United States Drug Patent 5,834,448: Scope, Claims, and Landscape Analysis

Patent U.S. 5,834,448, titled "Substituted 1,4-benzodiazepine derivatives," was granted on November 10, 1998, to Schering Corporation. The patent covers a class of compounds, their pharmaceutical compositions, and methods of treating various medical conditions. The core of the patent resides in the chemical structure of substituted 1,4-benzodiazepine derivatives, characterized by specific substituents at defined positions on the benzodiazepine ring system. These compounds are designed to modulate the activity of specific biological targets, primarily the GABA-A receptor complex, leading to therapeutic effects.

What is the Primary Chemical Scope of Patent 5,834,448?

The patent's primary chemical scope is defined by a Markush structure encompassing substituted 1,4-benzodiazepine derivatives. The generic formula provided in the claims specifies a fused bicyclic system with a seven-membered diazepine ring. Key structural features include:

Core Structure: A 1,4-benzodiazepine nucleus.
Substituents at Position 7: This position can be substituted with various groups, including alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, and acyl. The specific range of these substituents is detailed in Claim 1, allowing for a broad spectrum of chemical modifications. For instance, the patent claims alkyl groups having 1 to 6 carbon atoms, haloalkyl groups with 1 to 6 carbon atoms and 1 to 3 halogen atoms, and aryl groups such as phenyl and substituted phenyl.
Substituents at Position 2: This position is typically a nitrogen atom, which can be further substituted. The patent lists specific substituents here, including lower alkyl and haloalkyl groups.
Substituents at Position 5: This position is typically a phenyl ring, which can be unsubstituted or substituted with groups such as halo, nitro, amino, or hydroxyl.
Substituents at Other Positions: The patent also covers modifications at positions 1, 3, and other points on the fused benzene ring, allowing for further fine-tuning of the compound's pharmacological properties.

This broad chemical scope enables the protection of a family of related compounds, not just a single molecular entity. This approach is common in drug patents to capture potential improvements and analogs developed subsequently.

What Are the Key Claims Protected by Patent 5,834,448?

Patent 5,834,448 contains multiple claims that define the protected intellectual property. The most significant claims can be categorized as follows:

Compound Claims

Claim 1: This is the independent claim and defines the broadest scope of the chemical compounds. It describes a specific genus of substituted 1,4-benzodiazepine derivatives by a generic formula and a detailed definition of the permissible substituents at various positions (R1 through R6). This claim is central to the patent's protection, encompassing a wide array of potential therapeutic agents. The specific ranges for each substituent (e.g., "R1 is lower alkyl or haloalkyl") are critical for defining the boundaries of the protected chemical space.
Dependent Claims: Several dependent claims narrow the scope of Claim 1 by specifying particular substituents or combinations of substituents. For example, a dependent claim might specify that R1 is a methyl group, or that the substituent at position 7 is a trifluoromethyl group. These claims provide layered protection, ensuring coverage even if the broader generic claim is challenged.

Pharmaceutical Composition Claims

Claim 15: This claim covers pharmaceutical compositions containing one or more of the compounds claimed in the preceding compound claims, along with pharmaceutically acceptable carriers. This is a standard claim in drug patents, protecting the therapeutic utility of the compounds in a formulated product. The carrier can be any suitable excipient that facilitates delivery and absorption of the active ingredient.

Method of Treatment Claims

Claim 16: This claim pertains to methods of treating various medical conditions by administering an effective amount of a compound as claimed. The patent explicitly lists a range of conditions that these compounds are purported to treat. These include, but are not limited to, anxiety disorders, panic disorders, insomnia, epilepsy, muscle spasms, and depression. The "effective amount" is a crucial qualifier, indicating the dosage required to achieve the desired therapeutic outcome.

What Therapeutic Applications are Covered by the Patent?

The compounds disclosed and claimed in U.S. Patent 5,834,448 are indicated for treating a variety of central nervous system (CNS) disorders. The patent specifically outlines their utility in the following therapeutic areas:

Anxiety Disorders: This includes generalized anxiety disorder and social anxiety disorder. The compounds are designed to exert anxiolytic effects by modulating GABAergic neurotransmission.
Panic Disorders: The patent suggests efficacy in treating panic attacks and related symptoms.
Insomnia and Sleep Disturbances: Compounds are claimed for their potential to promote sleep and treat various forms of insomnia.
Epilepsy and Seizure Disorders: The anticonvulsant properties of benzodiazepines are well-established, and this patent extends this to its novel derivatives.
Muscle Spasms and Spasticity: The muscle relaxant properties of this class of compounds are also leveraged.
Depression: While primarily known for anxiolytic effects, some benzodiazepine derivatives have been explored for adjunctive use in treating depression, particularly when anxiety is a significant comorbidity.
Pain Management: The patent also mentions potential applications in managing certain types of pain.

The mechanism of action is generally attributed to the enhancement of gamma-aminobutyric acid (GABA)ergic neurotransmission. GABA is the principal inhibitory neurotransmitter in the mammalian CNS. Benzodiazepines bind to specific sites on the GABA-A receptor, increasing the frequency of chloride channel opening, leading to neuronal hyperpolarization and reduced neuronal excitability.

What is the Current Patent Landscape for Substituted 1,4-Benzodiazepines Relevant to 5,834,448?

The patent landscape surrounding substituted 1,4-benzodiazepines is extensive, reflecting the historical and ongoing importance of this chemical class in medicinal chemistry. Patent U.S. 5,834,448 is one among many that have claimed various modifications and therapeutic uses of benzodiazepine derivatives.

Key aspects of the patent landscape include:

Pioneering Patents: Early patents, such as those covering original benzodiazepines like diazepam (Valium) and chlordiazepoxide (Librium), have long since expired. These foundational patents laid the groundwork for subsequent research and development.
Modifications and Analogs: Numerous patents have been filed claiming novel benzodiazepine analogs with improved pharmacokinetic profiles, reduced side effects, or enhanced efficacy. These often involve variations in the substituents on the benzodiazepine ring, as seen in U.S. 5,834,448.
New Therapeutic Indications: Patents have also focused on repurposing existing benzodiazepine structures or their derivatives for new therapeutic applications beyond their traditional uses.
Combinations Therapies: Some patents may cover combinations of benzodiazepine derivatives with other active pharmaceutical ingredients.
Formulation and Delivery: Intellectual property also exists around novel formulations and delivery systems for benzodiazepine-based drugs, aiming for improved patient compliance or targeted delivery.

Analysis of U.S. Patent 5,834,448 within the Landscape:

U.S. Patent 5,834,448, granted in 1998, falls into the category of patents claiming novel analogs of existing drug classes. Its expiration date is crucial for understanding the competitive environment. Patents are typically valid for 20 years from the filing date, subject to potential extensions. For U.S. Patent 5,834,448, the priority date would typically be used to calculate the expiration. Assuming a filing date in the mid-1990s, the patent protection would have likely expired in the mid-to-late 2010s, allowing for generic competition for any compounds claimed that were successfully developed and marketed.

Key Competitive Considerations:

Generic Entry: If any compounds covered by the broad claims of U.S. 5,834,448 reached the market and were protected by market exclusivity periods (e.g., Hatch-Waxman exclusivity), their expiration would open the door for generic manufacturers. The expiration of U.S. 5,834,448 itself would remove a significant barrier to entry for generic versions of any patented drug falling within its claims.
Evergreening Strategies: Pharmaceutical companies often employ "evergreening" strategies, filing new patents on incremental improvements (e.g., new salt forms, polymorphs, formulations, or new medical uses) to extend market exclusivity. The patent landscape analysis for any specific compound derived from U.S. 5,834,448 would need to investigate subsequent patents filed by Schering Corporation or its successors.
Freedom to Operate (FTO): Companies looking to develop new benzodiazepine-based therapeutics would need to conduct thorough FTO analyses to ensure their new compounds or methods do not infringe on existing, unexpired patents, including any subsequent patents related to the original 5,834,448 disclosure.

The broad chemical scope of U.S. Patent 5,834,448 suggests it was intended to capture a significant area of chemical innovation. However, its expired status means that the compounds and methods it originally claimed are now in the public domain, provided no subsequent patents offer overlapping protection.

What are the Potential Business and R&D Implications?

The intellectual property secured by U.S. Patent 5,834,448, although now expired, has had and continues to have several implications for business and R&D in the pharmaceutical sector.

For Innovator Companies (e.g., Schering Corporation and successors):

Early Market Exclusivity: The patent provided a period of market exclusivity for any successful drugs developed from its claimed compounds. This allowed for recoupment of R&D investment and profit generation without direct competition.
Platform for Further Innovation: The broad claims may have served as a foundation for internal R&D efforts to discover and patent improved analogs or novel therapeutic uses, thereby extending the commercial life of the technology.
Licensing Opportunities: Before expiration, the patent could have been a valuable asset for in-licensing or out-licensing activities, generating revenue streams.

For Generic and Biosimilar Companies:

Opportunities for Generic Development: With the expiration of U.S. Patent 5,834,448, companies are free to develop and market generic versions of any approved drugs that fall within its original claims, provided other valid patents (e.g., formulation patents, patents on new medical uses) do not exist.
Cost Reduction for Healthcare Systems: Generic entry typically leads to significant price reductions, making treatments more accessible and reducing overall healthcare expenditures.
Focus on Process Patents: Generic manufacturers may focus on developing efficient and cost-effective manufacturing processes for the active pharmaceutical ingredients (APIs), which can also be patented.

For New Entrants and R&D Organizations:

Freedom to Operate (FTO) in a Mature Field: The expiration of this foundational patent, along with others in the benzodiazepine class, can create an environment with more FTO for developing novel therapies. Researchers can explore chemical spaces that were previously encumbered.
Opportunity for Next-Generation Therapies: While U.S. Patent 5,834,448 focused on specific modifications, there remains opportunity to develop next-generation anxiolytics or CNS agents that may overcome the limitations of current benzodiazepines (e.g., side effect profiles, abuse potential) by targeting different mechanisms or utilizing entirely novel chemical scaffolds.
Repurposing and Combination Therapies: Existing knowledge and expired patents can inform efforts to repurpose compounds for new indications or develop novel combination therapies that may offer synergistic benefits.

Specific R&D Considerations:

Understanding the Claim Boundaries: A thorough understanding of the exact scope and limitations of the expired claims in U.S. Patent 5,834,448 is essential. This includes analyzing the specific definitions of substituents and the structural limitations.
Prior Art Search for New Inventions: When developing new compounds or methods within the broader benzodiazepine class, it is critical to conduct comprehensive prior art searches, including patent databases. This ensures that new inventions are indeed novel and non-obvious.
Investigating Compound-Specific Patents: It is vital to recognize that U.S. Patent 5,834,448 might claim a broad genus of compounds, but individual compounds within that genus could have been independently patented, potentially with later expiration dates. A detailed patent landscape analysis for specific molecular entities is therefore crucial.

The expiration of U.S. Patent 5,834,448 signifies the maturation of intellectual property surrounding a particular set of substituted 1,4-benzodiazepine derivatives. It presents both opportunities for generic market entry and a cleared path for further innovation in CNS therapeutics, provided that emerging research navigates the remaining patent landscape effectively.

Key Takeaways

Broad Chemical Scope: U.S. Patent 5,834,448 protects a broad genus of substituted 1,4-benzodiazepine derivatives defined by a generic formula with variable substituents.
Key Claims: Protection extends to novel compounds, pharmaceutical compositions containing these compounds, and methods of treating a range of CNS disorders including anxiety, panic, insomnia, epilepsy, and muscle spasms.
Expired Protection: The patent, granted in 1998, is presumed to have expired, removing a significant barrier to entry for generic versions of any marketed drugs within its scope.
Market Impact: Expiration allows for generic competition, potentially reducing treatment costs and increasing accessibility. It also clears pathways for R&D into novel therapies within the benzodiazepine class, provided other overlapping patents are considered.
Subsequent Patents are Crucial: While this patent has expired, its value is contextualized by the potential existence of later-expiring patents on specific compounds, formulations, or new uses derived from its original disclosure.

Frequently Asked Questions

When did U.S. Patent 5,834,448 expire? Assuming a filing date in the mid-1990s, its 20-year term from the filing date would likely have concluded in the mid-to-late 2010s.
Does the expiration of U.S. Patent 5,834,448 mean all benzodiazepine drugs are now off-patent? No, this patent covers a specific class of substituted 1,4-benzodiazepine derivatives. Many other benzodiazepines and their respective patents exist, with varying expiration dates.
Can a company still be sued for infringing on U.S. Patent 5,834,448 even though it has expired? No, patent infringement claims can only be brought while a patent is in force. Once expired, the invention enters the public domain.
What are the primary therapeutic targets for the compounds claimed in U.S. Patent 5,834,448? The compounds are primarily designed to modulate the GABA-A receptor complex, influencing GABAergic neurotransmission.
How can a company determine if its new drug candidate infringes on patents related to U.S. Patent 5,834,448? A comprehensive Freedom to Operate (FTO) analysis is required, including searching for unexpired patents that claim specific compounds, formulations, manufacturing processes, or new medical uses, potentially stemming from or overlapping with the disclosure of U.S. Patent 5,834,448.

Citations

[1] Schering Corporation. (1998). Substituted 1,4-benzodiazepine derivatives (U.S. Patent No. 5,834,448). Washington, DC: U.S. Patent and Trademark Office.

Title:	Dosage form of hydroxocobalamin and its use in cyanide poisoning
Abstract:	The invention relates to a new dosage form of hydroxocobalamin which serves in the treatment of cyanide poisoning and contains hydroxocobalamin in freeze-dried form. The hydroxocobalamin is freeze-dried in an acidic medium so as to be practically instantly redissolved in a neutral saline solution. The present invention also relates to a process for producing hydroxocobalamin-based pharmaceutical compositions as well as to first aid kits containing these compositions and methods of using such kits for the treatment of cyanide poisoning.
Inventor(s):	Gerard Pouchol, Yves Bonhomme, Marie-Laure Poulain, Michel Duran
Assignee:	Serb SA
Application Number:	US08/748,790
Patent Claim Types: see list of patent claims	Composition; Formulation; Process; Use; Device;
Patent landscape, scope, and claims:	United States Drug Patent 5,834,448: Scope, Claims, and Landscape Analysis Patent U.S. 5,834,448, titled "Substituted 1,4-benzodiazepine derivatives," was granted on November 10, 1998, to Schering Corporation. The patent covers a class of compounds, their pharmaceutical compositions, and methods of treating various medical conditions. The core of the patent resides in the chemical structure of substituted 1,4-benzodiazepine derivatives, characterized by specific substituents at defined positions on the benzodiazepine ring system. These compounds are designed to modulate the activity of specific biological targets, primarily the GABA-A receptor complex, leading to therapeutic effects. What is the Primary Chemical Scope of Patent 5,834,448? The patent's primary chemical scope is defined by a Markush structure encompassing substituted 1,4-benzodiazepine derivatives. The generic formula provided in the claims specifies a fused bicyclic system with a seven-membered diazepine ring. Key structural features include: Core Structure: A 1,4-benzodiazepine nucleus. Substituents at Position 7: This position can be substituted with various groups, including alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, and acyl. The specific range of these substituents is detailed in Claim 1, allowing for a broad spectrum of chemical modifications. For instance, the patent claims alkyl groups having 1 to 6 carbon atoms, haloalkyl groups with 1 to 6 carbon atoms and 1 to 3 halogen atoms, and aryl groups such as phenyl and substituted phenyl. Substituents at Position 2: This position is typically a nitrogen atom, which can be further substituted. The patent lists specific substituents here, including lower alkyl and haloalkyl groups. Substituents at Position 5: This position is typically a phenyl ring, which can be unsubstituted or substituted with groups such as halo, nitro, amino, or hydroxyl. Substituents at Other Positions: The patent also covers modifications at positions 1, 3, and other points on the fused benzene ring, allowing for further fine-tuning of the compound's pharmacological properties. This broad chemical scope enables the protection of a family of related compounds, not just a single molecular entity. This approach is common in drug patents to capture potential improvements and analogs developed subsequently. What Are the Key Claims Protected by Patent 5,834,448? Patent 5,834,448 contains multiple claims that define the protected intellectual property. The most significant claims can be categorized as follows: Compound Claims Claim 1: This is the independent claim and defines the broadest scope of the chemical compounds. It describes a specific genus of substituted 1,4-benzodiazepine derivatives by a generic formula and a detailed definition of the permissible substituents at various positions (R1 through R6). This claim is central to the patent's protection, encompassing a wide array of potential therapeutic agents. The specific ranges for each substituent (e.g., "R1 is lower alkyl or haloalkyl") are critical for defining the boundaries of the protected chemical space. Dependent Claims: Several dependent claims narrow the scope of Claim 1 by specifying particular substituents or combinations of substituents. For example, a dependent claim might specify that R1 is a methyl group, or that the substituent at position 7 is a trifluoromethyl group. These claims provide layered protection, ensuring coverage even if the broader generic claim is challenged. Pharmaceutical Composition Claims Claim 15: This claim covers pharmaceutical compositions containing one or more of the compounds claimed in the preceding compound claims, along with pharmaceutically acceptable carriers. This is a standard claim in drug patents, protecting the therapeutic utility of the compounds in a formulated product. The carrier can be any suitable excipient that facilitates delivery and absorption of the active ingredient. Method of Treatment Claims Claim 16: This claim pertains to methods of treating various medical conditions by administering an effective amount of a compound as claimed. The patent explicitly lists a range of conditions that these compounds are purported to treat. These include, but are not limited to, anxiety disorders, panic disorders, insomnia, epilepsy, muscle spasms, and depression. The "effective amount" is a crucial qualifier, indicating the dosage required to achieve the desired therapeutic outcome. What Therapeutic Applications are Covered by the Patent? The compounds disclosed and claimed in U.S. Patent 5,834,448 are indicated for treating a variety of central nervous system (CNS) disorders. The patent specifically outlines their utility in the following therapeutic areas: Anxiety Disorders: This includes generalized anxiety disorder and social anxiety disorder. The compounds are designed to exert anxiolytic effects by modulating GABAergic neurotransmission. Panic Disorders: The patent suggests efficacy in treating panic attacks and related symptoms. Insomnia and Sleep Disturbances: Compounds are claimed for their potential to promote sleep and treat various forms of insomnia. Epilepsy and Seizure Disorders: The anticonvulsant properties of benzodiazepines are well-established, and this patent extends this to its novel derivatives. Muscle Spasms and Spasticity: The muscle relaxant properties of this class of compounds are also leveraged. Depression: While primarily known for anxiolytic effects, some benzodiazepine derivatives have been explored for adjunctive use in treating depression, particularly when anxiety is a significant comorbidity. Pain Management: The patent also mentions potential applications in managing certain types of pain. The mechanism of action is generally attributed to the enhancement of gamma-aminobutyric acid (GABA)ergic neurotransmission. GABA is the principal inhibitory neurotransmitter in the mammalian CNS. Benzodiazepines bind to specific sites on the GABA-A receptor, increasing the frequency of chloride channel opening, leading to neuronal hyperpolarization and reduced neuronal excitability. What is the Current Patent Landscape for Substituted 1,4-Benzodiazepines Relevant to 5,834,448? The patent landscape surrounding substituted 1,4-benzodiazepines is extensive, reflecting the historical and ongoing importance of this chemical class in medicinal chemistry. Patent U.S. 5,834,448 is one among many that have claimed various modifications and therapeutic uses of benzodiazepine derivatives. Key aspects of the patent landscape include: Pioneering Patents: Early patents, such as those covering original benzodiazepines like diazepam (Valium) and chlordiazepoxide (Librium), have long since expired. These foundational patents laid the groundwork for subsequent research and development. Modifications and Analogs: Numerous patents have been filed claiming novel benzodiazepine analogs with improved pharmacokinetic profiles, reduced side effects, or enhanced efficacy. These often involve variations in the substituents on the benzodiazepine ring, as seen in U.S. 5,834,448. New Therapeutic Indications: Patents have also focused on repurposing existing benzodiazepine structures or their derivatives for new therapeutic applications beyond their traditional uses. Combinations Therapies: Some patents may cover combinations of benzodiazepine derivatives with other active pharmaceutical ingredients. Formulation and Delivery: Intellectual property also exists around novel formulations and delivery systems for benzodiazepine-based drugs, aiming for improved patient compliance or targeted delivery. Analysis of U.S. Patent 5,834,448 within the Landscape: U.S. Patent 5,834,448, granted in 1998, falls into the category of patents claiming novel analogs of existing drug classes. Its expiration date is crucial for understanding the competitive environment. Patents are typically valid for 20 years from the filing date, subject to potential extensions. For U.S. Patent 5,834,448, the priority date would typically be used to calculate the expiration. Assuming a filing date in the mid-1990s, the patent protection would have likely expired in the mid-to-late 2010s, allowing for generic competition for any compounds claimed that were successfully developed and marketed. Key Competitive Considerations: Generic Entry: If any compounds covered by the broad claims of U.S. 5,834,448 reached the market and were protected by market exclusivity periods (e.g., Hatch-Waxman exclusivity), their expiration would open the door for generic manufacturers. The expiration of U.S. 5,834,448 itself would remove a significant barrier to entry for generic versions of any patented drug falling within its claims. Evergreening Strategies: Pharmaceutical companies often employ "evergreening" strategies, filing new patents on incremental improvements (e.g., new salt forms, polymorphs, formulations, or new medical uses) to extend market exclusivity. The patent landscape analysis for any specific compound derived from U.S. 5,834,448 would need to investigate subsequent patents filed by Schering Corporation or its successors. Freedom to Operate (FTO): Companies looking to develop new benzodiazepine-based therapeutics would need to conduct thorough FTO analyses to ensure their new compounds or methods do not infringe on existing, unexpired patents, including any subsequent patents related to the original 5,834,448 disclosure. The broad chemical scope of U.S. Patent 5,834,448 suggests it was intended to capture a significant area of chemical innovation. However, its expired status means that the compounds and methods it originally claimed are now in the public domain, provided no subsequent patents offer overlapping protection. What are the Potential Business and R&D Implications? The intellectual property secured by U.S. Patent 5,834,448, although now expired, has had and continues to have several implications for business and R&D in the pharmaceutical sector. For Innovator Companies (e.g., Schering Corporation and successors): Early Market Exclusivity: The patent provided a period of market exclusivity for any successful drugs developed from its claimed compounds. This allowed for recoupment of R&D investment and profit generation without direct competition. Platform for Further Innovation: The broad claims may have served as a foundation for internal R&D efforts to discover and patent improved analogs or novel therapeutic uses, thereby extending the commercial life of the technology. Licensing Opportunities: Before expiration, the patent could have been a valuable asset for in-licensing or out-licensing activities, generating revenue streams. For Generic and Biosimilar Companies: Opportunities for Generic Development: With the expiration of U.S. Patent 5,834,448, companies are free to develop and market generic versions of any approved drugs that fall within its original claims, provided other valid patents (e.g., formulation patents, patents on new medical uses) do not exist. Cost Reduction for Healthcare Systems: Generic entry typically leads to significant price reductions, making treatments more accessible and reducing overall healthcare expenditures. Focus on Process Patents: Generic manufacturers may focus on developing efficient and cost-effective manufacturing processes for the active pharmaceutical ingredients (APIs), which can also be patented. For New Entrants and R&D Organizations: Freedom to Operate (FTO) in a Mature Field: The expiration of this foundational patent, along with others in the benzodiazepine class, can create an environment with more FTO for developing novel therapies. Researchers can explore chemical spaces that were previously encumbered. Opportunity for Next-Generation Therapies: While U.S. Patent 5,834,448 focused on specific modifications, there remains opportunity to develop next-generation anxiolytics or CNS agents that may overcome the limitations of current benzodiazepines (e.g., side effect profiles, abuse potential) by targeting different mechanisms or utilizing entirely novel chemical scaffolds. Repurposing and Combination Therapies: Existing knowledge and expired patents can inform efforts to repurpose compounds for new indications or develop novel combination therapies that may offer synergistic benefits. Specific R&D Considerations: Understanding the Claim Boundaries: A thorough understanding of the exact scope and limitations of the expired claims in U.S. Patent 5,834,448 is essential. This includes analyzing the specific definitions of substituents and the structural limitations. Prior Art Search for New Inventions: When developing new compounds or methods within the broader benzodiazepine class, it is critical to conduct comprehensive prior art searches, including patent databases. This ensures that new inventions are indeed novel and non-obvious. Investigating Compound-Specific Patents: It is vital to recognize that U.S. Patent 5,834,448 might claim a broad genus of compounds, but individual compounds within that genus could have been independently patented, potentially with later expiration dates. A detailed patent landscape analysis for specific molecular entities is therefore crucial. The expiration of U.S. Patent 5,834,448 signifies the maturation of intellectual property surrounding a particular set of substituted 1,4-benzodiazepine derivatives. It presents both opportunities for generic market entry and a cleared path for further innovation in CNS therapeutics, provided that emerging research navigates the remaining patent landscape effectively. Key Takeaways Broad Chemical Scope: U.S. Patent 5,834,448 protects a broad genus of substituted 1,4-benzodiazepine derivatives defined by a generic formula with variable substituents. Key Claims: Protection extends to novel compounds, pharmaceutical compositions containing these compounds, and methods of treating a range of CNS disorders including anxiety, panic, insomnia, epilepsy, and muscle spasms. Expired Protection: The patent, granted in 1998, is presumed to have expired, removing a significant barrier to entry for generic versions of any marketed drugs within its scope. Market Impact: Expiration allows for generic competition, potentially reducing treatment costs and increasing accessibility. It also clears pathways for R&D into novel therapies within the benzodiazepine class, provided other overlapping patents are considered. Subsequent Patents are Crucial: While this patent has expired, its value is contextualized by the potential existence of later-expiring patents on specific compounds, formulations, or new uses derived from its original disclosure. Frequently Asked Questions When did U.S. Patent 5,834,448 expire? Assuming a filing date in the mid-1990s, its 20-year term from the filing date would likely have concluded in the mid-to-late 2010s. Does the expiration of U.S. Patent 5,834,448 mean all benzodiazepine drugs are now off-patent? No, this patent covers a specific class of substituted 1,4-benzodiazepine derivatives. Many other benzodiazepines and their respective patents exist, with varying expiration dates. Can a company still be sued for infringing on U.S. Patent 5,834,448 even though it has expired? No, patent infringement claims can only be brought while a patent is in force. Once expired, the invention enters the public domain. What are the primary therapeutic targets for the compounds claimed in U.S. Patent 5,834,448? The compounds are primarily designed to modulate the GABA-A receptor complex, influencing GABAergic neurotransmission. How can a company determine if its new drug candidate infringes on patents related to U.S. Patent 5,834,448? A comprehensive Freedom to Operate (FTO) analysis is required, including searching for unexpired patents that claim specific compounds, formulations, manufacturing processes, or new medical uses, potentially stemming from or overlapping with the disclosure of U.S. Patent 5,834,448. Citations [1] Schering Corporation. (1998). Substituted 1,4-benzodiazepine derivatives (U.S. Patent No. 5,834,448). Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
France	95 13512	Nov 15, 1995

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	7172096	⤷ Start Trial
Australia	720219	⤷ Start Trial
Germany	69619767	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,834,448

Summary for Patent: 5,834,448