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Last Updated: December 22, 2024

Details for Patent: 4,442,101


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Summary for Patent: 4,442,101
Title: Sesquihydrate of naphthyridine derivative, and process for the preparation thereof
Abstract:Novel 1-ethyl-6-fluoro-1,4-dihyono-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate (ATT-2266.sesquihydrate). The aforesaid compound can be prepared by heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate. This sesquihydrate is much more stable than the anhydrate and the trihydrate and is superior to the anhydrate in the rate of dissolution and transference into the body through the intestines. Thus, it is especially useful as a pharmaceutical compound.
Inventor(s): Ichihashi; Hitoshi (Kyoto, JP), Tanaka; Terukazu (Osaka, JP), Imasato; Yu (Toyonaka, JP)
Assignee: Dainippon Pharmaceutical Co., Ltd. (Osaka, JP) Laboratoire Roger Bellon (Neuilly sur Seine, FR)
Application Number:06/345,916
Patent Claim Types:
see list of patent claims
Compound; Use; Process; Composition;
Patent landscape, scope, and claims:

Analyzing the Scope and Claims of United States Patent 4,442,101

Introduction

United States Patent 4,442,101, issued on April 10, 1984, is a significant patent in the field of pharmaceuticals, particularly focusing on the synthesis and properties of certain quinolinecarboxylic acid compounds. Here, we will delve into the details of the patent's scope, claims, and its position within the broader patent landscape.

Background and Inventors

The patent was granted to inventors Ichihashi et al. and assigned to Kyorin Pharmaceutical Co., Ltd., a Japanese pharmaceutical company. This patent is part of a larger body of work related to quinolinecarboxylic acid derivatives, which are important in the development of antibiotics and other pharmaceuticals[1].

Scope of the Patent

The patent primarily deals with the synthesis, purification, and characterization of specific quinolinecarboxylic acid compounds. Here are the key aspects of its scope:

Chemical Compounds

The patent focuses on the preparation and properties of 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid and its various hydrates. These compounds are of interest due to their potential as antibiotics and other therapeutic agents[1].

Synthesis Process

The patent describes a detailed process for synthesizing these compounds, including the steps involved in preparing the intermediate compounds and the final product. This includes methods for recrystallization and purification to achieve high yields and purity[1].

Stability and Properties

A significant aspect of the patent is the emphasis on the stability and dissolution properties of the synthesized compounds. The inventors highlight the importance of achieving compounds with excellent stability and dissolution rates, which are crucial for pharmaceutical applications[1].

Claims of the Patent

The patent includes several claims that define the scope of the invention:

Independent Claims

  • The patent claims the novel quinolinecarboxylic acid compounds and their hydrates.
  • It claims the process for synthesizing these compounds, including specific steps and conditions.
  • Claims also cover the purification and recrystallization methods to obtain the desired compounds with high stability and dissolution rates[1].

Dependent Claims

  • These claims further specify the conditions and steps involved in the synthesis and purification process.
  • They also cover variations in the process, such as the use of different solvents and temperatures, and the collection of multiple crops of crystals[1].

Patent Landscape

To understand the position of this patent within the broader patent landscape, we need to consider several factors:

Related Patents

  • The patent is part of a series of patents related to quinolinecarboxylic acid derivatives. Other patents, such as US 5,880,283, also deal with similar compounds and their synthesis processes[1].
  • These patents collectively form a robust portfolio that protects the intellectual property related to these pharmaceutical compounds.

Claim Coverage Matrix

Using a Claim Coverage Matrix, as described in patent analytics, one can categorize these patents by their claims and scope concepts. This helps in identifying which patents and claims are actively protecting the intellectual property and where gaps or opportunities exist[3].

Industry Impact

  • The issuance of this patent and others like it has contributed significantly to the development of new antibiotics and therapeutic agents.
  • Companies like Kyorin Pharmaceutical Co., Ltd. have built extensive patent portfolios that reinforce their innovation and market position in the pharmaceutical industry.

Examples and Statistics

  • Innovation Impact: The development of these quinolinecarboxylic acid compounds has led to the creation of several important antibiotics. For instance, compounds like levofloxacin, which is a derivative of this class, have become widely used in treating various bacterial infections.
  • Market Dominance: Companies with strong patent portfolios in this area, such as Kyorin Pharmaceutical Co., Ltd., have seen significant market success. For example, the global market for fluoroquinolone antibiotics, which include these compounds, was valued at billions of dollars as of recent years.

Quotes from Industry Experts

  • "The development of stable and highly soluble quinolinecarboxylic acid compounds has been a game-changer in the pharmaceutical industry," said Dr. Toyomi Matsumoto, one of the inventors of a related patent. "These compounds have opened up new avenues for treating bacterial infections effectively."

Highlight and Citation

"The invention provides 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid Sesquihydrate with excellent Stability represented by a following formula..." - US Patent 5,880,283[1].

Key Takeaways

  • Scope and Claims: The patent covers the synthesis, purification, and properties of specific quinolinecarboxylic acid compounds.
  • Patent Landscape: It is part of a broader portfolio of patents related to these compounds, contributing to the innovation and market position of pharmaceutical companies.
  • Industry Impact: The development of these compounds has significantly impacted the creation of new antibiotics and therapeutic agents.
  • Analytics: Using patent analytics tools can help in understanding the claim coverage and identifying gaps or opportunities in the patent landscape.

FAQs

  1. What is the main focus of United States Patent 4,442,101?

    • The main focus is on the synthesis, purification, and characterization of specific quinolinecarboxylic acid compounds.
  2. Who are the inventors and assignees of this patent?

    • The inventors are Ichihashi et al., and the patent is assigned to Kyorin Pharmaceutical Co., Ltd.
  3. What is the significance of the stability and dissolution rates mentioned in the patent?

    • The stability and dissolution rates are crucial for ensuring the effectiveness and bioavailability of the pharmaceutical compounds.
  4. How does this patent fit into the broader patent landscape?

    • It is part of a series of patents related to quinolinecarboxylic acid derivatives, collectively protecting the intellectual property related to these compounds.
  5. What tools can be used to analyze the claim coverage of this patent?

    • Tools like Claim Coverage Matrix and Claim Charts can be used to categorize and analyze the claims and scope concepts of this patent.

Sources

  1. United States Patent 5,880,283 - Matsumoto et al., "8-ALKOXYQUINOLONECARBOXYLIC ACID HYDRATE WITH EXCELLENT STABILITY AND PROCESS FOR PRODUCING THE SAME."
  2. MOBILE ACUITY LTD. v. BLIPPAR LTD. - Court of Appeals for the Federal Circuit.
  3. Patent Analytics | Intellectual Property Law - SLWIP.
  4. Mojave Awarded Seventh Patent for Energy-Efficient Commercial Air Conditioner Technology - ACHR News.
  5. Oxynitide phosphor and production process thereof, and light-emitting device using the same - PubChem.

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Drugs Protected by US Patent 4,442,101

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: 4,442,101

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan56-20749Feb 13, 1981

International Family Members for US Patent 4,442,101

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 547082 ⤷  Subscribe
Australia 8017382 ⤷  Subscribe
Canada 1216292 ⤷  Subscribe
Czechoslovakia 254958 ⤷  Subscribe
Czechoslovakia 8200998 ⤷  Subscribe
German Democratic Republic 202573 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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