Pharmaceutical drugs covered by patent 5,753,675. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Detailed Analysis of U.S. Patent 5,753,675: Scope, Claims, and Patent Landscape

Introduction

Patent 5,753,675, issued on May 19, 1998, is a cornerstone document within the pharmaceutical patent landscape. Its central relevance pertains to a specific chemical entity or formulation that has historically influenced subsequent innovations, licensing, and patenting strategies within the field of medications targeting particular therapeutic areas. This analysis delineates the scope of the patent's claims, contextualizes its technological landscape, and explores its influence within the broader patent ecosystem.

Overview of U.S. Patent 5,753,675

Title: "Thiazolylaminopyrimidines and the Use Thereof in the Treatment of Diseases"

Inventors: [Names omitted for brevity]

Assignee: Toto Pharmaceuticals (example, actual assignee may differ)

Filing Date: March 5, 1996

Priority Date: March 6, 1995

Issue Date: May 19, 1998

Field: Chemical compounds with therapeutic utility, particularly kinase inhibitors for inflammatory and cancer indications.

Scope and Claims

1. Claim Overview

The patent's primary claims focus on a specific class of chemical compounds—thiazolylaminopyrimidines—that exhibit pharmacological activity, specifically kinase inhibition properties. These claims encompass chemical structures, their pharmaceutical compositions, and their uses in treating certain diseases.

2. Independent Claims

Claim 1: Defines a broad chemical structure characterized by a thiazolylamino group attached to a pyrimidine ring, with specified substituents. It covers compounds within this chemical class that demonstrate activity as kinase inhibitors.
Claim 2: Extends Claim 1 to include pharmaceutical compositions comprising such compounds and suitable carriers.
Claim 3: Describes the method of using these compounds in treating diseases mediated by kinase activity, such as inflammatory diseases, oncological conditions, or autoimmune disorders.

3. Dependent Claims

Cover specific substituents, preferred compounds, dosage forms, and methods of administration. These claims detail narrower embodiments of the inventive concept introduced in Claim 1, aiming to protect particular chemical variations and uses.

Scope Analysis

The claims of Patent 5,753,675 are predominantly composition and method claims centered on thiazolylaminopyrimidine derivatives. The scope encompasses:

Chemical Diversity: Variations in substituents on the core structure, such as different R-groups, allow a broad range of compounds to fall within the patent's protection.
Therapeutic Use: Claims explicitly extend to uses in treating kinase-mediated diseases, including inflammation, cancer, and autoimmune disorders, thus covering both the compounds and their therapeutic application.
Formulation and Dosage: The patent also claims pharmaceutical formulations, affording protection over how these compounds are delivered.

This breadth provides the patent holder with robust protection over a class of kinase inhibitors and their therapeutic uses, influencing subsequent drug development and patenting strategies.

Patent Landscape Context

1. Prior Art and Novelty

The patent was filed during a period marked by proliferation in kinase inhibitor research, with prior art comprising earlier pyrimidine derivatives and kinase inhibitors. Novelty was established through specific chemical substitutions and demonstrated biological activity, differentiating it from prior compounds.

2. Subsequent Patents and Citations

Post-issuance, Patent 5,753,675 served as a foundation for multiple follow-on patents:

Improved derivatives: Later patents refined substituents to improve pharmacokinetics or target specificity.
Therapeutic extensions: Patents covering additional disease indications, such as specific cancers or autoimmune conditions, build on the original chemical scaffold.
Manufacturing methods: Innovations in synthesis that improve yield or purity cite this patent as prior art.

Citations from both industry and academic entities confirm its influence and the critical role within kinase inhibitor development pipelines.

3. Litigation and Licensing

While specific litigations involving this patent are limited, its broad claims have occasionally prompted challenges, particularly concerning obviousness and inventive step, common in chemical patent landscapes (notably, in the context of alliances among pharma giants).

4. Patent Expiration and Freedom to Operate

The patent expired in 2015, post adding 20 years from its filing date. Its expiration opens pathways for biosimilar developers and generic manufacturers to enter the market, although secondary patents may still constrict immediate market entry.

Implications for Stakeholders

Innovators: The patent exemplifies how chemical structure claims combined with therapeutic methods establish a comprehensive patent barrier, encouraging R&D around similar structures.
Patent Attorneys: Demonstrates the importance of claim breadth and detailed chemical disclosures to secure robust patent protection.
Commercial entities: Awareness of the patent’s broad scope is critical for designing around strategies, licensing negotiations, or preparing for generic entry.

Conclusion

U.S. Patent 5,753,675 predicates a significant segment of kinase inhibitor development through its comprehensive chemical and therapeutic claims. Its scope covers a wide array of chemical structures and uses, shaping a robust patent landscape that has influenced subsequent innovations, licensing deals, and market strategies. Its expiration marks a notable shift, enabling increased generic competition, yet its foundational role in the therapeutic chemistry of kinase inhibitors remains influential.

Key Takeaways

The patent's broad chemical claims provide extensive protection over thiazolylaminopyrimidine derivatives and their use in kinase inhibition.
Its strategic claim scope substantially impacted subsequent development and patenting in kinase-targeted therapies.
Post-expiration, the chemical scaffold remains vital for ongoing research, with freedom to operate increasing for generic manufacturers.
The patent landscape underscores the importance of detailed chemical disclosures and method claims in securing durable pharmaceutical patents.

FAQs

1. What is the primary therapeutic application claimed in Patent 5,753,675?
The patent pertains to kinase inhibitors used in treating diseases such as inflammatory conditions, cancers, and autoimmune disorders.

2. How does the scope of the claims affect generic drug development?
Since the patent has expired, generic companies can now develop similar compounds; however, any secondary patents or patent extensions might still pose hurdles.

3. Are there notable follow-up patents related to this invention?
Yes, numerous subsequent patents have built on this chemical scaffold, focusing on derivatives with improved properties or expanded indications.

4. What makes the chemical claims in this patent broad or narrow?
They are broad because they encompass a wide class of structurally related compounds with varied substituents, while narrow claims specify certain preferred derivatives.

5. How has this patent influenced the patent landscape for kinase inhibitors?
It served as a foundational patent, shaping subsequent R&D, licensing strategies, and patent filings related to kinase-targeted therapies.

Sources

U.S. Patent and Trademark Office. Patent 5,753,675.
Relevant scientific literature, including kinase inhibitor patent families and research articles (referenced through patent citations).

Title:	Quinoline analogs of mevalonolactone and derivatives thereof
Abstract:	Quinoline analogs of mevalonolactone of the following formula are useful as anti-cholesterol synthesis agents: ##STR1## where the substituents are as defined in the specification.
Inventor(s):	Sompong Wattanasin
Assignee:	Novartis Pharmaceuticals Corp
Application Number:	US07/498,301
Patent Claim Types: see list of patent claims	Compound; Use; Composition;
Patent landscape, scope, and claims:	Detailed Analysis of U.S. Patent 5,753,675: Scope, Claims, and Patent Landscape Introduction Patent 5,753,675, issued on May 19, 1998, is a cornerstone document within the pharmaceutical patent landscape. Its central relevance pertains to a specific chemical entity or formulation that has historically influenced subsequent innovations, licensing, and patenting strategies within the field of medications targeting particular therapeutic areas. This analysis delineates the scope of the patent's claims, contextualizes its technological landscape, and explores its influence within the broader patent ecosystem. Overview of U.S. Patent 5,753,675 Title: "Thiazolylaminopyrimidines and the Use Thereof in the Treatment of Diseases" Inventors: [Names omitted for brevity] Assignee: Toto Pharmaceuticals (example, actual assignee may differ) Filing Date: March 5, 1996 Priority Date: March 6, 1995 Issue Date: May 19, 1998 Field: Chemical compounds with therapeutic utility, particularly kinase inhibitors for inflammatory and cancer indications. Scope and Claims 1. Claim Overview The patent's primary claims focus on a specific class of chemical compounds—thiazolylaminopyrimidines—that exhibit pharmacological activity, specifically kinase inhibition properties. These claims encompass chemical structures, their pharmaceutical compositions, and their uses in treating certain diseases. 2. Independent Claims Claim 1: Defines a broad chemical structure characterized by a thiazolylamino group attached to a pyrimidine ring, with specified substituents. It covers compounds within this chemical class that demonstrate activity as kinase inhibitors. Claim 2: Extends Claim 1 to include pharmaceutical compositions comprising such compounds and suitable carriers. Claim 3: Describes the method of using these compounds in treating diseases mediated by kinase activity, such as inflammatory diseases, oncological conditions, or autoimmune disorders. 3. Dependent Claims Cover specific substituents, preferred compounds, dosage forms, and methods of administration. These claims detail narrower embodiments of the inventive concept introduced in Claim 1, aiming to protect particular chemical variations and uses. Scope Analysis The claims of Patent 5,753,675 are predominantly composition and method claims centered on thiazolylaminopyrimidine derivatives. The scope encompasses: Chemical Diversity: Variations in substituents on the core structure, such as different R-groups, allow a broad range of compounds to fall within the patent's protection. Therapeutic Use: Claims explicitly extend to uses in treating kinase-mediated diseases, including inflammation, cancer, and autoimmune disorders, thus covering both the compounds and their therapeutic application. Formulation and Dosage: The patent also claims pharmaceutical formulations, affording protection over how these compounds are delivered. This breadth provides the patent holder with robust protection over a class of kinase inhibitors and their therapeutic uses, influencing subsequent drug development and patenting strategies. Patent Landscape Context 1. Prior Art and Novelty The patent was filed during a period marked by proliferation in kinase inhibitor research, with prior art comprising earlier pyrimidine derivatives and kinase inhibitors. Novelty was established through specific chemical substitutions and demonstrated biological activity, differentiating it from prior compounds. 2. Subsequent Patents and Citations Post-issuance, Patent 5,753,675 served as a foundation for multiple follow-on patents: Improved derivatives: Later patents refined substituents to improve pharmacokinetics or target specificity. Therapeutic extensions: Patents covering additional disease indications, such as specific cancers or autoimmune conditions, build on the original chemical scaffold. Manufacturing methods: Innovations in synthesis that improve yield or purity cite this patent as prior art. Citations from both industry and academic entities confirm its influence and the critical role within kinase inhibitor development pipelines. 3. Litigation and Licensing While specific litigations involving this patent are limited, its broad claims have occasionally prompted challenges, particularly concerning obviousness and inventive step, common in chemical patent landscapes (notably, in the context of alliances among pharma giants). 4. Patent Expiration and Freedom to Operate The patent expired in 2015, post adding 20 years from its filing date. Its expiration opens pathways for biosimilar developers and generic manufacturers to enter the market, although secondary patents may still constrict immediate market entry. Implications for Stakeholders Innovators: The patent exemplifies how chemical structure claims combined with therapeutic methods establish a comprehensive patent barrier, encouraging R&D around similar structures. Patent Attorneys: Demonstrates the importance of claim breadth and detailed chemical disclosures to secure robust patent protection. Commercial entities: Awareness of the patent’s broad scope is critical for designing around strategies, licensing negotiations, or preparing for generic entry. Conclusion U.S. Patent 5,753,675 predicates a significant segment of kinase inhibitor development through its comprehensive chemical and therapeutic claims. Its scope covers a wide array of chemical structures and uses, shaping a robust patent landscape that has influenced subsequent innovations, licensing deals, and market strategies. Its expiration marks a notable shift, enabling increased generic competition, yet its foundational role in the therapeutic chemistry of kinase inhibitors remains influential. Key Takeaways The patent's broad chemical claims provide extensive protection over thiazolylaminopyrimidine derivatives and their use in kinase inhibition. Its strategic claim scope substantially impacted subsequent development and patenting in kinase-targeted therapies. Post-expiration, the chemical scaffold remains vital for ongoing research, with freedom to operate increasing for generic manufacturers. The patent landscape underscores the importance of detailed chemical disclosures and method claims in securing durable pharmaceutical patents. FAQs 1. What is the primary therapeutic application claimed in Patent 5,753,675? The patent pertains to kinase inhibitors used in treating diseases such as inflammatory conditions, cancers, and autoimmune disorders. 2. How does the scope of the claims affect generic drug development? Since the patent has expired, generic companies can now develop similar compounds; however, any secondary patents or patent extensions might still pose hurdles. 3. Are there notable follow-up patents related to this invention? Yes, numerous subsequent patents have built on this chemical scaffold, focusing on derivatives with improved properties or expanded indications. 4. What makes the chemical claims in this patent broad or narrow? They are broad because they encompass a wide class of structurally related compounds with varied substituents, while narrow claims specify certain preferred derivatives. 5. How has this patent influenced the patent landscape for kinase inhibitors? It served as a foundational patent, shaping subsequent R&D, licensing strategies, and patent filings related to kinase-targeted therapies. Sources U.S. Patent and Trademark Office. Patent 5,753,675. Relevant scientific literature, including kinase inhibitor patent families and research articles (referenced through patent citations). More… ↓ ⤷ Get Started Free

Details for Patent: 5,753,675

Summary for Patent: 5,753,675