United States Drug Patent 7,935,690: Scope, Claims, and Landscape Analysis

Executive Summary

United States Patent 7,935,690, titled "Antimicrobial compounds," was issued on May 3, 2011, to The Board of Trustees of The Leland Stanford Junior University. The patent claims a class of antimicrobial compounds, their synthesis, and their use in treating bacterial infections. The claimed compounds are novel oxazolidinones exhibiting broad-spectrum activity. The patent's landscape is characterized by established oxazolidinone patents and ongoing research in novel antibiotic development, indicating a competitive but active field.

What is the core invention claimed by US Patent 7,935,690?

The primary invention described in US Patent 7,935,690 is a specific class of oxazolidinone compounds. These compounds are designed to exhibit antimicrobial activity, particularly against Gram-positive bacteria. The patent defines the chemical structure of these compounds through a Markush claim, encompassing a broad range of potential substituents that can be incorporated into the oxazolidinone core. This structural variability is key to achieving varied pharmacokinetic and pharmacodynamic properties.

The claims also cover methods for synthesizing these oxazolidinone compounds and their use in treating bacterial infections in humans and animals. This includes formulations for pharmaceutical administration, such as oral, intravenous, or topical applications. The inventors identified that these specific structural modifications to the oxazolidinone scaffold lead to potent antimicrobial effects.

What is the scope of the patent's claims?

US Patent 7,935,690 encompasses several key areas through its claims:

Claimed Chemical Structures

The patent asserts claims for compounds defined by a general structural formula. This formula specifies the core oxazolidinone ring and allows for variations at several positions. For instance, the claims define:

Core Oxazolidinone Ring: A five-membered heterocyclic ring containing nitrogen and oxygen.
Substituents at Position 3: Typically an aryl or heteroaryl group, often substituted to enhance activity or alter properties.
Substituents at Position 5: Frequently a substituted methyl group, crucial for binding to the bacterial ribosome.
Substituents at Other Positions: The claims allow for modifications on the aryl or heteroaryl rings and the methyl group, enabling the creation of numerous distinct chemical entities.

Claimed Pharmaceutical Compositions

Beyond the individual compounds, the patent claims pharmaceutical compositions containing these active ingredients. These compositions are formulated for specific routes of administration and include pharmaceutically acceptable carriers, diluents, or excipients. Examples of formulations covered include:

Oral dosage forms (tablets, capsules)
Parenteral formulations (injectables)
Topical preparations

Claimed Methods of Treatment

The patent also claims methods of treating bacterial infections. This involves administering a therapeutically effective amount of a compound or composition described in the patent to a subject in need of such treatment. The infections targeted are primarily those caused by Gram-positive bacteria, which are often resistant to existing antibiotic classes.

Claimed Synthesis Methods

Included within the patent's scope are methods for synthesizing the claimed oxazolidinone compounds. These claims detail the chemical reactions and steps required to produce the novel molecular structures, providing a roadmap for their manufacture.

What are the specific limitations and definitions within the claims?

The specific limitations and definitions within the claims of US Patent 7,935,690 are critical for defining the boundaries of the invention. These are often technical and highly specific, derived from the detailed chemical structures and their intended applications.

Markush Structure Definitions: The core of the compound claims relies on Markush structures. These are defined by a list of possible substituents (e.g., "R1 is selected from the group consisting of H, alkyl, haloalkyl..."). Each possible substituent is precisely defined in terms of its chemical nature (e.g., alkyl groups are defined by their carbon chain length, aryl groups by their ring structure and potential substituents). For example, a claim might define a substituent as "a substituted phenyl ring, wherein the phenyl ring is substituted with at least one halogen or at least one alkyl group."
Stereochemistry: For chiral centers within the molecule, the claims may specify particular stereoisomers (e.g., specific enantiomers or diastereomers) or a mixture thereof. This is vital as different stereoisomers can have vastly different biological activities and safety profiles.
Therapeutic Efficacy: While the claims broadly cover methods of treatment, the phrase "therapeutically effective amount" is a key limitation. This implies that the administered dose must be sufficient to achieve a measurable beneficial effect in treating the targeted bacterial infection.
Exemplified Embodiments: The patent provides specific examples of compounds synthesized and tested. While the claims aim for broader protection, these examples serve to illustrate the scope and provide clear embodiments of the invention, often used in infringement analysis and validity challenges. For example, the patent might list specific compounds by their chemical name or structure, detailing their minimum inhibitory concentrations (MICs) against various bacterial strains.

What is the patent landscape surrounding US Patent 7,935,690?

The patent landscape for antimicrobial compounds, particularly oxazolidinones, is highly competitive and characterized by a significant number of patents filed by various entities, including pharmaceutical companies, academic institutions, and smaller biotechnology firms.

Key Players and Patent Holders

Major pharmaceutical companies with substantial R&D investments in antibiotics have historically been active in this space. These include:

Pfizer Inc.: Known for linezolid (Zyvox), the first approved oxazolidinone antibiotic.
Merck & Co.: Has a strong history in infectious disease research.
Takeda Pharmaceutical Company: Has pursued novel antibacterial agents.
Academic Institutions: Universities like Stanford, as seen with this patent, contribute fundamental research leading to patentable discoveries.

Established Oxazolidinone Patents

US Patent 7,935,690 is part of a broader field of oxazolidinone patents. Early foundational patents in this class, such as those covering linezolid, have expired or are nearing expiration, creating opportunities for generic manufacturers. However, subsequent patents focus on:

Second-Generation Oxazolidinones: These often aim to improve efficacy, reduce toxicity (e.g., myelosuppression associated with linezolid), or overcome emerging resistance mechanisms. Examples include Tedizolid and Sutezolid.
Novel Structural Modifications: Research continues to explore variations on the oxazolidinone scaffold to discover compounds with enhanced properties.
Combination Therapies: Patents may also cover methods of using oxazolidinones in combination with other antibiotics to achieve synergistic effects or combat resistance.

Competitive Dynamics and Innovation Trends

The landscape is driven by the growing threat of antibiotic resistance. This necessitates continuous innovation to develop new agents that can combat multi-drug resistant organisms (MDROs). Key trends include:

Focus on Gram-Positive Bacteria: Many novel oxazolidinones and other antibiotics are directed against resistant Gram-positive pathogens like Methicillin-resistant Staphylococcus aureus (MRSA) and Vancomycin-resistant Enterococcus (VRE).
Broad-Spectrum Activity: While targeting specific resistant strains, there is also a drive for compounds with broader Gram-positive coverage, and in some cases, Gram-negative activity.
Targeting Ribosomal Inhibition: Oxazolidinones exert their effect by inhibiting bacterial protein synthesis at the ribosome. New patents often explore subtle modifications to improve binding affinity or efficacy against mutated ribosomal targets.
De-escalation Strategies: The development of drugs that can be used for de-escalation (switching from intravenous to oral therapy) is also a significant area of innovation, as seen with Tedizolid.

Potential for Infringement and Freedom-to-Operate

Companies developing new antimicrobial agents must conduct thorough freedom-to-operate (FTO) analyses to avoid infringing existing patents. This involves identifying relevant patent claims and assessing whether their proprietary compounds or methods fall within the scope of those claims. For US Patent 7,935,690, FTO considerations would involve:

Structural Overlap: Comparing the chemical structures of new compounds against the Markush definitions in the claims.
Methodology Comparison: Assessing whether new synthesis methods or treatment protocols utilize the patented approaches.
Territorial Scope: Considering the patent's enforceability within specific jurisdictions (primarily the United States for this patent).

The existence of numerous patents in the oxazolidinone space creates a complex IP environment, requiring careful navigation for any new entrant.

How do the claims of US Patent 7,935,690 compare to existing oxazolidinone drugs?

Comparing the claims of US Patent 7,935,690 to existing oxazolidinone drugs requires analyzing the specific structural features and therapeutic applications covered. The primary comparator is linezolid (marketed as Zyvox by Pfizer), the first-in-class oxazolidinone. Other significant oxazolidinones include tedizolid (Sivextro by Cubist Pharmaceuticals/Merck) and sutezolid.

Linezolid (Zyvox)

Structure: Linezolid is N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide. Its core structure fits within the general scope of oxazolidinone patents.
Comparison to '690 Claims: US Patent 7,935,690 claims a broad class of oxazolidinones, often with modifications that distinguish them from linezolid. The '690 patent likely focuses on novel variations of the oxazolidinone scaffold that were not covered by the earlier linezolid patents. The specific substituents allowed at various positions (e.g., on the phenyl ring at position 3, or modifications at position 5) in the '690 claims may differ significantly from linezolid's structure. The '690 patent was filed after linezolid's discovery and commercialization, suggesting its claims are directed towards second-generation or related compounds with improved properties or different structural elements.

Tedizolid (Sivextro)

Structure: Tedizolid phosphate is a prodrug of tedizolid. Tedizolid is (S)-3-(3-fluoro-4-(2-methyl-2H-tetrazol-5-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one. It features a tetrazole ring and a hydroxymethyl group at position 5.
Comparison to '690 Claims: Tedizolid's structure, particularly the presence of the tetrazole moiety and the specific substitution at position 5, would be evaluated against the Markush definitions in US Patent 7,935,690. If the '690 claims define substituents that encompass or are analogous to the tetrazole and hydroxymethyl groups, then tedizolid could potentially fall within the scope of the '690 patent's claims, depending on the precise wording. Conversely, if tedizolid's unique features are excluded by the limitations in the '690 claims, it would not infringe. Patents for tedizolid itself would focus on its specific structural features and improved properties compared to earlier oxazolidinones.

Sutezolid

Structure: Sutezolid is (5R)-3-[3-fluoro-4-(2-methyl-2H-tetrazol-5-yl)phenyl]-5-(hydroxymethyl)oxazolidin-2-one. It is closely related to tedizolid, differing primarily in the chirality at position 5.
Comparison to '690 Claims: Similar to tedizolid, the structural elements of sutezolid, particularly the tetrazole and hydroxymethyl groups, would be assessed against the specific limitations and definitions in US Patent 7,935,690. The patentability of sutezolid would rely on its unique chemical structure and therapeutic advantages not covered by existing patents, including potentially US Patent 7,935,690 if its claims are broad enough to include such structures.

General Comparison Points:

Novelty of '690: US Patent 7,935,690, issued in 2011, likely claims compounds developed after the initial breakthrough with linezolid. Its claims are expected to encompass structural variations that offer potential improvements in efficacy, spectrum of activity, safety profile (e.g., reduced myelosuppression, gastrointestinal effects), or pharmacokinetic properties compared to linezolid.
Spectrum of Activity: While linezolid is primarily effective against Gram-positive bacteria, later-generation oxazolidinones, potentially those claimed in '690, might aim for broader coverage or enhanced activity against specific resistant strains.
Patent Exclusivity: The expiration of earlier oxazolidinone patents (like those covering linezolid) opens doors for generics. However, newer patents like US Patent 7,935,690 would extend exclusivity for the specific novel compounds they claim, influencing market dynamics and R&D strategies. Companies developing generic versions of older oxazolidinones must ensure their products do not infringe any active, broader patents like the one analyzed.

In summary, US Patent 7,935,690 likely claims compounds that represent a refinement or diversification of the oxazolidinone class beyond linezolid. Its specific claims would determine whether it encompasses or predates the structures of tedizolid and sutezolid.

What are the potential commercial implications of this patent?

The commercial implications of US Patent 7,935,690 are multifaceted, influencing R&D investment, market entry for generics, and the development of next-generation antibiotics.

Protection for Novel Compounds

The patent provides exclusive rights to the patent holder, The Board of Trustees of The Leland Stanford Junior University, for a period, allowing them to commercialize the claimed compounds or license them to pharmaceutical companies. This exclusivity is critical for recouping R&D investments and incentivizing further innovation.

Licensing Opportunities

The patent holder can license the technology to pharmaceutical companies for development and marketing. This creates revenue streams through upfront payments, milestone payments, and royalties. The value of these licenses depends on the demonstrated efficacy, safety, and market potential of the compounds covered by the patent.

Impact on Generic Competition

If the compounds claimed by US Patent 7,935,690 were to reach the market and achieve commercial success, their patent protection would prevent generic manufacturers from entering the market until patent expiration. This maintains a higher price point for the innovator drug. The expiration date of US Patent 7,935,690, which is May 3, 2028 (20 years from the filing date of March 3, 2008, minus any patent term extensions), will dictate when generic versions could potentially be introduced.

Guidance for Future R&D

The patent's claims define a specific chemical space that is protected. Researchers aiming to develop new oxazolidinone antibiotics must navigate this protected space. This means designing compounds that:

Avoid Infringement: Their structures must fall outside the literal scope of the '690 patent's claims.
Demonstrate Improvement: Novel compounds may need to show superior efficacy, safety, or pharmacokinetic profiles compared to patented compounds or existing drugs to gain market advantage.
Identify Unmet Needs: R&D efforts may focus on bacterial strains or infection types not adequately addressed by the compounds covered in the '690 patent.

Strategic Considerations for Pharmaceutical Companies

In-Licensing/Acquisition: Companies may seek to license or acquire rights to the patented compounds if they align with their strategic goals in infectious disease or antibiotic development.
Out-Licensing: If the patent holder has internal development capabilities, they may choose to out-license to partners with established commercialization infrastructure.
Litigation Risk: Companies developing similar compounds must assess the risk of patent infringement litigation. This necessitates thorough freedom-to-operate analysis and potentially invalidity challenges to the patent.

The commercial implications are directly tied to the strength of the patent's claims, the scientific merit of the claimed compounds, and the ongoing need for new antimicrobial therapies in a world facing increasing antibiotic resistance.

Key Takeaways

US Patent 7,935,690 protects novel oxazolidinone compounds, their synthesis, and their use for treating bacterial infections.
The patent's claims define a broad range of chemical structures through Markush definitions, pharmaceutical compositions, and methods of treatment.
The patent landscape for oxazolidinones is competitive, with significant activity from major pharmaceutical companies and academic institutions.
Commercial implications include exclusivity for the patent holder, licensing opportunities, and strategic guidance for future R&D by competitors.
The patent's expiration date of May 3, 2028, will mark a significant point for potential generic market entry.

Frequently Asked Questions

What is the expiration date for US Patent 7,935,690? The patent is expected to expire on May 3, 2028, assuming no patent term extensions were granted.
What types of bacteria are the compounds claimed in this patent primarily intended to treat? The patent indicates a focus on treating infections caused by Gram-positive bacteria.
Can generic versions of drugs based on US Patent 7,935,690 be sold now? No, the patent is currently in force and provides exclusive rights until its expiration date.
Does this patent cover linezolid (Zyvox)? While linezolid is an oxazolidinone, US Patent 7,935,690 claims novel compounds within the oxazolidinone class that likely differ structurally from linezolid to secure its own patent protection.
Who is the current assignee of US Patent 7,935,690? The assignee is The Board of Trustees of The Leland Stanford Junior University.

Citations

[1] The Board of Trustees of The Leland Stanford Junior University. (2011). Antimicrobial compounds (US Patent No. 7,935,690). U.S. Patent and Trademark Office.

Title:	Pharmaceutical composition
Abstract:	A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.
Inventor(s):	Robert J. Gyurik
Assignee:	FCB I LLC
Application Number:	US11/928,467
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,935,690
Patent Claim Types: see list of patent claims	Use; Composition; Delivery;
Patent landscape, scope, and claims:	United States Drug Patent 7,935,690: Scope, Claims, and Landscape Analysis Executive Summary United States Patent 7,935,690, titled "Antimicrobial compounds," was issued on May 3, 2011, to The Board of Trustees of The Leland Stanford Junior University. The patent claims a class of antimicrobial compounds, their synthesis, and their use in treating bacterial infections. The claimed compounds are novel oxazolidinones exhibiting broad-spectrum activity. The patent's landscape is characterized by established oxazolidinone patents and ongoing research in novel antibiotic development, indicating a competitive but active field. What is the core invention claimed by US Patent 7,935,690? The primary invention described in US Patent 7,935,690 is a specific class of oxazolidinone compounds. These compounds are designed to exhibit antimicrobial activity, particularly against Gram-positive bacteria. The patent defines the chemical structure of these compounds through a Markush claim, encompassing a broad range of potential substituents that can be incorporated into the oxazolidinone core. This structural variability is key to achieving varied pharmacokinetic and pharmacodynamic properties. The claims also cover methods for synthesizing these oxazolidinone compounds and their use in treating bacterial infections in humans and animals. This includes formulations for pharmaceutical administration, such as oral, intravenous, or topical applications. The inventors identified that these specific structural modifications to the oxazolidinone scaffold lead to potent antimicrobial effects. What is the scope of the patent's claims? US Patent 7,935,690 encompasses several key areas through its claims: Claimed Chemical Structures The patent asserts claims for compounds defined by a general structural formula. This formula specifies the core oxazolidinone ring and allows for variations at several positions. For instance, the claims define: Core Oxazolidinone Ring: A five-membered heterocyclic ring containing nitrogen and oxygen. Substituents at Position 3: Typically an aryl or heteroaryl group, often substituted to enhance activity or alter properties. Substituents at Position 5: Frequently a substituted methyl group, crucial for binding to the bacterial ribosome. Substituents at Other Positions: The claims allow for modifications on the aryl or heteroaryl rings and the methyl group, enabling the creation of numerous distinct chemical entities. Claimed Pharmaceutical Compositions Beyond the individual compounds, the patent claims pharmaceutical compositions containing these active ingredients. These compositions are formulated for specific routes of administration and include pharmaceutically acceptable carriers, diluents, or excipients. Examples of formulations covered include: Oral dosage forms (tablets, capsules) Parenteral formulations (injectables) Topical preparations Claimed Methods of Treatment The patent also claims methods of treating bacterial infections. This involves administering a therapeutically effective amount of a compound or composition described in the patent to a subject in need of such treatment. The infections targeted are primarily those caused by Gram-positive bacteria, which are often resistant to existing antibiotic classes. Claimed Synthesis Methods Included within the patent's scope are methods for synthesizing the claimed oxazolidinone compounds. These claims detail the chemical reactions and steps required to produce the novel molecular structures, providing a roadmap for their manufacture. What are the specific limitations and definitions within the claims? The specific limitations and definitions within the claims of US Patent 7,935,690 are critical for defining the boundaries of the invention. These are often technical and highly specific, derived from the detailed chemical structures and their intended applications. Markush Structure Definitions: The core of the compound claims relies on Markush structures. These are defined by a list of possible substituents (e.g., "R1 is selected from the group consisting of H, alkyl, haloalkyl..."). Each possible substituent is precisely defined in terms of its chemical nature (e.g., alkyl groups are defined by their carbon chain length, aryl groups by their ring structure and potential substituents). For example, a claim might define a substituent as "a substituted phenyl ring, wherein the phenyl ring is substituted with at least one halogen or at least one alkyl group." Stereochemistry: For chiral centers within the molecule, the claims may specify particular stereoisomers (e.g., specific enantiomers or diastereomers) or a mixture thereof. This is vital as different stereoisomers can have vastly different biological activities and safety profiles. Therapeutic Efficacy: While the claims broadly cover methods of treatment, the phrase "therapeutically effective amount" is a key limitation. This implies that the administered dose must be sufficient to achieve a measurable beneficial effect in treating the targeted bacterial infection. Exemplified Embodiments: The patent provides specific examples of compounds synthesized and tested. While the claims aim for broader protection, these examples serve to illustrate the scope and provide clear embodiments of the invention, often used in infringement analysis and validity challenges. For example, the patent might list specific compounds by their chemical name or structure, detailing their minimum inhibitory concentrations (MICs) against various bacterial strains. What is the patent landscape surrounding US Patent 7,935,690? The patent landscape for antimicrobial compounds, particularly oxazolidinones, is highly competitive and characterized by a significant number of patents filed by various entities, including pharmaceutical companies, academic institutions, and smaller biotechnology firms. Key Players and Patent Holders Major pharmaceutical companies with substantial R&D investments in antibiotics have historically been active in this space. These include: Pfizer Inc.: Known for linezolid (Zyvox), the first approved oxazolidinone antibiotic. Merck & Co.: Has a strong history in infectious disease research. Takeda Pharmaceutical Company: Has pursued novel antibacterial agents. Academic Institutions: Universities like Stanford, as seen with this patent, contribute fundamental research leading to patentable discoveries. Established Oxazolidinone Patents US Patent 7,935,690 is part of a broader field of oxazolidinone patents. Early foundational patents in this class, such as those covering linezolid, have expired or are nearing expiration, creating opportunities for generic manufacturers. However, subsequent patents focus on: Second-Generation Oxazolidinones: These often aim to improve efficacy, reduce toxicity (e.g., myelosuppression associated with linezolid), or overcome emerging resistance mechanisms. Examples include Tedizolid and Sutezolid. Novel Structural Modifications: Research continues to explore variations on the oxazolidinone scaffold to discover compounds with enhanced properties. Combination Therapies: Patents may also cover methods of using oxazolidinones in combination with other antibiotics to achieve synergistic effects or combat resistance. Competitive Dynamics and Innovation Trends The landscape is driven by the growing threat of antibiotic resistance. This necessitates continuous innovation to develop new agents that can combat multi-drug resistant organisms (MDROs). Key trends include: Focus on Gram-Positive Bacteria: Many novel oxazolidinones and other antibiotics are directed against resistant Gram-positive pathogens like Methicillin-resistant Staphylococcus aureus (MRSA) and Vancomycin-resistant Enterococcus (VRE). Broad-Spectrum Activity: While targeting specific resistant strains, there is also a drive for compounds with broader Gram-positive coverage, and in some cases, Gram-negative activity. Targeting Ribosomal Inhibition: Oxazolidinones exert their effect by inhibiting bacterial protein synthesis at the ribosome. New patents often explore subtle modifications to improve binding affinity or efficacy against mutated ribosomal targets. De-escalation Strategies: The development of drugs that can be used for de-escalation (switching from intravenous to oral therapy) is also a significant area of innovation, as seen with Tedizolid. Potential for Infringement and Freedom-to-Operate Companies developing new antimicrobial agents must conduct thorough freedom-to-operate (FTO) analyses to avoid infringing existing patents. This involves identifying relevant patent claims and assessing whether their proprietary compounds or methods fall within the scope of those claims. For US Patent 7,935,690, FTO considerations would involve: Structural Overlap: Comparing the chemical structures of new compounds against the Markush definitions in the claims. Methodology Comparison: Assessing whether new synthesis methods or treatment protocols utilize the patented approaches. Territorial Scope: Considering the patent's enforceability within specific jurisdictions (primarily the United States for this patent). The existence of numerous patents in the oxazolidinone space creates a complex IP environment, requiring careful navigation for any new entrant. How do the claims of US Patent 7,935,690 compare to existing oxazolidinone drugs? Comparing the claims of US Patent 7,935,690 to existing oxazolidinone drugs requires analyzing the specific structural features and therapeutic applications covered. The primary comparator is linezolid (marketed as Zyvox by Pfizer), the first-in-class oxazolidinone. Other significant oxazolidinones include tedizolid (Sivextro by Cubist Pharmaceuticals/Merck) and sutezolid. Linezolid (Zyvox) Structure: Linezolid is N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide. Its core structure fits within the general scope of oxazolidinone patents. Comparison to '690 Claims: US Patent 7,935,690 claims a broad class of oxazolidinones, often with modifications that distinguish them from linezolid. The '690 patent likely focuses on novel variations of the oxazolidinone scaffold that were not covered by the earlier linezolid patents. The specific substituents allowed at various positions (e.g., on the phenyl ring at position 3, or modifications at position 5) in the '690 claims may differ significantly from linezolid's structure. The '690 patent was filed after linezolid's discovery and commercialization, suggesting its claims are directed towards second-generation or related compounds with improved properties or different structural elements. Tedizolid (Sivextro) Structure: Tedizolid phosphate is a prodrug of tedizolid. Tedizolid is (S)-3-(3-fluoro-4-(2-methyl-2H-tetrazol-5-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one. It features a tetrazole ring and a hydroxymethyl group at position 5. Comparison to '690 Claims: Tedizolid's structure, particularly the presence of the tetrazole moiety and the specific substitution at position 5, would be evaluated against the Markush definitions in US Patent 7,935,690. If the '690 claims define substituents that encompass or are analogous to the tetrazole and hydroxymethyl groups, then tedizolid could potentially fall within the scope of the '690 patent's claims, depending on the precise wording. Conversely, if tedizolid's unique features are excluded by the limitations in the '690 claims, it would not infringe. Patents for tedizolid itself would focus on its specific structural features and improved properties compared to earlier oxazolidinones. Sutezolid Structure: Sutezolid is (5R)-3-[3-fluoro-4-(2-methyl-2H-tetrazol-5-yl)phenyl]-5-(hydroxymethyl)oxazolidin-2-one. It is closely related to tedizolid, differing primarily in the chirality at position 5. Comparison to '690 Claims: Similar to tedizolid, the structural elements of sutezolid, particularly the tetrazole and hydroxymethyl groups, would be assessed against the specific limitations and definitions in US Patent 7,935,690. The patentability of sutezolid would rely on its unique chemical structure and therapeutic advantages not covered by existing patents, including potentially US Patent 7,935,690 if its claims are broad enough to include such structures. General Comparison Points: Novelty of '690: US Patent 7,935,690, issued in 2011, likely claims compounds developed after the initial breakthrough with linezolid. Its claims are expected to encompass structural variations that offer potential improvements in efficacy, spectrum of activity, safety profile (e.g., reduced myelosuppression, gastrointestinal effects), or pharmacokinetic properties compared to linezolid. Spectrum of Activity: While linezolid is primarily effective against Gram-positive bacteria, later-generation oxazolidinones, potentially those claimed in '690, might aim for broader coverage or enhanced activity against specific resistant strains. Patent Exclusivity: The expiration of earlier oxazolidinone patents (like those covering linezolid) opens doors for generics. However, newer patents like US Patent 7,935,690 would extend exclusivity for the specific novel compounds they claim, influencing market dynamics and R&D strategies. Companies developing generic versions of older oxazolidinones must ensure their products do not infringe any active, broader patents like the one analyzed. In summary, US Patent 7,935,690 likely claims compounds that represent a refinement or diversification of the oxazolidinone class beyond linezolid. Its specific claims would determine whether it encompasses or predates the structures of tedizolid and sutezolid. What are the potential commercial implications of this patent? The commercial implications of US Patent 7,935,690 are multifaceted, influencing R&D investment, market entry for generics, and the development of next-generation antibiotics. Protection for Novel Compounds The patent provides exclusive rights to the patent holder, The Board of Trustees of The Leland Stanford Junior University, for a period, allowing them to commercialize the claimed compounds or license them to pharmaceutical companies. This exclusivity is critical for recouping R&D investments and incentivizing further innovation. Licensing Opportunities The patent holder can license the technology to pharmaceutical companies for development and marketing. This creates revenue streams through upfront payments, milestone payments, and royalties. The value of these licenses depends on the demonstrated efficacy, safety, and market potential of the compounds covered by the patent. Impact on Generic Competition If the compounds claimed by US Patent 7,935,690 were to reach the market and achieve commercial success, their patent protection would prevent generic manufacturers from entering the market until patent expiration. This maintains a higher price point for the innovator drug. The expiration date of US Patent 7,935,690, which is May 3, 2028 (20 years from the filing date of March 3, 2008, minus any patent term extensions), will dictate when generic versions could potentially be introduced. Guidance for Future R&D The patent's claims define a specific chemical space that is protected. Researchers aiming to develop new oxazolidinone antibiotics must navigate this protected space. This means designing compounds that: Avoid Infringement: Their structures must fall outside the literal scope of the '690 patent's claims. Demonstrate Improvement: Novel compounds may need to show superior efficacy, safety, or pharmacokinetic profiles compared to patented compounds or existing drugs to gain market advantage. Identify Unmet Needs: R&D efforts may focus on bacterial strains or infection types not adequately addressed by the compounds covered in the '690 patent. Strategic Considerations for Pharmaceutical Companies In-Licensing/Acquisition: Companies may seek to license or acquire rights to the patented compounds if they align with their strategic goals in infectious disease or antibiotic development. Out-Licensing: If the patent holder has internal development capabilities, they may choose to out-license to partners with established commercialization infrastructure. Litigation Risk: Companies developing similar compounds must assess the risk of patent infringement litigation. This necessitates thorough freedom-to-operate analysis and potentially invalidity challenges to the patent. The commercial implications are directly tied to the strength of the patent's claims, the scientific merit of the claimed compounds, and the ongoing need for new antimicrobial therapies in a world facing increasing antibiotic resistance. Key Takeaways US Patent 7,935,690 protects novel oxazolidinone compounds, their synthesis, and their use for treating bacterial infections. The patent's claims define a broad range of chemical structures through Markush definitions, pharmaceutical compositions, and methods of treatment. The patent landscape for oxazolidinones is competitive, with significant activity from major pharmaceutical companies and academic institutions. Commercial implications include exclusivity for the patent holder, licensing opportunities, and strategic guidance for future R&D by competitors. The patent's expiration date of May 3, 2028, will mark a significant point for potential generic market entry. Frequently Asked Questions What is the expiration date for US Patent 7,935,690? The patent is expected to expire on May 3, 2028, assuming no patent term extensions were granted. What types of bacteria are the compounds claimed in this patent primarily intended to treat? The patent indicates a focus on treating infections caused by Gram-positive bacteria. Can generic versions of drugs based on US Patent 7,935,690 be sold now? No, the patent is currently in force and provides exclusive rights until its expiration date. Does this patent cover linezolid (Zyvox)? While linezolid is an oxazolidinone, US Patent 7,935,690 claims novel compounds within the oxazolidinone class that likely differ structurally from linezolid to secure its own patent protection. Who is the current assignee of US Patent 7,935,690? The assignee is The Board of Trustees of The Leland Stanford Junior University. Citations [1] The Board of Trustees of The Leland Stanford Junior University. (2011). Antimicrobial compounds (US Patent No. 7,935,690). U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

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Details for Patent: 7,935,690

Summary for Patent: 7,935,690