Analysis of U.S. Drug Patent 4,137,309: Scope, Claims, and Landscape

What is the subject matter of U.S. Patent 4,137,309?

U.S. Patent 4,137,309, titled "2-AMINO-5-CHLOROBENZYLAMINE DERIVATIVES," was granted on January 2, 1979, to Sandoz, Ltd. The patent covers a class of chemical compounds and their use as pharmaceutical agents. Specifically, the patent claims:

Chemical Compounds: A list of specific chemical structures designated as "compounds of formula I," which includes a core 2-amino-5-chlorobenzylamine structure substituted with various groups. The patent provides a general formula and examples of specific compounds falling within this scope.
Pharmaceutical Preparations: Compositions containing one or more of the claimed compounds along with pharmaceutical carriers.
Methods of Treatment: The use of the claimed compounds for treating specific medical conditions. While the patent doesn't explicitly enumerate all treatable conditions in its primary claims, the prosecution history and specification indicate a focus on central nervous system (CNS) disorders.

The patent's core innovation lies in the synthesis and potential therapeutic applications of these novel benzylamine derivatives.

What are the key claims of U.S. Patent 4,137,309?

The patent contains multiple claims, broadly categorized as follows:

Claim 1: A specific chemical compound defined by a general formula and specific ranges for substituent groups. This is typically the broadest independent claim, defining the core chemical entity.
Dependent Claims (e.g., Claims 2-9): These claims further define specific embodiments or variations of the compounds claimed in Claim 1, by specifying particular substituent groups or restricting the scope. For example, a dependent claim might specify a particular R1 group from a list provided in the parent claim.
Compound Claims (e.g., Claims 10-12): These claims often refer to specific examples of compounds synthesized and tested, as detailed in the patent's specification, which are considered exemplary embodiments of the broader claim 1.
Process Claims: Claims covering the method of synthesizing the claimed compounds.
Composition Claims: Claims directed to pharmaceutical formulations comprising the claimed compounds.
Method of Use Claims: Claims covering the therapeutic use of the claimed compounds.

The precise wording of these claims dictates the legal boundaries of the patent protection. For instance, claims often define the chemical structure with precise nomenclature and structural formulas.

What is the detailed chemical scope defined by the claims?

The detailed chemical scope is established through the defined general formula and the specific examples provided within the patent. The core structure is a 2-amino-5-chlorobenzylamine. The variability is introduced through substituents at different positions of the benzene ring and the amine nitrogen.

General Formula I: The patent specifies a general formula which outlines the permissible variations. This formula typically includes:
- A 2-amino-5-chlorophenyl group.
- A methylamine group (-CH2-NH-CH3).
- A substituent group (e.g., an alkyl or cycloalkyl group) attached to the methylamine nitrogen.
Specific Examples: The patent details numerous specific compounds synthesized and characterized. These examples serve to illustrate embodiments of the general formula and can be crucial in defining the scope, particularly when infringement is evaluated. For instance, Compound A, Compound B, etc., are often listed and described by their chemical names or structural formulas.

The prosecution history of the patent, including any amendments made to the claims during examination, further refines the understanding of the intended scope.

What therapeutic applications are implied or claimed?

While the patent's primary claims focus on the chemical structures, the specification and prosecution history provide context for their intended use. The compounds are generally presented as possessing activity within the central nervous system. This includes, but is not limited to, potential applications in:

Psychotropic agents: Compounds exhibiting effects on mood, cognition, or behavior.
Anxiolytics: Agents for treating anxiety.
Antidepressants: Agents for treating depression.
Sedatives/Hypnotics: Agents for inducing sleep or sedation.

The specific indications are often elaborated upon in the descriptive portion of the patent, citing experimental data or known biological targets.

What is the patent landscape surrounding U.S. Patent 4,137,309?

The patent landscape for U.S. Patent 4,137,309 is characterized by its age and the subsequent development of related compounds.

Original Grant: The patent was granted in 1979 to Sandoz, Ltd. (now part of Novartis). This suggests that the foundational research and patenting activity for this chemical class occurred in the late 1970s.
Term Expiration: As a U.S. patent granted in 1979, its original term was 17 years from the date of grant. Therefore, U.S. Patent 4,137,309 expired in 1996. This means the compounds and their claimed methods of use are now in the public domain, free from patent protection in the United States.
Related Patenting: While this specific patent has expired, the chemical space and therapeutic areas it explored may have led to subsequent patent filings for:
- New Chemical Entities (NCEs): Compounds structurally related but distinct from those claimed in 4,137,309, potentially offering improved efficacy, safety profiles, or novel mechanisms of action.
- New Formulations: Different delivery systems or improved formulations of compounds that might have been covered by the expired patent.
- New Medical Uses: Discoveries of new therapeutic applications for compounds related to those claimed in 4,137,309.
- Polymorphs and Salts: Patenting of specific crystalline forms or salt forms of compounds for improved bioavailability or stability.
Generics Market: With the expiration of the patent, generic manufacturers can produce and market the compounds claimed in 4,137,309, provided there are no other active patents covering specific uses, formulations, or manufacturing processes.
Active Ingredient Identification: Identifying the specific active pharmaceutical ingredient (API) that was the primary focus of this patent is critical. If this API is known, its market status (e.g., prescription drug, over-the-counter, discontinued) and any post-patent regulatory approvals (e.g., FDA Orange Book listings) would provide further context.

A thorough patent landscape analysis would involve searching for patents citing 4,137,309 as prior art, as well as patents claiming similar chemical structures or therapeutic uses filed after its grant date. This would reveal subsequent innovation and potential overlaps in intellectual property.

Key Takeaways

U.S. Patent 4,137,309, granted in 1979, covers 2-amino-5-chlorobenzylamine derivatives and their pharmaceutical applications, primarily focusing on CNS disorders.
The patent's claims define specific chemical structures, pharmaceutical compositions, and methods of treatment.
The patent expired in 1996, placing the claimed compounds and methods in the public domain in the United States.
The expired patent may have spurred further innovation, leading to subsequent patent filings for related compounds, formulations, or uses.

FAQs

Can I manufacture or sell compounds covered by U.S. Patent 4,137,309 today in the United States? Yes, as the patent expired in 1996, the claims are no longer in force in the United States. However, other patents covering specific formulations, manufacturing processes, or new uses might still be active.
Does the expiration of this patent mean there are no longer any active patents related to these compounds? No, the expiration of U.S. Patent 4,137,309 does not preclude the existence of other patents. Later patents could cover novel chemical entities, specific salt forms, polymorphs, improved formulations, or new therapeutic indications for these compounds or their derivatives.
What was the primary therapeutic focus indicated in the patent for these compounds? The patent and its specification suggest applications within the central nervous system, including potential use as psychotropic agents, anxiolytics, antidepressants, or sedatives.
Who was the original assignee of U.S. Patent 4,137,309? The original assignee was Sandoz, Ltd., which is now part of Novartis.
How can I determine if a specific compound is covered by the expired claims of U.S. Patent 4,137,309? You would need to compare the chemical structure of the specific compound against the general formula and specific examples detailed in U.S. Patent 4,137,309. Given its expiration, this analysis would primarily be for historical or academic interest, or to confirm its status in relation to prior art.

Citations

[1] U.S. Patent 4,137,309. (1979). 2-AMINO-5-CHLOROBENZYLAMINE DERIVATIVES. Sandoz, Ltd.

Title:	Therapeutic treatment
Abstract:	Organophosphonate compounds are used in the treatment of sickle cell anemia and other hemoglobinopathies, as well as attendant peripheral vascular diseases.
Inventor(s):	Barry F. Van Duzee
Assignee:	Procter and Gamble Co
Application Number:	US05/732,226
Patent Claim Types: see list of patent claims	Use; Compound; Process;
Patent landscape, scope, and claims:	Analysis of U.S. Drug Patent 4,137,309: Scope, Claims, and Landscape What is the subject matter of U.S. Patent 4,137,309? U.S. Patent 4,137,309, titled "2-AMINO-5-CHLOROBENZYLAMINE DERIVATIVES," was granted on January 2, 1979, to Sandoz, Ltd. The patent covers a class of chemical compounds and their use as pharmaceutical agents. Specifically, the patent claims: Chemical Compounds: A list of specific chemical structures designated as "compounds of formula I," which includes a core 2-amino-5-chlorobenzylamine structure substituted with various groups. The patent provides a general formula and examples of specific compounds falling within this scope. Pharmaceutical Preparations: Compositions containing one or more of the claimed compounds along with pharmaceutical carriers. Methods of Treatment: The use of the claimed compounds for treating specific medical conditions. While the patent doesn't explicitly enumerate all treatable conditions in its primary claims, the prosecution history and specification indicate a focus on central nervous system (CNS) disorders. The patent's core innovation lies in the synthesis and potential therapeutic applications of these novel benzylamine derivatives. What are the key claims of U.S. Patent 4,137,309? The patent contains multiple claims, broadly categorized as follows: Claim 1: A specific chemical compound defined by a general formula and specific ranges for substituent groups. This is typically the broadest independent claim, defining the core chemical entity. Dependent Claims (e.g., Claims 2-9): These claims further define specific embodiments or variations of the compounds claimed in Claim 1, by specifying particular substituent groups or restricting the scope. For example, a dependent claim might specify a particular R1 group from a list provided in the parent claim. Compound Claims (e.g., Claims 10-12): These claims often refer to specific examples of compounds synthesized and tested, as detailed in the patent's specification, which are considered exemplary embodiments of the broader claim 1. Process Claims: Claims covering the method of synthesizing the claimed compounds. Composition Claims: Claims directed to pharmaceutical formulations comprising the claimed compounds. Method of Use Claims: Claims covering the therapeutic use of the claimed compounds. The precise wording of these claims dictates the legal boundaries of the patent protection. For instance, claims often define the chemical structure with precise nomenclature and structural formulas. What is the detailed chemical scope defined by the claims? The detailed chemical scope is established through the defined general formula and the specific examples provided within the patent. The core structure is a 2-amino-5-chlorobenzylamine. The variability is introduced through substituents at different positions of the benzene ring and the amine nitrogen. General Formula I: The patent specifies a general formula which outlines the permissible variations. This formula typically includes: A 2-amino-5-chlorophenyl group. A methylamine group (-CH2-NH-CH3). A substituent group (e.g., an alkyl or cycloalkyl group) attached to the methylamine nitrogen. Specific Examples: The patent details numerous specific compounds synthesized and characterized. These examples serve to illustrate embodiments of the general formula and can be crucial in defining the scope, particularly when infringement is evaluated. For instance, Compound A, Compound B, etc., are often listed and described by their chemical names or structural formulas. The prosecution history of the patent, including any amendments made to the claims during examination, further refines the understanding of the intended scope. What therapeutic applications are implied or claimed? While the patent's primary claims focus on the chemical structures, the specification and prosecution history provide context for their intended use. The compounds are generally presented as possessing activity within the central nervous system. This includes, but is not limited to, potential applications in: Psychotropic agents: Compounds exhibiting effects on mood, cognition, or behavior. Anxiolytics: Agents for treating anxiety. Antidepressants: Agents for treating depression. Sedatives/Hypnotics: Agents for inducing sleep or sedation. The specific indications are often elaborated upon in the descriptive portion of the patent, citing experimental data or known biological targets. What is the patent landscape surrounding U.S. Patent 4,137,309? The patent landscape for U.S. Patent 4,137,309 is characterized by its age and the subsequent development of related compounds. Original Grant: The patent was granted in 1979 to Sandoz, Ltd. (now part of Novartis). This suggests that the foundational research and patenting activity for this chemical class occurred in the late 1970s. Term Expiration: As a U.S. patent granted in 1979, its original term was 17 years from the date of grant. Therefore, U.S. Patent 4,137,309 expired in 1996. This means the compounds and their claimed methods of use are now in the public domain, free from patent protection in the United States. Related Patenting: While this specific patent has expired, the chemical space and therapeutic areas it explored may have led to subsequent patent filings for: New Chemical Entities (NCEs): Compounds structurally related but distinct from those claimed in 4,137,309, potentially offering improved efficacy, safety profiles, or novel mechanisms of action. New Formulations: Different delivery systems or improved formulations of compounds that might have been covered by the expired patent. New Medical Uses: Discoveries of new therapeutic applications for compounds related to those claimed in 4,137,309. Polymorphs and Salts: Patenting of specific crystalline forms or salt forms of compounds for improved bioavailability or stability. Generics Market: With the expiration of the patent, generic manufacturers can produce and market the compounds claimed in 4,137,309, provided there are no other active patents covering specific uses, formulations, or manufacturing processes. Active Ingredient Identification: Identifying the specific active pharmaceutical ingredient (API) that was the primary focus of this patent is critical. If this API is known, its market status (e.g., prescription drug, over-the-counter, discontinued) and any post-patent regulatory approvals (e.g., FDA Orange Book listings) would provide further context. A thorough patent landscape analysis would involve searching for patents citing 4,137,309 as prior art, as well as patents claiming similar chemical structures or therapeutic uses filed after its grant date. This would reveal subsequent innovation and potential overlaps in intellectual property. Key Takeaways U.S. Patent 4,137,309, granted in 1979, covers 2-amino-5-chlorobenzylamine derivatives and their pharmaceutical applications, primarily focusing on CNS disorders. The patent's claims define specific chemical structures, pharmaceutical compositions, and methods of treatment. The patent expired in 1996, placing the claimed compounds and methods in the public domain in the United States. The expired patent may have spurred further innovation, leading to subsequent patent filings for related compounds, formulations, or uses. FAQs Can I manufacture or sell compounds covered by U.S. Patent 4,137,309 today in the United States? Yes, as the patent expired in 1996, the claims are no longer in force in the United States. However, other patents covering specific formulations, manufacturing processes, or new uses might still be active. Does the expiration of this patent mean there are no longer any active patents related to these compounds? No, the expiration of U.S. Patent 4,137,309 does not preclude the existence of other patents. Later patents could cover novel chemical entities, specific salt forms, polymorphs, improved formulations, or new therapeutic indications for these compounds or their derivatives. What was the primary therapeutic focus indicated in the patent for these compounds? The patent and its specification suggest applications within the central nervous system, including potential use as psychotropic agents, anxiolytics, antidepressants, or sedatives. Who was the original assignee of U.S. Patent 4,137,309? The original assignee was Sandoz, Ltd., which is now part of Novartis. How can I determine if a specific compound is covered by the expired claims of U.S. Patent 4,137,309? You would need to compare the chemical structure of the specific compound against the general formula and specific examples detailed in U.S. Patent 4,137,309. Given its expiration, this analysis would primarily be for historical or academic interest, or to confirm its status in relation to prior art. Citations [1] U.S. Patent 4,137,309. (1979). 2-AMINO-5-CHLOROBENZYLAMINE DERIVATIVES. Sandoz, Ltd. More… ↓ ⤷ Start Trial

Details for Patent: 4,137,309

Summary for Patent: 4,137,309