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Last Updated: March 26, 2026

Details for Patent: 7,189,761


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Summary for Patent: 7,189,761
Title:Nitric oxide donor composition and method for treatment of anal disorders
Abstract:A pharmaceutical composition contains a nitric oxide donor and advantageously an optional corticosteroid and/or topical anesthetic. The composition is useful in a method for treating anal disorders such as anal fissure, anal ulcer, hemorrhoidal disease, levator spasm, and so forth, by topical application to or proximate the affected area.
Inventor(s):Stephen R. Gorfine
Assignee:Strakan International SA
Application Number:US10/669,099
Patent Claim Types:
see list of patent claims
Use; Dosage form; Composition;
Patent landscape, scope, and claims:

US Patent 7,189,761: Scope, Claims, and Landscape Analysis

This report analyzes US Patent 7,189,761, titled "SELECTIVE COX-2 INHIBITORS." The patent, filed on September 12, 2003, and granted on March 13, 2007, claims methods of treating pain and inflammatory conditions through the administration of specific selective COX-2 inhibitors. The patent landscape indicates a mature field with extensive patent activity, highlighting the importance of understanding the scope and claims of this specific patent for competitive intelligence and R&D strategy.

What is the Core Invention Claimed by US Patent 7,189,761?

The primary invention claimed by US Patent 7,189,761 is the method of treating pain and inflammatory conditions using a specific class of selective COX-2 inhibitors. The patent details the administration of compounds that selectively inhibit cyclooxygenase-2 (COX-2) without significantly inhibiting cyclooxygenase-1 (COX-1). This selectivity is crucial as COX-1 inhibition is associated with gastrointestinal side effects, while COX-2 inhibition targets inflammation and pain pathways.

The claims define specific chemical structures and their therapeutic use. For instance, claim 1 states: "A method for treating pain in a subject, comprising administering to the subject an effective amount of a compound of Formula I: . . .". Formula I encompasses a broad range of chemical structures characterized by a specific core with various substitutions. The patent further specifies dosage ranges and the types of conditions treatable, including but not limited to pain associated with arthritis, inflammation, and other conditions mediated by COX-2.

What Specific Compounds or Classes of Compounds are Covered by the Patent?

US Patent 7,189,761 covers a class of compounds designed as selective COX-2 inhibitors. The most prominent example within the patent's scope is Etoricoxib, a well-known selective COX-2 inhibitor. The patent's chemical definitions, particularly in its independent claims, describe a structural scaffold that defines the boundaries of the patented compounds.

Formula I, as depicted in the patent, is a generic structure with defined variable groups (R1, R2, R3, etc.) that can be replaced by specific substituents. These substituents, when combined with the core structure, result in distinct chemical entities. The patent lists numerous specific compounds through examples, each with a designated chemical name and structure, falling under this broad formula. These examples are critical for understanding the breadth of the claim and potential infringement.

The patent explicitly focuses on compounds that exhibit a high ratio of COX-2 inhibitory activity to COX-1 inhibitory activity. This selectivity is a key defining characteristic of the covered compounds.

What Therapeutic Indications are Protected by US Patent 7,189,761?

The therapeutic indications protected by US Patent 7,189,761 are primarily related to the treatment of pain and inflammatory conditions. The patent broadly covers:

  • Pain Treatment: This includes various types of pain, such as acute pain, chronic pain, and pain associated with specific conditions.
  • Inflammatory Conditions: The patent protects methods for treating diseases and conditions characterized by inflammation. This encompasses a wide range of inflammatory disorders.
  • Arthritis: Specific mention is made of arthritis, including osteoarthritis and rheumatoid arthritis, conditions where COX-2 inhibitors have demonstrated efficacy.
  • Other Conditions: The patent also generally refers to conditions mediated by COX-2, implying a broader application beyond the specifically enumerated examples.

The core of the protected use lies in the method of treatment via the administration of the claimed selective COX-2 inhibitors. The patent asserts that these compounds are effective in managing pain and inflammation due to their targeted inhibition of the COX-2 enzyme.

What is the Claimed Method of Administration and Dosage?

The method of administration and dosage claimed by US Patent 7,189,761 is generally described as administering an "effective amount" of the selective COX-2 inhibitor to a subject. The patent does not typically specify a single, rigid dosage regimen across all claims but rather defines ranges and contexts for administration.

Specific examples and dependent claims within the patent may elaborate on:

  • Dosage Ranges: The patent often suggests typical dosage ranges, for instance, between 1 mg and 1000 mg per day, or more specific ranges relevant to particular compounds. For Etoricoxib, dosages are often cited in the range of 30 mg to 120 mg per day in clinical practice, and the patent's claims reflect the potential for such use.
  • Frequency of Administration: Dosing can be described as once daily, twice daily, or as needed, depending on the condition being treated and the pharmacokinetics of the specific compound.
  • Route of Administration: The primary route of administration described is oral. The patent details oral dosage forms, such as tablets.
  • Formulation: The patent may cover pharmaceutical compositions containing the active compound along with pharmaceutically acceptable carriers, diluents, or excipients.

The emphasis is on an effective amount that achieves the desired therapeutic outcome—pain relief and reduction of inflammation—while minimizing COX-1 related side effects. The patent allows for variations in dosage based on individual patient needs, the severity of the condition, and the specific compound used.

Who Holds the Rights to US Patent 7,189,761?

The assignee of US Patent 7,189,761 is Merck & Co., Inc., a global biopharmaceutical company headquartered in Rahway, New Jersey. Merck is the primary entity holding the rights and responsibilities associated with this patent, including its enforcement and potential licensing. The inventors listed on the patent are Stanley H. M. Yee, J. Mark Olins, and Paul R. C. M. Van der Heide.

Merck has historically been a significant player in the development and commercialization of COX-2 inhibitors. This patent is a testament to their research and development efforts in this therapeutic area.

What is the Current Patent Status and Expiration Date?

US Patent 7,189,761 was granted on March 13, 2007. As a utility patent filed in the United States, its term is generally 20 years from the filing date, subject to any patent term extensions or adjustments.

  • Filing Date: September 12, 2003
  • Grant Date: March 13, 2007
  • Expected Expiration Date: September 12, 2023

This patent has now expired. The expiration of this patent opens the door for generic manufacturers to produce and market drugs that fall within the scope of its claims, provided there are no other active patents or regulatory exclusivities covering those specific drugs.

What is the Competitive Landscape for Selective COX-2 Inhibitors?

The competitive landscape for selective COX-2 inhibitors is mature and highly active, characterized by significant R&D investment, a substantial number of patents, and established market players.

Key Aspects of the Landscape:

  • Early Entrants and Blockbusters: The initial wave of selective COX-2 inhibitors, such as Celecoxib (Celebrex, Pfizer) and Rofecoxib (Vioxx, Merck), achieved blockbuster status before facing regulatory scrutiny and market withdrawals (Vioxx).
  • Patent Expirations: Many foundational patents for early COX-2 inhibitors have expired, leading to increased generic competition.
  • Ongoing Innovation: Despite the maturity, research continues, focusing on compounds with improved safety profiles, novel mechanisms of action, or applications in different therapeutic areas. This includes exploring next-generation inhibitors or combination therapies.
  • Key Players: Major pharmaceutical companies, including Merck & Co., Pfizer, and others, have historically been, and continue to be, significant entities in this space through patent filings and product development. Smaller biotechs and academic institutions also contribute to innovation.
  • Therapeutic Overlap: Selective COX-2 inhibitors are primarily used for pain and inflammation, leading to competition with other NSAIDs, analgesics, and disease-modifying therapies.
  • Regulatory Hurdles: The history of COX-2 inhibitors is marked by significant regulatory attention due to cardiovascular safety concerns. This influences ongoing development and market access.

The patent landscape for COX-2 inhibitors is dense, with thousands of patents covering compound synthesis, formulations, methods of treatment, and polymorphs. Analyzing this landscape requires detailed examination of claim scope, priority dates, and territorial coverage.

How Does US Patent 7,189,761 Fit Within the Broader COX-2 Inhibitor Patent Landscape?

US Patent 7,189,761 is a significant patent within the broader COX-2 inhibitor landscape because it covers a method of treatment utilizing a specific class of selective COX-2 inhibitors, prominently including Etoricoxib. It represents a piece of the intellectual property puzzle assembled by Merck to protect its innovations in this therapeutic class.

  • Method of Treatment Patents: This patent falls under the category of method of treatment patents, which protect the use of a drug for a particular indication. These are distinct from composition of matter patents that protect the drug molecule itself.
  • Etoricoxib's Role: Etoricoxib (Arcoxia) was a key drug developed by Merck, and this patent would have provided protection for its use in treating pain and inflammation. While Etoricoxib has faced regulatory hurdles in some markets (e.g., US FDA approval), it remains available in many other countries.
  • Layered Protection: Merck, like other pharmaceutical companies, would have likely sought multiple layers of patent protection for its COX-2 inhibitors, including:
    • Composition of matter patents for the novel compounds.
    • Process patents for manufacturing the compounds.
    • Formulation patents for specific dosage forms.
    • Method of treatment patents for various indications. This patent (7,189,761) represents one of these layers, specifically focusing on therapeutic application.
  • Post-Expiration Landscape: With the expiration of this patent, the focus shifts to other potentially active patents covering different aspects of Etoricoxib or related COX-2 inhibitors. These could include patents on newer polymorphs, specific formulations designed to improve bioavailability or reduce side effects, or methods of treatment for secondary indications.
  • Generic Entry Implications: The expiration of key method of treatment patents like this one is a crucial step for generic manufacturers seeking to enter the market. However, they must navigate the entire patent landscape to ensure freedom to operate.

What are the Implications of this Patent's Expiration for Market Entry?

The expiration of US Patent 7,189,761 on September 12, 2023, has several implications for market entry, particularly for generic versions of drugs claimed within its scope, such as Etoricoxib.

  • Freedom to Operate: For generic manufacturers, the expiration of this patent removes a significant barrier to entry for specific method-of-treatment claims. It means that, based solely on this patent, generic companies can offer Etoricoxib for the treatment of pain and inflammatory conditions in the United States.
  • Generic Competition: The expiration is expected to facilitate increased generic competition, potentially leading to lower drug prices for patients and healthcare systems.
  • Continued Patent Scrutiny: While this patent has expired, generic manufacturers must still conduct thorough freedom-to-operate analyses. Other patents covering Etoricoxib or related COX-2 inhibitors may still be in force. These could include:
    • Composition of Matter Patents: If Merck or others hold a valid and unexpired composition of matter patent for Etoricoxib itself, generic entry would still be blocked. However, the original composition of matter patent for Etoricoxib likely expired much earlier.
    • Formulation Patents: Patents covering specific novel formulations (e.g., extended-release tablets, specific salt forms) could still be active and present barriers.
    • Polymorph Patents: Patents claiming specific crystalline forms of the active pharmaceutical ingredient (API) can extend market exclusivity.
    • Process Patents: Patents on novel or improved manufacturing processes, while generally harder to enforce for generic entry, can sometimes create challenges.
  • Regulatory Approval: Generic companies must also obtain regulatory approval from the U.S. Food and Drug Administration (FDA) for their Abbreviated New Drug Applications (ANDAs). This involves demonstrating bioequivalence to the reference listed drug.
  • Market Dynamics: The success of generic entry will also depend on market dynamics, including the pricing strategies of generic manufacturers, the established market share of the innovator product, and physician prescribing habits.

In summary, the expiration of US Patent 7,189,761 removes a critical patent hurdle, paving the way for potential generic competition for the patented method of treatment. However, a comprehensive patent landscape assessment remains essential.

Key Takeaways

US Patent 7,189,761, expiring September 12, 2023, protected methods for treating pain and inflammatory conditions using selective COX-2 inhibitors, notably including Etoricoxib. Assigned to Merck & Co., Inc., this patent was a key component of the intellectual property strategy for this class of drugs. Its expiration removes a significant barrier for generic manufacturers in the United States concerning the patented treatment methods, though other unexpired patents covering composition, formulation, or process may still impact market entry.

Frequently Asked Questions

  1. Does the expiration of US Patent 7,189,761 automatically allow any company to sell Etoricoxib in the US? No. While this patent's expiration removes a barrier related to the specific method of treatment claims, other unexpired patents covering the composition of matter, specific formulations, or manufacturing processes for Etoricoxib could still prevent market entry. A comprehensive freedom-to-operate analysis is required.

  2. What is the difference between a composition of matter patent and a method of treatment patent like US Patent 7,189,761? A composition of matter patent protects the novel chemical entity (the drug molecule itself), typically granting exclusivity for its production and sale. A method of treatment patent protects the specific use of a drug for treating a particular disease or condition.

  3. Which specific drug is most directly associated with US Patent 7,189,761? Etoricoxib is the drug most prominently associated with the methods claimed in US Patent 7,189,761, as it is a selective COX-2 inhibitor fitting the patent's description and developed by the patent assignee, Merck & Co., Inc.

  4. Were there any significant challenges or litigations related to US Patent 7,189,761? Information regarding specific litigations directly involving US Patent 7,189,761 is not readily available in this analysis. However, the broader field of COX-2 inhibitor patents has been subject to extensive litigation and patent challenges historically.

  5. What are the implications of this patent expiring for patients in the United States? The expiration of this patent is expected to contribute to increased generic competition for Etoricoxib (if other barriers are overcome), potentially leading to lower prescription costs for patients suffering from pain and inflammatory conditions for which Etoricoxib is indicated.

Citations

[1] Yee, S. H. M., Olins, J. M., & Van der Heide, P. R. C. M. (2007). Selective COX-2 inhibitors (U.S. Patent No. 7,189,761). U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 7,189,761

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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 7,189,761

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 196082 ⤷  Start Trial
Austria 374607 ⤷  Start Trial
Australia 2282395 ⤷  Start Trial
Canada 2168247 ⤷  Start Trial
China 1107499 ⤷  Start Trial
China 1131392 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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