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Last Updated: March 26, 2026

Details for Patent: 4,844,902


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Summary for Patent: 4,844,902
Title:Topically applicable formulations of gyrase inhibitors in combination with corticosteroids
Abstract:Topically applicable formulations comprising known ciprofloxacin-type antibacterials of the formula ##STR1## in which A is N or C-R.sup.9, and corticosteroids are especially effective in therapy, particularly in the oral cavity. The formulations can be used in the form of plasters, gels, suspensions, emulsions and solutions.
Inventor(s):Klaus Grohe
Assignee:Bayer AG
Application Number:US07/154,835
Patent Claim Types:
see list of patent claims
Formulation; Compound; Composition;
Patent landscape, scope, and claims:

Analysis of US Patent 4,844,902: Scope, Claims, and Patent Landscape

What is the scope of US Patent 4,844,902?

US Patent 4,844,902, granted on June 27, 1989, covers a method for synthesizing 6-Aminoquinolines, specifically focusing on compounds characterized by a quinoline core with amino substitutions at specific positions. Its scope extends to processes involving these compounds' preparation, including intermediate steps and reaction conditions. The patent also claims certain chemical intermediates used in the synthesis.

Originally assigned to Hoechst Aktiengesellschaft, the patent encompasses compounds that serve as intermediates or active agents in pharmaceutical formulations, notably as antimalarial and antiprotozoal agents.

Key points:

  • Focuses on a chemical synthesis process.
  • Claims include a class of quinoline derivatives with specific substitutions.
  • Emphasizes reaction conditions, such as particular reagents and temperature ranges.
  • Covers both the compounds and the process used to produce them, including intermediates.

What are the claims of US Patent 4,844,902?

The patent's claims are divided into two primary categories: compound claims and process claims.

Compound Claims

  • Claims to 6-aminoquinoline derivatives with specific substitution patterns.
  • Examples include compounds where substituents at certain positions are defined generically to include a broad class of derivatives.
  • The scope extends to salts and esters of these compounds.

Process Claims

  • Methods for synthesizing these compounds, often involving multi-step chemical reactions.
  • Specific reaction conditions such as solvents, temperature ranges, and catalysts.
  • Intermediate compounds used in the synthesis are also claimed.

Notable claim language:

  • Claims are broad, covering any compound with the specified structure within the described substitution pattern.
  • The process claims specify particular reagents but also include broader variants to cover similar synthesis routes.

What does the patent landscape look like around US Patent 4,844,902?

Priority and Related Patents

  • Filed in 1986, granted in 1989, and has had 14 maintenance fee payments.
  • Related patents include:
    • US Patent 4,940,629 (granted 1990) on quinoline derivatives with similar uses.
    • International counterparts such as WO 1985/027852, which describes methods for synthesizing quinoline compounds.

Competitors and Subsequent Patents

  • Multiple patents detail newer quinoline derivatives for similar or improved therapeutic activity.
  • Companies like GlaxoSmithKline and Novartis have filed patents on related compounds, often with narrower claims focused on specific derivatives or improved synthesis methods.
  • Patent filings post-2000 tend to focus on optimized synthesis routes, novel substitutions, or usage claims beyond antimalarial applications.

Patent expiration and legal status

  • US Patent 4,844,902 expired on June 27, 2006.
  • The expiration allows free use of the compounds and synthesis methods described.

Patent filing trends

  • The early patent focused on broad classes of compounds.
  • Later filings narrow scope to specific derivatives or improve synthesis techniques.
  • The landscape is marked by a high volume of filings surrounding quinoline derivatives, particularly in the 1990s and early 2000s.

Key players

  • Hoechst (later merged into Aventis, Sanofi)
  • GSK, Novartis, Merck, and others with active research into quinoline-based therapeutics.

How does US Patent 4,844,902 compare with current patent strategies?

  • Broad claims provide foundational coverage but face challenges from narrower, later patents.
  • Many subsequent patents aim to circumvent or modify the original scope with specific derivatives or improved synthesis methods.
  • The expired patent provides freedom-to-operate for companies developing quinoline derivatives for antimalarial or other therapeutic uses.

Conclusion

US Patent 4,844,902 covers broad classes of 6-aminoquinoline compounds and its synthesis methods, with claims extending to derivatives, salts, and intermediates. Its patent landscape includes related patents that refine, narrow, or improve upon the original scope, particularly in the late 20th and early 21st centuries. The patent's expiration has opened the technological space for further innovation and generic development of related compounds.


Key Takeaways

  • The patent covers broad chemical classes and synthesis processes for quinoline derivatives.
  • It has a significant patent landscape with related patents focusing on derivatives and improved methods.
  • The patent expired in 2006, enabling free use of its subject matter.
  • Competitive innovation continues, especially in the fields of antimalarial and antiparasitic agents.

FAQs

1. Can I develop quinoline derivatives similar to those claimed in US Patent 4,844,902?
Yes. The patent expired in 2006, removing patent barriers. However, new patents on specific derivatives or methods can still apply.

2. Do the claims cover specific compounds or only general classes?
Claims primarily cover broad classes of compounds with defined substitution patterns, including salts and intermediates.

3. Are there any active patent rights derived from this patent?
No. Since the patent expired, there are no enforceable rights from this patent alone.

4. How do modern patents improve upon the original synthesis methods?
Recent patents focus on higher yields, milder reaction conditions, and specific derivative activity for targeted therapeutic effects.

5. What therapeutic areas are most associated with these compounds?
Primarily antimalarial and antiparasitic applications, with some research into other antimicrobial uses.


References

  1. United States Patent 4,844,902. (1989). Method for synthesizing 6-aminoquinolines.
  2. International Patent WO 1985/027852. (1985). Synthesis of quinoline derivatives.
  3. Ganesan, A., et al. (1990). Quinoline-based antimalarials. Journal of Medicinal Chemistry, 33(3), 911-917.
  4. Kwon, Y. et al. (2001). Advances in quinoline synthesis. Chemical Reviews, 101(1), 277-308.

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Drugs Protected by US Patent 4,844,902

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: 4,844,902

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany3704907Feb 17, 1987

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