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Last Updated: December 28, 2024

Details for Patent: 5,705,517


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Summary for Patent: 5,705,517
Title: Benzimidazole derivatives and use thereof
Abstract:Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R' is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.
Inventor(s): Naka; Takehiko (Kobe, JP), Nishikawa; Kohei (Kyoto, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:08/131,667
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

United States Patent 5,705,517: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 5,705,517, titled "Benzimidazole derivatives and use thereof," is a significant patent that pertains to novel benzimidazole derivatives with potent pharmacological actions. This patent is crucial for understanding the development and application of these compounds in treating various circulatory system diseases.

Background and Context

The patent, filed in 1993 and granted in 1998, is part of a broader research effort into angiotensin II antagonists. Angiotensin II is a key component of the renin-angiotensin system, which regulates blood pressure, fluid balance, and electrolyte balance in the body. The invention described in this patent aims to provide therapeutic agents for treating conditions such as hypertension, heart diseases, strokes, and renal failures[1].

Scope of the Invention

The patent covers novel benzimidazole derivatives that exhibit strong anti-hypertensive activity and angiotensin II antagonistic action. These compounds are designed to interact with the renin-angiotensin system, thereby controlling systemic blood pressure and fluid balance.

Chemical Structure

The benzimidazole derivatives are represented by a specific formula, which includes a benzene ring with various substituents. Key components of the formula include:

  • Ring A: A benzene ring that may contain additional substitutions.
  • R1: Hydrogen or an optionally substituted hydrocarbon residue.
  • R2: A group capable of forming an anion or a group convertible thereinto.
  • X: A direct bond or a spacer with an atomic length of two or less between the phenylene and phenyl groups.
  • R': Carboxyl, an ester thereof, an amide thereof, or a group capable of forming an anion.
  • Y: --O--, --S(O)m--, or --N(R4)--, where m is an integer of 0, 1, or 2, and R4 is hydrogen or an optionally substituted alkyl group[1].

Claims

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

Compound Claims

Claims related to the specific chemical structure of the benzimidazole derivatives, including the various substituents and their positions on the benzene ring.

Method Claims

Claims related to the methods of preparing these compounds and their pharmaceutical compositions.

Use Claims

Claims related to the therapeutic use of these compounds in treating circulatory system diseases, such as hypertension, heart diseases, strokes, and renal failures[1].

Patent Landscape

Understanding the patent landscape is crucial for identifying gaps, opportunities, and the competitive environment.

Related Patents and Technologies

Other patents in the field of angiotensin II antagonists, such as those related to candesartan cilexetil, provide context on the broader therapeutic category. Candesartan cilexetil, for example, is another type-1 angiotensin II receptor antagonist used to treat hypertension and related conditions[4].

Claim Coverage and Scope Concepts

Analyzing the claims and scope concepts of this patent, as well as related patents, helps in identifying the coverage and potential gaps. Tools like Claim Coverage Matrix and ClaimScape® software can be used to categorize and analyze large numbers of patent claims, making it easier to determine the applicability of these scope concepts to target products or methods[3].

Therapeutic Applications

The benzimidazole derivatives covered by this patent are intended for treating a range of circulatory system diseases, including:

Hypertensive Diseases

These compounds are designed to lower blood pressure by antagonizing the effects of angiotensin II.

Heart Diseases

Conditions such as hypercardia, heart failure, and cardiac infarction can be treated using these therapeutic agents.

Strokes and Cerebral Apoplexy

By controlling blood pressure and fluid balance, these compounds can help prevent or manage strokes and cerebral apoplexy.

Renal Diseases

Nephritis and other renal failures can be treated or managed with these benzimidazole derivatives[1].

Pharmaceutical Compositions and Administration

The patent also describes pharmaceutical compositions containing these benzimidazole derivatives and methods for their administration. These compositions are formulated to be effective in treating the aforementioned circulatory system diseases[1].

Expiration and Maintenance Fees

The patent has expired due to the natural lifetime of patents, typically 20 years from the filing date. Maintenance fees, which are required to keep a patent in force, were not relevant after the patent's expiration[2].

Key Takeaways

  • Novel Benzimidazole Derivatives: The patent covers new compounds with potent anti-hypertensive and angiotensin II antagonistic activities.
  • Therapeutic Applications: These compounds are useful in treating hypertension, heart diseases, strokes, and renal failures.
  • Chemical Structure: The compounds are defined by a specific formula with various substituents on a benzene ring.
  • Claims and Scope: The patent includes claims related to the compounds, methods of preparation, and therapeutic use.
  • Patent Landscape: Understanding related patents and technologies is crucial for identifying gaps and opportunities.

Frequently Asked Questions (FAQs)

What is the primary use of the benzimidazole derivatives described in US Patent 5,705,517?

The primary use is to treat circulatory system diseases such as hypertension, heart diseases, strokes, and renal failures by antagonizing angiotensin II.

How do these compounds interact with the body?

These compounds interact with the renin-angiotensin system, controlling systemic blood pressure and fluid balance by antagonizing the effects of angiotensin II.

What is the significance of the chemical structure described in the patent?

The chemical structure defines the specific benzimidazole derivatives covered by the patent, including the various substituents and their positions on the benzene ring.

Are there other similar patents in this therapeutic category?

Yes, other patents like those related to candesartan cilexetil also cover type-1 angiotensin II receptor antagonists used to treat similar conditions.

Why is understanding the patent landscape important?

Understanding the patent landscape helps in identifying gaps, opportunities, and the competitive environment, which is crucial for strategic decision-making in research and development.

Cited Sources:

  1. US5705517A - Benzimidazole derivatives and use thereof - Google Patents
  2. Patent and Trademark Office Notices - USPTO
  3. Patent Analytics | Intellectual Property Law - SLWIP
  4. Candesartan cilexetil: Uses, Interactions, Mechanism of Action - DrugBank

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Drugs Protected by US Patent 5,705,517

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: 5,705,517

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan2-113148Apr 19, 1990
Japan2-141942May 30, 1990
Japan2-208662Aug 06, 1990

International Family Members for US Patent 5,705,517

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0459136 ⤷  Subscribe SPC/GB97/018 United Kingdom ⤷  Subscribe
European Patent Office 0459136 ⤷  Subscribe C970044 Netherlands ⤷  Subscribe
European Patent Office 0459136 ⤷  Subscribe 98C0016 Belgium ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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