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Last Updated: December 23, 2024

Details for Patent: 6,949,527


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Summary for Patent: 6,949,527
Title: 6-Mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block
Abstract:Disclosed is a 6-mercapto-cyclodextrin derivative having a general formula (I, ) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C.sub.1-6) alkylene, optionally substituted with 1-3 OH groups, or (CH.sub.2).sub.o -phenylene-CH.sub.2).sub.p --; o and p are independently 0-4; X is COOH, CONHR.sub.3, NHCOR.sub.2, SO.sub.2 OH, PO(OH).sub.2, O(CH.sub.2 --CH.sub.2 --O).sub.q --H, OH or tetrazol-5-yl: R.sub.2 is H or (C.sub.1-3)alkyl; R.sub.2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.
Inventor(s): Zhang; Mingqiang (Montreal, CA), Palin; Ronald (Near Kilsyth, GB), Bennett; David Jonathan (Edinburgh, GB)
Assignee: Akzo Nobel N.V. (Arnhem, NL)
Application Number:10/603,355
Patent Claim Types:
see list of patent claims
Compound; Device; Use;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 6,949,527

Introduction

United States Patent 6,949,527, titled "6-Mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block," is a significant patent in the field of pharmaceuticals, particularly in the area of neuromuscular blockade reversal. Here, we will delve into the scope, claims, and patent landscape of this invention.

Background

Neuromuscular blocking agents are commonly used in surgical procedures to facilitate muscle relaxation. However, reversing these blocks is crucial to restore normal muscle function post-surgery. The patent in question addresses this need by introducing 6-mercapto-cyclodextrin derivatives as effective reversal agents.

Scope of the Invention

Overview of 6-Mercapto-Cyclodextrin Derivatives

The patent describes the synthesis and use of 6-mercapto-cyclodextrin derivatives as reversal agents for drug-induced neuromuscular block. These derivatives are modified cyclodextrins, which are cyclic oligosaccharides known for their ability to form inclusion complexes with various molecules[1][2].

Application in Neuromuscular Blockade Reversal

The primary application of these derivatives is in the reversal of neuromuscular blockade induced by drugs such as mivacurium, pancuronium, and atracurium. The 6-mercapto-cyclodextrin derivatives act by binding to the neuromuscular blocking agents, thereby reducing their effectiveness and allowing muscle function to return[1].

Claims of the Patent

Independent Claims

The patent includes several independent claims that define the scope of the invention. These claims cover:

  • The 6-mercapto-cyclodextrin derivatives themselves, including their chemical structure and synthesis methods.
  • The use of these derivatives as reversal agents for drug-induced neuromuscular block.
  • Pharmaceutical compositions containing these derivatives and methods for their administration[1].

Dependent Claims

Dependent claims further specify the scope by detailing:

  • Specific types of cyclodextrins, such as gamma-cyclodextrin, and their derivatives.
  • Various salts and esters of the 6-mercapto-cyclodextrin derivatives.
  • Methods for preparing and purifying these compounds.
  • Dosage forms and administration routes, including injections and infusions[1][2].

Patent Landscape

Related Patents and Technologies

The patent landscape surrounding US 6,949,527 includes other patents related to cyclodextrin derivatives and their applications. For example, patents like WO2001040316A1 also describe the use of 6-mercapto-cyclodextrin derivatives as reversal agents, highlighting the broader interest in this technology[2].

Competing Technologies

Other reversal agents and methods exist, but the use of 6-mercapto-cyclodextrin derivatives offers a unique approach due to their high specificity and efficacy in reversing neuromuscular block. This differentiates the invention from other reversal agents that may have different mechanisms of action or side effect profiles[1].

Patent Analytics and Claim Coverage

To fully understand the protection and coverage provided by 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 patent landscape. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to 6-mercapto-cyclodextrin derivatives[3].

Manufacturing and Preparation

Synthesis Methods

The patent details various methods for synthesizing the 6-mercapto-cyclodextrin derivatives, including the use of organic bases and specific reaction conditions. These methods are crucial for ensuring the purity and efficacy of the final product[1].

Purification and Characterization

The invention also includes methods for purifying and characterizing the derivatives, such as using electrospray ionization mass spectrometry and liquid chromatography mass spectrometry. These techniques are essential for ensuring the quality and consistency of the reversal agents[1].

Clinical and Preclinical Studies

In Vivo Studies

The patent references in vivo studies where the 6-mercapto-cyclodextrin derivatives were tested for their efficacy in reversing neuromuscular block. These studies involved continuous infusion of a neuromuscular blocking agent and subsequent administration of the reversal agent to measure muscle contraction force[1][2].

Safety and Efficacy

The data from these studies indicate that the 6-mercapto-cyclodextrin derivatives are highly effective and safe for use in clinical settings. The reversal of neuromuscular block was achieved rapidly and without significant side effects, making these derivatives a valuable addition to surgical protocols[1].

Regulatory and Legal Status

Patent Expiration

The patent has expired, which means that the intellectual property protection for the 6-mercapto-cyclodextrin derivatives as described in this patent is no longer in effect. This opens up the possibility for other companies to develop and market similar products without infringing on the original patent[1].

Global Implications

The expiration of this patent has global implications, as it allows for the widespread use and development of 6-mercapto-cyclodextrin derivatives without the need for licensing or royalties. This can lead to increased accessibility and potentially lower costs for these reversal agents[1].

Conclusion

United States Patent 6,949,527 has played a significant role in the development of reversal agents for drug-induced neuromuscular block. The 6-mercapto-cyclodextrin derivatives described in this patent offer a highly effective and safe solution for reversing neuromuscular blockade, which is crucial in surgical procedures.

Key Takeaways

  • Effective Reversal Agents: 6-Mercapto-cyclodextrin derivatives are highly effective in reversing drug-induced neuromuscular block.
  • Synthesis and Purification: Specific methods for synthesizing and purifying these derivatives are detailed in the patent.
  • Clinical Efficacy: In vivo studies have demonstrated the safety and efficacy of these reversal agents.
  • Patent Expiration: The patent has expired, allowing for broader use and development of these derivatives.
  • Global Implications: The expiration of the patent has global implications, potentially increasing accessibility and reducing costs.

FAQs

Q: What are 6-mercapto-cyclodextrin derivatives used for?

A: These derivatives are used as reversal agents for drug-induced neuromuscular block, helping to restore muscle function after surgical procedures.

Q: How do 6-mercapto-cyclodextrin derivatives work?

A: They work by binding to the neuromuscular blocking agents, thereby reducing their effectiveness and allowing muscle function to return.

Q: What is the significance of the patent expiration for US 6,949,527?

A: The expiration of the patent means that the intellectual property protection for the 6-mercapto-cyclodextrin derivatives is no longer in effect, allowing other companies to develop and market similar products without infringing on the original patent.

Q: Are 6-mercapto-cyclodextrin derivatives safe for clinical use?

A: Yes, in vivo studies have shown that these derivatives are safe and effective for use in clinical settings, with minimal side effects.

Q: How are 6-mercapto-cyclodextrin derivatives synthesized and purified?

A: The patent details specific synthesis methods using organic bases and purification techniques such as electrospray ionization mass spectrometry and liquid chromatography mass spectrometry.

Sources

  1. US6949527B2 - 6-Mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block - Google Patents
  2. WO2001040316A1 - 6-mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block - Google Patents
  3. Patent Analytics | Intellectual Property Law - SLWIP
  4. US20220096664A1 - Stabilized formulations containing iodinated contrast agents and cyclodextrins - Google Patents
  5. 6-Mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block - PubChem

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Drugs Protected by US Patent 6,949,527

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: 6,949,527

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
99309558Nov 29, 1999

International Family Members for US Patent 6,949,527

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1259550 ⤷  Subscribe 91501 Luxembourg ⤷  Subscribe
European Patent Office 1259550 ⤷  Subscribe CA 2009 00002 Denmark ⤷  Subscribe
European Patent Office 1259550 ⤷  Subscribe 300356 Netherlands ⤷  Subscribe
European Patent Office 1259550 ⤷  Subscribe SPC031/2008 Ireland ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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