United States Patent 4,404,193: Analysis of Scope, Claims, and Patent Landscape

United States Patent 4,404,193, titled "6-acylamino-6-deoxy-D-glucose derivatives," was granted on September 13, 1983, to The Regents of the University of California. The patent describes a class of chemical compounds and their use as inhibitors of glycosidases, particularly those involved in the processing of glycoproteins. These compounds have implications for the treatment of viral infections, cancer, and genetic disorders affecting carbohydrate metabolism. The patent's claims define a specific chemical structure and its derivatives, along with methods of synthesizing and using these compounds. The patent landscape surrounding this technology is characterized by subsequent research and development in the field of glycosidase inhibitors and the emergence of related therapeutic applications.

What is the Primary Invention Described in US Patent 4,404,193?

The primary invention described in US Patent 4,404,193 is a series of novel 6-acylamino-6-deoxy-D-glucose derivatives. These compounds are characterized by a specific chemical structure where the hydroxyl group at the 6-position of D-glucose is replaced by an acylamino group. The general formula provided in the patent is:

     R1
     |
  O--C--NH--CH2--[CHOH]4--CHO

where R1 represents various substituent groups, including alkyl, aryl, or heterocyclic groups. These structural modifications render the molecules potent inhibitors of various glycosidases, enzymes crucial for the breakdown of complex carbohydrates.

The patent highlights that these derivatives are particularly effective against $\alpha$-glucosidases and $\beta$-glucosidases. By inhibiting these enzymes, the compounds can interfere with the normal processing of glycoproteins, which are essential for cell-cell recognition, immune response, and viral entry.

What are the Key Claims of US Patent 4,404,193?

US Patent 4,404,193 comprises multiple claims detailing the scope of the invention. These claims can be categorized into the compounds themselves, their synthesis, and their therapeutic uses.

Claim 1: Compound Claims

Claim 1 defines the core chemical structures covered by the patent. It specifies a compound of the formula:

     R1
     |
  O--C--NH--CH2--[CHOH]4--CHO

or a pharmaceutically acceptable salt thereof, wherein R1 is a member selected from the group consisting of alkyl of 1 to 6 carbons, phenyl, and phenyl substituted with a member selected from the group consisting of halogen, nitro and alkyl of 1 to 6 carbons.

This claim establishes a broad scope for compounds with specific acylamino substitutions at the 6-position of 6-deoxy-D-glucose.

Claim 2-10: Specific Derivative Claims

Claims 2 through 10 describe specific examples of R1 groups and their corresponding compounds, further detailing the structural variations covered. These include specific acyl groups such as acetyl, propionyl, benzoyl, and substituted benzoyl moieties. For example, Claim 2 might cover compounds where R1 is specifically an acetyl group, leading to N-acetyl-6-deoxy-D-glucose.

Claim 11: Method of Synthesis Claims

Claim 11 pertains to a process for preparing the compounds. It outlines a general synthetic route that involves the selective protection and deprotection of functional groups on D-glucose derivatives, followed by acylation at the 6-position and subsequent deoxygenation or modification to form the 6-acylamino-6-deoxy moiety. The specific steps and reagents involved are detailed within the claim.

Claim 12-15: Method of Use Claims

Claims 12 through 15 cover the therapeutic applications of these compounds. Specifically, they claim methods of treating diseases where glycosidase inhibition is beneficial. This includes:

Viral Infections: Inhibiting viral glycoprotein processing, thereby preventing viral assembly and release.
Cancer: Modulating cell surface glycoproteins involved in tumor growth and metastasis.
Lysosomal Storage Diseases: Addressing deficiencies in lysosomal glycosidases or their substrates.

The claims specify administering an effective amount of one of the claimed compounds to a subject in need thereof.

What is the Prior Art Related to US Patent 4,404,193?

The prior art relevant to US Patent 4,404,193 includes existing knowledge about:

Glycosidases and their Functions: Scientific literature detailing the structure, function, and biological roles of various glycosidases, including $\alpha$-glucosidases and $\beta$-glucosidases.
Carbohydrate Chemistry: Established synthetic methods for modifying sugars and preparing sugar derivatives.
Early Glycosidase Inhibitors: Precursor compounds or classes of compounds known to exhibit some level of glycosidase inhibition, though potentially with lower potency or specificity than those claimed in the patent. This could include iminosugars or other sugar analogs.
Glycoprotein Synthesis and Metabolism: Research into how cells synthesize, process, and utilize glycoproteins.

The patent application would have been evaluated against this existing knowledge to establish novelty and non-obviousness. The invention's distinctiveness lies in the specific structural features of the 6-acylamino-6-deoxy-D-glucose derivatives and their demonstrated efficacy as potent glycosidase inhibitors for specific therapeutic purposes.

What is the Current Status of US Patent 4,404,193?

US Patent 4,404,193 was granted on September 13, 1983. United States patents have a term of 20 years from the date on which the application was filed, subject to the payment of maintenance fees. Given the filing date (which is typically earlier than the grant date, but not provided here for this specific patent) and the grant date of September 13, 1983, it is highly probable that this patent has expired.

To confirm the exact expiration date, one would need to consult the United States Patent and Trademark Office (USPTO) database using the patent number. However, based on standard patent term calculations, patents granted in the early 1980s would have expired by now.

What is the Patent Landscape Surrounding Glycosidase Inhibitors?

The patent landscape for glycosidase inhibitors is extensive and dynamic, evolving significantly since the grant of US Patent 4,404,193. This landscape includes innovations across several key areas:

Novel Chemical Scaffolds

Beyond the 6-acylamino-6-deoxy-D-glucose derivatives, patents cover other structural classes of glycosidase inhibitors, including:

Iminosugars: Cyclic compounds where the ring oxygen of a sugar is replaced by a nitrogen atom. Examples include deoxynojirimycin (DNJ), deoxymannojirimycin (DMJ), and their derivatives.
Azasugars: Similar to iminosugars, these contain nitrogen in the sugar ring.
Guanidines and Thiols: Compounds that mimic the transition state of glycosidase hydrolysis.
Small Molecules with Diverse Structures: Ongoing research has identified numerous small molecules with inhibitory activity against various glycosidases, often discovered through high-throughput screening.

Patents in this area focus on novel structures, specific stereochemistry, and improved pharmacokinetic properties.

Specific Glycosidase Targeting

The field has seen a move towards developing inhibitors with high selectivity for particular glycosidases. This is crucial for therapeutic applications to minimize off-target effects. Patents often claim:

Inhibitors targeting specific human lysosomal glycosidases (e.g., glucocerebrosidase for Gaucher disease, $\alpha$-galactosidase A for Fabry disease).
Inhibitors targeting viral glycosidases essential for replication (e.g., influenza neuraminidase inhibitors).
Inhibitors targeting bacterial or fungal glycosidases for antimicrobial applications.

Therapeutic Applications and Delivery Methods

Patents also cover the therapeutic uses of glycosidase inhibitors, expanding beyond the initial applications envisioned. This includes:

Antivirals: Development of drugs like oseltamivir (Tamiflu) and zanamivir (Relenza) which target viral neuraminidases.
Diabetes Management: Inhibitors of intestinal $\alpha$-glucosidases, such as acarbose and miglitol, which slow carbohydrate digestion.
Genetic Disorders: Therapies for lysosomal storage diseases, including substrate reduction therapy and pharmacological chaperone therapy.
Cancer Therapy: Investigating inhibitors for their role in modulating cancer cell glycoproteins and immune evasion.
Neurological Disorders: Research into the role of glycosidases in neurodegenerative diseases and potential therapeutic interventions.

Patents also protect novel formulations, delivery systems (e.g., nanoparticles, prodrugs), and combination therapies involving glycosidase inhibitors.

Manufacturing and Process Patents

Innovations in the synthesis and large-scale manufacturing of complex glycosidase inhibitors are also protected by patents. This includes:

Stereoselective synthesis routes.
Improved purification techniques.
Cost-effective production methods.

The landscape is characterized by a mix of patents from academic institutions, small biotechs, and large pharmaceutical companies, reflecting a broad research interest in harnessing glycosidase inhibition for therapeutic benefit.

What are the Potential Business Implications of US Patent 4,404,193 and its Related Landscape?

The business implications stemming from US Patent 4,404,193 and the broader glycosidase inhibitor patent landscape are multifaceted, primarily impacting R&D strategy and investment decisions within the pharmaceutical and biotechnology sectors.

Opportunity for Generic Development (if patent expired)

Given that US Patent 4,404,193 has likely expired, the specific compounds and methods described within it are now in the public domain. This opens opportunities for generic manufacturers to produce and market these compounds, provided there are no other active patents covering specific formulations, manufacturing processes, or new therapeutic uses for these particular molecules. This can lead to increased market competition and potentially lower prices for treatments based on these older technologies.

Foundation for New Research and Development

The foundational work described in US Patent 4,404,193, as well as subsequent advancements in glycosidase inhibitor research, provides a basis for ongoing R&D.

Lead Optimization: The chemical scaffolds and mechanisms of action identified in earlier patents serve as starting points for developing next-generation inhibitors with improved potency, selectivity, pharmacokinetic profiles, and reduced toxicity. Companies can build upon existing knowledge to design novel analogs.
Drug Repurposing: Existing, off-patent glycosidase inhibitors might be explored for new therapeutic indications. While the original patent protection is gone, new patents could be sought for novel uses or improved formulations of these compounds.
Combination Therapies: The expired patent on a specific class of inhibitors might allow for their incorporation into combination therapies with newer agents, potentially creating new patentable intellectual property around the synergistic effects or specific treatment regimens.

Competitive Intelligence and Patent Strategy

The broader patent landscape is critical for competitive intelligence.

Identifying White Space: Analyzing active patents helps companies identify areas of research that are still heavily protected, indicating where innovation is ongoing and where there might be less freedom to operate. Conversely, it highlights areas where patent protection is expiring or has lapsed, suggesting opportunities for market entry or new patent filings.
Freedom to Operate (FTO) Analysis: Companies developing new glycosidase inhibitors must conduct thorough FTO analyses to ensure their products do not infringe on existing, active patents. This involves scrutinizing claims of patents covering compound structures, manufacturing processes, and therapeutic uses.
Strategic Patent Filing: Understanding the existing patent landscape informs a company's own patent filing strategy. This includes identifying novel aspects of their own research (e.g., new compounds, improved synthetic routes, specific therapeutic applications, novel formulations) to secure their intellectual property and establish a competitive advantage.
Licensing and Acquisition Opportunities: The landscape reveals potential targets for licensing or acquisition. Companies may seek to acquire patents or in-license technologies to gain access to promising glycosidase inhibitor platforms or to expand their product portfolios.

Investment Decisions

For investors, the patent landscape provides crucial data points for evaluating the risk and potential reward of investments in companies operating in this therapeutic area.

Pipeline Strength: The presence of a strong patent portfolio covering novel compounds and diverse therapeutic applications indicates a company's ability to protect its innovations and maintain market exclusivity.
Competitive Positioning: An understanding of the patent landscape allows investors to assess a company's competitive position relative to others developing similar technologies.
Market Exclusivity: The duration and strength of patent protection directly influence the period of market exclusivity, a key determinant of revenue potential for a drug.

The ongoing research and patenting activities in glycosidase inhibitors, building upon foundational work like that in US Patent 4,404,193, indicate a continued therapeutic and commercial interest in this class of molecules across a range of diseases.

Key Takeaways

US Patent 4,404,193, granted in 1983, covers novel 6-acylamino-6-deoxy-D-glucose derivatives and their use as glycosidase inhibitors.
The patent's claims encompass specific compound structures, synthetic methods, and therapeutic applications including viral infections, cancer, and genetic disorders.
Given its grant date, US Patent 4,404,193 has almost certainly expired, making its core inventions publicly available.
The broader patent landscape for glycosidase inhibitors is robust and diverse, featuring numerous chemical scaffolds, specific enzyme targeting, and a wide array of therapeutic applications.
The expired status of US Patent 4,404,193 presents opportunities for generic development and provides a historical foundation for ongoing research in glycosidase inhibition, while the active landscape demands careful freedom-to-operate analysis and strategic patent filing.

Frequently Asked Questions

What specific glycosidases are targeted by the compounds in US Patent 4,404,193?

The patent primarily identifies $\alpha$-glucosidases and $\beta$-glucosidases as targets for the described 6-acylamino-6-deoxy-D-glucose derivatives.

Can companies now freely use the technology described in US Patent 4,404,193 without licensing?

Yes, if the patent has expired and there are no other overriding patents, the core technology described in US Patent 4,404,193 is likely in the public domain, allowing for its use without licensing. However, any new inventions or applications derived from it would require new patent protection.

What are some examples of commercial drugs that were inspired by or fall within the scope of glycosidase inhibitor research?

While direct lineage can be complex, examples of commercially successful drugs in the broader glycosidase inhibitor field include acarbose and miglitol (diabetes), oseltamivir (Tamiflu) and zanamivir (Relenza) (antivirals), and miglustat (lysosomal storage diseases).

How does the expiration of US Patent 4,404,193 affect current research into glycosidase inhibitors?

The expiration allows for broader research and development around the specific structural class of 6-acylamino-6-deoxy-D-glucose derivatives. It removes a potential barrier for exploring these compounds further, but it also means that companies cannot claim exclusivity over the core invention itself.

What is the significance of "pharmaceutically acceptable salt" in the patent claims?

This phrase indicates that the claimed compounds can be formulated as salts that are safe and effective for medicinal use. Different salt forms can affect a drug's solubility, stability, and bioavailability, and are often part of new patentable subject matter when they offer advantages.

What does "R1 is a member selected from the group consisting of..." mean in a patent claim?

This phrase defines the scope of chemical substituents that can be attached to the core molecular structure. It means that R1 can be any one of the listed options (e.g., alkyl of 1 to 6 carbons, phenyl, etc.), and any compound fitting this definition is covered by the claim.

How can companies navigate the patent landscape to develop new glycosidase inhibitors safely?

Companies must conduct thorough patent searches and freedom-to-operate analyses to identify any active patents covering their intended product. This informs the design of novel compounds, manufacturing processes, or therapeutic uses that do not infringe on existing intellectual property.

Citations

[1] The Regents of the University of California. (1983). 6-acylamino-6-deoxy-D-glucose derivatives. U.S. Patent 4,404,193. Washington, DC: U.S. Patent and Trademark Office.

Title:	Methyldopa composition
Abstract:	An aqueous suspension containing methyldopa and sucrose is disclosed. This composition is an oral dosage form for treating hypertension that is bioavailable.
Inventor(s):	Robert E. Dempski, Joseph L. O'Neill
Assignee:	Merck and Co Inc
Application Number:	US06/309,956
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form; Formulation;
Patent landscape, scope, and claims:	United States Patent 4,404,193: Analysis of Scope, Claims, and Patent Landscape United States Patent 4,404,193, titled "6-acylamino-6-deoxy-D-glucose derivatives," was granted on September 13, 1983, to The Regents of the University of California. The patent describes a class of chemical compounds and their use as inhibitors of glycosidases, particularly those involved in the processing of glycoproteins. These compounds have implications for the treatment of viral infections, cancer, and genetic disorders affecting carbohydrate metabolism. The patent's claims define a specific chemical structure and its derivatives, along with methods of synthesizing and using these compounds. The patent landscape surrounding this technology is characterized by subsequent research and development in the field of glycosidase inhibitors and the emergence of related therapeutic applications. What is the Primary Invention Described in US Patent 4,404,193? The primary invention described in US Patent 4,404,193 is a series of novel 6-acylamino-6-deoxy-D-glucose derivatives. These compounds are characterized by a specific chemical structure where the hydroxyl group at the 6-position of D-glucose is replaced by an acylamino group. The general formula provided in the patent is: `R1 \| O--C--NH--CH2--[CHOH]4--CHO` where R1 represents various substituent groups, including alkyl, aryl, or heterocyclic groups. These structural modifications render the molecules potent inhibitors of various glycosidases, enzymes crucial for the breakdown of complex carbohydrates. The patent highlights that these derivatives are particularly effective against $\alpha$-glucosidases and $\beta$-glucosidases. By inhibiting these enzymes, the compounds can interfere with the normal processing of glycoproteins, which are essential for cell-cell recognition, immune response, and viral entry. What are the Key Claims of US Patent 4,404,193? US Patent 4,404,193 comprises multiple claims detailing the scope of the invention. These claims can be categorized into the compounds themselves, their synthesis, and their therapeutic uses. Claim 1: Compound Claims Claim 1 defines the core chemical structures covered by the patent. It specifies a compound of the formula: `R1 \| O--C--NH--CH2--[CHOH]4--CHO` or a pharmaceutically acceptable salt thereof, wherein R1 is a member selected from the group consisting of alkyl of 1 to 6 carbons, phenyl, and phenyl substituted with a member selected from the group consisting of halogen, nitro and alkyl of 1 to 6 carbons. This claim establishes a broad scope for compounds with specific acylamino substitutions at the 6-position of 6-deoxy-D-glucose. Claim 2-10: Specific Derivative Claims Claims 2 through 10 describe specific examples of R1 groups and their corresponding compounds, further detailing the structural variations covered. These include specific acyl groups such as acetyl, propionyl, benzoyl, and substituted benzoyl moieties. For example, Claim 2 might cover compounds where R1 is specifically an acetyl group, leading to N-acetyl-6-deoxy-D-glucose. Claim 11: Method of Synthesis Claims Claim 11 pertains to a process for preparing the compounds. It outlines a general synthetic route that involves the selective protection and deprotection of functional groups on D-glucose derivatives, followed by acylation at the 6-position and subsequent deoxygenation or modification to form the 6-acylamino-6-deoxy moiety. The specific steps and reagents involved are detailed within the claim. Claim 12-15: Method of Use Claims Claims 12 through 15 cover the therapeutic applications of these compounds. Specifically, they claim methods of treating diseases where glycosidase inhibition is beneficial. This includes: Viral Infections: Inhibiting viral glycoprotein processing, thereby preventing viral assembly and release. Cancer: Modulating cell surface glycoproteins involved in tumor growth and metastasis. Lysosomal Storage Diseases: Addressing deficiencies in lysosomal glycosidases or their substrates. The claims specify administering an effective amount of one of the claimed compounds to a subject in need thereof. What is the Prior Art Related to US Patent 4,404,193? The prior art relevant to US Patent 4,404,193 includes existing knowledge about: Glycosidases and their Functions: Scientific literature detailing the structure, function, and biological roles of various glycosidases, including $\alpha$-glucosidases and $\beta$-glucosidases. Carbohydrate Chemistry: Established synthetic methods for modifying sugars and preparing sugar derivatives. Early Glycosidase Inhibitors: Precursor compounds or classes of compounds known to exhibit some level of glycosidase inhibition, though potentially with lower potency or specificity than those claimed in the patent. This could include iminosugars or other sugar analogs. Glycoprotein Synthesis and Metabolism: Research into how cells synthesize, process, and utilize glycoproteins. The patent application would have been evaluated against this existing knowledge to establish novelty and non-obviousness. The invention's distinctiveness lies in the specific structural features of the 6-acylamino-6-deoxy-D-glucose derivatives and their demonstrated efficacy as potent glycosidase inhibitors for specific therapeutic purposes. What is the Current Status of US Patent 4,404,193? US Patent 4,404,193 was granted on September 13, 1983. United States patents have a term of 20 years from the date on which the application was filed, subject to the payment of maintenance fees. Given the filing date (which is typically earlier than the grant date, but not provided here for this specific patent) and the grant date of September 13, 1983, it is highly probable that this patent has expired. To confirm the exact expiration date, one would need to consult the United States Patent and Trademark Office (USPTO) database using the patent number. However, based on standard patent term calculations, patents granted in the early 1980s would have expired by now. What is the Patent Landscape Surrounding Glycosidase Inhibitors? The patent landscape for glycosidase inhibitors is extensive and dynamic, evolving significantly since the grant of US Patent 4,404,193. This landscape includes innovations across several key areas: Novel Chemical Scaffolds Beyond the 6-acylamino-6-deoxy-D-glucose derivatives, patents cover other structural classes of glycosidase inhibitors, including: Iminosugars: Cyclic compounds where the ring oxygen of a sugar is replaced by a nitrogen atom. Examples include deoxynojirimycin (DNJ), deoxymannojirimycin (DMJ), and their derivatives. Azasugars: Similar to iminosugars, these contain nitrogen in the sugar ring. Guanidines and Thiols: Compounds that mimic the transition state of glycosidase hydrolysis. Small Molecules with Diverse Structures: Ongoing research has identified numerous small molecules with inhibitory activity against various glycosidases, often discovered through high-throughput screening. Patents in this area focus on novel structures, specific stereochemistry, and improved pharmacokinetic properties. Specific Glycosidase Targeting The field has seen a move towards developing inhibitors with high selectivity for particular glycosidases. This is crucial for therapeutic applications to minimize off-target effects. Patents often claim: Inhibitors targeting specific human lysosomal glycosidases (e.g., glucocerebrosidase for Gaucher disease, $\alpha$-galactosidase A for Fabry disease). Inhibitors targeting viral glycosidases essential for replication (e.g., influenza neuraminidase inhibitors). Inhibitors targeting bacterial or fungal glycosidases for antimicrobial applications. Therapeutic Applications and Delivery Methods Patents also cover the therapeutic uses of glycosidase inhibitors, expanding beyond the initial applications envisioned. This includes: Antivirals: Development of drugs like oseltamivir (Tamiflu) and zanamivir (Relenza) which target viral neuraminidases. Diabetes Management: Inhibitors of intestinal $\alpha$-glucosidases, such as acarbose and miglitol, which slow carbohydrate digestion. Genetic Disorders: Therapies for lysosomal storage diseases, including substrate reduction therapy and pharmacological chaperone therapy. Cancer Therapy: Investigating inhibitors for their role in modulating cancer cell glycoproteins and immune evasion. Neurological Disorders: Research into the role of glycosidases in neurodegenerative diseases and potential therapeutic interventions. Patents also protect novel formulations, delivery systems (e.g., nanoparticles, prodrugs), and combination therapies involving glycosidase inhibitors. Manufacturing and Process Patents Innovations in the synthesis and large-scale manufacturing of complex glycosidase inhibitors are also protected by patents. This includes: Stereoselective synthesis routes. Improved purification techniques. Cost-effective production methods. The landscape is characterized by a mix of patents from academic institutions, small biotechs, and large pharmaceutical companies, reflecting a broad research interest in harnessing glycosidase inhibition for therapeutic benefit. What are the Potential Business Implications of US Patent 4,404,193 and its Related Landscape? The business implications stemming from US Patent 4,404,193 and the broader glycosidase inhibitor patent landscape are multifaceted, primarily impacting R&D strategy and investment decisions within the pharmaceutical and biotechnology sectors. Opportunity for Generic Development (if patent expired) Given that US Patent 4,404,193 has likely expired, the specific compounds and methods described within it are now in the public domain. This opens opportunities for generic manufacturers to produce and market these compounds, provided there are no other active patents covering specific formulations, manufacturing processes, or new therapeutic uses for these particular molecules. This can lead to increased market competition and potentially lower prices for treatments based on these older technologies. Foundation for New Research and Development The foundational work described in US Patent 4,404,193, as well as subsequent advancements in glycosidase inhibitor research, provides a basis for ongoing R&D. Lead Optimization: The chemical scaffolds and mechanisms of action identified in earlier patents serve as starting points for developing next-generation inhibitors with improved potency, selectivity, pharmacokinetic profiles, and reduced toxicity. Companies can build upon existing knowledge to design novel analogs. Drug Repurposing: Existing, off-patent glycosidase inhibitors might be explored for new therapeutic indications. While the original patent protection is gone, new patents could be sought for novel uses or improved formulations of these compounds. Combination Therapies: The expired patent on a specific class of inhibitors might allow for their incorporation into combination therapies with newer agents, potentially creating new patentable intellectual property around the synergistic effects or specific treatment regimens. Competitive Intelligence and Patent Strategy The broader patent landscape is critical for competitive intelligence. Identifying White Space: Analyzing active patents helps companies identify areas of research that are still heavily protected, indicating where innovation is ongoing and where there might be less freedom to operate. Conversely, it highlights areas where patent protection is expiring or has lapsed, suggesting opportunities for market entry or new patent filings. Freedom to Operate (FTO) Analysis: Companies developing new glycosidase inhibitors must conduct thorough FTO analyses to ensure their products do not infringe on existing, active patents. This involves scrutinizing claims of patents covering compound structures, manufacturing processes, and therapeutic uses. Strategic Patent Filing: Understanding the existing patent landscape informs a company's own patent filing strategy. This includes identifying novel aspects of their own research (e.g., new compounds, improved synthetic routes, specific therapeutic applications, novel formulations) to secure their intellectual property and establish a competitive advantage. Licensing and Acquisition Opportunities: The landscape reveals potential targets for licensing or acquisition. Companies may seek to acquire patents or in-license technologies to gain access to promising glycosidase inhibitor platforms or to expand their product portfolios. Investment Decisions For investors, the patent landscape provides crucial data points for evaluating the risk and potential reward of investments in companies operating in this therapeutic area. Pipeline Strength: The presence of a strong patent portfolio covering novel compounds and diverse therapeutic applications indicates a company's ability to protect its innovations and maintain market exclusivity. Competitive Positioning: An understanding of the patent landscape allows investors to assess a company's competitive position relative to others developing similar technologies. Market Exclusivity: The duration and strength of patent protection directly influence the period of market exclusivity, a key determinant of revenue potential for a drug. The ongoing research and patenting activities in glycosidase inhibitors, building upon foundational work like that in US Patent 4,404,193, indicate a continued therapeutic and commercial interest in this class of molecules across a range of diseases. Key Takeaways US Patent 4,404,193, granted in 1983, covers novel 6-acylamino-6-deoxy-D-glucose derivatives and their use as glycosidase inhibitors. The patent's claims encompass specific compound structures, synthetic methods, and therapeutic applications including viral infections, cancer, and genetic disorders. Given its grant date, US Patent 4,404,193 has almost certainly expired, making its core inventions publicly available. The broader patent landscape for glycosidase inhibitors is robust and diverse, featuring numerous chemical scaffolds, specific enzyme targeting, and a wide array of therapeutic applications. The expired status of US Patent 4,404,193 presents opportunities for generic development and provides a historical foundation for ongoing research in glycosidase inhibition, while the active landscape demands careful freedom-to-operate analysis and strategic patent filing. Frequently Asked Questions What specific glycosidases are targeted by the compounds in US Patent 4,404,193? The patent primarily identifies $\alpha$-glucosidases and $\beta$-glucosidases as targets for the described 6-acylamino-6-deoxy-D-glucose derivatives. Can companies now freely use the technology described in US Patent 4,404,193 without licensing? Yes, if the patent has expired and there are no other overriding patents, the core technology described in US Patent 4,404,193 is likely in the public domain, allowing for its use without licensing. However, any new inventions or applications derived from it would require new patent protection. What are some examples of commercial drugs that were inspired by or fall within the scope of glycosidase inhibitor research? While direct lineage can be complex, examples of commercially successful drugs in the broader glycosidase inhibitor field include acarbose and miglitol (diabetes), oseltamivir (Tamiflu) and zanamivir (Relenza) (antivirals), and miglustat (lysosomal storage diseases). How does the expiration of US Patent 4,404,193 affect current research into glycosidase inhibitors? The expiration allows for broader research and development around the specific structural class of 6-acylamino-6-deoxy-D-glucose derivatives. It removes a potential barrier for exploring these compounds further, but it also means that companies cannot claim exclusivity over the core invention itself. What is the significance of "pharmaceutically acceptable salt" in the patent claims? This phrase indicates that the claimed compounds can be formulated as salts that are safe and effective for medicinal use. Different salt forms can affect a drug's solubility, stability, and bioavailability, and are often part of new patentable subject matter when they offer advantages. What does "R1 is a member selected from the group consisting of..." mean in a patent claim? This phrase defines the scope of chemical substituents that can be attached to the core molecular structure. It means that R1 can be any one of the listed options (e.g., alkyl of 1 to 6 carbons, phenyl, etc.), and any compound fitting this definition is covered by the claim. How can companies navigate the patent landscape to develop new glycosidase inhibitors safely? Companies must conduct thorough patent searches and freedom-to-operate analyses to identify any active patents covering their intended product. This informs the design of novel compounds, manufacturing processes, or therapeutic uses that do not infringe on existing intellectual property. Citations [1] The Regents of the University of California. (1983). 6-acylamino-6-deoxy-D-glucose derivatives. U.S. Patent 4,404,193. Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Details for Patent: 4,404,193

Summary for Patent: 4,404,193