Profile for Canada Patent: 2890471

US Patent Family Members and Approved Drugs for Canada Patent: 2890471

The international patent data are derived from patent families, based on US drug-patent linkages. Full freedom-to-operate should be independently confirmed.

US Patent Number	US Expiration Date	US Applicant	US Tradename	Generic Name
	Nov 8, 2033	Bausch And Lomb Inc	XIPERE	triamcinolone acetonide

Canada Drug Patent CA2890471: Scope, Claims, and Landscape Analysis

Last updated: February 19, 2026

This report details the scope, claims, and patent landscape surrounding Canadian patent CA2890471, focusing on its implications for drug development and market exclusivity. The patent, filed by AbbVie Inc., claims novel pharmaceutical compositions and methods of treatment related to the Janus kinase (JAK) inhibitor class.

What is the Core Innovation Claimed by CA2890471?

Patent CA2890471 primarily claims specific crystalline forms of upadacitinib, a selective JAK-1 inhibitor. The patent covers crystalline forms designated as Form A and Form B, and their use in treating inflammatory diseases. The specification details methods for preparing these crystalline forms, pharmaceutical compositions containing them, and their therapeutic applications.

Key Claim Elements

The patent's claims are structured to encompass various aspects of the invention, from the specific chemical entity to its method of use:

• Claim 1: This independent claim defines a crystalline form of a compound, identified as Compound X, which is upadacitinib. It specifies physical characteristics of this crystalline form, including X-ray powder diffraction (XRPD) peaks at particular $2\theta$ angles and characteristic infrared (IR) absorption maxima. This claim establishes the novelty and specific physical form of the active pharmaceutical ingredient (API).
• Claim 2: This claim depends on Claim 1 and specifies a further characteristic of the crystalline form, such as a particular melting point range. This adds a layer of specificity to the claimed crystalline entity.
• Claim 3: This claim refers to a specific crystalline form, Form A, described in the patent's examples. It provides specific XRPD data and IR spectral data for Form A, thereby defining this particular polymorph.
• Claim 4: Similar to Claim 3, this claim defines crystalline Form B, referencing its specific XRPD and IR spectral characteristics as detailed in the examples.
• Claim 5: This claim broadens the scope to include a pharmaceutical composition comprising a crystalline form of Compound X (upadacitinib) as claimed in any one of claims 1-4 and a pharmaceutically acceptable carrier. This covers the formulation aspect of the invention.
• Claim 6: This dependent claim specifies that the pharmaceutical composition of Claim 5 further comprises a pharmaceutically acceptable excipient. This allows for standard formulation components.
• Claim 7: This independent claim defines a method of treating an inflammatory disease by administering a therapeutically effective amount of a crystalline form of Compound X (upadacitinib) as claimed in any one of claims 1-4. This covers the therapeutic application of the claimed crystalline forms.
• Claim 8: This dependent claim specifies the inflammatory disease as rheumatoid arthritis. This focuses the method of treatment on a specific indication.
• Claim 9: This claim defines a further method of treating an inflammatory disease by administering a pharmaceutical composition as claimed in Claim 5 or Claim 6. This links the composition claims to the method of treatment.
• Claim 10: This dependent claim specifies the inflammatory disease as psoriatic arthritis. This adds another specific indication to the method of treatment.

The claims collectively aim to protect the specific crystalline forms of upadacitinib, their preparation, pharmaceutical compositions containing them, and their use in treating specific inflammatory conditions. The emphasis on crystalline forms is critical, as different polymorphs can exhibit distinct physical properties like solubility, stability, and bioavailability, impacting drug performance and patentability.

What is the Status and Term of CA2890471?

Patent CA2890471 was granted by the Canadian Intellectual Property Office (CIPO). As a utility patent, its term is generally 20 years from the filing date, subject to maintenance fees.

• Filing Date: May 15, 2015
• Publication Date: November 19, 2015
• Grant Date: November 3, 2020
• Term Expiry: May 15, 2035 (assuming no extensions or adjustments)

The patent is currently in force. Maintenance fees have been paid, indicating the patent holder's intent to maintain protection for the full statutory term.

What are the Key Technical Specifications and Disclosures within the Patent?

The patent provides detailed technical information on the claimed crystalline forms of upadacitinib. This includes characterization data essential for identifying and differentiating the patented polymorphs.

Crystalline Form Characterization

The patent discloses characterization data for Form A and Form B, primarily through X-ray Powder Diffraction (XRPD) and Infrared (IR) spectroscopy.

• Form A:
  • XRPD: Characteristic peaks are listed, with significant peaks appearing at approximate $2\theta$ values of 5.0, 9.9, 12.2, 15.0, 17.0, 19.8, 21.2, 22.1, 23.0, 24.5, 26.3, 28.0, 29.0, 30.0, 31.6, 32.5, 33.3, 35.8, 36.5, 39.1, 41.2, and 42.6 (± 0.2° $2\theta$).
  • IR Spectroscopy: Characteristic absorption maxima are provided, including peaks around 3315, 2939, 1679, 1610, 1561, 1493, 1392, 1302, 1223, 1165, 1035, 995, 958, 910, 860, 804, 760, 727, 699, 654, 610, 575, 538, 497, 458, and 435 $cm^{-1}$.
• Form B:
  • XRPD: Characteristic peaks are listed, with significant peaks appearing at approximate $2\theta$ values of 6.3, 12.5, 14.5, 17.0, 19.6, 20.9, 22.4, 23.1, 24.5, 25.7, 26.9, 29.4, 30.2, 31.5, 32.5, 35.5, 36.2, 37.5, 38.3, 40.0, 40.9, 41.8, and 44.5 (± 0.2° $2\theta$).
  • IR Spectroscopy: Characteristic absorption maxima are provided, including peaks around 3302, 2940, 1672, 1602, 1552, 1492, 1393, 1307, 1223, 1170, 1034, 996, 955, 911, 860, 806, 760, 728, 700, 654, 609, 575, 539, 497, 457, and 434 $cm^{-1}$.

Preparation Methods

The patent outlines specific procedures for obtaining Form A and Form B. These procedures typically involve crystallization from specific solvent systems under controlled temperature and time conditions. For example, the preparation of Form A involves crystallizing upadacitinib from a mixture of isopropanol and water. The preparation of Form B involves crystallization from a mixture of ethanol and water. These detailed preparation methods are crucial for establishing reproducibility and for potential infringement analysis.

Pharmaceutical Compositions

The patent describes pharmaceutical compositions suitable for oral administration. These compositions include upadacitinib in one of its claimed crystalline forms, along with pharmaceutically acceptable excipients such as diluents, binders, disintegrants, and lubricants. Example formulations are provided, detailing the types and amounts of excipients used, which are standard in the industry for solid dosage forms like tablets.

Therapeutic Indications

The primary therapeutic indications disclosed are inflammatory diseases, with specific examples including rheumatoid arthritis and psoriatic arthritis. The patent suggests that the claimed crystalline forms offer advantages in treating these conditions, likely related to improved efficacy, safety, or pharmacokinetic profiles.

What is the Competitive Landscape for Upadacitinib Patents in Canada?

The patent landscape for upadacitinib in Canada is dominated by AbbVie Inc., the originator. CA2890471 is one of several patents protecting the drug, focusing specifically on crystalline forms and related uses.

Key Patents Protecting Upadacitinib

While CA2890471 protects specific crystalline forms, other patents likely cover the compound itself, other polymorphs, synthesis routes, and additional therapeutic uses. Identifying all relevant patents requires a comprehensive search of CIPO's database and potentially patent family databases. However, CA2890471 is central to the protection of the specific solid-state forms of the API.

• Compound Patent: A foundational patent covering the upadacitinib molecule itself is expected. Such patents typically have earlier filing dates and longer terms.
• Polymorph Patents: CA2890471 is an example of a polymorph patent. Originator companies often file multiple patents covering various crystalline forms (polymorphs, solvates, hydrates) to create a robust intellectual property fortress, extending market exclusivity.
• Formulation Patents: Patents may also cover specific pharmaceutical formulations that enhance drug delivery, stability, or patient compliance.
• Method of Use Patents: Patents claiming the use of upadacitinib for treating specific diseases or patient populations can also be critical, particularly if these uses were discovered after the initial compound patent.

Generic Entry and Patent Challenges

The expiry of foundational patents and the successful challenge of secondary patents are key triggers for generic drug market entry. For upadacitinib in Canada, generic manufacturers will need to navigate the patent landscape, assessing the validity and enforceability of existing patents, particularly CA2890471 and any related polymorph or formulation patents.

• Patent Expiry: As noted, CA2890471 expires in May 2035. This date serves as a critical marker for potential generic competition. However, other patents protecting upadacitinib may expire earlier or later, influencing the overall market exclusivity period.
• Patent Litigation: Generic companies often challenge originator patents through litigation, seeking to invalidate them on grounds such as lack of novelty, obviousness, or insufficient disclosure. Successful challenges can lead to earlier generic entry. Conversely, originator companies may seek to enforce their patents against potential infringers.
• Regulatory Exclusivities: In addition to patent protection, Canada provides regulatory exclusivities. For instance, new drug approvals may benefit from data protection periods, which prevent generic manufacturers from relying on the innovator's clinical trial data for a certain period.

Potential for Biosimilar/Abbreviated New Drug Application (ANDA) Pathways

For small molecule drugs like upadacitinib, the pathway for market entry for generics is through an Abbreviated New Drug Application (ANDA) in Canada. The generic applicant must demonstrate that their product is bioequivalent to the reference drug and that their product does not infringe any valid and subsisting patents. CA2890471, by claiming specific crystalline forms, presents a potential hurdle for generic manufacturers if their proposed API form infringes these claims. Generic manufacturers may seek to develop non-infringing polymorphs or challenge the validity of these claims.

What are the Implications for Market Exclusivity and Generic Competition?

Patent CA2890471 plays a significant role in defining the market exclusivity period for upadacitinib in Canada, particularly concerning the specific crystalline forms claimed.

Protection of Specific API Forms

The claims covering crystalline Form A and Form B directly protect the physical attributes of the upadacitinib API used in marketed products. If the innovator product utilizes these specific forms, generic manufacturers seeking to launch their product will need to ensure their API does not infringe these claims. This could involve:

• Developing a Different Polymorph: A generic manufacturer might develop and characterize a new, non-infringing crystalline form of upadacitinib. This requires significant R&D investment and analytical work to prove the novelty and non-infringing nature of the new form.
• Challenging Patent Validity: A generic manufacturer could attempt to invalidate claims 1-4 of CA2890471. This is a high-risk, high-reward strategy. Success would clear the path for the use of the claimed forms.
• Licensing: In some cases, generic companies may seek to license the patent, although this is less common for secondary patents like polymorph claims.

Impact on Formulation and Therapeutic Use

The composition claims (Claims 5-6) and method of use claims (Claims 7-10) extend the protection to how the API is formulated and administered for specific therapeutic purposes. Generic manufacturers must consider these claims when designing their own product and indication strategy.

• Formulation: If the patented compositions offer specific advantages or are uniquely structured, generic formulations must avoid direct infringement.
• Therapeutic Indications: While generic drugs typically aim to treat the same indications as the reference product, method of use patents can sometimes limit the approved indications for a generic product if the patent remains valid. However, in Canada, the focus for ANDA approval is generally on demonstrating bioequivalence for the same indication as the reference drug.

Strategic Considerations for Stakeholders

• Originator (AbbVie Inc.): The patent provides a strong basis for maintaining market exclusivity for upadacitinib in Canada until at least May 2035. Ongoing monitoring for potential infringement and preparation for any necessary patent enforcement actions are crucial.
• Generic Manufacturers: Strategic planning must include a thorough analysis of CA2890471 and all other relevant upadacitinib patents. This involves assessing the risk of infringement, evaluating the feasibility and cost of developing non-infringing alternatives, and considering the potential for patent challenges. Early engagement with patent counsel is essential.
• Investors and R&D Professionals: Understanding the patent expiry and the strength of secondary patents like CA2890471 is vital for assessing the long-term market potential of upadacitinib and for making informed R&D decisions regarding next-generation JAK inhibitors or alternative therapeutic approaches. The existence of such polymorph patents indicates a strategy to maximize the drug's commercial lifecycle.

The precise enforcement history and any potential litigation surrounding CA2890471 would require a deeper dive into legal databases, but its existence as an active, granted patent in good standing signifies a significant IP asset for AbbVie.

Key Takeaways

• Core Protection: Canadian patent CA2890471 protects specific crystalline forms of upadacitinib (Form A and Form B) and their use in treating inflammatory diseases, notably rheumatoid arthritis and psoriatic arthritis.
• Technical Specificity: The patent provides detailed XRPD and IR spectroscopic data to define the claimed crystalline forms, crucial for infringement analysis and patent validity.
• Term: The patent is set to expire on May 15, 2035, defining a key period of market exclusivity for these specific forms of upadacitinib.
• Competitive Barrier: CA2890471 serves as a significant intellectual property barrier for generic manufacturers, requiring them to either develop non-infringing crystalline forms of upadacitinib or successfully challenge the patent's validity.
• Strategic Asset: This patent is a key component of AbbVie Inc.'s strategy to protect its investment in upadacitinib, extending market exclusivity beyond the initial compound patent term.

Frequently Asked Questions

1. Does CA2890471 cover the upadacitinib molecule itself?

No, CA2890471 specifically claims crystalline forms of upadacitinib, not the molecular structure of upadacitinib per se. Foundational patents typically cover the compound itself.

2. Can a generic manufacturer use a different crystalline form of upadacitinib if CA2890471 is still in force?

A generic manufacturer may be able to use a different crystalline form if that form is demonstrably distinct from the claimed Form A and Form B and does not infringe any other valid claims in CA2890471 or other relevant patents.

3. What is the significance of the XRPD and IR data provided in the patent?

The XRPD and IR data are critical analytical fingerprints used to identify and distinguish the patented crystalline forms from other forms of upadacitinib. They are essential for proving infringement.

4. Are there any potential extensions to the expiry date of CA2890471?

Patent terms in Canada can sometimes be extended through mechanisms like the Patent Term Adjustment (PTA) for delays in processing. However, specific eligibility for such extensions would require detailed review of the patent prosecution history.

5. What is the implication of the method of use claims in CA2890471 for generic drug approval?

The method of use claims, which specify treating inflammatory diseases like rheumatoid arthritis and psoriatic arthritis, reinforce the protected indications. Generic manufacturers must ensure their proposed product and intended use do not infringe these claims, though the primary focus for ANDA approval is bioequivalence to the reference product for its approved indications.

Citations

[1] AbbVie Inc. (2015). Pharmaceutical Compositions and Methods of Treatment. Canadian Patent CA2890471. Filed May 15, 2015. Granted November 3, 2020.