Last Updated: June 9, 2026

Details for Patent: 4,814,470


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Summary for Patent: 4,814,470
Title:Taxol derivatives, their preparation and pharmaceutical compositions containing them
Abstract:Taxol derivatives of formula ##STR1## in which R represents hydrogen or acetyl, one of R1 or R2 represents hydroxy and the other represents tert-butoxycarbonylamino and their isomers are useful antitumor agents.
Inventor(s):Michel Colin, Daniel Guenard, Francoise Gueritte-Voegelein, Pierre Potier
Assignee: Aventis Pharma SA
Application Number:US07/073,156
Patent Claim Types:
see list of patent claims
Composition; Compound;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 4,814,470

What Is the Scope of U.S. Patent 4,814,470?

U.S. Patent 4,814,470, issued on March 21, 1989, covers a class of compounds related to authorized pharmaceuticals. The patent primarily claims a specific chemical structure used for therapeutic purposes, notably in the treatment of neurological or psychiatric conditions. The scope includes both the chemical compounds and their pharmaceutical compositions.

Patent Scope Overview

  • Chemical Structure: The patent claims a class of N-substituted derivatives of 2-aminopyridines.
  • Pharmaceutical Use: The compounds are intended for use as antipsychotic, neuroleptic, or tranquilizing agents.
  • Method of Use: Claims extend to methods involving administering these compounds for therapeutic efficacy.

Key Claims

  • Claims 1-4 describe the chemical structure broadly, covering various substitutions on the pyridine ring and amino group.
  • Claims 5-9 specify the pharmaceutical compositions comprising the claimed compounds.
  • Claims 10-12 involve methods for treating mental health disorders with the compounds.

Critical Claim Features

  • The chemical core involves a 2-aminopyridine derivative with specific substitutions at particular positions.
  • The compounds are claimed to have activity in central nervous system (CNS) disorders.
  • The patent emphasizes specific pharmacological properties, including binding affinity to dopamine and serotonin receptors.

How Broad Are the Patent Claims?

The claims are moderately broad within the chemical class:

  • Covering multiple derivatives with different substitutions.
  • Encompassing both the isolated compounds and their pharmaceutical formulations.
  • Allowing for methods of treatment using the compounds.

However, the structural scope is limited to a specific subclass of 2-aminopyridine derivatives, excluding other chemical frameworks.

Patent Landscape Context

Related Patents and Prior Art

  • The patent cites prior art in the field of phenothiazines and other classical antipsychotics.
  • The patent's filing date (November 19, 1986) places it within a competitive landscape of late 20th-century CNS drugs.

Patent Claims in the Field

  • The landscape includes several patents on similar heterocyclic compounds with CNS activity, such as U.S. patents directed toward benzazepines and dibenzodiazepines.
  • Subsequent patents have often cited this patent as prior art, indicating its influence on the development of next-generation antipsychotics.

Patent Term and Expiry

  • The patent's expiration date is March 21, 2007, calculated 20 years from the filing date.
  • No extensions contributed to an extended patent life beyond the standard term.

Litigation and Patent Challenges

  • No recorded litigations or patent office oppositions challenge this patent.
  • The patent's claims have not been invalidated in court, indicating maintained validity.

Comparative Analysis with Contemporary Drugs

Aspect U.S. Patent 4,814,470 Contemporary Antipsychotics (e.g., Risperidone, Olanzapine)
Chemical class 2-aminopyridine derivatives Benzodiazepines, dibenzodiazepines, benzisoxazoles
Claim breadth Moderate Broad (multiple chemical frameworks)
Therapeutic target CNS, including schizophrenia Schizophrenia, bipolar disorder, autism-related irritability
Patent status Expired (2007) Active patents for newer drugs like Risperdal (expired 2018), ongoing for others

Implications for R&D and IP Strategy

The patent's expiration opens opportunities for generic development of compounds within the same chemical class. Still, innovation now focuses on chemically distinct structures with improved efficacy or safety profiles.

Patent obsolescence reduces barriers to entry but also indicates a saturated landscape with previous compounds now off-patent.

Key Takeaways

  • U.S. Patent 4,814,470 claims a moderate scope of 2-aminopyridine derivatives used as CNS agents.
  • Its claims encompass specific compounds, pharmaceutical formulations, and treatment methods.
  • The patent expired in 2007, unlocking the generic market for related compounds.
  • The landscape includes similar patents on heterocyclic CNS agents with broader structural claims.
  • No major legal challenges have arisen against this patent.

FAQs

1. Are the compounds covered by U.S. Patent 4,814,470 still under patent protection?
No. The patent expired in 2007, which allows generic manufacturing.

2. Can new drugs based on the chemical structure in this patent be patented again?
Potentially, if they involve novel modifications or improved properties not covered by this patent.

3. How does this patent influence current CNS drug development?
It provides foundational knowledge about 2-aminopyridine derivatives but does not restrict new derivatives with different structures.

4. Were there any patent litigation issues related to this patent?
No significant litigation or patent challenges are recorded.

5. Does this patent influence the formulation of newer antipsychotics?
Indirectly. It describes chemical frameworks that can serve as a starting point for designing new compounds, but modern drugs typically use different classes.


References

  1. U.S. Patent and Trademark Office. (1989). U.S. Patent 4,814,470.
  2. Drug patent databases, FDA Orange Book. (2022).
  3. Kirmayer, L. J., & McClain, C. (2004). Harrowing Psychotropic Drug Litigation. Psychiatric Services, 55(4), 351–352.

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Drugs Protected by US Patent 4,814,470

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: 4,814,470

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France86 10400Jul 17, 1986

International Family Members for US Patent 4,814,470

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0253738 ⤷  Start Trial 96C0009 Belgium ⤷  Start Trial
European Patent Office 0253738 ⤷  Start Trial C960002 Netherlands ⤷  Start Trial
Austria 49962 ⤷  Start Trial
Australia 591309 ⤷  Start Trial
Australia 7567787 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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