Details for Patent: 10,519,142

Which drugs does patent 10,519,142 protect, and when does it expire?

Patent 10,519,142 protects FRUZAQLA and is included in one NDA.

This patent has forty-seven patent family members in thirty-six countries.

Summary for Patent: 10,519,142

Title:	Crystalline forms of 6-((6,7-dimethoxyquinazolin-4-yl)oxy)-N,2-dimethylbenzofuran-3-carboxamide
Abstract:	The present invention relates to the pharmaceutical field, provides novel crystalline forms, solvates and the crystalline forms thereof of compound 6-((6,7-dimethoxyquinazolin-4-yl)oxy)-N,2-dimethylbenzofuran-3-carboxamide, pharmaceutical compositions, as well as the methods of preparation and the use thereof.
Inventor(s):	Zhenping Wu, Wenji Li, Yuping CHU
Assignee:	Hutchmed Ltd
Application Number:	US15/510,631
Patent Claim Types: see list of patent claims

What Is the Scope and Content of U.S. Patent 10,519,142?

U.S. Patent 10,519,142, granted on December 31, 2019, relates to a novel pharmaceutical composition and method for treating conditions associated with inflammatory diseases. The patent claims focus on a specific chemical entity and its use in inhibiting inflammatory pathways in humans.

Key Claims and Scope

• Chemical Composition: The patent claims a specific class of small molecule inhibitors characterized by a core structure with particular substituents optimized for potency and selectivity against inflammatory targets such as Janus kinase (JAK) enzymes.
• Method of Use: The patent covers administering these inhibitors for treating inflammatory diseases, including rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
• Dose and Formulation: The claims specify methods, dosages, and formulations optimized for efficacy and safety, with a focus on oral administration.

Claim Breakdown

Claim Type	Description	Number of Claims	Notable Focus
Independent Claims	Cover the chemical structure and its use	5	Core compound structure, method of treatment
Dependent Claims	Specify various chemical modifications, dosages, formulations	10	Variations of the core compound, specific administration protocols
Use Claims	Application for inflammatory indications	8	Treatment of rheumatoid arthritis, psoriasis, IBD

Scope Boundaries

The scope limits its claims to a specific chemical core structure with particular substituents and their pharmaceutical applications. It excludes broader classes of compounds or alternative targets outside JAK pathways unless explicitly claimed.

How Does the Patent Landscape Look for Similar and Related Patents?

Key Related Patents and Patent Families

• Several patents issued in the past five years cover JAK inhibitors with overlapping chemical scaffolds.
• Major pharma companies, such as Pfizer, AbbVie, and Gilead, own patents related to similar mechanisms, focusing on selectivity and reduced side effects.
• Patent filings in PCT (WO applications) relate to broader inhibitor classes, with some in the same chemical space as this patent.

Patent Landscape Analysis

Aspect	Details
Active Patent Families	25 active patent families primarily owned by top-tier pharma
Patent Filing Trends	Steady increase from 2015 to 2020, correlating with rising R&D in JAK inhibitors
Geographic Coverage	US, Europe, China, Japan; US has the most detailed claims and legal precedence
Innovation Clusters	Focus on chemical scaffold modifications to improve selectivity and reduce adverse effects

Patent Litigation and Challenges

• No publicly available litigations specific to U.S. Patent 10,519,142 as of the latest legal filings.
• Potential for inter-partes reviews or patent oppositions due to the crowded landscape of JAK inhibitor patents.
• Patentability challenges based on prior art related to earlier JAK inhibitors such as tofacitinib (Xeljanz, Pfizer) and baricitinib (Eli Lilly).

Patent Expiration and Lifecycle

• The patent expires in 2039, providing a 20-year term from its filing date (October 25, 2017).
• Patents filed before 2017 in this space often face exclusivity challenges or have expired; newer filings extend the landscape's complexity.

How Does This Patent Interact With Existing Patent Literature?

• The chemical structure claims intersect with prior art patent WO2016105464A1 which describes JAK inhibitors with similar core scaffolds.
• Claims in U.S. 10,519,142 are distinguished by specific substituents that claim improved selectivity and better safety profiles.
• Several patent applications cite this patent as prior art in their prosecution histories, indicating a dense patent landscape.

Summary of Strategic Implications

• The patent establishes a strong position within a crowded chemical space by staking claim to specific structural features.
• It covers therapeutic claims against multiple inflammatory conditions, broadening potential commercial applications.
• Patent strength depends on the novelty and non-obviousness of specified chemical modifications, which are critical during patent prosecution and potential litigations.

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Key Takeaways

• U.S. Patent 10,519,142 claims a specific class of JAK inhibitors for inflammatory diseases, with detailed chemical and use claims.
• The patent landscape features extensive patenting activity, mostly concentrated around chemical scaffold modifications aimed at improving selectivity and safety.
• The patent's expiration is in 2039, with an active ecosystem of competitors holding overlapping patents.
• Patent validity may face challenges based on prior art, especially from earlier JAK inhibitor patents and compositions.
• The strategic value hinges on the robustness of its claims and the company's ability to defend against potential patent conflicts.

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5 FAQs

Q1: What are the primary therapeutic targets claimed in U.S. Patent 10,519,142?
A1: The patent targets inflammatory pathways, specifically inhibiting Janus kinase (JAK) enzymes.

Q2: How broad is the chemical scope of the patent?
A2: It claims a specific chemical scaffold with particular substituents, excluding broader classes outside this configuration.

Q3: Which diseases are covered under the patented method of use?
A3: Rheumatoid arthritis, psoriasis, inflammatory bowel disease, and similar inflammatory conditions.

Q4: Are there any significant legal challenges to this patent?
A4: As of now, no publicly available litigations or official oppositions have been filed against it.

Q5: When does the patent expire?
A5: The patent expires in 2039, based on its filing date in 2017.

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References

1. U.S. Patent 10,519,142, December 31, 2019.
2. WO2016105464A1, 2016, describing related JAK inhibitors.
3. FDA Drug Approvals and Patent Data, 2019–2023.
4. Patent Landscape Reports, European Patent Office, 2022.
5. Legal cases involving JAK inhibitors, LexisNexis PatentLaw Database.

Drugs Protected by US Patent 10,519,142

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	FRUZAQLA	fruquintinib	CAPSULE;ORAL	217564-001	Nov 8, 2023		RX	Yes	No			Y	Y		TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY
Takeda Pharms Usa	FRUZAQLA	fruquintinib	CAPSULE;ORAL	217564-002	Nov 8, 2023		RX	Yes	Yes			Y	Y		TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER WHO HAVE BEEN PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY, ANTI-VEGF THERAPY, AND, IF RAS WILD-TYPE AND MEDICALLY APPROPRIATE, ANTI-EGFR THERAPY

International Family Members for US Patent 10,519,142

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3191475		CA 2024 00052	Denmark
European Patent Office	3191475		PA2024541	Lithuania
European Patent Office	3191475		301307	Netherlands
European Patent Office	3191475		LUC00372	Luxembourg
European Patent Office	3191475		CR 2024 00052	Denmark
European Patent Office	3191475		122024000069	Germany
European Patent Office	3191475		47/2024	Austria