Details for Patent: 5,466,700

Summary for Patent: 5,466,700

Title:	Anesthetic use of N-phenyl-N-(4-piperidinyl)amides
Abstract:	The use of particular opioids to induce and maintain anesthesia and conscious sedation is disclosed. The opioids used in the method of the present invention relate to the anesthetic action of the N-phenyl-N-(4-piperidinyl)amides as disclosed in U.S. Pat. No. 5,019,583 to Feldman, et al.
Inventor(s):	Batenhorst; Randal L. (Raleigh, NC), Fox; Anthony W. (Raleigh, NC)
Assignee:	Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:	08/114,032
Patent Claim Types: see list of patent claims	Use;

United States Patent 5,466,700: A Detailed Analysis

Introduction

United States Patent 5,466,700, titled "Anesthetic use of N-phenyl-N-(4-piperidinyl)amides," is a significant patent in the field of anesthesiology, particularly focusing on the use of specific opioid compounds for anesthesia and conscious sedation. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Scope of the Patent

The patent describes a method for the induction and maintenance of anesthesia, as well as conscious sedation, using N-phenyl-N-(4-piperidinyl)amides. These compounds, particularly remifentanil, are highlighted for their potent analgesic properties, rapid onset, and exceptionally short terminal half-life. This short half-life is attributed to their rapid enzymatic metabolism by plasma and tissue esterases, making them ideal for variable rate infusion[1].

Key Compounds and Their Characteristics

• Remifentanil: A specific compound mentioned is methyl[4-(methoxycarbonyl)-4-[(1-oxopropyl)phenylamino]-1-piperidine]-propanoate, monohydrochloride, known as remifentanil. This compound is characterized by its rapid onset and short half-life, which are critical for anesthetic use[1].
• Metabolism: The ester linkage in the pendant chain from the piperidine nitrogen makes these amides susceptible to inactivation by plasma and tissue esterases, contributing to their short half-life[1].

Claims of the Patent

The patent claims include:

• Method of Use: The method of using N-phenyl-N-(4-piperidinyl)amides as primary anesthetics for induction and maintenance of anesthesia and conscious sedation.
• Dosage Levels: The compounds can be administered at dosage levels in excess of those required for inducing and maintaining analgesia without many of the undesirable side effects associated with other opioids[1].
• Pharmaceutically Acceptable Forms: The patent includes claims for pharmaceutically acceptable salts and isomers of these compounds, as well as methods for converting these forms[1].

Patent Landscape Analysis

Geographical Spread and Saturation

• The patent space for anesthetic compounds, particularly opioids, is highly saturated. This saturation indicates a competitive and well-researched area, making it challenging to secure new patents without significant innovation[3].

Competitors and New Entrants

• Major pharmaceutical companies are key players in this patent space. New entrants must navigate a complex landscape of existing patents to avoid infringement and find novel approaches to anesthetic compounds[3].

Time-Slicing and Trends

• Over time, there has been a shift towards compounds with shorter half-lives and fewer side effects, reflecting the industry's focus on safer and more efficient anesthetics. The patent in question aligns with this trend by highlighting the benefits of rapid metabolism[1][3].

Niche Areas

• Despite the saturation, there are niche areas within the anesthetic patent space that focus on specific types of compounds or delivery methods. For example, the development of novel crystalline forms of existing compounds like remifentanil hydrochloride represents a niche area of innovation[5].

Strategic Insights

Patentability and Landscape Analysis

• Conducting a comprehensive patent landscape analysis is crucial for companies considering investment in new drug technologies. This analysis helps in identifying saturated areas and potential opportunities for innovation, guiding long-term R&D decisions[3].

Going Beyond Known Competitors

• A thorough analysis must look beyond known competitors to uncover underappreciated niche areas and emerging trends. This approach can help companies pivot to newer inventive spaces as they observe high levels of patent saturation in mature technology areas[3].

Case Study: Remifentanil

• Remifentanil, a key compound in the patent, has seen significant development and use in clinical settings. Its unique pharmacokinetic profile makes it an ideal choice for various anesthetic procedures. The patent's focus on remifentanil highlights the importance of this compound in the broader landscape of anesthetic drugs[1].

Clinical and Practical Implications

• The use of N-phenyl-N-(4-piperidinyl)amides, such as remifentanil, has significant clinical implications. These compounds offer rapid onset and offset of action, which is beneficial in surgical settings where quick recovery is desired. The short half-life also reduces the risk of prolonged respiratory depression, a common side effect of opioids[1].

Future Directions

• Future research and development in this area may focus on optimizing the delivery methods of these compounds, exploring new formulations, and identifying other compounds with similar or improved profiles. The patent landscape analysis will continue to play a crucial role in guiding these efforts[3].

Key Takeaways

• Innovative Compounds: The patent highlights the use of N-phenyl-N-(4-piperidinyl)amides, particularly remifentanil, for anesthesia and conscious sedation.
• Pharmacokinetics: The rapid onset and short half-life of these compounds make them ideal for clinical use.
• Patent Landscape: The anesthetic patent space is highly saturated, requiring thorough landscape analysis to identify opportunities for innovation.
• Strategic Decisions: Comprehensive patent landscape analysis is essential for guiding R&D and investment decisions in the pharmaceutical industry.

FAQs

1. What are the key compounds discussed in US Patent 5,466,700?

   • The patent focuses on N-phenyl-N-(4-piperidinyl)amides, with a particular emphasis on remifentanil.

2. Why are these compounds ideal for anesthetic use?

   • These compounds have a rapid onset and an exceptionally short terminal half-life due to their rapid enzymatic metabolism.

3. What is the significance of the short half-life of these compounds?

   • The short half-life reduces the risk of prolonged side effects, such as respiratory depression, and makes them suitable for variable rate infusion.

4. How does the patent landscape affect new entrants in the anesthetic drug market?

   • The highly saturated patent space makes it challenging for new entrants to secure new patents without significant innovation.

5. What future directions might research take in this area?

   • Future research may focus on optimizing delivery methods, exploring new formulations, and identifying other compounds with similar or improved profiles.

Sources

1. US5466700A - Anesthetic use of N-phenyl-N-(4-piperidinyl)amides - Google Patents
2. Patent Landscape Analysis - Uncovering Strategic Insights - AcclaimIP
3. US Patent Application for Crystalline Form of Remifentanil - Justia Patents
4. Pharmaceutical drugs covered by patent 5,466,700 - Drug Patent Watch

Drugs Protected by US Patent 5,466,700

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate