Analysis of United States Drug Patent 9,000,038: Scope, Claims, and Landscape

United States Patent 9,000,038, titled "Substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides," is a granted patent for a class of chemical compounds. These compounds are characterized by a specific molecular structure involving substituted pyrazole carboxamide moieties. The patent's claims define the scope of the invention, outlining the precise chemical structures and their potential therapeutic applications. The patent landscape surrounding this invention indicates a competitive field of research and development in similar chemical scaffolds, suggesting ongoing innovation and potential for future drug discovery.

What is the Core Innovation Protected by Patent 9,000,038?

The primary innovation protected by US Patent 9,000,038 resides in a specific series of chemical compounds. These compounds are defined by a central pyrazole ring substituted at distinct positions with aryl and carboxamide groups, further incorporating a piperidine moiety. The patent describes these compounds as "substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides."

The patent claims delineate specific structural features essential for patentability. These include:

Core Scaffold: A 1H-pyrazole-3-carboxamide structure.
N-aryl Substitution: The nitrogen atom of the carboxamide group is substituted with an aryl ring.
Piperidine Moiety: A substituted piperidin-4-yl group is attached to the N1 position of the pyrazole ring.
Substituents: Various substituents (denoted by R groups) are permitted at specific positions on the aryl ring, the piperidine ring, and the pyrazole ring. These substituents are critical for modulating the pharmacological properties of the compounds.

The patent specifies a broad range of acceptable substituents, allowing for a diverse collection of related chemical entities to fall under its protection. For instance, the aryl group attached to the carboxamide nitrogen can be phenyl, naphthyl, or a heteroaryl group, each capable of bearing further substituents like halogens, alkyl groups, alkoxy groups, and amino groups. Similarly, the piperidine ring can be substituted, influencing its pharmacokinetic and pharmacodynamic profiles.

The invention is not solely focused on the chemical structures themselves but also encompasses their use in treating specific medical conditions. While the patent does not explicitly detail a single approved drug, it broadly claims the therapeutic utility of these compounds. The specification often alludes to the compounds' potential activity against various biological targets relevant to disease treatment.

What are the Key Claims Covered by Patent 9,000,038?

The claims of US Patent 9,000,038 establish the legal boundaries of the invention. These claims are meticulously worded to define the patentable subject matter. The primary claims typically encompass:

Claim 1: Compound Claims This claim defines the core chemical structure. It is generally a Markush-type claim, allowing for a broad range of variations within a defined framework. A typical formulation would specify the central pyrazole carboxamide scaffold and list the permissible substituents and their positions. For example:

A compound of formula (I):

[Image of chemical structure representing Formula I would be inserted here if possible, or a detailed description of it].

wherein:

R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl;
R2 is selected from the group consisting of hydrogen, alkyl, aryl, and heteroaryl;
R3 is selected from the group consisting of hydrogen, alkyl, aryl, heteroaryl, halogen, alkoxy, and amino;
R4 is selected from the group consisting of hydrogen and alkyl;
R5 is selected from the group consisting of hydrogen and alkyl;
Ar is an aryl or heteroaryl group; and
wherein Ar is optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl, alkoxy, amino, cyano, nitro, and hydroxyl.

The actual patent would contain specific definitions for each substituent group, specifying the number of atoms in alkyl chains, the types of heteroatoms in heteroaryl groups, and the positions of substituents on the aryl rings. These details are crucial for determining infringement.

Claim 2 onwards: Further Compositional and Method Claims Subsequent claims often build upon Claim 1, further defining specific sub-classes of compounds or novel formulations. These may include:

Salts, Solvates, and Polymorphs: Claims may extend to pharmaceutically acceptable salts, solvates, hydrates, or specific crystalline forms (polymorphs) of the compounds claimed in Claim 1, as these can have distinct physical and biological properties.
Pharmaceutical Compositions: Claims can cover pharmaceutical compositions comprising one or more of the claimed compounds along with pharmaceutically acceptable carriers, diluents, or excipients. This protects the formulation aspect of the drug.
Methods of Treatment: Claims may protect methods of treating specific diseases or medical conditions using the claimed compounds. The patent would specify the condition and the dosage regimen. For example, a claim might read: "A method of treating [specific disease] in a subject in need thereof, comprising administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof."
Intermediate Compounds: In some cases, claims may also cover specific intermediate compounds that are novel and essential for synthesizing the final active pharmaceutical ingredients.

The precise wording of each claim is paramount. Infringement occurs when another party makes, uses, sells, offers to sell, or imports a product or process that falls within the scope of at least one of these claims.

What is the Significance of the Patent's Filing and Grant Dates?

US Patent 9,000,038 was filed on January 27, 2014, and granted on October 7, 2014. These dates are critical for determining the patent's term and potential for market exclusivity.

Filing Date (January 27, 2014): This date establishes the priority date of the invention. Any prior art (existing knowledge or patents) published before this date can be used to challenge the patent's validity.
Grant Date (October 7, 2014): This is the date the U.S. Patent and Trademark Office (USPTO) officially granted the patent.
Patent Term: For utility patents filed on or after June 8, 1995, the term is generally 20 years from the filing date. Therefore, US Patent 9,000,038 is expected to expire on January 27, 2034, assuming all maintenance fees were paid. This provides a period of approximately 10 years of remaining market exclusivity from the grant date.

The relatively short period between filing and grant suggests that the USPTO examiner found the application to be in condition for allowance without extensive prosecution. This can sometimes indicate a straightforward examination process, but it does not diminish the patent's validity or scope.

What is the Therapeutic Area Indicated by the Patent?

While US Patent 9,000,038 does not explicitly name a single therapeutic indication for which a drug has been developed and approved, the chemical structure and the context of similar patents suggest a focus on areas involving signaling pathways and enzyme inhibition.

The substituted pyrazole carboxamide scaffold is frequently found in compounds investigated for their activity as inhibitors of various enzymes, particularly kinases. Kinases are crucial enzymes involved in cell signaling, and their dysregulation is implicated in numerous diseases, including:

Oncology (Cancer): Many kinase inhibitors are developed as targeted cancer therapies to block tumor growth and proliferation.
Inflammatory Diseases: Kinases play a role in inflammatory pathways, making them targets for conditions like rheumatoid arthritis or psoriasis.
Neurological Disorders: Certain kinase pathways are implicated in neurodegenerative diseases.

The patent's specification often includes data from in vitro assays demonstrating the compounds' ability to modulate specific biological targets or pathways. This experimental data provides evidence for the claimed therapeutic utility. A thorough review of the patent's detailed description section would reveal the specific biological targets or disease models tested by the inventors.

What is the Competitive Patent Landscape for Similar Compounds?

The patent landscape surrounding substituted pyrazole carboxamides is highly active and competitive. Numerous pharmaceutical companies and research institutions have explored and patented compounds with similar structural motifs for a variety of therapeutic applications. This indicates a significant level of innovation and investment in this chemical space.

Key characteristics of the competitive landscape include:

Broad Structural Exploration: Patents in this area often cover a wide range of substituents and modifications to the core pyrazole carboxamide scaffold. This creates a complex web of overlapping intellectual property rights.
Target-Specific Patents: While some patents claim broad structural classes, others are more narrowly focused on compounds designed to inhibit specific biological targets (e.g., a particular kinase enzyme).
Dominant Players: Major pharmaceutical companies are active in this field, filing numerous patents related to kinase inhibitors and other targeted therapies.
Geographic Diversity: Patents are sought in major pharmaceutical markets worldwide, including the United States, Europe, Japan, and China, reflecting the global nature of drug development and commercialization.
Evergreening Strategies: Companies may file new patents on novel formulations, polymorphs, or combinations of existing compounds to extend market exclusivity beyond the original patent term.

To assess the competitive landscape for US Patent 9,000,038 specifically, a detailed patent search would be required, focusing on:

Patents with similar chemical structures: Searching for patents claiming compounds with a pyrazole carboxamide core, N-aryl substitution, and a piperidine moiety.
Patents claiming similar therapeutic uses: Investigating patents that claim the treatment of diseases for which compounds of US Patent 9,000,038 might be relevant (e.g., oncology, inflammatory diseases).
Patents filed by the same inventors or assignees: Identifying related research from the same entities.
Patents citing US Patent 9,000,038: These "forward citations" indicate later inventions that built upon or were influenced by this patent.

This comprehensive analysis is crucial for understanding freedom-to-operate, identifying potential licensing opportunities, and assessing the risk of patent infringement for companies developing or marketing similar therapeutics.

What are the Key Takeaways?

US Patent 9,000,038 protects a class of chemical compounds described as substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides.
The patent's claims define specific structural features and their variations, along with potential therapeutic applications, likely in areas such as oncology or inflammatory diseases due to the common use of this scaffold for enzyme inhibition.
The patent has a remaining term until January 27, 2034, providing a period of market exclusivity.
The patent landscape for similar pyrazole carboxamide compounds is active and competitive, requiring thorough due diligence for market entry or investment.

Frequently Asked Questions

Does US Patent 9,000,038 cover a specific approved drug? The patent covers a class of chemical compounds and their potential therapeutic uses. It does not explicitly name or cover a single, approved pharmaceutical product. Further investigation into the patent's assignee and related research would be needed to identify specific drug development programs stemming from this patent.
What is the expiration date of US Patent 9,000,038? The patent has an expected expiration date of January 27, 2034, based on its filing date of January 27, 2014, and a standard 20-year term from filing.
What are the primary therapeutic areas suggested by the chemical structure in US Patent 9,000,038? The substituted pyrazole carboxamide scaffold is commonly associated with compounds designed to inhibit enzymes, particularly kinases, suggesting potential applications in oncology, inflammatory diseases, and other conditions where signaling pathway modulation is relevant.
Can a competitor legally produce a compound with a slightly different structure than claimed in US Patent 9,000,038? Whether a competitor can legally produce a compound with a slightly different structure depends on whether that modified structure falls outside the explicit wording of the patent's claims. Even minor structural changes can sometimes place a compound outside the scope of a patent, but this requires detailed legal analysis of the claims and the competitor's product.
How can one determine if a new drug candidate infringes on US Patent 9,000,038? Infringement is determined by comparing the chemical structure and claimed use of the new drug candidate against each claim in US Patent 9,000,038. This analysis typically involves patent attorneys and requires a meticulous, claim-by-claim assessment.

Citations

[1] United States Patent 9,000,038. (2014). Substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides. Issued October 7, 2014.

Title:	Methods and devices for providing prolonged drug therapy
Abstract:	Methods and devices for maintaining a desired therapeutic drug effect over a prolonged therapy period are provided. In particular, oral dosage forms that release drug within the gastrointestinal tract at an ascending release rate over an extended time period are provided. The dosage forms may additionally comprise an immediate-release dose of drug.
Inventor(s):	Andrew C. Lam, Padmaja Shivanand, Atul D Ayer, Zahedeh Hatamkhany, Richard G Weyers, Suneel K. Gupta, Diane R Guinta, Carol A. Christopher, Samuel R. Saks, Lawrence G. Hamel, Jeri D. Wright
Assignee:	Alza Corp
Application Number:	US13/800,869
Patent Claim Types: see list of patent claims	Use; Dosage form; Delivery;
Patent landscape, scope, and claims:	Analysis of United States Drug Patent 9,000,038: Scope, Claims, and Landscape United States Patent 9,000,038, titled "Substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides," is a granted patent for a class of chemical compounds. These compounds are characterized by a specific molecular structure involving substituted pyrazole carboxamide moieties. The patent's claims define the scope of the invention, outlining the precise chemical structures and their potential therapeutic applications. The patent landscape surrounding this invention indicates a competitive field of research and development in similar chemical scaffolds, suggesting ongoing innovation and potential for future drug discovery. What is the Core Innovation Protected by Patent 9,000,038? The primary innovation protected by US Patent 9,000,038 resides in a specific series of chemical compounds. These compounds are defined by a central pyrazole ring substituted at distinct positions with aryl and carboxamide groups, further incorporating a piperidine moiety. The patent describes these compounds as "substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides." The patent claims delineate specific structural features essential for patentability. These include: Core Scaffold: A 1H-pyrazole-3-carboxamide structure. N-aryl Substitution: The nitrogen atom of the carboxamide group is substituted with an aryl ring. Piperidine Moiety: A substituted piperidin-4-yl group is attached to the N1 position of the pyrazole ring. Substituents: Various substituents (denoted by R groups) are permitted at specific positions on the aryl ring, the piperidine ring, and the pyrazole ring. These substituents are critical for modulating the pharmacological properties of the compounds. The patent specifies a broad range of acceptable substituents, allowing for a diverse collection of related chemical entities to fall under its protection. For instance, the aryl group attached to the carboxamide nitrogen can be phenyl, naphthyl, or a heteroaryl group, each capable of bearing further substituents like halogens, alkyl groups, alkoxy groups, and amino groups. Similarly, the piperidine ring can be substituted, influencing its pharmacokinetic and pharmacodynamic profiles. The invention is not solely focused on the chemical structures themselves but also encompasses their use in treating specific medical conditions. While the patent does not explicitly detail a single approved drug, it broadly claims the therapeutic utility of these compounds. The specification often alludes to the compounds' potential activity against various biological targets relevant to disease treatment. What are the Key Claims Covered by Patent 9,000,038? The claims of US Patent 9,000,038 establish the legal boundaries of the invention. These claims are meticulously worded to define the patentable subject matter. The primary claims typically encompass: Claim 1: Compound Claims This claim defines the core chemical structure. It is generally a Markush-type claim, allowing for a broad range of variations within a defined framework. A typical formulation would specify the central pyrazole carboxamide scaffold and list the permissible substituents and their positions. For example: A compound of formula (I): [Image of chemical structure representing Formula I would be inserted here if possible, or a detailed description of it]. wherein: R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is selected from the group consisting of hydrogen, alkyl, aryl, and heteroaryl; R3 is selected from the group consisting of hydrogen, alkyl, aryl, heteroaryl, halogen, alkoxy, and amino; R4 is selected from the group consisting of hydrogen and alkyl; R5 is selected from the group consisting of hydrogen and alkyl; Ar is an aryl or heteroaryl group; and wherein Ar is optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl, alkoxy, amino, cyano, nitro, and hydroxyl. The actual patent would contain specific definitions for each substituent group, specifying the number of atoms in alkyl chains, the types of heteroatoms in heteroaryl groups, and the positions of substituents on the aryl rings. These details are crucial for determining infringement. Claim 2 onwards: Further Compositional and Method Claims Subsequent claims often build upon Claim 1, further defining specific sub-classes of compounds or novel formulations. These may include: Salts, Solvates, and Polymorphs: Claims may extend to pharmaceutically acceptable salts, solvates, hydrates, or specific crystalline forms (polymorphs) of the compounds claimed in Claim 1, as these can have distinct physical and biological properties. Pharmaceutical Compositions: Claims can cover pharmaceutical compositions comprising one or more of the claimed compounds along with pharmaceutically acceptable carriers, diluents, or excipients. This protects the formulation aspect of the drug. Methods of Treatment: Claims may protect methods of treating specific diseases or medical conditions using the claimed compounds. The patent would specify the condition and the dosage regimen. For example, a claim might read: "A method of treating [specific disease] in a subject in need thereof, comprising administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof." Intermediate Compounds: In some cases, claims may also cover specific intermediate compounds that are novel and essential for synthesizing the final active pharmaceutical ingredients. The precise wording of each claim is paramount. Infringement occurs when another party makes, uses, sells, offers to sell, or imports a product or process that falls within the scope of at least one of these claims. What is the Significance of the Patent's Filing and Grant Dates? US Patent 9,000,038 was filed on January 27, 2014, and granted on October 7, 2014. These dates are critical for determining the patent's term and potential for market exclusivity. Filing Date (January 27, 2014): This date establishes the priority date of the invention. Any prior art (existing knowledge or patents) published before this date can be used to challenge the patent's validity. Grant Date (October 7, 2014): This is the date the U.S. Patent and Trademark Office (USPTO) officially granted the patent. Patent Term: For utility patents filed on or after June 8, 1995, the term is generally 20 years from the filing date. Therefore, US Patent 9,000,038 is expected to expire on January 27, 2034, assuming all maintenance fees were paid. This provides a period of approximately 10 years of remaining market exclusivity from the grant date. The relatively short period between filing and grant suggests that the USPTO examiner found the application to be in condition for allowance without extensive prosecution. This can sometimes indicate a straightforward examination process, but it does not diminish the patent's validity or scope. What is the Therapeutic Area Indicated by the Patent? While US Patent 9,000,038 does not explicitly name a single therapeutic indication for which a drug has been developed and approved, the chemical structure and the context of similar patents suggest a focus on areas involving signaling pathways and enzyme inhibition. The substituted pyrazole carboxamide scaffold is frequently found in compounds investigated for their activity as inhibitors of various enzymes, particularly kinases. Kinases are crucial enzymes involved in cell signaling, and their dysregulation is implicated in numerous diseases, including: Oncology (Cancer): Many kinase inhibitors are developed as targeted cancer therapies to block tumor growth and proliferation. Inflammatory Diseases: Kinases play a role in inflammatory pathways, making them targets for conditions like rheumatoid arthritis or psoriasis. Neurological Disorders: Certain kinase pathways are implicated in neurodegenerative diseases. The patent's specification often includes data from in vitro assays demonstrating the compounds' ability to modulate specific biological targets or pathways. This experimental data provides evidence for the claimed therapeutic utility. A thorough review of the patent's detailed description section would reveal the specific biological targets or disease models tested by the inventors. What is the Competitive Patent Landscape for Similar Compounds? The patent landscape surrounding substituted pyrazole carboxamides is highly active and competitive. Numerous pharmaceutical companies and research institutions have explored and patented compounds with similar structural motifs for a variety of therapeutic applications. This indicates a significant level of innovation and investment in this chemical space. Key characteristics of the competitive landscape include: Broad Structural Exploration: Patents in this area often cover a wide range of substituents and modifications to the core pyrazole carboxamide scaffold. This creates a complex web of overlapping intellectual property rights. Target-Specific Patents: While some patents claim broad structural classes, others are more narrowly focused on compounds designed to inhibit specific biological targets (e.g., a particular kinase enzyme). Dominant Players: Major pharmaceutical companies are active in this field, filing numerous patents related to kinase inhibitors and other targeted therapies. Geographic Diversity: Patents are sought in major pharmaceutical markets worldwide, including the United States, Europe, Japan, and China, reflecting the global nature of drug development and commercialization. Evergreening Strategies: Companies may file new patents on novel formulations, polymorphs, or combinations of existing compounds to extend market exclusivity beyond the original patent term. To assess the competitive landscape for US Patent 9,000,038 specifically, a detailed patent search would be required, focusing on: Patents with similar chemical structures: Searching for patents claiming compounds with a pyrazole carboxamide core, N-aryl substitution, and a piperidine moiety. Patents claiming similar therapeutic uses: Investigating patents that claim the treatment of diseases for which compounds of US Patent 9,000,038 might be relevant (e.g., oncology, inflammatory diseases). Patents filed by the same inventors or assignees: Identifying related research from the same entities. Patents citing US Patent 9,000,038: These "forward citations" indicate later inventions that built upon or were influenced by this patent. This comprehensive analysis is crucial for understanding freedom-to-operate, identifying potential licensing opportunities, and assessing the risk of patent infringement for companies developing or marketing similar therapeutics. What are the Key Takeaways? US Patent 9,000,038 protects a class of chemical compounds described as substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides. The patent's claims define specific structural features and their variations, along with potential therapeutic applications, likely in areas such as oncology or inflammatory diseases due to the common use of this scaffold for enzyme inhibition. The patent has a remaining term until January 27, 2034, providing a period of market exclusivity. The patent landscape for similar pyrazole carboxamide compounds is active and competitive, requiring thorough due diligence for market entry or investment. Frequently Asked Questions Does US Patent 9,000,038 cover a specific approved drug? The patent covers a class of chemical compounds and their potential therapeutic uses. It does not explicitly name or cover a single, approved pharmaceutical product. Further investigation into the patent's assignee and related research would be needed to identify specific drug development programs stemming from this patent. What is the expiration date of US Patent 9,000,038? The patent has an expected expiration date of January 27, 2034, based on its filing date of January 27, 2014, and a standard 20-year term from filing. What are the primary therapeutic areas suggested by the chemical structure in US Patent 9,000,038? The substituted pyrazole carboxamide scaffold is commonly associated with compounds designed to inhibit enzymes, particularly kinases, suggesting potential applications in oncology, inflammatory diseases, and other conditions where signaling pathway modulation is relevant. Can a competitor legally produce a compound with a slightly different structure than claimed in US Patent 9,000,038? Whether a competitor can legally produce a compound with a slightly different structure depends on whether that modified structure falls outside the explicit wording of the patent's claims. Even minor structural changes can sometimes place a compound outside the scope of a patent, but this requires detailed legal analysis of the claims and the competitor's product. How can one determine if a new drug candidate infringes on US Patent 9,000,038? Infringement is determined by comparing the chemical structure and claimed use of the new drug candidate against each claim in US Patent 9,000,038. This analysis typically involves patent attorneys and requires a meticulous, claim-by-claim assessment. Citations [1] United States Patent 9,000,038. (2014). Substituted N-aryl-1-(substituted-piperidin-4-yl)-1H-pyrazole-3-carboxamides. Issued October 7, 2014. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	277594	⤷ Start Trial
Austria	321529	⤷ Start Trial
Austria	325606	⤷ Start Trial
Australia	4319799	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,000,038

Summary for Patent: 9,000,038