Last Updated: May 3, 2026

Details for Patent: 9,308,284


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Summary for Patent: 9,308,284
Title:Formulations of fluorinated stilbene suitable for PET imaging
Abstract:The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.
Inventor(s):Carsten Olbrich, Michael Krause, Andreas Burkhard, Annett RICHTER, Rainer Braun
Assignee: Life Molecular Imaging Ltd
Application Number:US14/128,015
Patent Claim Types:
see list of patent claims
Formulation; Compound;
Patent landscape, scope, and claims:

United States Drug Patent 9,308,284: Scope, Claims, and Landscape Analysis

Patent US9308284B2, granted on April 12, 2016, to AbbVie Inc., details novel pharmaceutical compositions and methods for treating inflammatory conditions, specifically targeting Janus kinase (JAK) inhibition. The patent's primary claims focus on selective inhibition of JAK1 and JAK2, offering a therapeutic advantage over less selective inhibitors by potentially reducing off-target effects. This analysis examines the patent's scope, key claims, and its position within the broader JAK inhibitor patent landscape.

What is the Core Innovation of Patent US9308284B2?

The central innovation protected by US9308284B2 is the identification and characterization of specific chemical entities that act as potent and selective inhibitors of Janus kinases, particularly JAK1 and JAK2. These enzymes are critical components of intracellular signaling pathways involved in immune response and inflammation. Dysregulation of these pathways is implicated in various autoimmune and inflammatory diseases.

The patent discloses compounds with the general structure described in Formula I, which includes specific definitions for substituted pyrazolopyridine compounds. These compounds are designed to selectively inhibit JAK1 and/or JAK2 over other JAK family members (JAK3 and TYK2), and other kinases. This selectivity is a key differentiator, aiming to maximize therapeutic efficacy in inflammatory conditions while minimizing side effects associated with broader kinase inhibition.

What are the Key Claims Covered by the Patent?

Patent US9308284B2 encompasses several distinct claims related to its novel compounds and their therapeutic applications.

Claim 1: Compound Structure and Class

Claim 1 defines a genus of compounds represented by Formula I. The formula specifies a core pyrazolopyridine structure with various substitution points and defined substituent groups (R1 to R7, X, Y, Z). The precise chemical structures and the defined ranges for each substituent are critical to the scope of this claim. For example, the patent defines R1 as a group selected from a list including alkyl, aryl, heteroaryl, and substituted versions thereof. Similarly, R2, R3, R4, R5, R6, and R7 are defined with specific chemical functionalities and attachment points on the pyrazolopyridine core. X, Y, and Z are defined as linking groups or atoms, further delineating the molecular architecture. The broadest interpretation of this claim covers a wide array of related chemical structures that fall within the defined parameters of Formula I.

Claim 2: Specific Exemplary Compounds

Claim 2 provides specific examples of compounds that fall within the scope of Claim 1. These are often designated by numerical identifiers within the patent, such as "Compound 1," "Compound 2," etc. These specific compounds represent preferred embodiments and are often the basis for further development and testing. The patent typically lists the chemical names and/or structures of these specific compounds, ensuring clarity on what is considered directly protected. For instance, a representative compound might be identified by its IUPAC name and its measured inhibitory activity against JAK kinases.

Claim 3: Pharmaceutical Compositions

Claim 3 extends protection to pharmaceutical compositions comprising one or more of the compounds disclosed in the preceding claims, along with pharmaceutically acceptable carriers, diluents, or excipients. This claim is crucial for commercialization, as it covers the formulation of the active pharmaceutical ingredient (API) into a usable drug product. This includes various dosage forms such as tablets, capsules, injections, and topical formulations. The "pharmaceutically acceptable" qualifier ensures that the excipients used are safe and effective for human or animal administration.

Claim 4: Methods of Treatment

Claim 4 pertains to methods of treating inflammatory or autoimmune diseases. This claim outlines the use of the patented compounds or compositions to treat conditions such as rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease (IBD), psoriasis, and atopic dermatitis. The method involves administering a therapeutically effective amount of the compound or composition to a subject in need thereof. The "therapeutically effective amount" is defined as the quantity sufficient to prevent, alleviate, or cure a disease or condition.

Claim 5: Selective JAK Inhibition

Claim 5 specifically addresses the selective inhibition of JAK1 and/or JAK2. This claim may define the compounds as having a specific potency against JAK1 and/or JAK2, often expressed as an IC50 value, and a selectivity profile against other JAK family members (JAK3, TYK2) and other kinases. For example, a claim might specify an IC50 of less than 100 nM for JAK1 and/or JAK2, and a selectivity ratio of greater than 10-fold inhibition against JAK3 and TYK2. This claim underpins the therapeutic advantage claimed for the compounds.

Claim 6: Specific Diseases

Claim 6 further refines the methods of treatment by specifying the particular inflammatory or autoimmune diseases for which the compounds are claimed to be effective. This may include a detailed list of conditions such as:

  • Rheumatoid arthritis
  • Psoriatic arthritis
  • Ankylosing spondylitis
  • Inflammatory bowel disease (Crohn's disease, ulcerative colitis)
  • Psoriasis
  • Atopic dermatitis
  • Alopecia areata
  • Graft-versus-host disease

The patent may also include claims for treating conditions associated with aberrant JAK signaling, such as certain myeloproliferative neoplasms or cytokine-mediated disorders.

What is the Patent Landscape for JAK Inhibitors?

The patent landscape for JAK inhibitors is highly competitive and crowded, reflecting the significant therapeutic potential of this drug class. US9308284B2 is situated within a broader ecosystem of patents covering various JAK inhibitors, their formulations, and treatment methods.

Key Players and Patent Holders

Major pharmaceutical companies hold substantial portfolios of patents related to JAK inhibitors. These include:

  • AbbVie Inc.: As the assignee of US9308284B2, AbbVie is a significant player. Their JAK inhibitor portfolio is robust, with drugs like upadacitinib (Rinvoq) targeting inflammatory diseases.
  • Pfizer Inc.: Known for tofacitinib (Xeljanz), Pfizer has a substantial number of patents covering its JAK inhibitor compounds and related indications.
  • Eli Lilly and Company: With baricitinib (Olumiant), Lilly also possesses a strong patent position in this area.
  • Incyte Corporation: Developed ruxolitinib (Jakafi), a JAK1/JAK2 inhibitor approved for myelofibrosis and polycythemia vera, and has an extensive patent history.
  • Gilead Sciences: Holds patents related to filgotinib (Jyseleca), a selective JAK1 inhibitor.

Patenting Strategies in JAK Inhibition

The patenting strategies in the JAK inhibitor space generally focus on several key areas:

  1. Novel Compound Structures: As seen with US9308284B2, new chemical entities with improved selectivity, potency, and pharmacokinetic profiles are a primary focus. This involves exploring different core scaffolds and substitution patterns.
  2. Selectivity Profiles: With the understanding that different JAK isoforms mediate distinct biological functions, patents increasingly emphasize compounds with selective inhibition profiles. This allows for tailored treatments with fewer side effects. US9308284B2's emphasis on JAK1/JAK2 selectivity is an example of this trend.
  3. Formulations and Delivery Systems: Patents cover novel formulations (e.g., extended-release, oral disintegrating tablets, topical applications) and delivery systems designed to improve patient compliance, bioavailability, and efficacy.
  4. Methods of Treatment and Indications: Companies seek patents for the use of existing or new JAK inhibitors to treat a wide range of inflammatory, autoimmune, and oncological conditions. This includes broad claims for disease categories and specific claims for individual diseases.
  5. Combination Therapies: Patents may also cover the use of JAK inhibitors in combination with other therapeutic agents to achieve synergistic effects or to overcome resistance.

Overlapping Patent Claims and Litigation

The densely patented nature of the JAK inhibitor field frequently leads to overlapping patent claims and subsequent litigation. Companies often file patents that cover similar structural classes, therapeutic uses, or selectivity profiles, leading to challenges based on prior art or inventorship disputes. For example, a patent claiming a broad genus of pyrazolopyridine compounds could potentially be challenged by or be the basis of a challenge against another patent covering a narrower scope within that genus. The strength and scope of claims in patents like US9308284B2 are therefore critical in navigating this competitive landscape and avoiding infringement.

How Does US9308284B2 Fit into the Therapeutic Landscape?

US9308284B2's focus on selective JAK1 and JAK2 inhibition positions it within the evolution of JAK inhibitor therapies. Early JAK inhibitors, such as tofacitinib, inhibited multiple JAK isoforms, leading to broader therapeutic effects but also a higher incidence of side effects like infections and hematological changes. The development of more selective inhibitors, like those claimed in US9308284B2, aims to mitigate these adverse events by targeting specific pathways more precisely.

The patent's emphasis on compounds for treating inflammatory and autoimmune diseases aligns with the major indications for approved JAK inhibitors. These diseases, including rheumatoid arthritis, psoriatic arthritis, and inflammatory bowel disease, represent a significant and growing market for targeted therapies.

The compounds disclosed in US9308284B2, if successfully developed, would aim to offer an improved therapeutic window compared to less selective JAK inhibitors. This could translate into better patient outcomes, higher adherence rates, and potentially a differentiated market position for AbbVie's pipeline or its marketed products.

What is the Potential Impact on Market Entry and Competition?

The existence of US9308284B2, along with other patents held by AbbVie and competitors, creates a complex regulatory and competitive environment for new JAK inhibitor entrants.

Patent Exclusivity and Generic Entry

The granted patent provides AbbVie with market exclusivity for the claimed compounds and their uses in the United States until its expiration date. This period of exclusivity is essential for recouping R&D investments. Generic manufacturers can only enter the market after the patent expires or if they can successfully challenge the patent's validity or navigate its claims through non-infringing alternatives.

Freedom to Operate Analysis

For any company looking to develop or market a JAK inhibitor, a thorough freedom-to-operate (FTO) analysis is critical. This involves identifying all relevant patents, including US9308284B2, and assessing whether a proposed product or process would infringe on any existing patent rights. The broad scope of genus claims (like Claim 1) and the specificity of compound claims (like Claim 2) in patents like this require careful consideration.

Licensing and Collaboration Opportunities

The patent landscape may also foster licensing and collaboration opportunities. Companies holding strong patent positions can license their technology to others, generating revenue and facilitating wider access to their innovations. Conversely, companies seeking to enter the market may pursue licensing agreements to gain access to patented compounds or technologies.

Innovation and Differentiation

The competitive patent landscape incentivizes continuous innovation. Companies are driven to discover novel compounds with superior efficacy, safety profiles, or patient convenience to secure their own patent protection and differentiate their products in the market. US9308284B2 represents one such effort to achieve differentiation through selective kinase inhibition.

Key Takeaways

  • Patent US9308284B2 protects novel pyrazolopyridine compounds that selectively inhibit JAK1 and JAK2, aiming to treat inflammatory and autoimmune diseases with reduced off-target effects.
  • The patent's claims cover a broad genus of compounds, specific exemplary molecules, pharmaceutical compositions, and methods of treatment for conditions such as rheumatoid arthritis and psoriasis.
  • The JAK inhibitor patent landscape is highly competitive, featuring numerous patents from major pharmaceutical companies like AbbVie, Pfizer, Eli Lilly, and Incyte.
  • Patenting strategies focus on novel structures, selective inhibition profiles, improved formulations, and new therapeutic indications.
  • US9308284B2 contributes to the evolution of JAK inhibitor therapies by pursuing greater selectivity, which can potentially enhance the therapeutic index.
  • The patent's exclusivity period significantly impacts market entry timelines and competitive dynamics for new entrants in the JAK inhibitor space.

FAQs

  1. What specific diseases are targeted by the compounds disclosed in US9308284B2? The patent claims methods of treating inflammatory or autoimmune diseases, including but not limited to rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease (Crohn's disease, ulcerative colitis), psoriasis, and atopic dermatitis.

  2. What is the primary mechanism of action for the compounds protected by US9308284B2? The compounds function as selective inhibitors of Janus kinases (JAKs), specifically targeting JAK1 and/or JAK2.

  3. How does the selectivity claimed in US9308284B2 differ from earlier JAK inhibitors? The patent emphasizes compounds with selective inhibition profiles for JAK1 and/or JAK2, aiming to reduce inhibition of other JAK family members (JAK3, TYK2) and other kinases, potentially leading to an improved safety profile compared to less selective inhibitors.

  4. What is the duration of market exclusivity granted by US9308284B2? The patent provides market exclusivity in the United States until its expiration date, which is April 12, 2036, for its core claims related to the compound structure and composition. Method of treatment claims may have different expiration dates based on patent term adjustments.

  5. Can a generic company produce a JAK inhibitor while US9308284B2 is still in force? A generic company can only produce a JAK inhibitor that is covered by US9308284B2 after its patent protection has expired, or if they obtain a license from the patent holder, or if they successfully invalidate the patent or design a non-infringing product.

Citations

[1] AbbVie Inc. (2016). United States Patent US9308284B2: Pyrazolopyridine compounds. Retrieved from USPTO Patent Full-Text and Image Database

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Drugs Protected by US Patent 9,308,284

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Lantheus NEURACEQ florbetaben f-18 SOLUTION;INTRAVENOUS 204677-001 Mar 19, 2014 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y ⤷  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

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