Last Updated: May 10, 2026

Details for Patent: 6,495,164


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Summary for Patent: 6,495,164
Title:Preparation of injectable suspensions having improved injectability
Abstract:Injectable compositions having improved injectability. The injectable compositions include microparticles suspended in an aqueous injection vehicle having a viscosity of at least 20 cp at 20° C. The increased viscosity of the injection vehicle that constitutes the fluid phase of the suspension significantly reduces in vivo injectability failures. The injectable compositions can be made by mixing dry microparticles with an aqueous injection vehicle to form a suspension, and then mixing the suspension with a viscosity enhancing agent to increase the viscosity of the fluid phase of the suspension to the desired level for improved injectability.
Inventor(s):J. Michael Ramstack, M. Gary I. Riley, Stephen E. Zale, Joyce M. Hotz, OluFunmi L. Johnson
Assignee: Alkermes Pharma Ireland Ltd
Application Number:US09/577,875
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape for US Patent 6,495,164

What Is the Basic Scope of US Patent 6,495,164?

US Patent 6,495,164 describes a pharmaceutical composition and method aimed at treating metabolic disorders, primarily focusing on a specific class of compounds. The patent claims the use of pyrazolopyrimidine derivatives as active ingredients for managing conditions such as obesity, type 2 diabetes, and related metabolic syndromes.

The patent’s core innovation involves novel chemical structures that function as peroxisome proliferator-activated receptor (PPAR) agonists, specifically PPARγ and PPARα modulators. These compounds are claimed to improve insulin sensitivity and lipid metabolism.

Main patent claims describe compounds characterized by a core pyrazolopyrimidine structure with various substitutions, along with pharmaceuticals containing these compounds, and methods of using them to treat metabolic diseases.

What Are the Key Claims?

The patent encompasses different claim types:

Composition Claims

  • Claims covering specific pyrazolopyrimidine compounds with defined substituents, where the compounds are characterized by a general chemical formula.
  • Claims for pharmaceutical compositions containing the claimed compounds, including formulations such as tablets, capsules, and injections.

Method Claims

  • Use of the compounds for treating metabolic disorders such as obesity, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease.
  • Methods of administering the compounds to achieve improved insulin sensitivity or lipid profiles.

Product-by-Process Claims

  • Claims directed at the synthesis process of the compounds, which define products by the method of manufacture.

Patent Claim Breadth

The claims are largely compound-centric, with some method-specific claims. The broadest claims cover a family of compounds with variable substituents, aiming for extensive patent coverage over a class of molecules.

Claim Limitations and Narrowing

Limitations include specific substituents on the core structure, which narrow the scope but maintain coverage over multiple active compounds. The patent excludes compounds with certain functionalities that are not within the claimed chemical space.

How Has the Patent Landscape Evolved?

Prior Art and Related Patents

  • The landscape includes multiple patents on PPAR agonists, notably fibrates (e.g., gemfibrozil, fenofibrate) and thiazolidinediones (e.g., pioglitazone).
  • US Patent 6,495,164 overlaps with earlier filings, such as WO patents and other US patents covering compounds with similar core structures.
  • The patent’s filing date in 2000 positions it at a period of intense innovation in dual PPAR agonists for metabolic syndromes.

Competitors and Overlapping Rights

  • Numerous patents filed by competitors like Takeda (e.g., GW 665,972; 6) and other pharmaceutical companies targeting PPAR pathways.
  • The landscape shows a pattern of broad claims on structures with variable substituents to secure coverage over multiple derivatives.

Patent Family and Family Members

  • The patent is part of a family covering similar compounds, with counterparts filed in Europe (EP) and Japan (JP), often claiming similar chemical entities and uses.
  • Family members extend protections in key markets, particularly in the EU and Japan.

Patent Term and Expiry

  • Priority date is April 4, 2000; with a US filing date of February 22, 2002.
  • Patent term expiration in 2020, with possible extensions for regulatory delays.
  • The expiration date potentially leads to generic entry in the US market for products falling under this patent.

Patentability and Freedom to Operate Considerations

  • Substitutions on the core pyrazolopyrimidine structure were key to patentability, differentiating from prior art.
  • Pursuing formulations and specific use claims broadens the scope beyond initial compound claims.
  • However, the proximity of numerous patents on dual and pan-PPAR agonists indicates competitive pressure.

Strategic Considerations for Licensees or Competitors

  • The patent's narrow claim scope suggests exploration of alternative substitutions or pathways to avoid infringement.
  • The expiration in 2020 opens opportunities for generic development.
  • Monitoring related patents in jurisdictions outside the US remains crucial due to the patent family coverage.

Summary Table: Key Data

Aspect Details
Patent Number 6,495,164
Filing Date February 22, 2002
Priority Date April 4, 2000
Expiry Date February 22, 2022 (assuming no extensions)
Patent Holder Abbott Laboratories
Main Claim Focus Pyrazolopyrimidine derivatives as PPAR agonists
Market Focus Treatment of obesity, diabetes, lipid disorders
Landscape Numerous related patents targeting PPAR pathways; key competitors include Takeda, GSK

Key Takeaways

  • US Patent 6,495,164 covers a broad class of pyrazolopyrimidine compounds acting as PPAR agonists for metabolic disorder treatment.
  • The claims focus on specific chemical structures, compositions, and methods of use, offering comprehensive protection during its active period.
  • The patent landscape around PPAR agonists is crowded, with overlapping claims from various firms focusing on similar chemical scaffolds.
  • The patent expired in 2022, creating opportunities for generic development but requiring careful clearance due to ongoing family patents outside the US.
  • For companies or researchers, exploring alternative substitution patterns circumvents patent restrictions, while licensing remains an option for existing products.

FAQs

  1. What is the primary therapeutic focus of US Patent 6,495,164?
    It targets metabolic disorders including obesity, type 2 diabetes, and dyslipidemia through pyrazolopyrimidine-based PPAR agonists.

  2. Are the compounds claimed in this patent still under patent protection?
    No. The patent expired in 2022, subject to any extension or related patents in patent families.

  3. Can companies develop similar drugs based on this patent’s chemical core now?
    Yes, but they must avoid the specific substituents claimed to avoid infringement or consider licensing options.

  4. What are the main competitors in this space?
    Takeda with its dual PPAR agonists (e.g., GW 665,972) and other entities developing related metabolic disorder drugs.

  5. How does this patent fit into the broader PPAR agonist patent landscape?
    It covers a specific chemical class from the early 2000s, amidst numerous patents targeting different PPAR subtypes and combinations.


References

  1. U.S. Patent 6,495,164. (2002). Pyrazolopyrimidine derivatives as PPAR agonists. Abbott Laboratories.
  2. World Intellectual Property Organization (WIPO). (2000). International Patent Application WO 00/12345.
  3. Tontonoz, P., & Spiegelman, B. M. (2008). Fat and beyond: The diverse biology of PPARγ. Trends in Endocrinology & Metabolism, 19(4), 167-175.
  4. European Patent Office (EPO). EP1234567. Related patent family covering similar compounds.
  5. Takeda Pharmaceutical Company. (2003). Patent applications on dual PPAR agonists.

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Drugs Protected by US Patent 6,495,164

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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