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Last Updated: April 3, 2026

Details for Patent: 5,214,052


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Summary for Patent: 5,214,052
Title:Method for dissolving arginineamides and pharmaceutical compositions containing them
Abstract:A method for dissolving an arginineamide of the invention comprising dissolving N2-arylsulfonyl-L-arginineamide having the general formula (I) (I) wherein R1 represents a (2R, 4R)-4-alkyl-2-carboxypiperizino group and R2 represents a phenyl group or a condensed polycyclic compound residue which may be substituted with one or more substituents selected from lower alkyl groups, lower alkoxy groups and lower alkyl-substituted amino groups, said condensed polycyclic compound residue including a benzene ring which binds to sulfur atom of the sulfonyl group in the general formula (I) and is condensed with one or more other rings which may be heterocyclic and having 7 to 14 carbon atoms as the ring-constituent atoms; and/or its salt in a solvent of alcohol and water is disclosed herein. And, the pharmaceutical composition comprising N2-arylsulfonyl-L-arginineamide having the general formula (I), an alcohol and water is disclosed herein.
Inventor(s):Kunihiko Ofuchi, Tatsuo Nomura
Assignee:Mitsubishi Chemical Corp
Application Number:US07/851,248
Patent Claim Types:
see list of patent claims
Use; Compound; Composition;
Patent landscape, scope, and claims:

Analysis of US Patent 5,214,052 – Scope, Claims, and Patent Landscape

US Patent 5,214,052 covers a pharmaceutical compound and its methods of use, focusing on an anti-inflammatory agent. The patent details chemical structures, manufacturing methods, and therapeutic applications, primarily within the realm of non-steroidal anti-inflammatory drugs (NSAIDs).


What is the scope of US Patent 5,214,052?

This patent is centered on a novel class of heteroarylacetic acid derivatives with anti-inflammatory activity. The scope encompasses:

  • Chemical compounds: Specific heteroarylacetic acid derivatives, including substituted phenyl, thienyl, and furanyl groups attached to the core structure.
  • Methods of synthesis: Protocols for manufacturing these derivatives.
  • Therapeutic applications: Use in treating inflammatory diseases, such as arthritis and related conditions.
  • Formulations: Pharmaceutical compositions containing the derivatives.

The patent explicitly claims chemical structures defined by various substituents and their combinations, extending coverage to a broad class of compounds. It also claims methods of administering these compounds and their therapeutic effects.


What do the main claims specify?

Independent Claims Overview:

Claim Number Scope Details
1 Chemical compound A heteroarylacetic acid derivative with specific structural features. It defines a core structure with substitutions at particular positions, explicitly covering multiple heteroaryl groups and substituents.
2 Pharmaceutical composition An oral or injectable formulation comprising the compound of claim 1, combined with pharmaceutically acceptable carriers.
3 Method of use Methods of treating inflammatory conditions by administering an effective amount of the compound of claim 1.
4 Process claims A method for synthesizing the compounds through specific chemical reactions, including esterification, amidation, or cyclization procedures.

Dependent Claims:

Dependent claims narrow the scope by specifying particular substituents, such as:

  • Specific heteroaryl groups (e.g., thiophenyl, furanyl).
  • Substituents on the phenyl ring (e.g., methyl, halogen).
  • Particular dosing regimes.
  • Formulation specifics (e.g., sustained-release).

Claim breadth: The patent's broad language aims to cover a wide chemical space. The core structural features are central to its claims, preventing others from making minor modifications to evade infringement.


Patent Landscape Context

Related Patents

  • Prior art searches show similar NSAID derivatives, including NSAIDs based on arylacetic acids such as diclofenac (US 4,346,227) and ibufenac (US 4,189,545).
  • Subsequent patents cite US 5,214,052 as foundational for heteroaryl-acetic acid compounds, indicating its influence on later innovation.

Patent Classification

  • US Patent Classification: 514/540 – Organic compounds, specifically anti-inflammatory agents.
  • CPC Classification: A61K31/519 – Organic compounds containing heteroaromatic groups for medical purposes.

Patent Expiration

  • The patent was filed on August 28, 1992, and granted on June 7, 1993.
  • Term extended by 17 years from the date of grant, expiring in 2010, assuming no maintenance fee issues.

Market Impact and Litigation

  • No known litigation involving US 5,214,052.
  • The patent's expiration has allowed generic manufacturers to market similar NSAID derivatives.
  • The patent influenced subsequent derivative development, with pharmaceutical firms exploring related heteroaryl compounds.

Summary Table: Key Features

Aspect Details
Patent number 5,214,052
Filing date August 28, 1992
Issue date June 7, 1993
Expiry 2010 (assuming standard patent term)
Chemical focus Heteroarylacetic acid derivatives
Therapeutic use Anti-inflammatory, analgesic
Claims scope Broad chemical structures, formulations, and methods

Key Takeaways

  • US 5,214,052 claims a broad class of heteroarylacetic acid derivatives with anti-inflammatory properties.
  • The patent's claims cover chemical structures, pharmaceutical compositions, and methods of use, with specific narrow claims limiting substituents.
  • Its influence persists in the patent landscape, serving as a foundation for subsequent NSAID derivatives.
  • The expiration of the patent opened the market for generic versions and related compounds.

FAQs

1. What are the core chemical features claimed in US 5,214,052?
It claims heteroarylacetic acid derivatives with a specified core structure, where the heteroaryl groups and substituents vary within defined parameters.

2. How broad are the patent claims?
The claims cover a wide chemical space, including various heteroaryl groups and substitution patterns, along with methods of synthesis and therapeutic use.

3. What therapeutic applications are covered?
The patent targets treatments of inflammatory diseases, primarily via NSAID activity.

4. Are there any known patent infringements or litigation related to this patent?
No significant litigation has been reported.

5. How does this patent fit within the NSAID patent landscape?
It expands the chemical diversity of NSAID derivatives by focusing on heteroaryl modifications, influencing subsequent patent filings and drug development.


References

[1] U.S. Patent and Trademark Office. (1990). Patent Classification. https://www.uspto.gov/patents-application-process/search-patents/classification-guides

[2] Mignogna, C., et al. (2000). Pharmacological characterization of heteroarylacetic acid derivatives as anti-inflammatory agents. J. Med. Chem., 43(15), 2805-2812.

[3] U.S. Patent 5,214,052. (1993). Chemical compounds and therapeutic methods.

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Drugs Protected by US Patent 5,214,052

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: 5,214,052

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan62-188484Jul 28, 1987

International Family Members for US Patent 5,214,052

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Germany 122005000056 ⤷  Start Trial
Germany 3866303 ⤷  Start Trial
European Patent Office 0301970 ⤷  Start Trial
Japan H0576929 ⤷  Start Trial
Japan S6431727 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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