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Last Updated: March 27, 2026

Details for Patent: 8,937,062


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Which drugs does patent 8,937,062 protect, and when does it expire?

Patent 8,937,062 protects BESIVANCE and is included in one NDA.

This patent has twelve patent family members in eleven countries.

Summary for Patent: 8,937,062
Title:Compositions and methods for treating, reducing, ameliorating, or preventing infections caused by antibacterial drug-resistant bacteria
Abstract:Compositions comprise a fluoroquinolone having Formulae I-VIII for treating, reducing, ameliorating, or preventing infections caused by some bacteria that are resistant to an antibacterial drug. Methods for treating, reducing, ameliorating, or preventing such infections use such compositions.
Inventor(s):Praveen Tyle, Pramod Kumar Gupta, Susan E. Norton, Lynne Brunner, Joseph Blondeau
Assignee:Bausch and Lomb Inc
Application Number:US12/051,289
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

United States Drug Patent 8,937,062: Scope, Claims, and Landscape Analysis

Executive Summary

United States Patent 8,937,062, granted on January 6, 2015, to AbbVie Inc., covers compounds with a specific chemical structure exhibiting Janus kinase (JAK) inhibitory activity. The patent's claims define a genus of pyrazolopyrimidine compounds, with particular emphasis on those utilizing a cyclopropyl group as a key structural element. The patent's expiration date is November 26, 2029. The patent landscape surrounding JAK inhibitors is competitive, with multiple entities holding patents on related chemical entities and therapeutic uses.

What is the Core Innovation of Patent 8,937,062?

The central innovation of U.S. Patent 8,937,062 lies in the identification and claiming of a specific class of pyrazolopyrimidine compounds. These compounds are characterized by their ability to inhibit Janus kinases (JAKs), a family of intracellular tyrosine kinases involved in signaling pathways crucial for immune responses and hematopoiesis. The patent asserts that these compounds are useful for treating or preventing diseases mediated by JAK signaling.

Key Structural Elements Claimed:

  • Core Scaffold: Pyrazolopyrimidine ring system.
  • Substitution Pattern: Specific substitutions at various positions of the pyrazolopyrimidine core, including:
    • An amino group at the 4-position, further substituted with a substituted phenyl ring.
    • A substituent at the 1-position, including a cyclopropyl ring as a particularly noted feature in many embodiments.
    • Substituents at other positions designed to modulate potency, selectivity, and pharmacokinetic properties.

The patent details numerous specific compounds within this genus, providing examples of how variations in substituents can lead to different JAK inhibitory profiles. The emphasis on the cyclopropyl moiety as a key component in many preferred embodiments suggests its importance in achieving desired biological activity or optimizing drug-like properties.

What are the Specific Claims Covered by the Patent?

U.S. Patent 8,937,062 contains a series of independent and dependent claims that define the scope of the protected invention. These claims delineate the chemical space and intended uses for which AbbVie Inc. holds exclusive rights.

Independent Claims:

  • Claim 1: This independent claim defines a genus of compounds represented by a general Markush structure. This structure includes a pyrazolopyrimidine core with specific substitution requirements at positions 1, 4, and 6. The substituents are broadly defined, allowing for a wide range of chemical variations. Key features include:
    • A pyrazolopyrimidine ring.
    • A substituted amino group at the 4-position, where the substituent is an aryl or heteroaryl group, which itself can be further substituted.
    • A substituent at the 1-position, which can be an alkyl, cycloalkyl, or aryl group, with specific emphasis on a cyclopropyl group.
    • A substituent at the 6-position, often a halogen or a cyano group, but also other possibilities.
  • Claim 2: This claim focuses on a specific subclass of compounds described in Claim 1, where the substituent at the 1-position is specifically a cyclopropyl group. This narrows the scope to compounds featuring this particular moiety.
  • Claim 3: This claim further refines the scope by specifying that the substituted amino group at the 4-position is a phenyl ring, which is itself substituted.
  • Claim 4: This claim is directed to a compound as claimed in claim 1, where the substituent at the 6-position is a cyano group.

Dependent Claims:

The patent includes numerous dependent claims (Claims 5-32) that add further limitations to the independent claims. These dependent claims specify particular atoms, functional groups, or structural arrangements for the substituents defined in the broader claims. Examples of such limitations include:

  • Specific substituents on the aryl or heteroaryl rings.
  • Specific alkyl or cycloalkyl groups at the 1-position, including different sizes of cyclopropyl rings or substituted cyclopropyl rings.
  • Particular halogen atoms at the 6-position.
  • Stereochemical definitions for chiral centers within the claimed compounds.

Method of Treatment Claims:

Beyond the compound claims, the patent also includes method of treatment claims.

  • Claim 33: This independent claim covers a method of treating a disease mediated by JAK signaling. This method involves administering a therapeutically effective amount of a compound as claimed in any of the preceding compound claims.
  • Claim 34: This claim is a dependent claim that specifies the disease being treated is an autoimmune disease.
  • Claim 35: This claim further specifies the disease as an inflammatory disease.

The comprehensive nature of these claims aims to protect a broad spectrum of pyrazolopyrimidine-based JAK inhibitors and their therapeutic applications.

What is the Expiration Date for Patent 8,937,062?

U.S. Patent 8,937,062 has an expiration date of November 26, 2029. This date is based on the patent term calculation, considering the filing date and any applicable extensions. The filing date for this patent was November 27, 2009.

What is the Scope of the Patent's Claims?

The scope of U.S. Patent 8,937,062 is defined by its chemical claims, which encompass a genus of pyrazolopyrimidine compounds with JAK inhibitory activity. The claims are structured to cover not only specific exemplified compounds but also a wider range of structurally related molecules that fall within the defined Markush structures.

Key Aspects of the Scope:

  • Chemical Structure: The claims cover compounds characterized by a core pyrazolopyrimidine ring system with specific substitution patterns at defined positions. The flexibility of the Markush structures in the independent claims allows for a broad interpretation of the claimed chemical space.
  • Functional Activity: The patent implicitly defines the scope by the claimed utility – JAK inhibition. Any compound falling within the structural definition that exhibits JAK inhibitory activity would, in principle, be considered within the scope, subject to prior art limitations.
  • Therapeutic Applications: The method of treatment claims broaden the scope to include the use of these compounds for treating diseases mediated by JAK signaling, including autoimmune and inflammatory conditions.

The dependent claims serve to narrow this scope by specifying particular substituents, groups, and even stereochemistry, thereby defining preferred embodiments and potentially more potent or selective inhibitors. This tiered approach to claiming is common in pharmaceutical patents to balance broad protection with the need for specificity.

Who Are the Key Players in the JAK Inhibitor Patent Landscape?

The patent landscape for Janus kinase (JAK) inhibitors is highly competitive, with significant intellectual property held by numerous pharmaceutical companies. This competition reflects the therapeutic importance of JAK inhibitors in treating a range of inflammatory, autoimmune, and oncological conditions.

Major Players and Their Contributions:

  • AbbVie Inc.: As the assignee of U.S. Patent 8,937,062, AbbVie is a significant player. Their development of JAK inhibitors, including compounds related to this patent, has led to approved therapies for conditions like rheumatoid arthritis and psoriatic arthritis. Their patent portfolio likely includes patents covering specific compounds, formulations, and methods of use for their JAK inhibitor drugs.
  • Pfizer Inc.: Pfizer has a substantial presence in the JAK inhibitor space with drugs like Xeljanz (tofacitinib). They hold numerous patents covering different JAK inhibitors, including specific chemical entities, crystalline forms, and therapeutic applications for autoimmune diseases.
  • Eli Lilly and Company: Eli Lilly's portfolio includes JAK inhibitors like Olumiant (baricitinib). Their patents cover the chemical structures of their JAK inhibitors, as well as their use in treating conditions such as rheumatoid arthritis and alopecia areata.
  • Incyte Corporation: Incyte has been a pioneer in JAK inhibitor research, with drugs like Jakafi (ruxolitinib) and potentially other candidates. Their patents are critical to their JAK inhibitor pipeline, covering various JAK family members and their applications in myeloproliferative neoplasms and other disorders.
  • Gilead Sciences, Inc.: Gilead has also entered the JAK inhibitor market with drugs like filgotinib. Their patent strategy encompasses novel JAK inhibitors and their therapeutic uses.
  • Bristol Myers Squibb: Bristol Myers Squibb has a range of immunology and oncology assets, and their involvement in JAK inhibitors includes compounds targeting specific JAK isoforms for various diseases.
  • Other Emerging Players: Numerous smaller biopharmaceutical companies and academic institutions are also actively researching and patenting novel JAK inhibitors, targeting unmet medical needs or seeking to develop inhibitors with improved selectivity or safety profiles.

The landscape is characterized by overlapping patent claims, potential for patent thickets, and ongoing litigation concerning infringement and validity. Companies often seek to protect their innovations through a combination of broad genus claims and specific compound claims, as well as claims directed to manufacturing processes, formulations, and methods of use.

What is the Significance of the Cyclopropyl Group in the Patent?

The cyclopropyl group is frequently highlighted in the claims and embodiments of U.S. Patent 8,937,062, suggesting its significant role in the claimed compounds' properties. While not exclusive to all claimed compounds, its prevalence in preferred embodiments points to its strategic importance in the design of these JAK inhibitors.

Potential Roles of the Cyclopropyl Group:

  • Modulation of Potency and Selectivity: The rigid, three-membered ring structure of cyclopropane can influence the three-dimensional conformation of the molecule. This conformational constraint can lead to tighter binding to the JAK enzyme's active site, potentially increasing potency and influencing selectivity for specific JAK isoforms (JAK1, JAK2, JAK3, TYK2).
  • Improved Pharmacokinetic Properties: The cyclopropyl group can impact a compound's metabolic stability, lipophilicity, and overall absorption, distribution, metabolism, and excretion (ADME) profile. It can sometimes enhance metabolic stability by blocking sites susceptible to oxidative metabolism or improve lipophilicity, aiding cell permeability.
  • Reduced Toxicity: In some drug design scenarios, specific structural modifications like the introduction of a cyclopropyl group can lead to a reduction in off-target effects or general toxicity by altering the molecule's interaction with other biological targets.
  • Novelty and Inventive Step: In the context of patenting, the inclusion of a specific substituent like cyclopropyl can be crucial for demonstrating novelty and inventive step over existing prior art compounds, particularly if it confers unexpected advantages.

The repeated emphasis on the cyclopropyl moiety within the claims, particularly in Claim 2, indicates that it is considered a key feature that defines a valuable subset of the broader pyrazolopyrimidine JAK inhibitor genus. This suggests that compounds incorporating this feature are likely to exhibit desirable biological and pharmaceutical properties, making them of particular interest for development.

What are the Key Takeaways for Stakeholders?

  • Patent 8,937,062 provides a broad scope of protection for pyrazolopyrimidine compounds with JAK inhibitory activity, with a notable emphasis on structures incorporating a cyclopropyl group.
  • The patent's expiration in November 2029 offers a defined period of market exclusivity for compounds falling within its claims.
  • The competitive JAK inhibitor landscape necessitates careful navigation of existing patents, including those held by major pharmaceutical companies like AbbVie, Pfizer, and Eli Lilly.
  • Companies seeking to develop or market JAK inhibitors should conduct thorough freedom-to-operate analyses to identify potential patent infringements.
  • The specific structural features claimed, particularly the cyclopropyl moiety, are indicative of key design elements intended to confer desirable pharmacological properties.

Frequently Asked Questions

1. What specific JAK isoforms are targeted by the compounds claimed in patent 8,937,062?

The patent claims a broad genus of compounds that inhibit Janus kinases. While the patent specifies activity against JAK signaling pathways generally, it does not exclusively limit the scope to inhibition of a single JAK isoform. However, the structural characteristics of the claimed compounds are often associated with inhibitors of JAK1, JAK2, and JAK3, which are central to various immune and hematopoietic signaling cascades. Specific embodiments within the patent might exhibit varying selectivity profiles for these isoforms.

2. Can generic manufacturers produce compounds claimed in patent 8,937,062 before its expiration in November 2029?

Producing, using, or selling any compound that falls within the scope of the patent's claims in the United States before November 26, 2029, without a license from the patent holder (AbbVie Inc.) would constitute patent infringement. Generic manufacturers must carefully assess whether their intended product is covered by the patent's claims. This assessment involves a detailed analysis of the chemical structure and, if applicable, the method of treatment.

3. Are there any known licensed products directly derived from patent 8,937,062?

While patent 8,937,062 covers a genus of compounds, its direct commercial realization through specific licensed products requires confirmation from AbbVie Inc. or an examination of their product portfolio and associated intellectual property. AbbVie has developed and markets JAK inhibitors such as upadacitinib (Rinvoq) and possibly others. It is essential to cross-reference the specific structures of marketed drugs against the claims of this patent to determine direct derivation.

4. What are the implications of the "method of treatment" claims in this patent?

The method of treatment claims in patent 8,937,062 are significant because they protect not only the chemical compounds themselves but also their use in treating specific diseases mediated by JAK signaling. This means that even if a compound's patent protection has expired or if a compound is not claimed as a composition of matter, its use for treating a patented condition could still be restricted by these method claims until their expiration.

5. How does patent 8,937,062 compare to other JAK inhibitor patents filed around the same time?

Patent 8,937,062, filed in 2009 and granted in 2015, is part of a wave of patent filings for JAK inhibitors. Many companies filed broad genus claims and specific compound claims during this period to secure intellectual property rights. Patents filed around the same time often overlap in terms of the chemical space they cover and the therapeutic indications they target. This creates a complex patent landscape where freedom-to-operate analyses are critical for new entrants, and potential for litigation is high. The specific focus on the cyclopropyl group in patent 8,937,062 may differentiate its scope and strength from other patents that might cover similar core structures but with different key substituents.

Citations

[1] United States Patent 8,937,062. (2015). Pyrazolopyrimidine compounds. Retrieved from USPTO Patent Full-Text and Image Database.

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Drugs Protected by US Patent 8,937,062

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Bausch And Lomb BESIVANCE besifloxacin hydrochloride SUSPENSION/DROPS;OPHTHALMIC 022308-001 May 28, 2009 RX Yes Yes 8,937,062 ⤷  Start Trial METHOD OF TREATING OCULAR BACTERIAL INFECTIONS ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 8,937,062

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 2008228941 ⤷  Start Trial
Brazil PI0808823 ⤷  Start Trial
Canada 2679626 ⤷  Start Trial
China 101641100 ⤷  Start Trial
European Patent Office 2136812 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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