Drugs covered by patent 3,968,249. Claims, international patent equivalents, patent expiration dates, and generic entry

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,968,249

Introduction

United States Patent 3,968,249 (the '249 patent), granted on March 30, 1976, represents a foundational intellectual property asset in the pharmaceutical arena. It pertains to a novel chemical compound, its synthesis, pharmaceutical compositions, and potential therapeutic uses. This analysis dissects the scope and claims of the patent, contextualizing its position within the broader patent landscape of related compounds and therapeutic indications, and evaluates its implications for stakeholders ranging from innovators to competitors.

Overview of the '249 Patent

The '249 patent, assigned to a pioneering pharmaceutical entity, embodies an inventive step in medicinal chemistry through its directed compounds. Primarily, the patent claims cover a specific class of chemical entities characterized by a defined core structure and particular substituents, which exhibit promising pharmacological activity—most notably as central nervous system (CNS) agents.

The patent's filing date, August 11, 1973, predates many subsequent approvals and innovations, marking it as a significant early milestone. Its claims extend to the compound itself, methods of synthesis, pharmaceutical formulations, and methods of therapeutic use for specific indications such as anxiolytic, sedative, or anticonvulsant effects.

Scope of the Patent Claims

1. Composition of Matter Claims

The core claims focus on a class of compounds characterized by a benzodiazepine-like structure, with specific substitutions on the aromatic rings and heterocycles. These claims define a broad chemical genus, potentially encompassing numerous compounds with similar core frameworks but varying substituents.

Claim 1 specifies a chemical compound within the class, delineated by the chemical formula provided, including particular groups attached to the heterocyclic core.
Dependent Claims (2-10) narrow the scope to specific substitutions, such as halogen, methyl, or alkoxy groups at certain positions, enhancing the patent's coverage of particular derivatives.

2. Methods of Synthesis

Claims extend to processes for preparing the claimed compounds, typically involving multi-step organic reactions, including condensation, cyclization, or substitution reactions. These process claims ensure broad protection for synthesis routes known or developed after the patent issuance.

3. Pharmaceutical Use Claims

The patent claims include methods of treating CNS disorders by administering the claimed compounds, covering both the compounds themselves and their medical uses. This dual claim strategy provides a safeguard against design-arounds that could bypass chemical composition claims by shifting to method assertions.

Treatment of anxiety, insomnia, and epilepsy are specifically cited indications, supported by pharmacological data generated and included in the patent specification.

Implications of the Scope

The broad chemical class claims create a sizable patent estate, covering numerous derivatives, which can impact subsequent medicinal chemistry efforts. The method-of-use claims further extend the patent protection into therapeutic applications, vital for downstream drug development and licensing strategies.

However, the scope's breadth can be challenged based on prior art or obviousness grounds, especially with compounds published or synthesized pre-1976. The specificity of substitutions and particular pharmacological data can influence patent enforceability and the likelihood of infringement findings.

Patent Landscape Analysis

1. Preceding and Related Patents

Before the '249 patent, earlier patents covered benzodiazepine derivatives for CNS therapeutics, such as U.S. Patent 3,382,183 (the first benzodiazepines, including chlordiazepoxide). The '249 patent built upon these foundations, differentiating through chemical structure modifications and enhanced pharmacological profiles.

Subsequently, numerous patents have claimed related benzodiazepine derivatives, including improvements in potency, reduced side effects, or novel pharmacokinetics. Notably, later innovations have sought to avoid licensing blocks or to circumvent the '249 patent ambiguities through structural modifications.

2. Patent Expiration and Generic Entry

Given its filing and granting dates, the '249 patent would have expired around 1993, absent terminal disclaimers or adjustments for term extensions. Expiry opens the landscape for generics, which subsequently entered markets for benzodiazepine sedatives, anxiolytics, and anticonvulsants.

3. Contemporary Patent Strategies

Modern patenting strategies often involve filing supplementary patents relating to specific formulations, methods of use for new indications, or polymorphic forms. The original '249 patent's broad claims do not preclude such incremental patentings, which can extend exclusivity periods via patent term extensions, or new use patents under the Hatch-Waxman framework.

Legal and Commercial Significance

The '249 patent's broad chemical scope provided a strategic advantage, preventing competitors from readily designing around its claims during patent life. Its claims on therapeutic methods amplified that protection, fostering licensing and commercialization efforts.

Over time, generic manufacturers exploited patent expirations, leading to wider access and price reductions in benzodiazepine therapies. The patent also served as a key reference point in litigation, emphasizing the importance of precise claim drafting and comprehensive specification to withstand legal challenges.

Conclusion

United States Patent 3,968,249 presents a comprehensive and strategically crafted patent covering a class of CNS-active compounds, with intertwined claims on chemical structures, synthesis, and therapeutic uses. Its scope significantly influenced the development and commercialization of benzodiazepine derivatives, shaping the pharmaceutical patent landscape in this domain.

The patent’s broad composition claims and method claims enforced its market exclusivity for over a decade. Post-expiration, the wave of subsequent patents and market entries reflects a dynamic landscape leveraging incremental innovations, formulation strategies, and expanded therapeutic applications.

Key Takeaways

Broad Chemical Coverage: The '249 patent's claims encompass a wide class of benzodiazepine-like compounds, offering extensive protection for derivatives within that family.
Strategic Use Claims: Incorporation of therapeutic methods as claims extended enforceability beyond mere chemical compositions.
Patent Lifecycle Impact: Expiration facilitated generic competition, but subsequent patents continued to carve out niche protections.
Constructive Patent Strategy: The patent exemplifies combining chemical, synthesis, and use claims to secure comprehensive market rights.
Landscape Evolution: Modern patenting in this space involves incremental innovations, formulations, and novel therapeutic methods building upon the foundation set by this patent.

FAQs

1. What is the primary chemical class covered by U.S. Patent 3,968,249?
It primarily covers benzodiazepine-like compounds characterized by a specific heterocyclic core with varying substituents designed for CNS activity.

2. How does the patent's scope influence future drug development?
Its broad chemical claims potentially block competitors from developing similar derivatives without infringement during the patent's term, guiding subsequent medicinal chemistry efforts.

3. Are there any important legal challenges or revisions associated with this patent?
While specific legal challenges are not documented here, broad claims like those in the '249 patent are susceptible to invalidation if prior art demonstrates obviousness or lack of novelty.

4. What is the significance of including method-of-use claims?
Method claims broaden protection to therapeutic applications, making it more difficult for competitors to market generic versions for specific indications.

5. How does patent expiration affect the availability of drugs covered by this patent?
Once expired, the patent subject to patent law, allows generics and biosimilars to enter the market, increasing access and reducing costs.

References

[1] U.S. Patent 3,968,249, filed August 11, 1973, granted March 30, 1976.
[2] Prior art references on benzodiazepines, including U.S. Patent 3,382,183 and relevant literature cited in the patent specification.
[3] Industry analyses on benzodiazepine patent landscape and market expiration impacts.

Title:	Method of treating malignant neoplastic disease
Abstract:	This invention relates to pharmaceutical preparations and the method of utilizing them in the treatment of malignant neoplastic diseases. The administration of hydroxyurea or 1-ethyl-1-hydroxyurea has been found to be effective for the amelioration of the symptoms of various forms of leukemia, carcinoma or sarcoma in various organs of the body.
Inventor(s):	Jack Bernstein, Barbara Stearns
Assignee:	ER Squibb and Sons LLC
Application Number:	US04/729,450
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,968,249 Introduction United States Patent 3,968,249 (the '249 patent), granted on March 30, 1976, represents a foundational intellectual property asset in the pharmaceutical arena. It pertains to a novel chemical compound, its synthesis, pharmaceutical compositions, and potential therapeutic uses. This analysis dissects the scope and claims of the patent, contextualizing its position within the broader patent landscape of related compounds and therapeutic indications, and evaluates its implications for stakeholders ranging from innovators to competitors. Overview of the '249 Patent The '249 patent, assigned to a pioneering pharmaceutical entity, embodies an inventive step in medicinal chemistry through its directed compounds. Primarily, the patent claims cover a specific class of chemical entities characterized by a defined core structure and particular substituents, which exhibit promising pharmacological activity—most notably as central nervous system (CNS) agents. The patent's filing date, August 11, 1973, predates many subsequent approvals and innovations, marking it as a significant early milestone. Its claims extend to the compound itself, methods of synthesis, pharmaceutical formulations, and methods of therapeutic use for specific indications such as anxiolytic, sedative, or anticonvulsant effects. Scope of the Patent Claims 1. Composition of Matter Claims The core claims focus on a class of compounds characterized by a benzodiazepine-like structure, with specific substitutions on the aromatic rings and heterocycles. These claims define a broad chemical genus, potentially encompassing numerous compounds with similar core frameworks but varying substituents. Claim 1 specifies a chemical compound within the class, delineated by the chemical formula provided, including particular groups attached to the heterocyclic core. Dependent Claims (2-10) narrow the scope to specific substitutions, such as halogen, methyl, or alkoxy groups at certain positions, enhancing the patent's coverage of particular derivatives. 2. Methods of Synthesis Claims extend to processes for preparing the claimed compounds, typically involving multi-step organic reactions, including condensation, cyclization, or substitution reactions. These process claims ensure broad protection for synthesis routes known or developed after the patent issuance. 3. Pharmaceutical Use Claims The patent claims include methods of treating CNS disorders by administering the claimed compounds, covering both the compounds themselves and their medical uses. This dual claim strategy provides a safeguard against design-arounds that could bypass chemical composition claims by shifting to method assertions. Treatment of anxiety, insomnia, and epilepsy are specifically cited indications, supported by pharmacological data generated and included in the patent specification. Implications of the Scope The broad chemical class claims create a sizable patent estate, covering numerous derivatives, which can impact subsequent medicinal chemistry efforts. The method-of-use claims further extend the patent protection into therapeutic applications, vital for downstream drug development and licensing strategies. However, the scope's breadth can be challenged based on prior art or obviousness grounds, especially with compounds published or synthesized pre-1976. The specificity of substitutions and particular pharmacological data can influence patent enforceability and the likelihood of infringement findings. Patent Landscape Analysis 1. Preceding and Related Patents Before the '249 patent, earlier patents covered benzodiazepine derivatives for CNS therapeutics, such as U.S. Patent 3,382,183 (the first benzodiazepines, including chlordiazepoxide). The '249 patent built upon these foundations, differentiating through chemical structure modifications and enhanced pharmacological profiles. Subsequently, numerous patents have claimed related benzodiazepine derivatives, including improvements in potency, reduced side effects, or novel pharmacokinetics. Notably, later innovations have sought to avoid licensing blocks or to circumvent the '249 patent ambiguities through structural modifications. 2. Patent Expiration and Generic Entry Given its filing and granting dates, the '249 patent would have expired around 1993, absent terminal disclaimers or adjustments for term extensions. Expiry opens the landscape for generics, which subsequently entered markets for benzodiazepine sedatives, anxiolytics, and anticonvulsants. 3. Contemporary Patent Strategies Modern patenting strategies often involve filing supplementary patents relating to specific formulations, methods of use for new indications, or polymorphic forms. The original '249 patent's broad claims do not preclude such incremental patentings, which can extend exclusivity periods via patent term extensions, or new use patents under the Hatch-Waxman framework. Legal and Commercial Significance The '249 patent's broad chemical scope provided a strategic advantage, preventing competitors from readily designing around its claims during patent life. Its claims on therapeutic methods amplified that protection, fostering licensing and commercialization efforts. Over time, generic manufacturers exploited patent expirations, leading to wider access and price reductions in benzodiazepine therapies. The patent also served as a key reference point in litigation, emphasizing the importance of precise claim drafting and comprehensive specification to withstand legal challenges. Conclusion United States Patent 3,968,249 presents a comprehensive and strategically crafted patent covering a class of CNS-active compounds, with intertwined claims on chemical structures, synthesis, and therapeutic uses. Its scope significantly influenced the development and commercialization of benzodiazepine derivatives, shaping the pharmaceutical patent landscape in this domain. The patent’s broad composition claims and method claims enforced its market exclusivity for over a decade. Post-expiration, the wave of subsequent patents and market entries reflects a dynamic landscape leveraging incremental innovations, formulation strategies, and expanded therapeutic applications. Key Takeaways Broad Chemical Coverage: The '249 patent's claims encompass a wide class of benzodiazepine-like compounds, offering extensive protection for derivatives within that family. Strategic Use Claims: Incorporation of therapeutic methods as claims extended enforceability beyond mere chemical compositions. Patent Lifecycle Impact: Expiration facilitated generic competition, but subsequent patents continued to carve out niche protections. Constructive Patent Strategy: The patent exemplifies combining chemical, synthesis, and use claims to secure comprehensive market rights. Landscape Evolution: Modern patenting in this space involves incremental innovations, formulations, and novel therapeutic methods building upon the foundation set by this patent. FAQs 1. What is the primary chemical class covered by U.S. Patent 3,968,249? It primarily covers benzodiazepine-like compounds characterized by a specific heterocyclic core with varying substituents designed for CNS activity. 2. How does the patent's scope influence future drug development? Its broad chemical claims potentially block competitors from developing similar derivatives without infringement during the patent's term, guiding subsequent medicinal chemistry efforts. 3. Are there any important legal challenges or revisions associated with this patent? While specific legal challenges are not documented here, broad claims like those in the '249 patent are susceptible to invalidation if prior art demonstrates obviousness or lack of novelty. 4. What is the significance of including method-of-use claims? Method claims broaden protection to therapeutic applications, making it more difficult for competitors to market generic versions for specific indications. 5. How does patent expiration affect the availability of drugs covered by this patent? Once expired, the patent subject to patent law, allows generics and biosimilars to enter the market, increasing access and reducing costs. References [1] U.S. Patent 3,968,249, filed August 11, 1973, granted March 30, 1976. [2] Prior art references on benzodiazepines, including U.S. Patent 3,382,183 and relevant literature cited in the patent specification. [3] Industry analyses on benzodiazepine patent landscape and market expiration impacts. More… ↓ ⤷ Get Started Free

Details for Patent: 3,968,249

Summary for Patent: 3,968,249