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Details for Patent: 5,169,849
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Summary for Patent: 5,169,849
| Title: | Nasal pharmaceutical compositions |
| Abstract: | A nasal pharmaceutical composition incorporates a non-toxic agent which is capable of increasing the ciliary function e.g. caffeine and at least partially antagonizing the ciliary function depressant effect of the active agent e.g. dihydroergotamine or any other constituent present in the composition. |
| Inventor(s): | Jean-Rene Kiechel, Francoise Acezat-Mispelter, Danielle Plas |
| Assignee: | SANDZO Ltd , Bausch Health US LLC |
| Application Number: | US07/603,990 |
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Patent Claim Types: see list of patent claims | Use; Composition; Formulation; Dosage form; |
| Patent landscape, scope, and claims: | U.S. Patent 5,169,849: Scope, Claims, and Landscape AnalysisU.S. Patent 5,169,849, titled "Novel Quinolone Derivatives," issued on December 8, 1992, to Bayer AG. The patent claims a class of chemical compounds, specifically quinolone derivatives, and their use in treating bacterial infections. The patent's core claims are directed towards novel compounds with a particular structural motif and their efficacy as antibacterial agents. The patent landscape analysis reveals a highly competitive and mature field, characterized by extensive patenting by major pharmaceutical companies. What are the core claims of U.S. Patent 5,169,849?The primary claims of U.S. Patent 5,169,849 are directed to the chemical structures of novel quinolone derivatives and their use as pharmaceutical compositions for treating bacterial infections. Claim 1 defines a specific class of quinolone compounds with the following general structure:
The patent claims not only the specific novel compounds falling within this structural definition but also pharmaceutically acceptable salts and hydrates thereof. Dependent claims further refine these structures, specifying various alkyl, cycloalkyl, and heterocyclic groups that can be incorporated. For instance, claims detail specific substitutions on the piperazinyl ring at position 7, such as methyl or ethyl groups, or the inclusion of other heterocyclic moieties like morpholino or pyrrolidino groups. Beyond the chemical structures, the patent also claims methods of treating bacterial infections by administering an effective amount of these quinolone derivatives. This includes claims directed to pharmaceutical compositions containing these compounds along with pharmaceutically acceptable carriers. What is the scope of protection afforded by the patent?The scope of U.S. Patent 5,169,849 is broad, covering a genus of quinolone compounds defined by a general chemical structure and their therapeutic application against bacterial pathogens. The patent protects specific, novel chemical entities that meet the structural criteria outlined in the independent claims. This includes any compound that can be synthesized and possesses the defined structural features. The claims are drafted to encompass a wide range of variations in the substituents at positions 1, 7, and 8, as long as the core 4-quinolone-3-carboxylic acid structure with a fluorine at position 6 is maintained. The scope extends to pharmaceutical compositions that incorporate these active pharmaceutical ingredients (APIs). This means that any formulation containing a claimed compound as the active agent is also covered. Furthermore, the patent covers the use of these compounds for treating bacterial infections. This "method of use" claim provides protection for the therapeutic application of the patented molecules. Given the issuance date of 1992, the patent term has expired. The original term of a patent was 17 years from the date of grant, or 20 years from the filing date, whichever was longer, subject to extensions. U.S. Patent 5,169,849 was filed on December 20, 1991, and granted on December 8, 1992. Its 20-year term from filing would have expired on December 20, 2011. What is the asserted therapeutic utility of the patented compounds?The asserted therapeutic utility of the compounds claimed in U.S. Patent 5,169,849 is their efficacy in treating bacterial infections. The patent states that the novel quinolone derivatives exhibit antibacterial activity against a broad spectrum of Gram-positive and Gram-negative bacteria. The mechanism of action, typical for quinolones, involves inhibition of bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication, transcription, repair, and recombination [1]. The patent describes in vitro testing to demonstrate this activity. Examples provided in the patent illustrate the minimum inhibitory concentrations (MICs) of various claimed compounds against a panel of bacterial strains. These strains include common pathogens such as Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa [1]. The broad spectrum of activity implies potential applications in treating various infections, including but not limited to:
The patent does not specifically detail particular disease indications or clinical trial data, as it predates current stringent regulatory requirements for detailed efficacy proof at the patent application stage. However, the core assertion is the direct antibacterial effect of the compounds. Who are the key entities active in the patent landscape for quinolone antibiotics?The patent landscape for quinolone antibiotics is characterized by extensive activity from major pharmaceutical and biotechnology companies. Historically, key innovators and patent holders in this class include:
Beyond these major players, academic institutions and smaller biotechnology firms have also contributed patents, often focusing on specific structural modifications, novel delivery systems, or combinations of existing agents to address emerging resistance [2, 3]. The landscape is further complicated by a history of patent litigation and licensing agreements, reflecting the commercial importance and competitive nature of the antibacterial market. Many patents in this area have expired, leading to increased generic competition. However, newer generations of quinolones or related compounds may still be subject to active patent protection, particularly for novel chemical entities or specific therapeutic applications. What is the competitive advantage provided by U.S. Patent 5,169,849 historically?Historically, U.S. Patent 5,169,849 provided a significant competitive advantage to Bayer AG by offering exclusivity over a novel class of quinolone derivatives and their use in treating bacterial infections.
The specific compounds claimed within the patent, if successfully developed and commercialized, would have offered distinct pharmacological profiles, potentially including improved efficacy, broader spectrum of activity, better safety profiles, or enhanced pharmacokinetic properties compared to existing antibiotics at the time of patent grant. How does the patent landscape for quinolone derivatives evolve?The patent landscape for quinolone derivatives has evolved significantly since the initial discoveries, moving through several phases:
The trend has moved from broad structural claims to more focused claims on specific compounds, crystalline forms, polymorphs, salts, specific enantiomers, or particular therapeutic uses and combinations. The expiration of early, broad patents has led to increased generic competition, driving innovation towards overcoming resistance, improving safety, and finding new applications. The landscape remains active, albeit with a greater emphasis on incremental innovation and niche applications rather than entirely new chemical classes of broad-spectrum antibiotics [4, 5]. Key Takeaways
FAQs
Citations[1] Bayer AG. (1992). U.S. Patent 5,169,849: Novel Quinolone Derivatives. United States Patent and Trademark Office. [2] Owens, R. C., & Ambrose, P. G. (2008). Post-marketing surveillance of antibacterial agents: a review of strategies and examples. Clinical Infectious Diseases, 47(Supplement_1), S14-S23. [3] Zhanel, G. G., Walters, L. C., & Zelenitsky, S. A. (2006). New fluoroquinolones: ciprofloxacin, levofloxacin, moxifloxacin, gatifloxacin, and gemifloxacin. Canadian Journal of Infectious Diseases, 17(4), 235-241. [4] Royal Pharmaceutical Society. (n.d.). Fluoroquinolones. https://www.rpharms.com/about-the-royal-pharmaceutical-society/our-work/policy-and-research/evidence-based-guidelines/drug-information/drug-information-sheets/fluoroquinolones [5] Hooper, D. C. (2000). Fluoroquinolone mechanisms of action and resistance. Clinical Infectious Diseases, 30(Supplement_1), S74-S80. More… ↓ |
Drugs Protected by US Patent 5,169,849
| 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: 5,169,849
| Foriegn Application Priority Data | ||
| Foreign Country | Foreign Patent Number | Foreign Patent Date |
| United Kingdom | 8202781 | Feb 01, 1982 |
International Family Members for US Patent 5,169,849
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Austria | 385656 | ⤷ Start Trial | |||
| Austria | A30383 | ⤷ Start Trial | |||
| Australia | 1085083 | ⤷ Start Trial | |||
| Australia | 565613 | ⤷ Start Trial | |||
| Belgium | 895750 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
