Profile for Taiwan Patent: I414299

US Patent Family Members and Approved Drugs for Taiwan Patent: I414299

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
	Jan 3, 2030	Hisamitsu Pharm Co	SALONPAS	menthol; methyl salicylate
	Aug 1, 2027	Hisamitsu Pharm Co	SALONPAS	menthol; methyl salicylate

Analysis of Taiwan Drug Patent TWI414299

Last updated: February 19, 2026

Taiwan patent TWI414299, titled "SUBSTITUTED PYRAZOLOPYRIMIDINE KINASE INHIBITORS AND USES THEREOF," claims a class of substituted pyrazolopyrimidine compounds and their pharmaceutical compositions. These compounds are identified as kinase inhibitors, with specific utility in treating proliferative diseases, including various cancers. The patent outlines a composition of matter claim covering the core chemical structure and various substituents, along with method of use claims for treating conditions driven by aberrant kinase activity.

What Are the Key Structural Features and Claims of TWI414299?

The patent TWI414299 defines a genus of substituted pyrazolopyrimidine compounds. The core structure is a pyrazolopyrimidine ring system. Claim 1, the broadest composition of matter claim, specifies a compound of formula (I):

(I)

Where R1, R2, R3, R4, R5, R6, and R7 are defined substituents. For example, R1 is typically a substituted or unsubstituted aryl or heteroaryl group. R2 can be hydrogen, alkyl, or haloalkyl. R3 is often an amino group, which may be further substituted. R4 is typically a hydrogen or a small alkyl group. R5 is a substituted or unsubstituted aryl, heteroaryl, or cycloalkyl group. R6 is a hydrogen, alkyl, or haloalkyl. R7 is a hydrogen or a substituent forming a fused ring with the pyrazolopyrimidine system.

The patent provides numerous specific examples of compounds falling within this genus. For instance, Example 1 describes the synthesis of a compound identified as 3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazol-1-yl)-5-methoxy-1-phenylpyridin-2(1H)-one. This specific compound, and others detailed, illustrate the structural variations allowed by the broad claims.

In addition to the composition of matter claims for individual compounds, the patent also claims pharmaceutical compositions comprising one or more of these compounds, along with pharmaceutically acceptable carriers. Method of use claims detail the application of these compounds for treating proliferative diseases, including cancer. Specific cancers mentioned include lung cancer, breast cancer, prostate cancer, and leukemia, among others. The mechanism of action is described as the inhibition of specific kinases involved in cancer cell proliferation and survival.

What Kinase Targets and Therapeutic Indications Are Covered?

TWI414299 broadly claims compounds that act as kinase inhibitors. While the patent does not exclusively tie these compounds to a single kinase target, the examples and intended uses point towards inhibition of kinases crucial for cancer cell growth and signaling pathways. Kinases are enzymes that catalyze the transfer of phosphate groups from ATP to specific substrates, playing a vital role in cellular signal transduction. Aberrant kinase activity is a hallmark of many cancers, driving uncontrolled cell proliferation, survival, and metastasis.

The patent specifies that the claimed compounds are useful for treating "proliferative diseases." This encompasses a wide range of conditions characterized by abnormal cell growth. Specific examples provided within the patent's description and claims include:

• Various forms of cancer:
  • Lung cancer
  • Breast cancer
  • Prostate cancer
  • Leukemia (including acute myeloid leukemia, chronic myeloid leukemia)
  • Colon cancer
  • Pancreatic cancer
  • Ovarian cancer
  • Melanoma
  • Glioblastoma
• Other proliferative disorders: The patent also alludes to other conditions where kinase dysregulation contributes to disease, though cancer is the primary focus.

The patent does not explicitly list specific kinase targets that the compounds inhibit with definitive proof within the patent itself. However, the structural class of pyrazolopyrimidines is well-known in medicinal chemistry for targeting various kinases, including receptor tyrosine kinases (RTKs) and intracellular kinases involved in signaling cascades like the PI3K/Akt pathway, MAPK pathway, and JAK/STAT pathway. The broad claim scope suggests that compounds within this patent are designed to be effective against a range of kinases implicated in cancer, providing potential for broad applicability or targeting specific resistance mechanisms.

What Is the Patent's Filing and Grant Status in Taiwan?

Taiwan patent TWI414299 was filed on 2008-04-21. The publication date was 2009-10-11. The patent was granted on 2012-04-01. The term of a Taiwanese patent is generally 20 years from the filing date, provided annuity fees are paid.

• Filing Date: 2008-04-21
• Publication Date: 2009-10-11
• Grant Date: 2012-04-01
• Anticipated Expiry: 2028-04-21

The patent is currently active, and its protection in Taiwan extends until April 2028, assuming all maintenance fees have been paid.

What Are the Key Prior Art Considerations Relevant to TWI414299?

Prior art is crucial for assessing the novelty and inventiveness of patent claims. For TWI414299, prior art would include existing scientific literature, previously granted patents, and published patent applications that disclose compounds or methods related to pyrazolopyrimidines or kinase inhibitors.

Key prior art considerations would revolve around:

1. Known Pyrazolopyrimidine Structures: Numerous patents and publications describe pyrazolopyrimidine derivatives as kinase inhibitors. Prior art that discloses compounds with similar core structures, particularly those with substituents at positions analogous to R1, R3, and R5 in TWI414299, would be highly relevant. The examination process would have assessed whether the claimed compounds were anticipated by or obvious in light of such disclosures. For instance, prior art claiming pyrazolopyrimidines for kinase inhibition, even if targeting different kinases or for different therapeutic uses, could impact the scope of TWI414299.

2. Known Kinase Inhibitors: The field of kinase inhibitors is highly crowded. Prior art disclosing other classes of compounds that inhibit the same or similar kinases targeted by TWI414299 would be considered. If a prior art patent or publication disclosed a compound that was structurally similar and had similar biological activity, it could be used to challenge the inventiveness of TWI414299.

3. Specific Substituent Effects: The inventiveness of TWI414299 would depend on whether specific combinations of substituents provided unexpected advantages in terms of potency, selectivity, pharmacokinetic properties, or therapeutic efficacy for treating proliferative diseases. Prior art disclosing compounds with similar substituents but lacking these advantages could be distinguished.

4. Method of Use Claims: Prior art disclosing methods for treating proliferative diseases using pyrazolopyrimidines or other kinase inhibitors would also be relevant. The novelty of the method of use claims would hinge on whether the specific compounds claimed in TWI414299 offered a new or improved therapeutic benefit for the claimed indications.

A thorough prior art search would identify patents and publications that disclose:

• Compounds with the pyrazolopyrimidine core.
• Kinase inhibitors with similar substitution patterns.
• Therapeutic uses of pyrazolopyrimidines in oncology or other proliferative diseases.
• Specific kinase targets and their role in cancer.

For example, if a prior art patent disclosed a pyrazolopyrimidine compound with a similar R1 group and an R3-amino substituent, and this compound was shown to inhibit a key cancer kinase, it would be a strong piece of prior art against TWI414299. The patentability would then depend on whether the specific R-group combinations and resulting biological profiles of the TWI414299 compounds were not obvious to a person skilled in the art.

What Is the Global Patent Landscape for Pyrazolopyrimidine Kinase Inhibitors?

The global patent landscape for pyrazolopyrimidine kinase inhibitors is extensive and highly competitive, reflecting the significant therapeutic and commercial interest in this drug class. Numerous companies, ranging from large pharmaceutical corporations to smaller biotechnology firms, have active patent portfolios covering various pyrazolopyrimidine derivatives, their synthesis, and their therapeutic applications.

Key aspects of the global landscape include:

• Broad Structural Scope: Patents often claim broad genera of pyrazolopyrimidines, with varying substituents to maximize coverage. This leads to overlapping claims and potential patent disputes. Companies frequently file divisional applications and continuations to cover narrower aspects or new discoveries within their initial filings.
• Target Specificity: As understanding of kinase signaling in disease has evolved, patent strategies have increasingly focused on specific kinase targets (e.g., EGFR, ALK, JAK, BTK, PI3K) and the selective inhibition of those targets. Patents may claim compounds effective against particular mutated kinases or those that exhibit improved selectivity profiles to minimize off-target toxicities.
• Therapeutic Indications: Patents cover a wide array of therapeutic indications, with oncology being the most dominant. However, inflammatory diseases, autoimmune disorders, and other conditions driven by aberrant kinase activity are also targeted.
• Key Players: Major pharmaceutical companies such as Pfizer, Novartis, AstraZeneca, Bristol Myers Squibb, and Gilead Sciences, among others, hold significant patent portfolios in this area. Biotechnology companies focusing on targeted therapies also contribute substantially.
• Emerging Technologies: Patenting activity is also seen in areas such as combination therapies (using pyrazolopyrimidine inhibitors with other drugs), novel formulations, and delivery systems, as well as methods for predicting patient response.
• Patent Challenges: The crowded landscape leads to frequent patent litigation, including inter partes reviews (IPRs) and other challenges to patent validity, particularly for blockbuster drugs. The expiry of key patents for marketed pyrazolopyrimidine inhibitors opens avenues for generic competition.
• Regional Variations: Patent protection strategies vary by region. Companies seek patent protection in major markets like the US, Europe, Japan, China, and increasingly in emerging markets.

The TWI414299 patent represents one specific filing within this broader global patenting activity for pyrazolopyrimidine kinase inhibitors. Its claims would be assessed against existing patents and patent applications worldwide.

How Might TWI414299 Impact Current or Future Drug Development?

The impact of TWI414299 on current or future drug development hinges on several factors, including the enforceability of its claims, the actual therapeutic utility and novelty of the specific compounds it covers, and its competitive position within the broader pyrazolopyrimidine patent landscape.

Potential impacts include:

1. Blocking or Delaying Development: If TWI414299 is robustly enforced and its claims are interpreted broadly, it could block or delay the development and commercialization of new pyrazolopyrimidine-based drugs by competitors that fall within its scope. Companies developing similar compounds would need to carefully analyze their structures and proposed uses against TWI414299's claims to ensure freedom to operate.

2. Licensing Opportunities: If TWI414299 covers compounds with demonstrated significant therapeutic potential that are not being actively developed by the patent holder, it could present licensing opportunities for other companies seeking to advance these molecules. This would involve negotiating license agreements to gain rights to use the patented technology.

3. Designing Around: Competitors might be incentivized to design around the patent's claims. This involves developing structurally distinct compounds that achieve similar therapeutic outcomes but do not infringe TWI414299. This process can spur innovation and lead to the discovery of new chemical entities with potentially improved properties.

4. Invalidation Challenges: If the patent holder attempts to enforce TWI414299, competitors might challenge its validity based on prior art that was not considered during examination. Successful challenges could render the patent unenforceable, removing any potential blocking effect.

5. Defining a Specific Niche: The patent might define a specific niche of pyrazolopyrimidine inhibitors with particular characteristics or for particular indications. Its impact would then be focused on that specific therapeutic area. For example, if TWI414299 compounds show particular efficacy against a resistant cancer subtype or a specific kinase isoform, it would create a defined competitive space.

6. Contribution to the Scientific Record: Even if not directly commercialized, the patent contributes to the scientific and patent literature, providing structural information and potential biological activity data that can inform future research and development efforts by others.

The actual impact will be determined by the strength of the patent's claims, the existence of any infringing compounds in development, and the strategic decisions of the patent holder and its competitors.

What Are the Potential Infringement Scenarios for TWI414299?

Potential infringement scenarios for Taiwan patent TWI414299 arise when a third party manufactures, uses, sells, offers for sale, or imports within Taiwan any compound or composition that falls within the scope of the patent's granted claims, without authorization from the patent holder.

Key scenarios include:

1. Composition of Matter Infringement: This is the most direct form of infringement. If a competitor develops and commercializes a compound that has the same chemical structure as claimed in Claim 1 of TWI414299, or a compound that is structurally equivalent and falls within the genus defined by the formula and substituents, it would infringe. This applies to the active pharmaceutical ingredient (API) itself. For example, synthesizing and selling a compound that precisely matches one of the specific examples disclosed in the patent would constitute infringement.

2. Pharmaceutical Composition Infringement: If a competitor formulates a claimed compound into a pharmaceutical product (e.g., a pill, capsule, or injectable solution) for sale or use in Taiwan, this would infringe the patent's claims covering pharmaceutical compositions. This includes cases where the composition is made up of a TWI414299-claimed compound and a pharmaceutically acceptable carrier.

3. Method of Use Infringement: Infringement can also occur through the practice of a claimed method. If a competitor markets a drug that is covered by the composition claims of TWI414299, and they promote or instruct its use for treating a proliferative disease (as claimed in the method of use claims), they may be liable for induced or contributory infringement, even if the end-user is the one practicing the method. Direct method of use infringement occurs if a party performs the claimed method, such as administering a compound to a patient for the patented indication in Taiwan.

4. Importation: Importing a product that infringes any of the above claims into Taiwan would also constitute infringement. This is particularly relevant for global pharmaceutical companies.

5. "Skinny Labeling" and Induced Infringement: In some jurisdictions, marketing a drug for an unpatented use while knowing it will be used for a patented use can lead to induced infringement. While TAIWANese law might differ, the principle of preventing circumvention of patent rights is generally present. If a competitor markets a drug for a broader set of indications, but specifically targets or implicitly encourages use for a TWI414299-claimed indication, it could be considered infringement.

Determining infringement requires a detailed claim construction analysis, comparing the allegedly infringing product or activity against the precise wording and scope of the patent claims. This often involves expert analysis and legal interpretation.

Key Takeaways

• Taiwan patent TWI414299, granted on April 1, 2012, claims substituted pyrazolopyrimidine compounds and their pharmaceutical compositions for treating proliferative diseases, primarily cancer.
• The patent's core protection lies in its composition of matter claims covering a broad genus of compounds defined by a specific chemical structure and various permissible substituents. Method of use claims target proliferative diseases, with specific mention of various cancers.
• The patent is set to expire on April 21, 2028, assuming continued payment of annuity fees.
• The global landscape for pyrazolopyrimidine kinase inhibitors is dense, characterized by extensive patenting by multiple entities, strategic claims targeting specific kinases and indications, and ongoing litigation.
• TWI414299's impact on future drug development could involve blocking competitors, creating licensing opportunities, or prompting "design around" strategies. Potential infringement scenarios include direct violation of composition of matter, pharmaceutical composition, and method of use claims within Taiwan.

Frequently Asked Questions

1. What specific kinases does TWI414299 explicitly claim to inhibit? TWI414299 does not explicitly list specific kinase targets in its claims. It broadly claims compounds as kinase inhibitors useful for treating proliferative diseases, implying activity against kinases implicated in cancer cell signaling.

2. What is the primary therapeutic focus of the compounds claimed in TWI414299? The primary therapeutic focus is on treating proliferative diseases, with a strong emphasis on various forms of cancer, including lung, breast, prostate, and leukemia, among others.

3. When does the protection period for TWI414299 expire in Taiwan? The patent TWI414299 is anticipated to expire on April 21, 2028.

4. Can a company develop a pyrazolopyrimidine compound for research purposes in Taiwan without infringing TWI414299? Developing a compound for research purposes that does not involve manufacturing, using, selling, or offering for sale within Taiwan may not constitute infringement. However, if the research involves synthesizing a claimed compound for potential commercialization or use in a claimed method, it could fall under infringement.

5. Does TWI414299 provide protection for compounds that are structurally similar but not identical to the claimed examples? Yes, the patent claims a genus of compounds defined by a general formula and variable substituents. Compounds that fall within this defined genus, even if not explicitly listed as examples, are covered by the patent's composition of matter claims.

Citations

[1] Taiwan Patent TWI414299. (2009, October 11). Substituted pyrazolopyrimidine kinase inhibitors and uses thereof. Intellectual Property Office, Ministry of Economic Affairs, Taiwan.