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Last Updated: December 23, 2024

Details for Patent: 7,105,530


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Summary for Patent: 7,105,530
Title:Pyrimidineamines as angiogenesis modulators
Abstract:Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also Includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Inventor(s): Boloor; Amogh (Lubbock, TX), Cheung; Mui (Durham, NC), Davis; Ronda (Durham, NC), Harris; Philip Anthony (Durham, NC), Hinkle; Kevin (Durham, NC), Mook, Jr.; Robert Anthony (Durham, NC), Stafford; Jeffery Alan (San Diego, CA), Veal; James Marvin (Durham, NC)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:10/451,305
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 7,105,530

Introduction

United States Patent 7,105,530, titled "Pyrimidineamines as Angiogenesis Modulators," is a significant patent in the field of pharmaceuticals, particularly in the development of treatments for hyperproliferative diseases such as cancer. This patent, assigned to SmithKline Beecham Corporation (now part of GlaxoSmithKline), was granted on September 12, 2006.

Background and Invention Overview

The patent describes pyrimidine derivatives, their compositions, and their use as angiogenesis modulators. Angiogenesis, the process of new blood vessel formation, is a critical aspect of tumor growth and metastasis. The inventors, including Amogh Boloor, Mui Cheung, and others, developed these compounds to inhibit angiogenesis, thereby providing a therapeutic approach to treating cancer and other hyperproliferative diseases[5].

Scope of the Patent

Claims

The patent includes multiple claims that define the scope of the invention. Here are some key aspects:

  • Compound Claims: The patent claims various pyrimidine derivatives, including specific structures and their pharmaceutical salts. For example, Claim 1 describes a compound of the formula: [ \text{where R}^1 \text{, R}^2 \text{, R}^3 \text{, and R}^4 \text{are defined in the claim}[5]. ]
  • Method of Preparation Claims: The patent also claims methods for preparing these pyrimidine derivatives. These methods involve specific chemical reactions and conditions, such as the condensation of 2,3-dimethyl-2H-indazol-6-amine with 2,4-dichloropyrimidine in the presence of a base[5].
  • Therapeutic Use Claims: Claims related to the therapeutic use of these compounds are also included. For instance, Claim 15 describes a method of treating cancer in a mammal by administering one of the claimed compounds[5].

Pharmaceutical Compositions

The patent covers pharmaceutical compositions containing the pyrimidine derivatives. These compositions can be formulated in various ways, including tablets, capsules, and injectable solutions, and are designed for oral or parenteral administration[5].

Novelty and Non-Obviousness

The patent emphasizes the novelty and non-obviousness of the pyrimidine derivatives and their therapeutic applications. The inventors demonstrated that these compounds have significant angiogenesis inhibitory activity, which was not previously known or obvious from the prior art[5].

Prior Art and Related Patents

The patent landscape surrounding US 7,105,530 includes several related patents and publications:

  • U.S. Pat. No. 7,262,203: This patent is a continuation of the application that led to US 7,105,530 and further discloses methods of making and using pyrimidine derivatives[2].
  • U.S. Pat. No. 8,114,885: This patent, also related to the same inventors and assignee, includes additional methods and compositions for pyrimidine derivatives and their use in treating hyperproliferative diseases[2].
  • WO 2011/050159: This international patent application discloses another process for preparing pazopanib hydrochloride, a specific pyrimidine derivative, which is related to the compounds claimed in US 7,105,530[1].

Patent Scope Metrics

The scope of the patent can be analyzed using metrics such as independent claim length and count. Research suggests that narrower claims, as measured by these metrics, are associated with a higher probability of grant and a shorter examination process. The claims in US 7,105,530 are detailed and specific, indicating a well-defined scope that was likely refined during the examination process to ensure clarity and validity[3].

Impact and Commercial Significance

The compounds described in US 7,105,530, particularly pazopanib, have significant commercial and therapeutic importance. Pazopanib, marketed under the brand name Votrient, is used to treat certain types of cancer, including renal cell carcinoma and soft tissue sarcoma. The patent has contributed to the development of targeted therapies in oncology, highlighting the importance of intellectual property in driving innovation in the pharmaceutical industry.

Expiration and Licensing

The patent has expired, as it was granted in 2006 and the term of a U.S. patent is generally 20 years from the earliest filing date. The expiration of this patent allows for the generic production of pazopanib and other related compounds, potentially increasing access to these life-saving medications.

Key Takeaways

  • Invention Overview: The patent covers pyrimidine derivatives as angiogenesis modulators for treating hyperproliferative diseases.
  • Claims: Specific compound structures, methods of preparation, and therapeutic uses are claimed.
  • Pharmaceutical Compositions: Various formulations for oral or parenteral administration are described.
  • Novelty and Non-Obviousness: The patent emphasizes the novelty and non-obviousness of the compounds and their therapeutic applications.
  • Related Patents: Several related patents and publications are part of the broader patent landscape.
  • Commercial Significance: The patent has significant commercial and therapeutic importance, particularly for pazopanib.

FAQs

What is the main subject of United States Patent 7,105,530?

The main subject is pyrimidine derivatives as angiogenesis modulators for treating hyperproliferative diseases.

Who are the inventors of this patent?

The inventors include Amogh Boloor, Mui Cheung, Ronda Davis, Philip Anthony Harris, Kevin Hinkle, Robert Anthony Mook Jr., Jeffery Alan Stafford, and James Marvin Veal.

What is the therapeutic use of the compounds described in this patent?

The compounds are used to treat hyperproliferative diseases, particularly cancer, by inhibiting angiogenesis.

Is the patent still in force?

No, the patent has expired as it was granted in 2006 and the term of a U.S. patent is generally 20 years from the earliest filing date.

What is the commercial significance of this patent?

The patent is significant as it led to the development of targeted therapies in oncology, particularly pazopanib (Votrient), which is used to treat certain types of cancer.

Sources

  1. US20160280689A1 - Patent Application Publication
  2. US8114885B2 - United States Patent
  3. Patent Claims and Patent Scope - Hoover Institution
  4. US7105530B2 - Pyrimidineamines as Angiogenesis Modulators
  5. US7105530B2 - United States Patent

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Drugs Protected by US Patent 7,105,530

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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: 7,105,530

PCT Information
PCT FiledDecember 19, 2001PCT Application Number:PCT/US01/49367
PCT Publication Date:August 01, 2002PCT Publication Number: WO02/059110

International Family Members for US Patent 7,105,530

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1343782 ⤷  Subscribe C300456 Netherlands ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe CA 2010 00024 Denmark ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe 91710 Luxembourg ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe SPC025/2010 Ireland ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe 10C0037 France ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe SPC/GB10/032 United Kingdom ⤷  Subscribe
European Patent Office 1343782 ⤷  Subscribe C01343782/01 Switzerland ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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