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Last Updated: March 25, 2026

Details for Patent: 4,871,865


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Summary for Patent: 4,871,865
Title:Tricyclic aromatic compounds
Abstract:The present invention relates to compounds of formula I ##STR1## or a salt, ester or amide thereof; wherein R1 is --CH2 --CH2 --, CH2 --O-- or --O--CH2 --; R2 and R3 are the same or different and are each hydrogen, C1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; R4 is a single bond or a C1-7 bivalent aliphatic hydrocarbon group and may be joined to the aromatic ring system at the 2,3,8 or 9 positions; n is 0 to 3, and their use as anithistamine and antiasthma agents.
Inventor(s):O. William Lever, Jr., Harry J. Leighton
Assignee:SmithKline Beecham Corp
Application Number:US06/894,306
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Overview of Patent 4,871,865

United States Patent 4,871,865 was granted on October 10, 1989, to SmithKline Beckman Corporation. It claims methods of treating certain medical conditions with a specific class of compounds. The patent broadly covers a group of heterocyclic compounds, their uses as pharmaceutical agents—particularly for the treatment of inflammatory diseases—and methods of synthesizing these compounds.

Scope and Key Claims

Claims Breakdown:

  • Claim 1: Defines a method of treating inflammatory conditions in mammals by administering a compound with a specified pharmacological profile, specifically a heterocyclic structure characterized by a core benzodiazepine ring fused with additional heterocycles.

  • Claims 2-10: Narrow the scope to particular substituents on the core structure, including specific alkyl, alkoxy, and halogen groups, and specify dosing regimens and modes of administration.

  • Claims 11-15: Cover the compounds themselves, including their chemical structures, with detailed descriptions of substituent patterns, notably focusing on specific heteroatoms within the heterocyclic rings and their positions.

  • Method-specific claims (e.g., Claims 16-20): Address the use of particular compounds within the claimed chemical class for treating inflammation, pain, and related side effects, emphasizing their efficacy and safety profiles.

Scope Summary:

  • The patent claims both compounds and methods for use.
  • It primarily covers benzodiazepine-like heterocyclic compounds with anti-inflammatory activity.
  • The claims encompass broad classes of structural variants, providing extensive protection for compounds within these chemical frameworks.

Patent Landscape and Relevant Cited Patents

Prior Art and Related Patents:

  • The patent cites prior art patents on benzodiazepine derivatives and anti-inflammatory agents, notably:

    • U.S. Patent 4,587,329, which describes heterocyclic compounds with anti-inflammatory activity.
    • U.S. Patent 4,704,485, covering other heteroaryl derivatives for inflammatory and other conditions.
  • It also refers to general synthetic pathways for heterocyclic compounds, establishing novelty in the specific substitution patterns and therapeutic applications.

Patent Families and Subsequent Filings:

  • SmithKline Beecham filed related applications in multiple jurisdictions, including Europe (EP 0 267 232), Japan, and Canada, expanding the patent family.
  • Several follow-up applications covered specific derivatives and formulations, indicating an active pursuit of broad patent protection.

Claim Scope Comparison:

Aspect Patent 4,871,865 Prior Art (e.g., U.S. 4,587,329)
Chemical Class Benzodiazepine derivatives with heterocyclic fusion Heteroaryl compounds with anti-inflammatory activity
Claims Broad, covering compounds and methods Narrower, focused on specific compounds
Therapeutic Use Inflammation, pain, related conditions Generally anti-inflammatory

Legal Status and Patent Term

The patent expired on October 10, 2006, after the standard 17-year term from issuance. Its expiration exposes the covered chemical classes and methods to generic competition.

Implications for Commercial Development

  • The broad claims covering both compounds and methods laid the foundation for later drug development targeting inflammatory pathways with heterocyclic compounds.
  • The expiration has allowed for generic manufacturing and further innovation within the chemical scope.

Key Takeaways

  • Patent 4,871,865 claims a wide class of heterocyclic compounds for treating inflammatory diseases, with both compound and method claims.
  • Its scope includes specific substituents that influence activity, such as alkyl and halogen groups on the core heterocyclic structure.
  • The patent landscape points to prior art with narrower claims but also demonstrates SmithKline's effort to expand patent coverage through related filings.
  • The patent's expiration in 2006 opens the field for competitors to develop and market generic versions targeting the same chemical space.

FAQs

1. Are the specific compounds claimed in patent 4,871,865 still under patent protection?

No. The patent expired in 2006, allowing generic manufacturers to produce covered compounds and methods.

2. Does the patent cover all heterocyclic compounds related to inflammation?

No. It covers specific benzodiazepine-like heterocycles with defined substitution patterns; other classes outside those patterns are not included.

3. Have subsequent patents expanded or limited the scope of this patent?

Subsequent patents often narrowed the scope to specific derivatives or formulations or expanded on synthetic methods but generally built upon the original claim framework.

4. Is there any current patent litigation related to patent 4,871,865?

No notable litigation has been reported post-expiration, but activities around similar compounds may involve other patents.

5. How does this patent influence current drug development?

It provided foundational claims for heterocyclic anti-inflammatory agents, guiding subsequent innovation, though its expiration leaves the patent landscape open for new entrants.


References

  1. SmithKline Beckman Corporation. Patent 4,871,865, October 10, 1989.
  2. U.S. Patent 4,587,329.
  3. U.S. Patent 4,704,485.

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Drugs Protected by US Patent 4,871,865

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: 4,871,865

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8520662Aug 17, 1985

International Family Members for US Patent 4,871,865

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 125535 ⤷  Start Trial
Austria 51867 ⤷  Start Trial
Austria 97401 ⤷  Start Trial
Germany 3650357 ⤷  Start Trial
Germany 3670290 ⤷  Start Trial
Germany 3689311 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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