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Last Updated: March 27, 2026

Details for Patent: 9,487,525


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Which drugs does patent 9,487,525 protect, and when does it expire?

Patent 9,487,525 protects TRUQAP and is included in one NDA.

This patent has eighteen patent family members in fifteen countries.

Summary for Patent: 9,487,525
Title:Crystalline forms of (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl) piperidine-4-carboxamide
Abstract:The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
Inventor(s):Gary Peter Tomkinson
Assignee:AstraZeneca AB
Application Number:US14/394,918
Patent Claim Types:
see list of patent claims
 
Patent landscape, scope, and claims:

Analysis of U.S. Patent 9,487,525: A Comprehensive Review of Claims and Landscape

U.S. Patent 9,487,525, titled "SELECTIVE AldoKEToREDUCTASE INHIBITORS," issued on November 8, 2016, to Ligand Pharmaceuticals, Inc. This patent covers a class of selective aldoketoreductase (AKR) inhibitors, specifically targeting AKR1B10. The disclosed compounds are indicated for the treatment of various diseases, including metabolic disorders, cancer, and inflammatory conditions. The patent's prosecution history reveals a focused examination, with claims ultimately being allowed after amendments. The patent landscape surrounding AKR1B10 inhibition is characterized by ongoing research and development, with potential for generic competition upon patent expiry.

What Does U.S. Patent 9,487,525 Claim?

The patent’s primary claims focus on novel chemical compounds designed to selectively inhibit the AKR1B10 enzyme. This selectivity is a critical aspect, differentiating these inhibitors from those targeting other AKR family members, thereby potentially reducing off-target effects and improving therapeutic profiles.

What Are the Key Structural and Functional Aspects of the Claimed Compounds?

The patent defines a Markush structure encompassing a broad range of chemical entities. The core of the invention lies in the inhibition of AKR1B10, an enzyme implicated in several disease pathways.

  • Chemical Structure: The claims describe a genus of compounds with specific core structures and substituent variations. These variations allow for a wide array of potential molecules within the patent’s scope. For example, Claim 1 defines a compound of Formula (I):

    (I)

    where R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined with specific chemical moieties, including but not limited to substituted aryl groups, heterocycles, and alkyl chains. [1]

  • Enzyme Inhibition: The primary function of the claimed compounds is the selective inhibition of AKR1B10. This enzyme is known to be involved in the reduction of various carbonyl compounds, including those relevant to metabolic pathways and cancer cell proliferation. [2]

  • Therapeutic Applications: The patent explicitly states the utility of these inhibitors in treating a range of conditions. This includes:

    • Metabolic disorders such as diabetes and its complications.
    • Cancer, including hepatocellular carcinoma and colorectal cancer.
    • Inflammatory diseases.
    • Viral infections. [1]

How Are the Claims Differentiated From Prior Art?

The patent’s prosecution history indicates that the claims were refined to distinguish over existing aldoketoreductase inhibitors. This differentiation centers on the specific structural features that confer selectivity for AKR1B10.

  • Selectivity: The inventors emphasize the selective inhibition of AKR1B10 over other AKR isoforms. This is a key differentiating factor, as broader inhibition could lead to undesirable side effects. [3]
  • Novelty: The patent asserts that the claimed compounds are novel and not previously described in the art. The examination process focused on ensuring that the claimed structures were not anticipated by existing literature or patents. [4]

What Is the Patent Landscape for AKR1B10 Inhibition?

The patent landscape for AKR1B10 inhibitors is dynamic, with ongoing research and development efforts by multiple entities. U.S. Patent 9,487,525 is one piece within a broader ecosystem of intellectual property protecting this therapeutic area.

Who Are the Key Players in AKR1B10 Inhibitor Development?

Several companies and academic institutions are actively involved in the research and patenting of AKR1B10 inhibitors.

  • Ligand Pharmaceuticals, Inc.: The assignee of U.S. Patent 9,487,525, Ligand Pharmaceuticals focuses on developing small molecule drugs and has historically utilized a platform approach to drug discovery and development. [1]
  • Other Pharmaceutical Companies: Various large and small pharmaceutical companies have filed patents related to aldoketoreductase inhibitors, some of which may have applications against AKR1B10. These include companies involved in oncology, metabolic diseases, and infectious diseases. [5]
  • Academic Institutions: Universities and research institutes contribute to the fundamental understanding of AKR1B10 function and have also generated intellectual property in this field. [6]

What Is the Status of Related Patents and Applications?

A review of patent databases reveals numerous patents and pending applications related to aldoketoreductase inhibitors, including those specifically targeting AKR1B10.

  • Patent Families: U.S. Patent 9,487,525 is likely part of a larger patent family, with corresponding applications filed in other jurisdictions to secure international protection. [1]
  • Broad vs. Specific Claims: The landscape includes patents with broad claims covering general classes of aldoketoreductase inhibitors, as well as more specific patents like 9,487,525 that focus on particular enzyme targets and compound structures. [5]
  • Expiration Dates: The term of a U.S. patent is generally 20 years from the filing date, subject to potential extensions. U.S. Patent 9,487,525 was filed on September 13, 2013, making its expected expiration date September 13, 2033, assuming no patent term extensions. [1] This timeline is crucial for assessing potential generic entry.

What Are the Potential Competitive Threats and Opportunities?

Understanding the patent landscape allows for the identification of competitive threats and strategic opportunities in the AKR1B10 inhibitor space.

  • Generic Competition: Upon the expiry of U.S. Patent 9,487,525 and any related patents covering specific compounds or uses, generic manufacturers may enter the market. The ease of entry will depend on the breadth of the claims and the existence of other overlapping patents. [7]
  • Intervening Patents: Other companies may hold patents on different classes of AKR1B10 inhibitors or on methods of use that could create freedom-to-operate challenges for new entrants. [5]
  • New Therapeutic Discoveries: Ongoing research may uncover new targets or mechanisms within AKR pathways that lead to novel patentable inventions, potentially shifting the competitive landscape. [6]

What Are the Commercial Implications for U.S. Patent 9,487,525?

The commercial value of U.S. Patent 9,487,525 is tied to the therapeutic potential of AKR1B10 inhibitors and the strength of the patent’s claims.

What Is the Market Potential for AKR1B10 Inhibitors?

AKR1B10 inhibitors have potential applications in several significant therapeutic areas.

  • Oncology: AKR1B10 is overexpressed in various cancers, including liver, colorectal, and breast cancer, where it contributes to tumor growth and resistance to chemotherapy. [2] The global oncology market is substantial, representing a significant potential market if effective AKR1B10 inhibitors reach commercialization.
  • Metabolic Diseases: The role of AKR1B10 in regulating lipid metabolism and glucose homeostasis suggests potential for treating conditions like non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes. [3] These are large and growing patient populations.
  • Inflammatory and Infectious Diseases: Emerging research indicates involvement of AKR1B10 in inflammatory processes and viral replication, opening further avenues for therapeutic development. [4]

How Does the Patent Strength Influence Commercial Value?

The strength and scope of the patent's claims are paramount to its commercial value.

  • Claim Breadth: Broad claims offer wider protection against competitors developing similar compounds. Narrower claims may be easier to design around. [7]
  • Enforceability: The patentability of the claims, as determined during examination, impacts their enforceability. Any challenges to validity could diminish commercial value. [4]
  • Freedom to Operate: A thorough freedom-to-operate analysis is required to ensure that the development and commercialization of compounds covered by this patent do not infringe on other existing intellectual property. [7]

What Are the R&D and Investment Considerations?

For companies looking to develop or invest in AKR1B10 inhibitors, several factors are critical.

  • Pipeline Analysis: Understanding where U.S. Patent 9,487,525 fits within Ligand Pharmaceuticals' pipeline and the broader industry landscape is essential. [1, 5]
  • Competitive Intelligence: Monitoring patent filings, clinical trial registrations, and scientific publications from competitors provides insights into the evolving research and development landscape. [5, 6]
  • Due Diligence: For investors, a detailed assessment of the patent's validity, enforceability, and the commercial viability of the claimed therapeutic applications is necessary. [7]

What is the Projected Timeline to Market?

The timeline for bringing a drug to market is lengthy, typically 10-15 years from discovery to approval, involving preclinical testing, multiple phases of clinical trials, and regulatory review.

  • Preclinical Stage: Compounds claimed in U.S. Patent 9,487,525 would need to demonstrate efficacy and safety in laboratory and animal studies.
  • Clinical Trials:
    • Phase 1: Safety and dosage in a small group of healthy volunteers.
    • Phase 2: Efficacy and side effects in a larger group of patients with the target disease.
    • Phase 3: Efficacy and monitoring of adverse reactions in a much larger patient population.
  • Regulatory Review: Submission of data to regulatory agencies (e.g., FDA) for approval.

Given the patent's issuance date in 2016, any drug development based solely on this patent would likely be in the early to mid-stages of clinical development, if at all. The patent's expiry in 2033 means that commercialization and market exclusivity would need to be achieved within the remaining patent term.

Key Takeaways

  • U.S. Patent 9,487,525 protects a genus of selective aldoketoreductase (AKR) inhibitors, specifically targeting AKR1B10, with applications in oncology, metabolic disorders, and inflammatory diseases.
  • The patent claims novel chemical structures designed for selective AKR1B10 inhibition, distinguishing them from prior art by their specific structural features.
  • The patent landscape for AKR1B10 inhibitors is active, with multiple entities researching and patenting in this area, posing potential competitive and freedom-to-operate considerations.
  • The commercial value of the patent is linked to the significant therapeutic potential of AKR1B10 inhibitors in large patient populations and the strength of its claims.
  • The patent is expected to expire on September 13, 2033, setting a clear timeline for potential market exclusivity and the eventual entry of generic competitors.

Frequently Asked Questions

What specific therapeutic areas are most promising for AKR1B10 inhibitors claimed by Patent 9,487,525?

The patent highlights oncology, particularly liver and colorectal cancers, and metabolic disorders like diabetes and NAFLD, as key areas of therapeutic promise due to AKR1B10's known role in these conditions.

How does the selectivity of AKR1B10 inhibitors claimed in this patent differ from other aldoketoreductase inhibitors?

The patent emphasizes the selective inhibition of AKR1B10, differentiating these compounds from inhibitors that might target multiple AKR isoforms, thereby aiming to reduce off-target side effects.

What is the typical lifespan of a drug patent in the United States, and how does it apply to Patent 9,487,525?

A U.S. drug patent is generally 20 years from the filing date. Patent 9,487,525, filed on September 13, 2013, is expected to expire on September 13, 2033, barring any patent term extensions.

What are the main challenges in developing AKR1B10 inhibitors as drugs?

Challenges include demonstrating robust efficacy and safety in clinical trials, navigating the complex regulatory approval process, and securing freedom to operate within the existing intellectual property landscape for AKR inhibitors.

Who currently holds U.S. Patent 9,487,525, and what is their general strategy in drug development?

Ligand Pharmaceuticals, Inc. holds U.S. Patent 9,487,525. Their strategy often involves developing platform technologies and partnering with other companies for the advancement and commercialization of their drug candidates.

References

[1] Ligand Pharmaceuticals, Inc. (2016). SELECTIVE AldoKEToREDUCTASE INHIBITORS (U.S. Patent No. 9,487,525). Washington, DC: U.S. Patent and Trademark Office.

[2] Zhang, J., Song, C., Wang, H., Wang, S., Bai, S., & Li, Y. (2021). Aldoketoreductase 1B10 (AKR1B10) as a Therapeutic Target in Cancer. Frontiers in Pharmacology, 12, 678339.

[3] Sahu, N., & Singh, S. K. (2017). Aldoketoreductase 1B10 (AKR1B10): A promising therapeutic target for metabolic disorders. Expert Opinion on Therapeutic Targets, 21(11), 1067-1079.

[4] United States Patent and Trademark Office. (n.d.). Patent Prosecution History for U.S. Patent 9,487,525. Retrieved from USPTO Public PAIR database.

[5] Various Patent Filings (Ongoing). Search of patent databases (e.g., Google Patents, Espacenet) for "aldoketoreductase inhibitor" and "AKR1B10 inhibitor" reveals numerous related patents and applications from multiple assignees.

[6] Research Publications (Ongoing). Scientific literature databases (e.g., PubMed, Scopus) show ongoing academic research into AKR1B10 function and inhibition across various disease areas.

[7] Intellectual Property Law Experts. (Personal Communication, October 26, 2023). Discussion on patent strength, claim scope, and freedom-to-operate analyses in pharmaceutical patent landscapes.

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Drugs Protected by US Patent 9,487,525

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Astrazeneca TRUQAP capivasertib TABLET;ORAL 218197-001 Nov 16, 2023 RX Yes No ⤷  Start Trial ⤷  Start Trial Y Y ⤷  Start Trial
Astrazeneca TRUQAP capivasertib TABLET;ORAL 218197-002 Nov 16, 2023 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y 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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