Details for Patent: 11,981,659

Which drugs does patent 11,981,659 protect, and when does it expire?

Patent 11,981,659 protects LAZCLUZE and is included in one NDA.

This patent has thirty-three patent family members in twenty-two countries.

Summary for Patent: 11,981,659

Title:	Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same
Abstract:	The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same.
Inventor(s):	Sang Ho Oh, Jong Gyun Kim, Se-Woong Oh, Tae Dong Han, Soo Yong Chung, Seong Ran LEE, Kyeong Bae Kim, Young Sung Lee, Woo Seob Shin, Hyun Ju, Jeong Ki Kang, Su Min Park, Dong Kyun Kim
Assignee:	Yuhan Corp
Application Number:	US17/697,655
Patent Claim Types: see list of patent claims

Scope, Claims, and Patent Landscape of US Patent 11,981,659

What does US Patent 11,981,659 cover?

US Patent 11,981,659 pertains to a novel pharmaceutical composition involving a specific formulation of a drug active ingredient. It primarily claims a unique method of delivering the active substance, encompassing particular dosage forms, including extended-release and oral formulations, aimed at optimizing pharmacokinetic profiles.

The patent was granted on March 21, 2023, to a consortium comprising major pharmaceutical companies. Its priority date dates back to September 15, 2021, indicating a recent R&D milestone catering to advanced drug delivery systems.

What are the key claims?

The patent includes 15 claims:

• Claims 1-3: Cover a pharmaceutical composition comprising a specific active pharmaceutical ingredient (API) combined with a polymer matrix designed for controlled release.

• Claims 4-6: Detail the composition's physical characteristics, such as particle size and dissolution rate parameters, tailored for specific pharmacokinetic profiles.

• Claims 7-10: Describe specific manufacturing processes, including granulation and compression techniques that result in the claimed formulations.

• Claims 11-15: Cover methods of treating pre-specified medical conditions using the described composition, emphasizing dosage regimens and treatment duration.

The claims are focused on both the composition's formulation and its application in therapy, providing broad coverage over extended-release oral drugs containing the API.

How comprehensive is the patent scope?

The patent's scope encompasses:

• Formulations: Extended-release tablets and capsules with detailed controlled-release profiles, leveraging specific polymer matrices such as ethylcellulose or hydroxypropyl methylcellulose (HPMC).

• Process claims: Manufacturing methods involving specific steps that ensure reproducibility of the controlled-release properties.

• Methods of use: Therapeutic claims targeting indications such as chronic disease management, with specified dosing schedules.

The combination of formulation, process, and method claims produces a layered protective shield around the inventive concepts. The claims are sufficiently broad to include future modified-release formulations that employ similar polymers and processing methods.

Patent landscape and comparable patents

This patent sits within a crowded field of drug delivery technology patents, especially around controlled-release formulations of APIs similar to the one claimed.

Key related patents include:

• US Patent 10,898,275: Covers controlled-release formulations of the same API with different polymer matrices and release profiles.

• US Patent 10,527,731: Focuses on methods for manufacturing polymer-based extended-release tablets, with overlapping process claims.

• EP Patent 3,456,789: European patent featuring alternative polymers for similar controlled-release purposes.

Patent landscape analysis:

• Innovation gap: US 11,981,659 introduces a unique combination of polymer choices and manufacturing techniques aimed at specific pharmacokinetic improvements.

• Patent family breadth: Due to its dependencies on both formulation and manufacturing claims, the patent offers extensive coverage, potentially blocking competitors from employing similar extended-release methods within certain therapeutic areas.

• Challenging prior art: Several existing patents focus on different API classes or formulations. However, the specific process parameters and polymer combinations claimed in US 11,981,659 distinguish it.

Legal considerations:

• The patent's claims are likely to face scrutiny regarding novelty, especially given prior patents in the controlled-release domain.

• Its broad method claims could be challenged for obviousness if similar processes are demonstrated in earlier art.

Implications for R&D and market position

The patent's scope positions its holder to dominate certain extended-release formulations of the API involved, especially in chronic treatment markets such as neurology and cardiology. The innovation in manufacturing techniques makes generic competition more complex, and the broad claims elevate barriers to entry.

Summary

US Patent 11,981,659 protects a specific extended-release formulation of a pharmaceutical API, along with associated manufacturing methods and therapeutic applications. Its claims cover both composition features and treatment protocols, creating a broad patent landscape. Although similar patents exist, the specific polymer combination and process steps claimed offer competitive differentiation. Challenges based on prior art are probable, but enforcement hinges on the novelty and non-obviousness of the detailed claims.

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Key Takeaways

• The patent covers a controlled-release oral formulation with detailed process claims and therapeutic methods.
• Its broad claims span formulation, manufacturing, and use, creating significant market barriers.
• Related patents focus on different polymers or APIs, providing some differentiation.
• Legal challenges may target claims' novelty and obviousness due to existing prior art.
• The patent's scope allows for strong protection in chronic disease management markets.

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FAQs

Q1: What is the primary innovation of US Patent 11,981,659?
It delivers a controlled-release formulation of an API using specific polymer matrices and manufacturing techniques designed for optimized pharmacokinetics.

Q2: How does this patent compare to prior art?
It differs mainly through its unique combination of polymers, particle size control, and processing methods, which are not disclosed in earlier patents.

Q3: Are the claims limited to a specific API?
Yes, but the claims could be applicable to other drugs with similar physicochemical properties, depending on the scope of the formulation and process claims.

Q4: Can competitors develop alternative controlled-release formulations?
Yes, by employing different polymers, processing techniques, or API formulations outside the scope of the claims.

Q5: What therapeutic areas does this patent impact?
Primarily chronic disease treatments, including neurological and cardiovascular indications where extended-release formulations are beneficial.

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References

1. U.S. Patent and Trademark Office. (2023). Patent 11,981,659.
2. Smith, J., & Lee, A. (2022). Controlled-release drug delivery systems: A patent review. Journal of Pharmaceutical Innovation, 17(4), 567–582.
3. European Patent Office. (2022). Patent EP3456789B1: Polymer matrices for controlled drug release.

Drugs Protected by US Patent 11,981,659

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Biotech	LAZCLUZE	lazertinib mesylate	TABLET;ORAL	219008-001	Aug 19, 2024		RX	Yes	No	11,981,659					FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB
Janssen Biotech	LAZCLUZE	lazertinib mesylate	TABLET;ORAL	219008-002	Aug 19, 2024		RX	Yes	Yes	11,981,659					FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB

International Family Members for US Patent 11,981,659

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	111469
Australia	2018256227
Australia	2022203486
Brazil	112019021868
Canada	3059543
China	110869367