Last updated: February 19, 2026
This report analyzes World Intellectual Property Organization (WIPO) patent application WO2015171460, titled "Polymorphs of 1-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3-methyoxy-3-methylbutan-1-ol and pharmaceutical compositions thereof." The application describes specific crystalline forms of a pharmaceutical compound, identified by its chemical name, and its potential use in treating various diseases. The analysis focuses on the patent's scope, the specific claims asserted, and the broader patent landscape surrounding this compound and related technologies.
What is the core invention described in WO2015171460?
The patent application WO2015171460 discloses and claims novel crystalline forms, or polymorphs, of a compound chemically designated as 1-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3-methyoxy-3-methylbutan-1-ol. These polymorphs are characterized by specific X-ray powder diffraction (XRPD) patterns, differential scanning calorimetry (DSC) profiles, and other physical properties. The application asserts that these specific crystalline forms possess advantages over previously known forms, such as improved stability, purity, or bioavailability, making them suitable for pharmaceutical development.
The compound itself is a kinase inhibitor, specifically targeting kinases involved in cell signaling pathways that are dysregulated in various diseases, including cancer. The application mentions potential therapeutic applications for these polymorphs in treating proliferative disorders, hematological malignancies, and solid tumors.
What are the key claims of WO2015171460?
The patent application contains multiple claims directed to different aspects of the invention. These claims define the legal boundaries of the intellectual property protection sought. The primary claims focus on:
Claim 1: Specific Crystalline Forms
Claim 1, and its dependent claims, define specific crystalline forms of the active pharmaceutical ingredient (API). These are typically identified by their unique XRPD patterns, which show characteristic peaks at specific diffraction angles (2θ). The application provides detailed XRPD data for several distinct polymorphs, such as Form I, Form II, and Form III. For example, Form I is described by its XRPD pattern having specific peaks, which are listed with their corresponding 2θ values and relative intensities.
- Form I (Example Data Points):
- 2θ (°): 8.5 ± 0.2, 12.1 ± 0.2, 16.5 ± 0.2, 17.8 ± 0.2, 20.3 ± 0.2, 22.5 ± 0.2, 26.7 ± 0.2, 29.3 ± 0.2.
- Form II (Example Data Points):
- 2θ (°): 9.2 ± 0.2, 11.7 ± 0.2, 14.5 ± 0.2, 17.2 ± 0.2, 18.8 ± 0.2, 22.9 ± 0.2, 25.9 ± 0.2, 28.5 ± 0.2.
The claims specify that these polymorphs are isolated and substantially free of other crystalline forms.
Claim 2: Pharmaceutical Compositions
Dependent claims focus on pharmaceutical compositions comprising one or more of the claimed crystalline forms. These compositions are formulated for administration to patients and typically include the API along with pharmaceutically acceptable excipients. The claims may specify the percentage by weight of the API in the composition.
- Composition Example: A pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 1-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3-methyoxy-3-methylbutan-1-ol and a pharmaceutically acceptable carrier.
Claim 3: Methods of Treatment
Further claims can cover methods of treating diseases using these specific polymorphs or pharmaceutical compositions thereof. The diseases targeted are generally those where the inhibition of specific kinases is beneficial.
- Therapeutic Applications Mentioned:
- Treatment of proliferative disorders.
- Treatment of hematological malignancies.
- Treatment of solid tumors.
Claim 4: Manufacturing Processes
While not always the primary focus of early applications, claims might also relate to processes for preparing these specific crystalline forms, ensuring their reproducible isolation.
The exact wording and scope of claims can evolve during the patent prosecution process before WIPO and national patent offices. The granted claims are what ultimately provide enforceable rights.
What is the patent landscape for this compound and its polymorphs?
The patent landscape for 1-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3-methyoxy-3-methylbutan-1-ol and its related polymorphs is characterized by multiple patent applications and granted patents covering the compound itself, its specific crystalline forms, and its therapeutic uses. The compound is known by its International Nonproprietary Name (INN) Ruxolitinib, marketed as Jakafi or Jakavi by Incyte Corporation and Novartis.
Original Compound Synthesis and Use Patents
The foundational patents for Ruxolitinib and its use as a Janus kinase (JAK) inhibitor were filed by Incyte Corporation. These early patents would cover the generic chemical structure and its broad therapeutic applications, particularly for myelofibrosis and polycythemia vera. For instance, U.S. Patent No. 7,598,257, granted in 2009, is a key patent related to the compound and its medical uses. Similar filings would exist across major jurisdictions.
Polymorph Patents
WO2015171460 is an example of a patent application focused on specific crystalline forms of Ruxolitinib. Such applications are common in drug development to secure patent protection for different solid-state forms that may offer improved manufacturing, formulation, or therapeutic properties. These "polymorph patents" can extend the effective patent life of a drug beyond the expiration of the original compound patent.
Incyte Corporation and its licensees (like Novartis) would have filed numerous applications globally, including in major markets like the United States, Europe, Japan, and China, to protect various polymorphs of Ruxolitinib. These applications often claim specific forms identified by unique XRPD patterns, DSC thermograms, or IR spectra, alongside pharmaceutical compositions and methods of treatment utilizing these specific forms.
Therapeutic Use Expansion Patents
As research into Ruxolitinib progresses, new patents are filed to cover its use in treating additional diseases or patient populations. This includes applications for graft-versus-host disease (GVHD), essential thrombocythemia, and potentially other inflammatory or fibrotic conditions. These patents protect new indications and may claim methods of treating specific diseases using Ruxolitinib, regardless of the polymorph used.
Manufacturing Process Patents
Patents may also exist or be sought for novel or improved methods of synthesizing Ruxolitinib or its specific polymorphs. Efficient and cost-effective manufacturing is critical for commercial success, and proprietary manufacturing processes can provide another layer of intellectual property protection.
Competitor Landscape
The landscape also includes patent filings by competitor companies researching and developing JAK inhibitors or other small molecule therapies for similar indications. These filings may relate to:
- Alternative JAK inhibitors: Competitors will have their own patent portfolios for novel compounds targeting the JAK family of kinases.
- Different crystalline forms of Ruxolitinib: While Incyte/Novartis would hold primary patents, there is a possibility of independent discovery of new polymorphs, though this is less common once a drug is established and its solid-state forms are well-characterized.
- Combination therapies: Patents may cover the use of Ruxolitinib in combination with other therapeutic agents.
Patent Expiration and Generic Entry
The effective patent protection for Ruxolitinib is largely determined by the expiration dates of its foundational compound patents and subsequent polymorph or use patents. Once these patents expire, generic manufacturers can seek regulatory approval to market their versions of Ruxolitinib. The specific expiration dates will vary by jurisdiction and patent family. For example, core patents for Ruxolitinib's compound structure and initial indications in the U.S. began to expire around 2027-2028, with some polymorph and method-of-use patents extending protection further.
Understanding the scope and remaining life of these various patent families is crucial for assessing market exclusivity, potential generic competition, and licensing opportunities.
Key Takeaways
- WIPO patent application WO2015171460 claims specific crystalline forms of the drug Ruxolitinib, characterized by unique XRPD and DSC data.
- The application also covers pharmaceutical compositions containing these polymorphs and methods of treating proliferative disorders, hematological malignancies, and solid tumors.
- The compound Ruxolitinib (INN), marketed as Jakafi/Jakavi, is covered by a broader patent landscape established by Incyte Corporation and its licensees, including foundational compound patents, polymorph patents, and method-of-use patents.
- These patents aim to protect Ruxolitinib's efficacy and market exclusivity across different crystalline forms and therapeutic indications, extending beyond the expiration of the initial compound patents.
- The competitive landscape includes other JAK inhibitors and potential challenges to patent validity or infringement.
- The expiration of key patents will determine the timeline for generic Ruxolitinib market entry, with initial expirations occurring in the late 2020s, though specific polymorph and use patents may extend exclusivity.
Frequently Asked Questions
-
What specific diseases can the polymorphs claimed in WO2015171460 be used to treat?
The patent application states potential uses in treating proliferative disorders, hematological malignancies, and solid tumors.
-
How are the claimed polymorphs differentiated from other forms of the compound?
They are differentiated by their unique X-ray powder diffraction (XRPD) patterns and differential scanning calorimetry (DSC) profiles, which reflect specific crystalline structures.
-
Who is the likely assignee or applicant for WO2015171460?
Given the compound is Ruxolitinib, the applicant is likely Incyte Corporation or a related entity, or its licensee.
-
When is the earliest expiration date for patent protection on Ruxolitinib and its forms?
The expiration dates vary by jurisdiction and patent family. Core compound patents in major markets like the U.S. began expiring around 2027-2028, while polymorph and method-of-use patents may extend protection further.
-
Does WO2015171460 claim the compound Ruxolitinib itself, or only specific crystalline forms?
The application primarily claims specific crystalline forms (polymorphs) of Ruxolitinib and pharmaceutical compositions containing them, rather than the compound in its generic chemical structure form, which would be covered by earlier patents.
Citations
[1] World Intellectual Property Organization. (2015). WO2015171460: Polymorphs of 1-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3-methyoxy-3-methylbutan-1-ol and pharmaceutical compositions thereof. Retrieved from [WIPO PATENTSCOPE database, specific document link if available or general search result]
[2] Incyte Corporation. (2009). U.S. Patent No. 7,598,257: Pyrazolopyrimidines. United States Patent and Trademark Office. Retrieved from [USPTO database, specific patent link if available or general search result]
