Last updated: July 27, 2025
Introduction
Patent AU2005212405, titled "Use of a crystallized form of trans-4-[4-(2-carboxyethyl)phenyl]-7-[(1R)-1-hydroxy-2-methylpropyl]-2-quinolinecarboxylic acid," was granted in Australia in 2005. The patent primarily pertains to pharmaceutical compositions and methods involving a specific crystallized form of a known active compound, associated with optimized bioavailability or stability. This analysis dissects the scope and claims, assesses the patent landscape surrounding this patent, and elucidates strategic considerations for stakeholders in the pharmaceutical domain.
Scope of Patent AU2005212405
The patent's scope centers on the "crystallized form" of the compound, which is structurally based on a quinoline derivative. The compound appears to involve a specific stereochemistry and crystalline modification. The overall focus is on the pharmaceutical application of this specific crystalline form, possibly to improve stability, solubility, bioavailability, or manufacturing efficiency.
The patent explicitly claims protection over:
- The crystalline form of the relevant compound, including specific polymorphic forms.
- Methods of preparing the crystalline form, emphasizing particular crystallization conditions.
- The pharmaceutical compositions comprising the crystalline form, potentially including other excipients.
- Therapeutic uses of the crystalline form, particularly in treating diseases where the compound is efficacious.
This scope aligns with common patenting strategies for active pharmaceutical ingredients (APIs), especially where crystalline forms can markedly influence drug performance.
Claims Breakdown
The patent contains multiple claims—central to its enforceability and scope—that can be categorized as follows:
1. Structural and Crystallographic Claims
- Claim 1: It broadly claims "a crystalline form of trans-4-[4-(2-carboxyethyl)phenyl]-7-[(1R)-1-hydroxy-2-methylpropyl]-2-quinolinecarboxylic acid," characterized by specific X-ray diffraction patterns, melting points, or other analytical parameters distinguishing it from other forms.
- Dependent Claims: Narrowed to specific polymorphs, crystal sizes, or methods of isolating the crystalline material.
2. Method of Preparation Claims
- Cover procedures for producing the crystalline form, including crystallization solvents, temperature profiles, and purity criteria.
- Claims may specify steps to obtain high purity or particular polymorphic forms with defined stability profiles.
3. Pharmaceutical Composition Claims
- Claims directed toward formulations comprising the crystalline form, possibly including other pharmacologically active agents, carriers, or excipients.
- Claims can specify dosage forms, such as tablets, capsules, or injectables, with parameters such as particle size or purity.
4. Therapeutic Use Claims
- Methods of using the crystalline form or compositions in treating specific medical conditions, likely related to the therapeutic areas where the compound has efficacy.
- These claims often employ "purposive" language, claiming the use of the crystalline form for particular indications.
Note: Under Australian patent law, claims are interpreted broadly, covering equivalents and similar forms that fall within the scope of the language used. The specific wording in each claim determines the breadth of exclusivity.
Patent Landscape Overview
The patent landscape surrounding this compound and its crystalline forms in Australia involves multiple layers:
1. Parent and Related Patents
- The compound’s structure resembles known quinoline derivatives, notably related to fingolimod (Gilenya), a Sphingosine-1-phosphate receptor modulator.
- Patent families likely include composition of matter, polymorph, and methods of use patents filed across global jurisdictions.
2. Crystalline Form Patents
- Crystalline forms are a common avenue in pharmaceutical patents, especially where polymorphs exhibit distinct stability, solubility, or bioavailability profiles.
- Several patents globally protect specific polymorphs of this class, such as WO2005044352 (European Patent Application) covering various crystalline forms of similar compounds.
- For Australia, the patent AU2005212405 itself is a critical coverage point for crystalline forms, providing exclusivity over this specific manifestation.
3. Constraints and Challenges
- Patentability of crystalline forms requires demonstration of novelty, inventive step, and utility. Evidence of unexpected technical advantages can strengthen patent scope.
- Australian patent law has a nuanced approach to crystallization inventions; prior art references can potentially challenge novelty if similar crystalline forms are documented.
- Any "obvious" modifications to existing crystalline forms or preparation methods may risk invalidation, especially if the crystallization procedures are routine.
4. Post-Grant and Litigation Records
- To date, there are no publicly available reports of patent validity challenges or litigation concerning AU2005212405, indicating relatively stable patent protection.
- The patent's lifespan, extending until around 2025 (20 years from application), offers market exclusivity for a critical period.
Strategic Implications for Stakeholders
- Pharmaceutical companies aiming to develop similar compounds should evaluate whether their crystalline forms or preparation methods infringe upon this patent, especially if utilizing identical or similar polymorphs.
- Generic manufacturers must assess the scope of this patent; if invalidated or expired, generic versions could enter the Australian market.
- Researchers studying polymorphs or formulations must recognize that such patents can restrict freedom to operate unless they design around or challenge the patent.
Conclusion
Patent AU2005212405 secures intellectual property rights over a specific crystalline form of a quinoline derivative, with claims encompassing its structure, preparation, and therapeutic uses. Its scope provides substantial protection for formulations and methods involving this crystalline form, influencing both clinical development and generic entry strategies within Australia. The patent landscape remains competitive, with multiple patents globally focusing on the same class of compounds and crystalline modifications.
Key Takeaways
- Broad Claims: The patent encompasses the crystalline form, preparation method, and patient use, offering comprehensive coverage.
- Crystalline Form Significance: Such patents are vital for securing market exclusivity, especially when crystalline stability or solubility enhances drug performance.
- Patent Landscape: Complementary patents worldwide cover similar compounds and polymorphs; due diligence is necessary for freedom to operate.
- Market Strategies: Patent holders can leverage the patent for licensing or partnership opportunities; generics should monitor expiry dates.
- Legal Vigilance: The patent's enforceability depends on maintaining novelty and non-obviousness, with potential for challenges based on prior art.
FAQs
1. What is the primary innovation protected by AU2005212405?
It protects a specific crystalline form of a quinoline-based compound, potentially conferring improved stability or bioavailability, alongside methods for preparing and using that form.
2. How does this patent influence generic drug entry in Australia?
Given its scope, it could delay generic entry unless the patent expires, is invalidated, or a design-around method is employed.
3. Are polymorph patents like AU2005212405 common in pharmaceutical IP?
Yes, polymorph patents are a strategic focus in pharma for differentiating formulations and extending patent life.
4. Can competitors develop alternative crystalline forms without infringement?
Potentially, if they invent a crystalline form with distinct properties or prepare it using different processes that do not infringe the claims.
5. What should stakeholders consider regarding the patent landscape?
They should conduct thorough freedom-to-operate assessments, monitor patent expiry dates, and evaluate opportunities for licensing or challenge proceedings.
References
[1] Australian Patent AU2005212405.
[2] WIPO Patent Database. Global patent filings related to quinoline derivatives and polymorphs.
[3] European Patent Application WO2005044352.
[4] Patent law analysis resources on crystalline form patentability.
[5] Market reports on pharmaceutical patent landscapes in Australia.
This analysis aims to inform strategic decision-making, highlighting the patent’s scope, landscape, and implications for stakeholders engaged in drug development and commercialization in Australia.
