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Last Updated: December 22, 2024

Details for Patent: 5,196,438


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Summary for Patent: 5,196,438
Title: Amino acid derivatives
Abstract:Compounds having the formula ##STR1## wherein R is benzyloxycarbonyl or 2-quinolylcarbonyl, and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of prophylaxis of viral infections in mammals, humans or non-humans.
Inventor(s): Martin; Joseph A. (Harpenden, GB2), Redshaw; Sally (Stevenage, GB2)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Application Number:07/615,534
Patent Claim Types:
see list of patent claims
Compound; Composition; Dosage form; Formulation; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 5,196,438

Introduction

United States Patent 5,196,438, titled "Amino acid derivatives," is a significant patent that has contributed to the field of medicinal chemistry, particularly in the treatment and prophylaxis of viral infections. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background and Context

The patent, filed in 1990 and granted in 1993, pertains to novel amino acid derivatives that exhibit valuable pharmacological properties. These compounds are designed to inhibit proteases of viral origin, making them crucial in the fight against viral infections such as those caused by HIV and other retroviruses[1][2].

Scope of the Invention

Chemical Structure and Composition

The amino acid derivatives described in the patent have a specific chemical structure, represented by the formula: [ \text{R-CO-NH-CHR'-CO-NH-CHR''-CO-NH-CHR'''-COOH} ] where ( R ) can be benzyloxycarbonyl or 2-quinolylcarbonyl, and the compounds also include their pharmaceutically acceptable acid addition salts[1].

Pharmacological Properties

These compounds are novel and possess significant pharmacological properties, particularly in inhibiting proteases of viral origin. This makes them effective in the treatment and prophylaxis of viral infections, especially those caused by HIV and other retroviruses[1][2].

Claims of the Patent

Compound Claims

The patent claims the amino acid derivatives themselves, as well as their pharmaceutically acceptable acid addition salts. These claims are specific to the compounds having the defined chemical structure and their salts[1].

Method of Manufacture

The patent also claims the process for the manufacture of these compounds and their salts. This includes the intermediates used in the manufacturing process, which are crucial for the synthesis of the final products[1].

Therapeutic Use

A key aspect of the patent is the use of these compounds as therapeutically active substances. The claims include the use of these compounds in medicaments for the treatment or prophylaxis of viral infections[1].

Medicaments and Pharmaceutical Compositions

The patent covers medicaments containing these amino acid derivatives and their salts. It also includes the use of these compounds in the manufacture of medicaments for treating or preventing viral infections[1].

Patent Landscape

Innovation Tracks and Protection

The patent landscape surrounding this invention is complex and involves multiple innovation tracks. Similar to the analysis of Ritonavir patents, the protection of these amino acid derivatives extends beyond the initial patent filing. This includes various aspects such as liquid and solid dosage formulations, synthesis methods, and polymorphs, which are common strategies in pharmaceutical patent protection to ensure continued innovation and protection[4].

Assignees and Patent Families

The patent is part of a larger family of patents related to viral protease inhibitors. Large pharmaceutical corporations, similar to those involved in the Ritonavir patents, are typically the assignees of such patents. These companies often have extensive patent portfolios that cover various aspects of the compounds, including their synthesis, formulations, and therapeutic uses[4].

Search Methodology and Citation Analysis

To analyze the patent landscape, a thorough search methodology is employed, including text-based searching, backward and forward citation searches, and the use of chemical identifiers to ensure all relevant documents are captured. This approach helps in identifying earlier patent publications and subsequent innovations that build upon the original patent[4].

Impact on the Pharmaceutical Industry

Treatment of Viral Infections

The amino acid derivatives described in this patent have been instrumental in the development of treatments for viral infections, particularly HIV. These compounds, by inhibiting viral proteases, have significantly improved the therapeutic options available for patients suffering from such infections[1].

Future Directions

The patent's focus on novel chemical structures and their pharmacological properties opens up avenues for further research and development. Future innovations may involve modifying these compounds to enhance their efficacy or to target other viral infections[1].

Claim Coverage and Patent Analytics

To effectively manage and analyze the claims of this patent, tools such as Claim Coverage Matrix and ClaimScape® software can be utilized. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps in coverage and potential future design opportunities[3].

Key Takeaways

  • Novel Compounds: The patent introduces novel amino acid derivatives with specific chemical structures.
  • Pharmacological Properties: These compounds inhibit proteases of viral origin, making them valuable in treating viral infections.
  • Therapeutic Use: The patent covers the use of these compounds in medicaments for treating or preventing viral infections.
  • Manufacturing Process: The patent includes claims for the process of manufacturing these compounds and their intermediates.
  • Patent Landscape: The protection extends beyond the initial patent, involving various innovation tracks and strategies to ensure continued protection.

FAQs

What are the primary uses of the amino acid derivatives described in US Patent 5,196,438?

The primary uses are in the treatment and prophylaxis of viral infections, particularly those caused by HIV and other retroviruses.

Who are the typical assignees of such pharmaceutical patents?

Large pharmaceutical corporations are typically the assignees of such patents.

How do backward and forward citation searches contribute to patent landscape analysis?

These searches help in identifying earlier patent publications and subsequent innovations that build upon the original patent, ensuring a comprehensive understanding of the patent landscape.

What tools can be used to manage and analyze the claims of this patent?

Tools such as Claim Coverage Matrix and ClaimScape® software can be used to categorize patents by claims and scope concepts, helping to identify gaps in coverage and potential future design opportunities.

How do these compounds inhibit viral infections?

These compounds inhibit proteases of viral origin, which are essential enzymes for the replication of viruses like HIV.

Sources

  1. US5196438A - Amino acid derivatives - Google Patents
  2. US Patent for Amino acid derivatives Patent (Patent # 5,196,438) - Justia Patents
  3. Patent Analytics | Intellectual Property Law - SLWIP
  4. Patent Landscape Report on Ritonavir - WIPO

More… ↓

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Drugs Protected by US Patent 5,196,438

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: 5,196,438

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8927913Dec 11, 1989

International Family Members for US Patent 5,196,438

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0432695 ⤷  Subscribe 96C0044 Belgium ⤷  Subscribe
European Patent Office 0432695 ⤷  Subscribe C970013 Netherlands ⤷  Subscribe
European Patent Office 0432695 ⤷  Subscribe 32/1996 Austria ⤷  Subscribe
Austria 122661 ⤷  Subscribe
Australia 634319 ⤷  Subscribe
Australia 6787690 ⤷  Subscribe
Bulgaria 51452 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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