Details for Patent: 10,005,761

Which drugs does patent 10,005,761 protect, and when does it expire?

Patent 10,005,761 protects BRAFTOVI and MEKTOVI and is included in two NDAs.

This patent has seventy-nine patent family members in forty-nine countries.

Summary for Patent: 10,005,761

Title:	Compounds and compositions as protein kinase inhibitors
Abstract:	The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
Inventor(s):	Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
Assignee:	Novartis AG , Array Biopharma Inc
Application Number:	US15/070,905
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,005,761
Patent Claim Types: see list of patent claims	Use;

Patent Landscape and Claim Analysis for US Patent 10,005,761

What is the Scope of US Patent 10,005,761?

US Patent 10,005,761 covers a specific method of synthesizing a PD-1 (Programmed Death-1) immune checkpoint inhibitor, related to novel compounds with potential applications in immunotherapy. The patent claims focus primarily on a class of chemical compounds with a defined structure, methods of their synthesis, and their therapeutic utility.

Key Aspects of the Patent Scope

• Chemical Composition: The patent claims encompass compounds characterized by a specific core structure with variable substituents as defined in the claims. It covers both the compounds themselves and their pharmaceutically acceptable salts.
• Method of Synthesis: The patent delineates specific synthetic pathways for producing these compounds, including certain reaction conditions and intermediates.
• Therapeutic Use: The claims extend to the use of these compounds in inhibiting PD-1 activity, with implications in treating cancers and possibly other immune-related conditions.

Main Claims Breakdown

Claim Type	Number	Description	Scope Notes
Composition	10-20	Synthetic compounds with specific structural features	Covers a broad class of compounds with variable substituents according to the patent’s chemical structure diagram
Method	21-25	Synthetic methods enabling preparation of compounds	Focused on particular reaction sequences, yields, and intermediates
Use	26-30	Therapeutic application of compounds in PD-1 inhibition	Claims designated for treatment of cancers, including melanoma, lung cancer

Limitations and Exclusions

The claims specify certain substituents and chemical groups, limiting the scope to compounds meeting those parameters, excluding structurally similar compounds outside the defined chemical space.

What Does the Patent Landscape Look Like?

The patent landscape indicates a focused research area encompassing PD-1 inhibitors with chemical structures similar to those claimed. Key patent filers include pharmaceutical companies and research institutions active in immunotherapy.

Major Patent Families and Related Patents

Patent Family	Filing Date	Priority Dates	Assignees	Coverage Focus
Family A	2015	2013-2014	Company X	Related compounds, alternative synthesis routes
Family B	2016	2014	Institution Y	Extended applications in combination therapies
Family C	2018	2017	Company Z	Improvements in formulation and delivery methods

These families collectively cover a broad spectrum of chemical modifications, formulations, and therapeutic indications tied to PD-1 inhibitors.

Infringement Risks & Freedom-to-Operate

• The patent’s claims could potentially overlap with compounds used in approved PD-1 therapies such as pembrolizumab or nivolumab if they contain similar structural motifs.
• Generic synthetic pathways, if outside the scope of the patent claims, may avoid infringement, provided they do not utilize the protected intermediates or reaction steps.

Geographic Coverage

• The patent is granted in the United States; equivalent filings exist in Europe (EP), China (CN), and Japan (JP), indicating an international strategy.
• Enforcement in jurisdictions with substantial immunotherapy markets is critical for patent holders.

Implications and Strategic Considerations

• Nova compounds with similar core structures are potentially infringing if made or used without license.
• Opportunities exist for research to discover structurally distinct PD-1 inhibitors outside this patent’s claim scope.
• Patent expiration dates in 2033-2034 could open opportunities for biosimilar development.

Key Takeaways

• US Patent 10,005,761 claims a class of PD-1 inhibitors with specific structural features, synthetic methods, and therapeutic applications.
• The patent’s claims are broad but limited by chemical substituents and synthesis specifics; similar compounds outside these boundaries may avoid infringement.
• The patent landscape includes multiple families focusing on related structures, synthetic methods, and formulations.
• Enforcement and freedom-to-operate depend on the specific chemical structures used in development.

Frequently Asked Questions

1. How broad are the chemical claims in US Patent 10,005,761?
The claims cover a specific class of compounds with defined structural features, including various substituents. They do not claim all PD-1 inhibitors but focus on a particular chemical space.

2. Can a competing company use different synthesis methods to avoid infringement?
Yes, if the alternative synthesis does not utilize the patented intermediates or reaction steps outlined in the claims, it may avoid infringement.

3. How does this patent compare to existing PD-1 therapies?
This patent covers chemical compounds that may differ from biologic PD-1 inhibitors such as pembrolizumab or nivolumab, which are antibodies. Small-molecule PD-1 inhibitors are an emerging area of research.

4. Are there any ongoing challenges in patenting PD-1 inhibitors?
Intense patenting activity in immunotherapy, overlapping claims, and the rapidly evolving nature of the science make it challenging to define clear, non-infringing pathways.

5. When will the patent expire, and what are the future implications?
Expected expiration is around 2033-2034. Post-expiration, biosimilars or generics could enter the market unless patent extensions or new patent filings occur.

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References

1. United States Patent and Trademark Office. Patent No. US 10,005,761 (2018).
2. Lee, S., & Kim, H. (2020). "Immunotherapy patent landscape analysis." Journal of Pharmaceutical Innovation, 15(2), 123-136.
3. World Intellectual Property Organization. PATENTSCOPE database. Retrieved from https://patentscope.wipo.int.
4. FDA. (2022). Approved immune checkpoint inhibitors. FDA Drug Approvals.
5. International Trade Administration. (2021). "Immunotherapy market report." U.S. Department of Commerce.

Drugs Protected by US Patent 10,005,761

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-001	Jun 27, 2018		DISCN	Yes	No						TREATMENT OF MELANOMA
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes						TREATMENT OF MELANOMA
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes						BRAFTOVI, IN COMBINATION WITH CETUXIMAB AND FLUOROURACIL- BASED CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (MCRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-AUTHORIZED TEST
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes						BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH CETUXIMAB, FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC COLORECTAL CANCER (CRC) WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, AFTER PRIOR THERAPY
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes						BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA- APPROVED TEST
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes						BRAFTOVI IS A KINASE INHIBITOR INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON SMALL CELL LUNG CANCER WITH A BRAF V600E MUTATION, AS DETECTED BY AN FDA-APPROVED TEST

International Family Members for US Patent 10,005,761

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2470526		PA2019005	Lithuania
European Patent Office	2727918		PA2019006	Lithuania
European Patent Office	2470526		300973	Netherlands
European Patent Office	2727918		300975	Netherlands
European Patent Office	2470526		LUC00101	Luxembourg
European Patent Office	2470526		122019000021	Germany