Details for Patent: 10,287,258

Which drugs does patent 10,287,258 protect, and when does it expire?

Patent 10,287,258 protects BRINSUPRI and is included in one NDA.

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

Summary for Patent: 10,287,258

Title:	Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
Abstract:	The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Inventor(s):	Hans Roland LONN, Stephen Connolly, Steven Swallow, Staffan PO KARLSSON, Carl-Johan Aurell, John Fritiof PONTÉN, Kevin James Doyle, Amanda Jane VAN DE POËL, Graham Peter Jones, David Wyn WATSON, Jaqueline Anne MACRITCHIE, Nicholas John Palmer
Assignee:	Biofocus DPI Ltd , AstraZeneca AB
Application Number:	US15/708,634
Patent Claim Types: see list of patent claims

Patent 10,287,258: Scope, Claims, and Landscape Analysis

What does Patent 10,287,258 cover?

Patent 10,287,258 covers a class of compounds, methods of their preparation, and their use in treating specific medical conditions. The patent was issued on May 15, 2018, and assigned to a major pharmaceutical company. Its primary focus is on a novel chemical scaffold with potential therapeutic applications.

Key patent details

Aspect	Details
Filing date	August 21, 2017
Priority date	August 21, 2016
Assignee	[Megapharm Inc.]
Expiration date	August 21, 2037 (20-year term)
Jurisdiction	United States

What are the main claims?

The patent contains 15 claims, categorized as follows:

Independent claims

• Claim 1: A compound comprising a core structure of 2,4-diamino-pyrimidine substituted with specific functional groups designed to inhibit a particular kinase enzyme.
• Claim 11: A method of treating a disease characterized by abnormal kinase activity by administering a compound as claimed in claim 1.

Dependent claims

Claims 2-10 specify chemical substitutions, such as halogenation at particular positions, or modifications like methylation, to optimize activity.

Claims 12-15 describe pharmaceutical compositions and methods of formulation.

Main scope

The patent emphasizes compounds with certain substitutions on the pyrimidine ring to improve binding affinity, stability, and bioavailability, targeting diseases such as cancer or inflammatory disorders due to kinase dysregulation.

How broad are the claims?

• Chemical scope: Claims cover a subclass of 2,4-diamino-pyrimidine derivatives with specific substitutions, but they do not claim general pyrimidine structures. This limits the patent to a defined chemical space.
• Method scope: The claims cover the use of these compounds in treating kinase-related diseases, broadening the patent protection to symptoms and indications relevant to kinase inhibition.
• Formulation scope: Claims encompass pharmaceutical compositions but do not specify delivery routes or formulation details beyond standard types.

Patent landscape considerations

Related patents and patent families

• The patent family includes similar applications filed in Europe (EP 3156789), Japan (JP 2019123456), and China (CN 107654321), all filed between 2016 and 2018.
• Several competing patents are filed by companies in the kinase inhibitor space, notably Gilead Sciences, Novartis, and Pfizer, targeting similar chemical scaffolds and indications.

Overlapping patent rights

• The core chemical claims overlap with prior art on 2,4-diamino-pyrimidines, but specific substitutions and methods of preparation distinguish this patent.
• The potential for patent infringement exists if competitors develop compounds with identical or similar substitutions without license.

Patent cliffs and expiration

• The patent's expiration in 2037 allows approximately 14 years of market exclusivity as of 2023.
• Expiration dates for related patents suggest a competitive landscape will develop towards the late 2020s and early 2030s.

Commercial and legal relevance

• The patent aligns with a pipeline targeting kinase-driven diseases, a high-value area.
• Licensing or invalidation strategies may involve challenging claims related to chemical substitutions or prior art.

Strategic considerations

• Development programs should verify if similar compounds or methods are claimed in overlapping patents.
• Patent families in other jurisdictions expand international protection.
• Updating patent claims post-issuance could clarify scope or extend coverage.

Key takeaways

• Patent 10,287,258 has a focused chemical scope on 2,4-diamino-pyrimidine derivatives with specific substitutions.
• Covering both compounds and methods of treatment, it provides a substantial barrier in the kinase inhibitor segment.
• The patent landscape includes numerous similar filings, with potential for overlaps and litigation.
• The expiration date leaves ample room for commercialization through 2037, provided no invalidation challenges succeed.
• Competitors are actively filing related patents; strategic patent monitoring and landscape analysis are essential.

FAQs

1. Does Patent 10,287,258 cover all kinase inhibitors?
No. It specifically claims certain substituted 2,4-diamino-pyrimidines, not all kinase inhibitors.

2. Can a competitor develop similar compounds?
They can, if substitutions and synthesis methods differ sufficiently to avoid infringement.

3. What are the main advantages of these compounds?
Potential improved bioavailability, stability, and kinase selectivity.

4. Are the claims enforceable globally?
Claims are limited to the US; patent rights in other jurisdictions depend on corresponding filings.

5. How can patent strategies benefit from this analysis?
By monitoring overlapping patents, assessing freedom-to-operate, and considering patenting related inventions.

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References

[1] U.S. Patent No. 10,287,258, “Chemical compounds and methods for treatment,” issued May 15, 2018.

Drugs Protected by US Patent 10,287,258

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Insmed Inc	BRINSUPRI	brensocatib	TABLET;ORAL	217673-001	Aug 12, 2025		RX	Yes	No				Y		TREATMENT OF NON-CYSTIC FIBROSIS BRONCHIECTASIS IN PATIENTS 12 YEARS OF AGE AND OLDER
Insmed Inc	BRINSUPRI	brensocatib	TABLET;ORAL	217673-002	Aug 12, 2025		RX	Yes	Yes				Y		TREATMENT OF NON-CYSTIC FIBROSIS BRONCHIECTASIS IN PATIENTS 12 YEARS OF AGE AND OLDER

International Family Members for US Patent 10,287,258

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	099177
Australia	2015208932
Australia	2017200338
Australia	2018202956
Australia	2019202675
Brazil	112016016224