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Last Updated: December 22, 2024

Details for Patent: 5,712,298


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Summary for Patent: 5,712,298
Title: Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors
Abstract:Compounds of formula (I), in which one of the substituents R1 or R2 stands for hydrogen, 1-6C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, benzyloxy or totally or partially fluorine-substituted 1-4C-alkoxy, and the other stands for totally or partially fluorine-substituted 1-4C-alkoxy, and R3 stands for phenyl, pyridyl, R31, R32 and R33-substituted phenyl or R34, R35, R36 and R37-substituted pyridyl, in which R31 stands for hydroxy, halogen, cyano, carboxyl, trifluoromethyl 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, amino, mono- or di-1-4C-alkylamino or 1-4C-alkylcarbonylamino; R32 stands for hydrogen, hydroxy, halogen, amino, trifluoromethyl, 1-4C-alkyl or 1-4C-alkoxy; R33 stands for hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy; R34 stands for hydroxy, halogen, cyano, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl or amino; R35 stands for hydrogen, halogen, amino or 1-4C-alkyl; R36 stands for hydrogen or halogen; and R37 stands for hydrogen or halogen. These compounds constitute new effective bronchotherapeutic drugs. ##STR1##
Inventor(s): Amschler; Hermann (Radolfzell, DE)
Assignee: BYK Gulden Lomberg Chemische Fabrik GmbH (Konstanz, DE)
Application Number:08/564,322
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 5,712,298

Introduction

United States Patent 5,712,298, titled "Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors," is a significant patent in the pharmaceutical industry. This patent, granted on January 27, 1998, introduces novel compounds with specific substitutions that enhance their therapeutic properties.

Background of the Invention

The patent builds upon previous research in the field of benzamides, particularly those with phosphodiesterase (PDE) inhibiting properties. Earlier patents, such as International Patent Applications WO92/12961 and WO93/25517, described benzamides with PDE-inhibiting properties and selective PDE-IV inhibitors, respectively[2].

Scope of the Invention

The invention revolves around fluoroalkoxy-substituted benzamides, which are designed to inhibit cyclic nucleotide phosphodiesterases. These compounds are particularly useful in the production of medicaments, especially for bronchotherapeutic applications.

Chemical Structure

The patent describes compounds of the formula I, where various substituents (R1, R2, R3, etc.) can be modified to achieve the desired properties. Key substituents include:

  • R1: Can be hydrogen, 1-6C alkoxy, 3-7C cycloalkoxy, 3-7C cycloalkylmethoxy, benzyloxy, or 1-4C alkoxy partially or completely substituted by fluorine.
  • R2: Can be similar to R1, with specific combinations detailed in the patent.
  • R3: Can be phenyl or pyridyl, with further substitutions by R31, R32, and R33 for phenyl, or R34, R35, R36, and R37 for pyridyl[2][4].

Claims of the Patent

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

Claim 1

This claim describes the general formula of the compounds, including the specific substituents and their possible variations.

Claim 2-8

These claims detail various embodiments of the compounds, including specific combinations of substituents and their therapeutic applications. For example, Claim 2 specifies compounds where R1 is 1-4C alkoxy partially or completely substituted by fluorine, and R2 is methoxy[2].

Therapeutic Applications

The fluoroalkoxy-substituted benzamides are primarily used as cyclic nucleotide phosphodiesterase inhibitors. These inhibitors have significant therapeutic potential, particularly in treating respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

Patent Landscape

Prior Art

The patent references several prior art documents, including European Patent Application 0120352 and other international patent applications. These documents describe earlier work on benzamides and PDE inhibitors but lack the specific fluoroalkoxy substitutions that are the core of this invention[2].

Competitive Landscape

The patent landscape in the field of PDE inhibitors is complex, with multiple patents covering various aspects of benzamide chemistry. This patent distinguishes itself through the novel fluoroalkoxy substitutions, which provide enhanced therapeutic properties.

Intellectual Property Protection

The patent's claims are carefully crafted to protect the intellectual property related to these specific compounds and their use. This protection is crucial for the pharmaceutical industry, where the development and marketing of new drugs are heavily dependent on patent rights.

Analyzing Claims Coverage

To fully understand the patent's coverage, a Claim Coverage Matrix can be useful. This tool categorizes patents by claims and scope concepts, helping to identify gaps or opportunities in the patent landscape. For example, using Schwegman’s ClaimScape® software, one can generate interactive claim charts to review patent coverage and determine if there are gaps in current coverage or future design opportunities[3].

Evaluating the Value of Patent Claims

The value of the patent claims can be evaluated based on their current and potential future impact on the company. High-value claims are those that are directly relevant to current products or methods, while medium-value claims indicate potential future directions. Low-value claims may not be worth maintaining. This evaluation helps in strategic decision-making regarding patent maintenance and future research directions[3].

Conclusion and Future Implications

United States Patent 5,712,298 represents a significant advancement in the field of pharmaceuticals, particularly in the development of bronchotherapeutic drugs. The detailed analysis of its scope and claims highlights the importance of intellectual property protection in the pharmaceutical industry. As the patent landscape continues to evolve, understanding the specific claims and their implications will be crucial for companies looking to innovate and protect their intellectual property.

Key Takeaways

  • The patent introduces novel fluoroalkoxy-substituted benzamides as cyclic nucleotide phosphodiesterase inhibitors.
  • The compounds have specific therapeutic applications, particularly in respiratory diseases.
  • The patent's claims are detailed and protect the intellectual property related to these compounds.
  • Analyzing claims coverage using tools like Claim Coverage Matrix is essential for understanding the patent landscape.
  • Evaluating the value of patent claims helps in strategic decision-making.

FAQs

What are the primary therapeutic applications of the compounds described in US Patent 5,712,298?

The primary therapeutic applications are as bronchotherapeutic drugs, particularly for treating respiratory diseases such as asthma and COPD.

How do the fluoroalkoxy substitutions enhance the therapeutic properties of the benzamides?

The fluoroalkoxy substitutions provide enhanced PDE inhibiting properties, which are crucial for the therapeutic efficacy of the compounds.

What tools can be used to analyze the claims coverage of this patent?

Tools like Schwegman’s ClaimScape® software can be used to generate interactive claim charts and analyze the claims coverage.

Why is intellectual property protection important for this patent?

Intellectual property protection is crucial for the pharmaceutical industry to safeguard the investment in research and development and to prevent unauthorized use of the patented compounds.

How can the value of the patent claims be evaluated?

The value of the patent claims can be evaluated based on their current and potential future impact on the company, categorizing them as high, medium, or low value.

Cited Sources:

  1. US5712298A - Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors - Google Patents.
  2. United States Patent 19 - googleapis.com.
  3. Patent Analytics | Intellectual Property Law - SLWIP.
  4. Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors - Google Patents.
  5. Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors - PubChem.

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Drugs Protected by US Patent 5,712,298

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: 5,712,298

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Switzerland01 996/99Jul 02, 1993
PCT Information
PCT FiledJuly 02, 1994PCT Application Number:PCT/EP94/02169
PCT Publication Date:January 12, 1995PCT Publication Number: WO95/01338

International Family Members for US Patent 5,712,298

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0706513 ⤷  Subscribe 91709 Luxembourg ⤷  Subscribe
European Patent Office 0706513 ⤷  Subscribe C300462 Netherlands ⤷  Subscribe
European Patent Office 0706513 ⤷  Subscribe CA 2010 00028 Denmark ⤷  Subscribe
European Patent Office 0706513 ⤷  Subscribe SPC031/2010 Ireland ⤷  Subscribe
European Patent Office 0706513 ⤷  Subscribe 10C0052 France ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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