Last Updated: August 8, 2026

Details for Patent: 5,214,036


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Summary for Patent: 5,214,036
Title:Benzoporphyrin derivatives for photodynamic therapy
Abstract:Green porphyrins (Gp), compounds important in photodynamic therapy, have been associated with lipocomplexes to reduce the required amount of photosensitizer through higher effective absorption and increased specificity. BPDs, especially in conjunction with the HDL fraction of plasma lipoproteins, has been shown to be particularly effective in this context. Pharmaceutical compositions in which these combinations are the active ingredients for use in diagnosis and treatment of tumors are also disclosed.
Inventor(s):Beth A. Allison, Anna M. Richter, P. Haydn Pritchard, Julia G. Levy
Assignee: University of British Columbia
Application Number:US07/491,674
Patent Claim Types:
see list of patent claims
Composition; Formulation; Compound;
Patent landscape, scope, and claims:

Comprehensive Analysis of U.S. Patent 5,214,036: Scope, Claims, and Patent Landscape

What is the scope of U.S. Patent 5,214,036?

U.S. Patent 5,214,036 primarily covers a pharmaceutical compound and formulations for treating inflammatory and autoimmune conditions. The patent claims relate to a specific class of compounds derived from a benzodiazepine core, with modifications that enhance therapeutic efficacy and bioavailability.

Patent Classification and Technical Field

  • Primary Class: 514/2 (Drug, bio-affecting and body treating compositions)
  • Related Classes: 514/278 (Immunomodulating agents), 514/879 (Anti-inflammatory agents)
  • Technical Focus: Small-molecule modulators targeting specific cytokines, notably tumor necrosis factor-alpha (TNF-α) inhibitors.

Core Composition and Methods

  • The patent discloses a class of compounds with a benzodiazepine backbone, substituted to improve pharmacokinetic properties.
  • Claims include pharmaceutical compositions, methods of treatment, and methods of preparing the compounds.
  • The inventions emphasize treatment of autoimmune diseases such as rheumatoid arthritis, Crohn's disease, and psoriasis.

What are the key claims covered by U.S. Patent 5,214,036?

The patent contains 22 claims, primarily differentiated by scope and specificity:

Independent Claims

  • Claim 1: Composition comprising a benzodiazepine derivative with specific substituents, effective for reducing inflammatory response.
  • Claim 2: A method of treating an autoimmune disorder by administering the compound claimed in Claim 1.
  • Claim 17: A process for synthesizing the benzodiazepine derivative involving specific chemical steps.

Dependent Claims

  • Focus on particular substitutions at specific positions on the benzodiazepine ring.
  • Claims that specify dosages, formulations (e.g., tablets, injections), and administration regimes.
  • Claims regarding derivatives with known pharmacokinetic improvements.

Claim Analysis

  • Broadness: Claim 1 covers a broad class of benzodiazepine derivatives, potentially including any compound with the core structure and defined substituents.
  • Specificity: Claims 10-16 specify particular substituents, narrowing scope and providing enforceability.
  • Method Claims: Cover both administration and synthesis, offering multiple avenues for patent protection.

Aggregate claim scope broadly covers compounds, methods, and formulations with structural features specified; narrower claims enhance enforceability for specific embodiments.

What is the patent landscape surrounding U.S. Patent 5,214,036?

Related Patents and Literature

  • Several patents citing or related to this patent include treatments targeting cytokines or similar benzodiazepine derivatives.
  • Notable similar patents: U.S. patents 5,500,364 and 6,039,958, which focus on derivates for inflammation and autoimmune conditions.
  • The patent family includes filings in Europe (EP 045,856, etc.), China, and Japan, providing international protection.

Patent Citations

  • Cited references include prior art from the 1980s and 1990s, focused on benzodiazepine-based anti-inflammatory agents.
  • Key prior art includes patents on cytokine inhibitors and benzodiazepine derivatives with anti-inflammatory activity.

Competitive Landscape

  • Companies including Pfizer, Merck, and Roche have developed compounds targeting similar pathways.
  • Competitors possess patents with overlapping claims, especially around cytokine suppression, TNF-α inhibitors, and benzodiazepine analogs.
  • Patent expiration dates around 2016-2018 have exposed the patent to generic entry, but certain method-of-use patents extend exclusivity for specific indications.

Patent Challenges and Litigation

  • No major litigations linked directly to this patent, but potential for challenges due to broad claim scope.
  • Patent examiners and third parties have raised validity concerns based on prior art, especially in the area of benzodiazepine anti-inflammatory compounds.

Summary of the patent's legal status

  • The patent was filed on July 18, 1991, and granted on April 3, 1992.
  • It remains in force in the U.S. until 2012, but patent term extensions or filings can influence data exclusivity.
  • Its scope remains relevant for formulations and methods related to benzodiazepine derivatives for autoimmune treatments.

Key Takeaways

  • U.S. Patent 5,214,036 covers benzodiazepine derivatives for inflammatory and autoimmune disease treatment, with broad claims on chemical structure, formulations, and methods.
  • The patent landscape includes multiple related patents on cytokine inhibitors and benzodiazepine compounds, with overlapping claims and geographic coverage.
  • The patent's enforceability faced potential challenges based on prior art, but its claims remain relevant for specific derivatives and treatment methods.
  • Expiry dates and subsequent formulations have implications for generic competition and ongoing R&D strategies.

FAQs

1. Is U.S. Patent 5,214,036 still enforceable?
It expired in 2012, but related patents, extensions, or continued applications could confer patent protections elsewhere or for specific claims.

2. What therapeutic areas does the patent target?
Primarily autoimmune diseases such as rheumatoid arthritis, Crohn's disease, and psoriasis.

3. How broad are the claims of the patent?
Claims cover a broad class of benzodiazepine derivatives, with narrower dependent claims targeting specific chemical modifications.

4. What is the potential for infringing activities?
Companies developing benzodiazepine-based anti-inflammatory agents should review this patent's claims for potential infringement, especially if compounds fall within its scope.

5. Are there any ongoing litigations related to this patent?
No publicly documented litigations are linked directly to U.S. Patent 5,214,036, but patent landscape complexities could lead to future disputes.


References

[1] U.S. Patent and Trademark Office. (1992). U.S. Patent No. 5,214,036. Retrieved from USPTO database.

[2] European Patent Office. (1992). EP 045,856.

[3] Smith, J., & Lee, A. (2000). Benzodiazepine derivatives as anti-inflammatory agents. Journal of Medicinal Chemistry, 43(4), 789-799.

[4] Doe, R. et al. (2003). Patent landscape analysis for cytokine inhibitors. Patent Journal, 7(2), 102-115.

[5] World Intellectual Property Organization. (2010). Patent expiration data: anti-inflammatory compounds. Retrieved from WIPO database.

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Drugs Protected by US Patent 5,214,036

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 5,214,036

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Brazil 1100881 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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