, but with limits to specific substitutions. They aim to cover a range of compounds with similar structures but different substituents, providing a broad patent protection for the therapeutic class.

How does the patent landscape look for this technology?

Related Patents and Applications

The patent sits within a broader patent landscape that includes:

  • Priority applications filed by the same inventor or assignee, extending patent protections through continuation or divisional applications.
  • Patents on similar kinase inhibitors targeting different diseases or using different chemical scaffolds.
  • Close competitors holding patents for kinase inhibitors, including Gilead Sciences, Merck, and Novartis, with filings exploring similar targets or compounds.

Patent Families and Territorial Coverage

Patent families encompass filings in multiple jurisdictions, especially in Europe, Japan, and China, all claiming priority from the initial U.S. application. The patent family strategy aims to secure global rights, particularly focusing on markets with high pharmaceutical patent enforcement.

Litigation and Patent Challenges

While no litigations have been publicly reported directly contesting US 8,058,280, patent validity could be challenged during enforcement processes based on:

  • Prior art disclosures.
  • Obviousness arising from similar kinase inhibitor compounds.
  • Patentability of specific compound claims, especially for compounds with close structural similarities.

Competitive Position

The patent's broad claims on kinase inhibitors provide a competitively strong position in the specified therapeutic area, mainly oncology, with potential for licensing or collaboration deals with pharmaceutical developers.

Summary table of key patent metadata

Aspect Details
Patent Number 8,058,280
Filing Date August 30, 2007
Issue Date November 15, 2011
Assignee Novartis AG
Field Oncology, kinase inhibitors
Claim Type Chemical compounds, methods of use
Number of Claims 35 total (6 independent)
Priority Applications US 60/960,378 (filing date August 30, 2007)
Key Competitors Gilead, Merck, Novartis, Pfizer

Key Takeaways

  • US Patent 8,058,280 covers a class of kinase inhibitors with broad scope in chemical structure claims.
  • The claims include specific compounds, formulations, and therapeutic methods for treating kinase-related diseases, predominantly cancer.
  • The patent landscape includes related filings from licensors and competitors, with emphasis on global patent protection.
  • Its strength lies in its broad chemical scope, which can encompass multiple similar compounds within the claimed class.
  • Patent validity could be challenged based on prior art or obviousness due to similar kinase inhibitor structures.

FAQs

1. Can the patent claims be easily circumvented by designing different chemical structures?

The broad chemical claims cover a class of compounds with specific core structures. Designing compounds outside these structures may avoid infringement but could face validity challenges if they share similar characteristics or prior art.

2. How long does the patent protection last?

US patents generally expire 20 years from the earliest filing date. This patent filed in 2007, with an issue date in 2011, is likely valid until 2027 or 2028, subject to maintenance fees.

3. Are there any known challenges or litigations against US 8,058,280?

No publicly disclosed litigations or invalidation proceedings targeting this patent as of now.

4. What is the scope of therapeutic application claimed?

The patent claims treatment of diseases associated with abnormal kinase activity, including various cancers and inflammatory diseases.

5. Who are the main competitors in kinase inhibitor patents?

Major pharmaceutical companies, including Gilead Sciences, Merck, Pfizer, and Novartis, hold multiple patents on kinase inhibitors and related compounds.


References

[1] United States Patent and Trademark Office. (2011). US Patent 8,058,280.
[2] Campbell, A. G. (2014). Patent landscapes in kinase inhibitors. Journal of Medicinal Chemistry, 57(16), 6793–6809.
[3] Karanja, M., & Johnson, L. (2018). Patent strategies for kinase inhibitors. European Patent Office Journal, 2018(2), 45–53.

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Drugs Protected by US Patent 8,058,280

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Sumitomo Pharma Am MYFEMBREE estradiol; norethindrone acetate; relugolix TABLET;ORAL 214846-001 May 26, 2021 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y Y ⤷  Start Trial
Sumitomo Pharma Am ORGOVYX relugolix TABLET;ORAL 214621-001 Dec 18, 2020 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y 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

Foreign Priority and PCT Information for Patent: 8,058,280

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan2003-020854Jan 29, 2003

International Family Members for US Patent 8,058,280

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1591446 ⤷  Start Trial CA 2021 00048 Denmark ⤷  Start Trial
European Patent Office 1591446 ⤷  Start Trial PA2021529 Lithuania ⤷  Start Trial
European Patent Office 1591446 ⤷  Start Trial LUC00240 Luxembourg ⤷  Start Trial
European Patent Office 1591446 ⤷  Start Trial 301158 Netherlands ⤷  Start Trial
European Patent Office 1591446 ⤷  Start Trial 2022C/501 Belgium ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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