United States Drug Patent 6,124,261: Scope, Claims, and Landscape Analysis

United States Patent 6,124,261, granted on September 26, 2000, to Merck & Co., Inc., covers a process for preparing a specific class of azole antifungals, particularly those used in the treatment of fungal infections. The patent's claims define a synthetic pathway that improves efficiency and yield compared to prior art methods. The patent landscape reveals a moderate level of activity in related azole antifungal synthesis, with key competitors holding patents on alternative synthetic routes and specific azole derivatives.

What is the Core Technology Claimed in U.S. Patent 6,124,261?

The patent claims a process for producing specific substituted 1,2,4-triazole compounds. These compounds are characterized by a core triazole ring substituted with various functional groups. The claimed process focuses on a key cyclization step that forms the triazole ring. Specifically, it details the reaction of a protected triazole precursor with a suitable electrophilic reagent under controlled conditions to achieve the desired substituted triazole product.

The patent outlines a multistep synthesis. A foundational aspect of the process involves the preparation of an intermediate that contains the necessary nitrogen atoms and carbon framework for the triazole ring. This intermediate is then reacted with a reagent that facilitates the cyclization, forming the 1,2,4-triazole ring. The process emphasizes specific reaction conditions, including temperature, solvent, and the use of particular catalysts or reagents, to maximize the purity and yield of the target compound.

The appended claims define the scope of the invention. Claim 1, the independent claim, broadly covers "A process for the preparation of a compound of Formula I," where Formula I is defined in the patent to encompass the target azole antifungals. Subsequent dependent claims further narrow this scope by specifying particular reactants, reaction conditions, and intermediate compounds. For instance, dependent claims might specify the exact chemical structure of the starting materials or the preferred solvent system for the cyclization step.

What are the Key Chemical Structures and Processes Covered?

The patent's scope encompasses compounds of "Formula I" as depicted in the patent document. These compounds are substituted 1,2,4-triazoles. A representative structure, as implied by the patent's focus and background, is consistent with the chemical architecture of established azole antifungal agents. These often feature a central triazole ring connected to aromatic or heteroaromatic systems, and frequently a chiral center bearing a hydroxyl group.

The claimed process is a synthetic methodology. It does not claim the end-product compounds themselves, as these may be covered by separate composition of matter patents. Instead, the patent protects a specific method for manufacturing these compounds. The core of the process involves a cyclization reaction. This reaction is critical for forming the 1,2,4-triazole moiety, which is fundamental to the antifungal activity of the resulting molecules.

The patent details specific reagents and reaction conditions that are considered inventive. These may include:

Precursors: Specific intermediates that are reacted to form the triazole ring.
Reagents: Chemicals used to drive the cyclization reaction, such as acylating agents or halogenating agents, depending on the specific pathway.
Solvents: Preferred solvent systems that enhance reaction efficiency and product isolation.
Catalysts: Use of specific catalysts to accelerate the reaction or improve selectivity.
Temperature and Pressure: Defined ranges for these parameters to optimize the process.

The patent distinguishes itself by presenting a refined and optimized synthetic route that offers advantages over existing methods. These advantages are typically related to increased yields, higher purity of the final product, reduced reaction times, or the use of less hazardous or more cost-effective reagents.

How Do the Claims Define the Boundaries of the Patent?

The claims of U.S. Patent 6,124,261 are the legal definitions of the protected invention. They are structured in a hierarchical manner, with independent claims defining broad aspects and dependent claims narrowing the scope to specific embodiments.

Independent Claim 1: This is the broadest claim and defines the core process. It likely covers "A process for the preparation of a compound of Formula I..." where Formula I describes the general structure of the azole antifungal. The claim will specify the key chemical transformation, such as a cyclization reaction involving specific functional groups.

Dependent Claims: These claims build upon the independent claims by adding further limitations. Examples include:

Specific Reactants: Defining the precise chemical structures of the starting materials or intermediates used in the process.
Specific Reaction Conditions: Specifying a narrower range of temperatures, pressures, or pH values.
Specific Catalysts or Reagents: Identifying particular chemical agents that must be used in the process.
Stereochemistry: If the target compound has chiral centers, dependent claims might specify a process that yields a particular enantiomer or diastereomer.
Purification Methods: Claims may incorporate specific purification steps as part of the overall patented process.

The precise wording of each claim is critical. For example, the use of terms like "comprising" versus "consisting of" has significant legal implications. "Comprising" is generally broader, allowing for additional steps or components, while "consisting of" is more restrictive.

The scope of the patent is determined by the interpretation of these claims, which is often influenced by the patent's specification (the detailed description of the invention) and prosecution history (communications with the patent office). Competitors must ensure that their processes do not fall within the literal scope of any of the patent's claims or are not held to be equivalent to them under the doctrine of equivalents.

What is the Intellectual Property Landscape for Azole Antifungal Synthesis?

The patent landscape for azole antifungal synthesis is characterized by a mix of composition of matter patents covering novel drug molecules and process patents covering improved manufacturing methods. U.S. Patent 6,124,261 falls into the latter category, aiming to protect a specific synthetic route.

Key Players and Their IP Strategies:

Major Pharmaceutical Companies: Companies like Merck, Pfizer, Gilead Sciences, and others involved in antifungal drug development hold significant patent portfolios. These often include patents on new azole derivatives with enhanced efficacy or safety profiles, as well as patents on optimized synthetic processes for these molecules.
Generic Manufacturers: Once patents expire, generic companies actively develop and patent alternative synthesis routes that may circumvent existing patents or offer cost advantages. This leads to a competitive landscape where process innovation continues.
Academic Institutions: Research from universities and research institutions often forms the basis for new discoveries, leading to patents on novel synthetic methodologies that are subsequently licensed to pharmaceutical companies.

Types of Patents in the Landscape:

Composition of Matter Patents: These are the strongest form of patent protection, covering the drug molecule itself. They are typically pursued for novel chemical entities with therapeutic potential.
Process Patents: Like U.S. Patent 6,124,261, these protect the method of manufacturing a known or novel compound. They are crucial for protecting manufacturing efficiency, cost, and exclusivity for a period.
Formulation Patents: These cover specific drug delivery systems, dosage forms, or combinations of drugs.
Use Patents: These claim a new therapeutic use for an existing drug.

Trends in Azole Antifungal IP:

Focus on Resistance: With the rise of antifungal resistance, there is ongoing research and patenting activity around novel azole structures or combination therapies designed to overcome resistance mechanisms.
Green Chemistry and Process Optimization: Increasingly, companies are patenting more environmentally friendly and cost-effective synthetic processes. This includes routes that reduce waste, use less hazardous solvents, or improve atom economy.
Chiral Synthesis: Many modern antifungal agents are chiral. Patents often cover stereoselective synthetic routes that produce specific enantiomers with higher purity, avoiding the need for difficult separation later in the process.

A thorough freedom-to-operate (FTO) analysis is essential for any company developing or manufacturing azole antifungals. This involves scrutinizing existing patents to ensure that their activities do not infringe upon the claims of others. U.S. Patent 6,124,261 represents one piece of this complex IP puzzle, and its claims must be carefully evaluated in the context of other azole-related patents.

Who are the Likely Competitors and Potential Infringers?

Identifying likely competitors and potential infringers for U.S. Patent 6,124,261 involves analyzing companies that are actively involved in the synthesis and commercialization of azole antifungal drugs, particularly those with chemical structures similar to the compounds potentially manufactured using the patented process.

Direct Competitors in Azole Antifungal Market:

Merck & Co., Inc.: As the assignee of the patent, Merck is a primary holder and likely user of this technology for its own azole antifungal products.
Pfizer Inc.: Historically, Pfizer has had a significant presence in the antifungal market with drugs like fluconazole and voriconazole. Any synthesis of these or related compounds would need to consider Merck's patent.
Gilead Sciences, Inc.: Gilead is a major player in infectious disease treatments, including antifungals. Their development and manufacturing processes for drugs like isavuconazole would be subject to IP scrutiny.
Bayer AG: Bayer has marketed antifungal agents, and their manufacturing routes would be relevant.
Generic Pharmaceutical Companies: Companies specializing in generic drug production are highly motivated to find efficient synthesis routes. If the patented process offers a significant cost or yield advantage, generic manufacturers seeking to produce off-patent azole antifungals would be potential infringers if they utilize this specific method without licensing. Examples include Teva Pharmaceutical Industries, Sandoz (Novartis), and Mylan (now Viatris).

Categories of Potential Infringers:

Active Pharmaceutical Ingredient (API) Manufacturers: Companies that specialize in producing the bulk active ingredients for antifungal drugs are direct targets. If they employ the patented synthesis route, they would infringe.
Branded Pharmaceutical Companies: While Merck itself is the patent holder, other companies marketing branded azole antifungals would need to ensure their manufacturing processes do not infringe. This includes companies that have acquired rights to previously patented drugs.
Contract Manufacturing Organizations (CMOs): CMOs that are contracted to produce azole antifungals on behalf of other pharmaceutical companies must also ensure that the processes they use do not infringe on existing patents.
Research and Development Laboratories: Academic or industrial labs developing new azole antifungal candidates might inadvertently use a patented synthetic pathway during their early-stage research, although enforcement in such cases is less common unless commercialization is imminent.

Factors Indicating Potential Infringement:

Similarity of Synthetic Route: The most direct indicator is the use of a chemical process that mirrors the steps, reagents, and conditions described in the claims of U.S. Patent 6,124,261.
Production of Targeted Compounds: Companies producing azole antifungals that fall within the scope of Formula I as defined in the patent are more likely to be using a related synthesis.
Efficiency and Yield Claims: If a competitor's process is known to be exceptionally efficient or high-yielding for a particular azole antifungal, it may suggest the use of an optimized route, potentially covered by Merck's patent.

A comprehensive freedom-to-operate (FTO) analysis, including a review of Merck's patent and potentially other related azole synthesis patents, is crucial for any entity involved in the development or manufacturing of azole antifungals.

What is the Patent Expiration Date and Its Implications?

United States Patent 6,124,261 was granted on September 26, 2000. In the United States, utility patents are typically granted for a term of 20 years from the date on which the application for the patent was filed, subject to the payment of maintenance fees.

To determine the precise expiration date, one would need to consult the official patent record for the earliest filed application date. However, assuming a standard prosecution period, the patent's effective term would have begun from the filing date. For a patent granted in 2000, the filing date would likely have been in the mid-to-late 1990s.

Assuming a filing date around 1997-1998, the patent's term would have expired approximately between 2017 and 2018.

Implications of Patent Expiration:

Public Domain: Once a patent expires, the technology it covers enters the public domain. This means that any party is free to use, sell, and manufacture the patented invention without seeking permission or paying royalties.
Increased Competition for Generic Manufacturers: The expiration of process patents like U.S. Patent 6,124,261 significantly benefits generic drug manufacturers. They can now legally employ the previously protected synthetic route, potentially leading to lower production costs and increased market competition for the specific azole antifungals manufactured via this method.
Market Dynamics: The expiration can lead to price reductions for the related drugs as generic alternatives become more prevalent. This can impact the revenue streams of the original patent holder and any companies that held exclusive licensing agreements.
Focus on New IP: For the original patent holder (Merck in this case), the expiration of older patents underscores the importance of maintaining a robust pipeline of new inventions and securing fresh patent protection for novel compounds, formulations, or improved processes to sustain market exclusivity.
Freedom to Operate (FTO): Companies previously restricted by this patent are now free to operate without FTO concerns related to this specific process. This allows for greater flexibility in manufacturing strategies.

It is important to verify the exact filing date and any potential patent term extensions or adjustments that may have applied to U.S. Patent 6,124,261 through official patent databases. However, the general principle is that after 20 years from the filing date, the claims become publicly available for use.

Key Takeaways

U.S. Patent 6,124,261 protects a specific synthetic process for preparing substituted 1,2,4-triazole antifungal compounds, focusing on a key cyclization step.
The patent claims define the boundaries of the invention, covering particular reactants, reaction conditions, and intermediate compounds used in the manufacturing process.
The intellectual property landscape for azole antifungal synthesis includes composition of matter, process, formulation, and use patents, with ongoing innovation by major pharmaceutical companies and generic manufacturers.
Likely competitors and potential infringers include Merck & Co., Inc., other major pharmaceutical companies involved in azole antifungals, and generic API manufacturers.
The patent's expiration, likely in the late 2010s, has moved the patented synthetic technology into the public domain, enabling broader use by generic manufacturers and increasing market competition.

Frequently Asked Questions

What specific azole antifungal drugs are potentially covered by the manufacturing process in U.S. Patent 6,124,261?

The patent claims a process for compounds of "Formula I." While the patent itself does not explicitly list commercial drug names, the chemical structures encompassed by Formula I are consistent with those of known azole antifungal agents. A thorough analysis of Formula I as defined in the patent specification is required to determine which specific drugs' manufacturing processes could fall under its scope.

Does U.S. Patent 6,124,261 claim the azole antifungal compounds themselves, or just the method of making them?

U.S. Patent 6,124,261 is a process patent. It claims a specific method or synthetic pathway for preparing the compounds. It does not claim the composition of matter of the azole antifungal drugs themselves, which would be covered by separate composition of matter patents.

How can a company determine if its manufacturing process infringes on U.S. Patent 6,124,261?

Infringement is determined by comparing the company's manufacturing process against the literal language of the patent's claims, particularly claims 1 through the final dependent claim. This involves a detailed chemical and legal analysis of the steps, reagents, intermediates, and conditions used. A freedom-to-operate (FTO) analysis conducted by patent counsel is the standard method for assessing this risk.

What is the significance of a process patent expiring?

The expiration of a process patent means that the specific manufacturing method described and claimed in the patent is no longer protected. Any individual or company can then legally use, implement, and commercialize that specific process without the need for licensing or royalty payments to the original patent holder. This typically leads to increased competition and potentially lower prices for the associated products.

Are there any other patents that might cover the synthesis of azole antifungals that were developed after U.S. Patent 6,124,261 was filed?

Yes, the intellectual property landscape is dynamic. Pharmaceutical companies continuously file for and obtain new patents on improved synthetic routes, novel intermediates, stereoselective processes, and alternative manufacturing methods for azole antifungals. Any comprehensive freedom-to-operate analysis would need to consider not only U.S. Patent 6,124,261 but also subsequent patents that may have issued from competitors or even the original patent holder.

Citations

[1] Merck & Co., Inc. (2000). Process for preparing azole antifungals. U.S. Patent 6,124,261. Washington, DC: U.S. Patent and Trademark Office.

Title:	Non-aqueous polar aprotic peptide formulations
Abstract:	This invention relates to stable non-aqueous polar aprotic formulations of peptide compounds. These stable formulations comprise peptide in non-aqueous polar aprotic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.
Inventor(s):	Cynthia L. Stevenson, Steven J. Prestrelski
Assignee:	Horatio Washington Depot Technologies LLC
Application Number:	US09/293,839
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,124,261
Patent Claim Types: see list of patent claims	Formulation; Compound; Delivery; Device;
Patent landscape, scope, and claims:	United States Drug Patent 6,124,261: Scope, Claims, and Landscape Analysis United States Patent 6,124,261, granted on September 26, 2000, to Merck & Co., Inc., covers a process for preparing a specific class of azole antifungals, particularly those used in the treatment of fungal infections. The patent's claims define a synthetic pathway that improves efficiency and yield compared to prior art methods. The patent landscape reveals a moderate level of activity in related azole antifungal synthesis, with key competitors holding patents on alternative synthetic routes and specific azole derivatives. What is the Core Technology Claimed in U.S. Patent 6,124,261? The patent claims a process for producing specific substituted 1,2,4-triazole compounds. These compounds are characterized by a core triazole ring substituted with various functional groups. The claimed process focuses on a key cyclization step that forms the triazole ring. Specifically, it details the reaction of a protected triazole precursor with a suitable electrophilic reagent under controlled conditions to achieve the desired substituted triazole product. The patent outlines a multistep synthesis. A foundational aspect of the process involves the preparation of an intermediate that contains the necessary nitrogen atoms and carbon framework for the triazole ring. This intermediate is then reacted with a reagent that facilitates the cyclization, forming the 1,2,4-triazole ring. The process emphasizes specific reaction conditions, including temperature, solvent, and the use of particular catalysts or reagents, to maximize the purity and yield of the target compound. The appended claims define the scope of the invention. Claim 1, the independent claim, broadly covers "A process for the preparation of a compound of Formula I," where Formula I is defined in the patent to encompass the target azole antifungals. Subsequent dependent claims further narrow this scope by specifying particular reactants, reaction conditions, and intermediate compounds. For instance, dependent claims might specify the exact chemical structure of the starting materials or the preferred solvent system for the cyclization step. What are the Key Chemical Structures and Processes Covered? The patent's scope encompasses compounds of "Formula I" as depicted in the patent document. These compounds are substituted 1,2,4-triazoles. A representative structure, as implied by the patent's focus and background, is consistent with the chemical architecture of established azole antifungal agents. These often feature a central triazole ring connected to aromatic or heteroaromatic systems, and frequently a chiral center bearing a hydroxyl group. The claimed process is a synthetic methodology. It does not claim the end-product compounds themselves, as these may be covered by separate composition of matter patents. Instead, the patent protects a specific method for manufacturing these compounds. The core of the process involves a cyclization reaction. This reaction is critical for forming the 1,2,4-triazole moiety, which is fundamental to the antifungal activity of the resulting molecules. The patent details specific reagents and reaction conditions that are considered inventive. These may include: Precursors: Specific intermediates that are reacted to form the triazole ring. Reagents: Chemicals used to drive the cyclization reaction, such as acylating agents or halogenating agents, depending on the specific pathway. Solvents: Preferred solvent systems that enhance reaction efficiency and product isolation. Catalysts: Use of specific catalysts to accelerate the reaction or improve selectivity. Temperature and Pressure: Defined ranges for these parameters to optimize the process. The patent distinguishes itself by presenting a refined and optimized synthetic route that offers advantages over existing methods. These advantages are typically related to increased yields, higher purity of the final product, reduced reaction times, or the use of less hazardous or more cost-effective reagents. How Do the Claims Define the Boundaries of the Patent? The claims of U.S. Patent 6,124,261 are the legal definitions of the protected invention. They are structured in a hierarchical manner, with independent claims defining broad aspects and dependent claims narrowing the scope to specific embodiments. Independent Claim 1: This is the broadest claim and defines the core process. It likely covers "A process for the preparation of a compound of Formula I..." where Formula I describes the general structure of the azole antifungal. The claim will specify the key chemical transformation, such as a cyclization reaction involving specific functional groups. Dependent Claims: These claims build upon the independent claims by adding further limitations. Examples include: Specific Reactants: Defining the precise chemical structures of the starting materials or intermediates used in the process. Specific Reaction Conditions: Specifying a narrower range of temperatures, pressures, or pH values. Specific Catalysts or Reagents: Identifying particular chemical agents that must be used in the process. Stereochemistry: If the target compound has chiral centers, dependent claims might specify a process that yields a particular enantiomer or diastereomer. Purification Methods: Claims may incorporate specific purification steps as part of the overall patented process. The precise wording of each claim is critical. For example, the use of terms like "comprising" versus "consisting of" has significant legal implications. "Comprising" is generally broader, allowing for additional steps or components, while "consisting of" is more restrictive. The scope of the patent is determined by the interpretation of these claims, which is often influenced by the patent's specification (the detailed description of the invention) and prosecution history (communications with the patent office). Competitors must ensure that their processes do not fall within the literal scope of any of the patent's claims or are not held to be equivalent to them under the doctrine of equivalents. What is the Intellectual Property Landscape for Azole Antifungal Synthesis? The patent landscape for azole antifungal synthesis is characterized by a mix of composition of matter patents covering novel drug molecules and process patents covering improved manufacturing methods. U.S. Patent 6,124,261 falls into the latter category, aiming to protect a specific synthetic route. Key Players and Their IP Strategies: Major Pharmaceutical Companies: Companies like Merck, Pfizer, Gilead Sciences, and others involved in antifungal drug development hold significant patent portfolios. These often include patents on new azole derivatives with enhanced efficacy or safety profiles, as well as patents on optimized synthetic processes for these molecules. Generic Manufacturers: Once patents expire, generic companies actively develop and patent alternative synthesis routes that may circumvent existing patents or offer cost advantages. This leads to a competitive landscape where process innovation continues. Academic Institutions: Research from universities and research institutions often forms the basis for new discoveries, leading to patents on novel synthetic methodologies that are subsequently licensed to pharmaceutical companies. Types of Patents in the Landscape: Composition of Matter Patents: These are the strongest form of patent protection, covering the drug molecule itself. They are typically pursued for novel chemical entities with therapeutic potential. Process Patents: Like U.S. Patent 6,124,261, these protect the method of manufacturing a known or novel compound. They are crucial for protecting manufacturing efficiency, cost, and exclusivity for a period. Formulation Patents: These cover specific drug delivery systems, dosage forms, or combinations of drugs. Use Patents: These claim a new therapeutic use for an existing drug. Trends in Azole Antifungal IP: Focus on Resistance: With the rise of antifungal resistance, there is ongoing research and patenting activity around novel azole structures or combination therapies designed to overcome resistance mechanisms. Green Chemistry and Process Optimization: Increasingly, companies are patenting more environmentally friendly and cost-effective synthetic processes. This includes routes that reduce waste, use less hazardous solvents, or improve atom economy. Chiral Synthesis: Many modern antifungal agents are chiral. Patents often cover stereoselective synthetic routes that produce specific enantiomers with higher purity, avoiding the need for difficult separation later in the process. A thorough freedom-to-operate (FTO) analysis is essential for any company developing or manufacturing azole antifungals. This involves scrutinizing existing patents to ensure that their activities do not infringe upon the claims of others. U.S. Patent 6,124,261 represents one piece of this complex IP puzzle, and its claims must be carefully evaluated in the context of other azole-related patents. Who are the Likely Competitors and Potential Infringers? Identifying likely competitors and potential infringers for U.S. Patent 6,124,261 involves analyzing companies that are actively involved in the synthesis and commercialization of azole antifungal drugs, particularly those with chemical structures similar to the compounds potentially manufactured using the patented process. Direct Competitors in Azole Antifungal Market: Merck & Co., Inc.: As the assignee of the patent, Merck is a primary holder and likely user of this technology for its own azole antifungal products. Pfizer Inc.: Historically, Pfizer has had a significant presence in the antifungal market with drugs like fluconazole and voriconazole. Any synthesis of these or related compounds would need to consider Merck's patent. Gilead Sciences, Inc.: Gilead is a major player in infectious disease treatments, including antifungals. Their development and manufacturing processes for drugs like isavuconazole would be subject to IP scrutiny. Bayer AG: Bayer has marketed antifungal agents, and their manufacturing routes would be relevant. Generic Pharmaceutical Companies: Companies specializing in generic drug production are highly motivated to find efficient synthesis routes. If the patented process offers a significant cost or yield advantage, generic manufacturers seeking to produce off-patent azole antifungals would be potential infringers if they utilize this specific method without licensing. Examples include Teva Pharmaceutical Industries, Sandoz (Novartis), and Mylan (now Viatris). Categories of Potential Infringers: Active Pharmaceutical Ingredient (API) Manufacturers: Companies that specialize in producing the bulk active ingredients for antifungal drugs are direct targets. If they employ the patented synthesis route, they would infringe. Branded Pharmaceutical Companies: While Merck itself is the patent holder, other companies marketing branded azole antifungals would need to ensure their manufacturing processes do not infringe. This includes companies that have acquired rights to previously patented drugs. Contract Manufacturing Organizations (CMOs): CMOs that are contracted to produce azole antifungals on behalf of other pharmaceutical companies must also ensure that the processes they use do not infringe on existing patents. Research and Development Laboratories: Academic or industrial labs developing new azole antifungal candidates might inadvertently use a patented synthetic pathway during their early-stage research, although enforcement in such cases is less common unless commercialization is imminent. Factors Indicating Potential Infringement: Similarity of Synthetic Route: The most direct indicator is the use of a chemical process that mirrors the steps, reagents, and conditions described in the claims of U.S. Patent 6,124,261. Production of Targeted Compounds: Companies producing azole antifungals that fall within the scope of Formula I as defined in the patent are more likely to be using a related synthesis. Efficiency and Yield Claims: If a competitor's process is known to be exceptionally efficient or high-yielding for a particular azole antifungal, it may suggest the use of an optimized route, potentially covered by Merck's patent. A comprehensive freedom-to-operate (FTO) analysis, including a review of Merck's patent and potentially other related azole synthesis patents, is crucial for any entity involved in the development or manufacturing of azole antifungals. What is the Patent Expiration Date and Its Implications? United States Patent 6,124,261 was granted on September 26, 2000. In the United States, utility patents are typically granted for a term of 20 years from the date on which the application for the patent was filed, subject to the payment of maintenance fees. To determine the precise expiration date, one would need to consult the official patent record for the earliest filed application date. However, assuming a standard prosecution period, the patent's effective term would have begun from the filing date. For a patent granted in 2000, the filing date would likely have been in the mid-to-late 1990s. Assuming a filing date around 1997-1998, the patent's term would have expired approximately between 2017 and 2018. Implications of Patent Expiration: Public Domain: Once a patent expires, the technology it covers enters the public domain. This means that any party is free to use, sell, and manufacture the patented invention without seeking permission or paying royalties. Increased Competition for Generic Manufacturers: The expiration of process patents like U.S. Patent 6,124,261 significantly benefits generic drug manufacturers. They can now legally employ the previously protected synthetic route, potentially leading to lower production costs and increased market competition for the specific azole antifungals manufactured via this method. Market Dynamics: The expiration can lead to price reductions for the related drugs as generic alternatives become more prevalent. This can impact the revenue streams of the original patent holder and any companies that held exclusive licensing agreements. Focus on New IP: For the original patent holder (Merck in this case), the expiration of older patents underscores the importance of maintaining a robust pipeline of new inventions and securing fresh patent protection for novel compounds, formulations, or improved processes to sustain market exclusivity. Freedom to Operate (FTO): Companies previously restricted by this patent are now free to operate without FTO concerns related to this specific process. This allows for greater flexibility in manufacturing strategies. It is important to verify the exact filing date and any potential patent term extensions or adjustments that may have applied to U.S. Patent 6,124,261 through official patent databases. However, the general principle is that after 20 years from the filing date, the claims become publicly available for use. Key Takeaways U.S. Patent 6,124,261 protects a specific synthetic process for preparing substituted 1,2,4-triazole antifungal compounds, focusing on a key cyclization step. The patent claims define the boundaries of the invention, covering particular reactants, reaction conditions, and intermediate compounds used in the manufacturing process. The intellectual property landscape for azole antifungal synthesis includes composition of matter, process, formulation, and use patents, with ongoing innovation by major pharmaceutical companies and generic manufacturers. Likely competitors and potential infringers include Merck & Co., Inc., other major pharmaceutical companies involved in azole antifungals, and generic API manufacturers. The patent's expiration, likely in the late 2010s, has moved the patented synthetic technology into the public domain, enabling broader use by generic manufacturers and increasing market competition. Frequently Asked Questions What specific azole antifungal drugs are potentially covered by the manufacturing process in U.S. Patent 6,124,261? The patent claims a process for compounds of "Formula I." While the patent itself does not explicitly list commercial drug names, the chemical structures encompassed by Formula I are consistent with those of known azole antifungal agents. A thorough analysis of Formula I as defined in the patent specification is required to determine which specific drugs' manufacturing processes could fall under its scope. Does U.S. Patent 6,124,261 claim the azole antifungal compounds themselves, or just the method of making them? U.S. Patent 6,124,261 is a process patent. It claims a specific method or synthetic pathway for preparing the compounds. It does not claim the composition of matter of the azole antifungal drugs themselves, which would be covered by separate composition of matter patents. How can a company determine if its manufacturing process infringes on U.S. Patent 6,124,261? Infringement is determined by comparing the company's manufacturing process against the literal language of the patent's claims, particularly claims 1 through the final dependent claim. This involves a detailed chemical and legal analysis of the steps, reagents, intermediates, and conditions used. A freedom-to-operate (FTO) analysis conducted by patent counsel is the standard method for assessing this risk. What is the significance of a process patent expiring? The expiration of a process patent means that the specific manufacturing method described and claimed in the patent is no longer protected. Any individual or company can then legally use, implement, and commercialize that specific process without the need for licensing or royalty payments to the original patent holder. This typically leads to increased competition and potentially lower prices for the associated products. Are there any other patents that might cover the synthesis of azole antifungals that were developed after U.S. Patent 6,124,261 was filed? Yes, the intellectual property landscape is dynamic. Pharmaceutical companies continuously file for and obtain new patents on improved synthetic routes, novel intermediates, stereoselective processes, and alternative manufacturing methods for azole antifungals. Any comprehensive freedom-to-operate analysis would need to consider not only U.S. Patent 6,124,261 but also subsequent patents that may have issued from competitors or even the original patent holder. Citations [1] Merck & Co., Inc. (2000). Process for preparing azole antifungals. U.S. Patent 6,124,261. Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

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Details for Patent: 6,124,261

Summary for Patent: 6,124,261