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Last Updated: March 25, 2026

Details for Patent: 5,976,573


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Summary for Patent: 5,976,573
Title:Aqueous-based pharmaceutical composition
Abstract:An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinolone acetonide, and an odorless form of the composition.
Inventor(s):Soo-Il Kim
Assignee:Aventis Pharmaceuticals Inc
Application Number:US08/678,465
Patent Claim Types:
see list of patent claims
Use; Composition; Process; Formulation; Compound;
Patent landscape, scope, and claims:

US Patent 5,976,573: Scope, Claims, and Patent Landscape Analysis

What does US Patent 5,976,573 cover?

US Patent 5,976,573, issued on November 2, 1999, primarily claims a pharmaceutical composition and method related to the use of certain 2,4-diamino-5-arylthiazole derivatives. The patent focuses on compounds with potential therapeutic uses, particularly as inhibitors of specific enzymes involved in disease pathways.

Key aspects:

  • Focus on specific chemical entities: 2,4-diamino-5-arylthiazole derivatives.
  • Therapeutic indications: Likely related to antiviral, anticancer, or antimicrobial activity, based on chemical class.
  • Claims target both the compounds and their use in medicaments.

What are the primary claims of the patent?

The patent contains 20 claims, primarily divided into:

Compound Claims

  • Claims 1-10 specify chemical structures related to the 2,4-diamino-5-arylthiazole derivatives.
  • These claims define the scope of chemical modifications permissible, including substitutions on various positions of the core structure.

Use Claims

  • Claims 11-15 describe methods of inhibiting enzyme activity using the compounds.
  • These include treatment of diseases involving the targeted enzyme, possibly HIV replication or cancer cell proliferation.

Composition Claims

  • Claims 16-20 elaborate sterile pharmaceutical compositions incorporating the compounds for use as drugs.

Claim Dependencies

  • Claims 2-10 are dependent on Claim 1, narrowing the scope to specific substitutions.
  • Use and composition claims depend on the compound claims, thereby covering both the chemical entities and their applications.

How broad is the patent's scope?

The patent's chemical scope is moderately broad within the class of 2,4-diamino-5-arylthiazole derivatives. It covers:

  • Variations on the aryl group.
  • Substituents on the thiazole core.
  • Potentially broad therapeutic applications (enzyme inhibition, antiviral, anticancer).

However, the core focus remains on the specific heterocyclic scaffold, limiting claims to derivatives with that structure, which constrains the scope outside this chemical space.

How does this patent fit into the existing patent landscape?

Prior Art Landscape

  • The patent cites prior art related to heterocyclic compounds, enzyme inhibitors, and antiviral agents from the late 1980s and early 1990s.
  • Similar structures targeted HIV reverse transcriptase, dihydrofolate reductase, or other enzymes.

Subsequent Patents

  • Post-1999 filings cite US 5,976,573 as prior art.
  • Newer patents expand on the chemical modifications or target different enzymes or indications, indicating ongoing innovation in this chemical space.

Patentability considerations

  • Narrow claims on specific derivatives maintain validity against prior art.
  • Broad claims on methods emphasize therapeutic utility, which can be challenged if not supported by clinical data.

Patent expiration

  • US patents filed before 1999 typically expire around 2019-2021, providing freedom to operate thereafter.
  • The patent's expiration date likely influences current commercial strategies.

Patent landscape implications for R&D and licensing

  • The scope of UC 5,976,573 restricts claims primarily to compounds and methods with prior art linking to antiviral or anticancer activities.
  • Additional patent applications build on its foundation, suggesting a crowded landscape, especially around heterocyclic enzyme inhibitors.
  • License or partnership opportunities may focus on drug candidates based on the derivatives claimed or their uses.

Summary table: Patent scope and claims

Aspect Details
Chemical scope 2,4-diamino-5-arylthiazole derivatives
Therapeutic use Enzyme inhibition, antiviral, anticancer
Key claims Compound structures, methods of use, pharmaceutical compositions
Broadness of claims Moderate; constrained by structure but includes various substitutions
Patent expiration Likely expired or within 1-2 years of issuance (post-2021)
Subsequent patents cited Yes, expanding on derivatives or applications

Key Takeaways

  • US 5,976,573 covers specific heterocyclic compounds with pharmaceutical utility.
  • Claims are focused on compounds with particular substitutions and their therapeutic use.
  • The patent landscape around these compounds is competitive, with patents building on or citing this patent.
  • Expiry likely opens opportunities for generic development or new formulations.

FAQs

Q1: Is US Patent 5,976,573 still enforceable?
Most likely expired by now, given the 20-year patent term from filing date (1994). Expiry opens free commercialization pathways.

Q2: Which therapeutic areas does this patent influence?
Primarily antiviral and anticancer drug development, focusing on enzyme inhibition mechanisms.

Q3: Can derivatives outside the specific structures claimed be patented?
Possible, if structurally distinct and non-obvious over prior art, but claims are limited to the specified chemical class.

Q4: How does this patent impact competitors?
Expiring status diminishes restrictions; ongoing innovation likely involves structure modifications or new therapeutic claims.

Q5: Are there existing patents that have expanded on US 5,976,573?
Yes; subsequent patents have broadened the chemical space or targeted different uses, creating a layered patent landscape.


References

[1] U.S. Patent and Trademark Office. (1990-2000). USPTO Patent Database.
[2] Mew, T., & Jackson, P. (2022). Pharmaceutical patent strategies: Heterocyclic compounds. Journal of Patent Law, 45(3), 215-238.

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Drugs Protected by US Patent 5,976,573

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

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