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Last Updated: December 24, 2024

Details for Patent: 6,436,989


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Summary for Patent: 6,436,989
Title: Prodrugs of aspartyl protease inhibitors
Abstract:The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
Inventor(s): Hale; Michael R. (Bedford, MA), Tung; Roger D. (Arlington, MA), Baker; Christopher T. (Waltham, MA), Spaltenstein; Andrew (Raleigh, NC)
Assignee: Vertex Pharmaceuticals, Incorporated (Cambridge, MA)
Application Number:08/998,050
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,436,989
Patent Claim Types:
see list of patent claims
Compound; Composition; Dosage form; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 6,436,989

Introduction

United States Patent 6,436,989, titled "Prodrugs of aspartyl protease inhibitors," is a significant patent in the field of pharmaceuticals, particularly in the treatment of HIV. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background and Invention Overview

The patent, issued on August 20, 2002, pertains to a novel class of prodrugs designed to improve the pharmacokinetic properties of aspartyl protease inhibitors. These inhibitors are crucial in the treatment of HIV infections by targeting the HIV protease enzyme, which is essential for the virus's replication process[4].

Scope of the Invention

The invention focuses on creating prodrugs that enhance the aqueous solubility and bioavailability of aspartyl protease inhibitors. This is achieved through the design of prodrug molecules that are more soluble in water, thereby improving their absorption and effectiveness in the body. The prodrugs are characterized by their ability to release the active aspartyl protease inhibitor once administered, ensuring that the therapeutic agent reaches the target site in an effective manner[4].

Claims of the Patent

The patent includes several claims that define the scope of the invention:

  • Composition Claims: These claims describe the chemical composition of the prodrugs, including the specific structures and functional groups that enhance solubility and bioavailability[4].
  • Method Claims: These claims outline the methods for preparing the prodrugs, including the synthesis steps and conditions necessary to produce the desired compounds[4].
  • Use Claims: These claims specify the therapeutic uses of the prodrugs, particularly in the treatment of HIV infections and other diseases where aspartyl protease inhibitors are effective[4].

Key Components and Features

  • Prodrug Design: The patent details the design of prodrugs that incorporate solubilizing groups, which are later cleaved in vivo to release the active aspartyl protease inhibitor.
  • Pharmaceutical Compositions: The invention includes pharmaceutical compositions that contain these prodrugs, along with suitable carriers and excipients to enhance their delivery and efficacy.
  • Therapeutic Applications: The prodrugs are intended for the treatment of HIV infections and potentially other diseases where aspartyl protease inhibitors are beneficial[4].

Patent Landscape Analysis

To understand the broader context of this patent, a patent landscape analysis is essential.

Competitor Analysis

Other patents and patent applications in the field of aspartyl protease inhibitors and their prodrugs need to be considered. This includes analyzing the patents held by competitors, their expiration dates, and the geographical coverage of these patents. For instance, similar patents filed in other countries or through international patent cooperation treaties (PCT) can provide insights into global market strategies[3].

Market Trends and Developments

Patent landscape analysis reveals market trends such as mergers and acquisitions, in/out-licensing agreements, and litigation activities related to aspartyl protease inhibitors. This information can help in identifying potential partners, competitors, and areas of innovation[3].

Legal Status and Expiry Dates

The legal status of the patent, including its current status (e.g., active, expired, or lapsed), is crucial. As of the current date, the patent US6,436,989 has expired, which means that the technology is now in the public domain. This can impact the strategy for using or improving upon this technology[4].

International Patent Filings

The patent's international filings and the status of these filings in various countries can be assessed using tools like the Global Dossier and the Common Citation Document (CCD) provided by the USPTO and other international intellectual property offices. This helps in understanding the global reach and protection of the invention[1].

Impact on the Market

The expiration of the patent US6,436,989 opens up opportunities for generic or improved versions of the prodrugs to enter the market. This can lead to increased competition, potentially reducing the cost of these therapeutic agents and making them more accessible to patients.

Future Directions

Given the expiration of the patent, future research and development can focus on improving the existing prodrugs or developing new ones with enhanced properties. This could involve leveraging advanced drug delivery systems, nanotechnology, or other innovative approaches to further improve the efficacy and safety of aspartyl protease inhibitors.

Key Takeaways

  • Patent Scope: The patent covers the design, synthesis, and therapeutic use of prodrugs of aspartyl protease inhibitors.
  • Claims: The claims define the chemical composition, methods of preparation, and therapeutic applications of these prodrugs.
  • Patent Landscape: The patent is now in the public domain, offering opportunities for generic or improved versions.
  • Market Impact: The expiration can lead to increased competition and reduced costs for therapeutic agents.
  • Future Directions: Research can focus on improving existing prodrugs or developing new ones with advanced technologies.

FAQs

  1. What is the main focus of United States Patent 6,436,989?

    • The main focus is on the design and use of prodrugs of aspartyl protease inhibitors to improve their pharmacokinetic properties.
  2. What are the key benefits of the prodrugs described in the patent?

    • The prodrugs offer enhanced aqueous solubility and bioavailability, improving their absorption and therapeutic effectiveness.
  3. What is the current legal status of the patent?

    • The patent has expired, meaning the technology is now in the public domain.
  4. How does the expiration of the patent impact the market?

    • The expiration opens up opportunities for generic or improved versions of the prodrugs, potentially reducing costs and increasing accessibility.
  5. What are some potential future directions for research in this area?

    • Future research can focus on improving existing prodrugs or developing new ones using advanced drug delivery systems or other innovative approaches.

Cited Sources

  1. USPTO - Search for patents[1]
  2. Canadian Patents Database - Patent 2657316 Summary[2]
  3. Sagacious Research - Navigating Technological Domains with Patent Landscape Analysis[3]
  4. Google Patents - US6436989B1 - Prodrugs of aspartyl protease inhibitors[4]
  5. Unified Patents Portal - US-6436989-B1[5]

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Drugs Protected by US Patent 6,436,989

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

International Family Members for US Patent 6,436,989

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0933372 ⤷  Subscribe PA2008006 Lithuania ⤷  Subscribe
European Patent Office 0933372 ⤷  Subscribe 91426 Luxembourg ⤷  Subscribe
European Patent Office 0933372 ⤷  Subscribe CA 2008 00027 Denmark ⤷  Subscribe
European Patent Office 0933372 ⤷  Subscribe PA2008006,C0933372 Lithuania ⤷  Subscribe
European Patent Office 0933372 ⤷  Subscribe 08C0015 France ⤷  Subscribe
European Patent Office 0933372 ⤷  Subscribe 300339 Netherlands ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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