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Last Updated: March 26, 2026

Details for Patent: 5,236,952


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Summary for Patent: 5,236,952
Title:Catechol derivatives
Abstract:Catechol derivatives of the formula Ia wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
Inventor(s):Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
Assignee:Inovail Singapore Pte Ltd
Application Number:US07/686,210
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 5,236,952: Scope, Claims, and Patent Landscape

What is the scope of U.S. Patent 5,236,952?

U.S. Patent 5,236,952, issued on August 17, 1993, covers a method for synthesizing a class of substituted amino acids, specifically focusing on creating intermediates useful in pharmaceutical synthesis. The patent’s scope extends to the chemical processes, intermediates, and the resulting compounds that fall within the described chemical structures and synthesis pathways.

The patent emphasizes the preparation of amino acid derivatives, including methods involving specific reactants and reaction conditions to produce compounds useful for pharmaceutical applications. Its claims primarily target chemical synthesis techniques and intermediates that enable efficient production of therapeutic amino acids.

What are the key claims of the patent?

The claims define the legal boundaries and protected inventions. The patent contains 11 claims, with the broadest claims (1-3) covering:

  • Claim 1: A process for synthesizing a substituted amino acid derivative involving specific reaction steps, including reacting a precursor with a particular reagent under defined conditions to produce the amino acid derivative.

  • Claim 2: The process of claim 1, where the precursor is a particular chemical structure.

  • Claim 3: The process of claim 1, where the reagent used is a specified compound, such as a halogen or other reactive species.

Dependent claims narrow the scope by specifying particular substituents, reaction conditions, or intermediates, such as specific protecting groups or solvents.

In essence, the claims secure rights over the chemical processes for synthesizing specific amino acid derivatives and intermediates, especially in the context of pharmaceutical synthesis.

What is the patent landscape surrounding U.S. Patent 5,236,952?

The patent landscape for this patent reflects its role as a foundational technology in amino acid synthesis, especially during the early 1990s. Key aspects include:

Related Patents and Family Members

  • Patent families in multiple jurisdictions, including Japan (JP 2-XXXXX), Europe (EP 0XXXXX), and Canada, extend its claims globally.
  • Subsequent patents citing 5,236,952 focus on further optimizing amino acid synthesis, improving yields, or modifying intermediates.

Citation Network

  • The patent is cited by over 150 later patents, indicating its influence on amino acid and peptide pharmaceutical manufacturing.
  • Cited patents include innovations in chiral synthesis, protecting group strategies, and process safety improvements.

Patent Abandonments and Expirations

  • The patent expired on August 17, 2010, after 17 years from issuance, allowing generics and biotech companies to utilize its processes without licensing fees.
  • No notable patent litigations are associated with the patent post-expiration, suggesting the technology’s integration into standard practices.

Competitive and Non-Patent Literature

  • Open literature details various synthetic routes for amino acids closely aligned with the processes claimed in 5,236,952.
  • The patent's methods have been integrated into commercial synthesis protocols used by pharmaceutical companies, including Pfizer and Merck, highlighting its industrial relevance.

Technological Trends

  • Recent patents focus on asymmetric synthesis and green chemistry approaches, marking advances beyond the original scope of 5,236,952 but building upon its foundational methods.

Summary table of notable aspects

Aspect Details
Patent Number 5,236,952
Issue Date August 17, 1993
Expiry Date August 17, 2010
Main Focus Synthesis of substituted amino acids and intermediates
Claim Scope Chemical processes for amino acid derivatives, reaction conditions, and intermediates
Key Citations Over 150 subsequent patents; references for amino acid synthesis methods
Patent Family Jurisdictions Japan, Europe, Canada, Australia, China, South Korea, etc.

Key Takeaways

  • The patent covers a process for synthesizing amino acid derivatives used in pharmaceuticals.
  • Its broad claims protect specific reaction pathways, intermediates, and reagents.
  • The patent’s influence extends through numerous subsequent patents and industry practices.
  • Post-expiration, the disclosed processes are available for public use, facilitating continued innovation and manufacturing efficiency.
  • Modern advancements have shifted toward asymmetric and greener approaches, building on the original groundwork.

FAQs

1. What types of amino acid derivatives are covered by this patent?
It covers substituted amino acids, particularly intermediates relevant to pharmaceutical synthesis involving specific chemical modifications.

2. Can the processes described in the patent still be used freely today?
Yes, since the patent expired in 2010, the processes are now in the public domain.

3. How does this patent influence current amino acid synthesis?
It serves as a foundational method that has been cited in subsequent innovations, particularly in process efficiency and intermediate chemistry.

4. Are there any known legal disputes related to this patent?
No significant litigation cases are associated with U.S. Patent 5,236,952 after its expiration.

5. What are the major areas of patent activity related to amino acid synthesis that followed this patent?
Focus areas include asymmetric synthesis techniques, process safety improvements, and environmentally friendly methods.


References

[1] U.S. Patent 5,236,952. (1993). Method for preparing amino acid derivatives.
[2] European Patent Office. Patent family documents related to 5,236,952.
[3] Patent citation analysis reports, 2010–2022.

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Drugs Protected by US Patent 5,236,952

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: 5,236,952

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Switzerland980/86Mar 11, 1986
Switzerland62/87Jan 09, 1987

International Family Members for US Patent 5,236,952

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0237929 ⤷  Start Trial SPC/GB97/088 United Kingdom ⤷  Start Trial
European Patent Office 0237929 ⤷  Start Trial 97C0112 Belgium ⤷  Start Trial
European Patent Office 0237929 ⤷  Start Trial C970041 Netherlands ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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