Detailed Analysis of the Scope and Claims of United States Patent 6,133,260
Introduction
United States Patent 6,133,260, titled "Use of 7-(2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-quinolone carboxylic acid and naphthyridone carboxylic acid derivatives," is a significant patent in the field of pharmaceuticals, particularly focusing on the treatment of various infections using quinolone and naphthyridonecarboxylic acid derivatives.
Background and Context
The patent, filed on October 25, 1996, and granted on October 17, 2000, addresses the need for new antimicrobial treatments due to the increasing resistance to conventional antibiotics. It falls under the classification of medicinal preparations containing organic active ingredients, specifically heterocyclic compounds with nitrogen as a ring hetero atom[4].
Scope of the Patent
Active Compounds
The patent describes the use of quinolone and naphthyridonecarboxylic acid derivatives substituted in the 7-position by a 2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl group. These compounds are highlighted for their antimicrobial properties, particularly against infections caused by bacteria such as Helicobacter pylori[4].
Specific Compounds
The patent details several specific compounds, including:
- 8-cyano-1-cyclopropyl-6-fluoro-7-(2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
- 1-cyclopropyl-8-difluoromethoxy-6-fluoro-1,4-dihydro-7-(2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-4-oxo-3-quinolinecarboxylic acid
These compounds are described in diastereomerically pure and enantiomerically pure forms, along with their pharmaceutically utilizable hydrates and salts[4].
Claims of the Patent
Therapeutic Uses
The patent claims cover the therapeutic use of these compounds for treating various infections, including:
- Helicobacter pylori infections and associated gastroduodenal diseases.
- Other bacterial infections where conventional treatments are less effective due to microbial resistance[4].
Synthesis Methods
The patent also includes methods for synthesizing these compounds. The synthesis involves several steps, including the preparation of the 2-oxa-5,8-diazabicyclo[4.3.0]nonane intermediate, which can be isolated and purified to high enantiomeric purity[4].
Pharmaceutical Formulations
The claims extend to pharmaceutical formulations of these compounds, including their salts, such as acid addition salts, and alkali metal, alkaline earth metal, silver, and guanidinium salts. These formulations are designed to be pharmaceutically utilizable, enhancing their therapeutic efficacy[4].
Patent Landscape
Related Patents
The patent is part of a broader landscape of patents related to quinolone and naphthyridonecarboxylic acid derivatives. For example, U.S. Patent 6,716,830 also discusses quinolone compounds for treating ophthalmic, otic, and nasal conditions, highlighting the versatility of these compounds across different therapeutic areas[1].
Patent Analytics
To fully understand the protection and coverage of this patent, patent analytics tools can be employed. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in the intellectual property landscape. For instance, using ClaimScape® software, one can generate interactive claim charts to review patent coverage and determine future design opportunities[3].
Legal Status and Extensions
The patent has expired, but there have been efforts to extend its protection. For example, a patent extension application for XTORO, which is based on this patent, was submitted to the FDA in 2016[5].
Key Takeaways
- Innovative Compounds: The patent introduces novel quinolone and naphthyridonecarboxylic acid derivatives with significant antimicrobial properties.
- Therapeutic Applications: It covers the treatment of Helicobacter pylori infections and other bacterial infections, addressing the issue of microbial resistance.
- Synthesis and Formulations: Detailed methods for synthesizing and formulating these compounds are provided.
- Patent Landscape: The patent is part of a larger intellectual property landscape related to quinolone derivatives, requiring careful analysis to understand its full scope and coverage.
FAQs
What are the main compounds described in U.S. Patent 6,133,260?
The main compounds are quinolone and naphthyridonecarboxylic acid derivatives substituted in the 7-position by a 2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl group.
What are the therapeutic uses of these compounds?
These compounds are used for treating Helicobacter pylori infections and associated gastroduodenal diseases, as well as other bacterial infections where conventional treatments are less effective.
How are these compounds synthesized?
The synthesis involves preparing the 2-oxa-5,8-diazabicyclo[4.3.0]nonane intermediate and then integrating it into the quinolone or naphthyridonecarboxylic acid framework.
What is the current legal status of this patent?
The patent has expired, but there have been efforts to extend its protection through applications like the one submitted for XTORO.
How can patent analytics help in understanding this patent?
Patent analytics tools help in categorizing patents by claims and scope concepts, identifying gaps or opportunities in the intellectual property landscape, and generating interactive claim charts to review patent coverage.
Sources
- US8536167B2 - Methods for treating ophthalmic, otic, or nasal infections - Google Patents
- US-6133260-A | Unified Patents - Unified Patents Portal
- Patent Analytics | Intellectual Property Law - Schwegman
- US6133260A - Use of 7-(2-oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-quinolone carboxylic acid and naphthyridon carboxylic acid derivatives - Google Patents
- Patent Extension Application for XTORO Patent No. 6133260 - FDA Docket Details
