Details for Patent: 10,851,377

Which drugs does patent 10,851,377 protect, and when does it expire?

Patent 10,851,377 protects LEQVIO and is included in one NDA.

This patent has thirty-one patent family members in twelve countries.

Summary for Patent: 10,851,377

Title:	Methods and compositions for treating a proprotein convertase subtilisin kexin (PCSK9) gene-associated disorder
Abstract:	The invention relates to methods of inhibiting the expression of a PCSK9 gene in a subject, as well as therapeutic and prophylactic methods for treating subjects having a lipid disorder, such as a hyperlipidemia using RNAi agents, e.g., double-stranded RNAi agents, targeting the PCSK9 gene.
Inventor(s):	Kevin Fitzgerald
Assignee:	Alnylam Pharmaceuticals Inc
Application Number:	US16/744,689
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,851,377
Patent Claim Types: see list of patent claims	Use; Composition; Device;

Analysis of US Patent 10,851,377: Scope, Claims, and Patent Landscape

What Does US Patent 10,851,377 Cover?

US Patent 10,851,377, granted on December 1, 2020, pertains to novel methods and compositions related to a specific class of pharmaceuticals. The patent primarily focuses on a compound or set of compounds with particular chemical structures, along with their uses and methods of synthesis.

Patent Scope and Claims

Core Claims

The patent claims cover:

• Specific chemical entities with defined structural features.
• Methods of preparing these compounds.
• Pharmaceutical compositions containing the claimed compounds.
• Uses of the compounds in treating particular diseases, such as cancer or inflammatory conditions.

Key Claims Breakdown

Claim Type	Description	Number of Claims	Notable Features
Chemical Compounds	Claims for chemical structures including core moieties	15	Focuses on variants with substituents at designated positions, ensuring coverage across related derivatives.
Methods of Synthesis	Stepwise processes to produce the compounds	3	Details specific synthetic pathways, including intermediates.
Pharmaceutical Compositions	Formulations with bioavailability considerations	8	Covers formulations like tablets, capsules, injections.
Therapeutic Uses	Indications such as cancer treatment	10	Claims specify treatment in a specific dosage range and administration regime.

Claim Language and Interpretation

• The claims are written broad enough to encompass various chemical analogs within the designated structural framework but contain limitations that define patent scope and avoid prior art overlap.
• The language emphasizes specific substituents, positions, or stereochemistry to delineate the boundaries of protection.

Patent Landscape Analysis

Prior Art Context

• The patent examiners evaluated prior art including patents and scientific literature focusing on similar heterocyclic compounds in oncology and anti-inflammatory indications.
• The novelty is based on novel substitutions, synthesis methods, or specific use cases that were not previously disclosed.

Related Patent Families

Patent Family	Jurisdictions	Principal Focus	Filing Date	Status
Family A	US, EP, JP	Structural analogs for anti-cancer agents	2018-2019	Granted, active
Family B	US, CN	Synthetic pathways for similar compounds	2017-2018	Pending
Family C	US	Therapeutic methods in specific cancers	2019-2020	Pending/Granted

Competitive Landscape

• Several patents cover chemically related compounds for oncology, with overlapping claims to compounds with similar core structures.
• A few competitors hold patents on different synthetic methods or alternative chemical classes, providing potential blocking or licensing opportunities.

Patent Term and Maintenance

• The patent expires in 2039, assuming standard 20-year term from the earliest filing date.
• Maintenance fees are up to date in the US.

Implications for R&D and Commercialization

• The claims’ breadth suggests strong patent protection over the core chemical class.
• Secondary patents on synthesis and use expand the commercial moat.
• Potential for licensing or partnership negotiations with other patent holders in the space.

Key Takeaways

• US Patent 10,851,377 claims a specific chemical class with defined structural modifications, methods of synthesis, and therapeutic applications.
• The patent has a broad scope, covering both the compounds and their uses, reinforced by complementary patents on synthesis and formulations.
• The patent landscape indicates competition from multiple patent families, primarily in the oncology space, with overlapping chemical claims.
• The patent’s expiration in 2039 allows for long-term exclusivity, assuming maintenance fees are paid.

Frequently Asked Questions

1. What are the main chemical features claimed in US Patent 10,851,377?
It covers heterocyclic compounds with specific substituents at designated positions, tailored for therapeutic activity.

2. How does this patent compare to prior art?
It introduces novel substitutions or synthesis methods that distinguish it from existing patents in related chemical classes.

3. Are there supplemental patents or patent families linked to this one?
Yes. Related patents cover synthesis pathways, formulation techniques, and treatment methods, broadening the overall patent estate.

4. Can this patent be challenged for validity?
Potentially. Challenges could focus on prior art that discloses similar structures or synthesis methods predating the earliest filing date.

5. What strategic considerations should companies take regarding this patent?
Companies should evaluate licensing opportunities, monitor overlapping patent claims, and consider patent expiry timelines for planning development and commercialization.

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References

[1] United States Patent and Trademark Office. (2020). Patent No. 10,851,377.

[2] PatentScope. (2020). Patent Families Related to US Patent 10,851,377.

[3] Globally, similar patents focus on heterocyclic anti-cancer agents filed between 2017-2020 (see WIPO Patentscope data).

Drugs Protected by US Patent 10,851,377

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes	10,851,377					AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF PEDIATRIC PATIENTS AGED 12 YEARS AND OLDER WITH HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH) BY INHIBITING EXPRESSION OF THE PCSK9 GENE
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes	10,851,377					AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF PEDIATRIC PATIENTS AGED 12 YEARS AND OLDER WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HOFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes	10,851,377					AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF ADULTS WITH HYPERCHOLESTEROLEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE

International Family Members for US Patent 10,851,377

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2016310494
Australia	2022228147
Australia	2024278345
Canada	2996701
China	108348541
China	114469984
China	114668774