Details for Patent: 10,131,907

Which drugs does patent 10,131,907 protect, and when does it expire?

Patent 10,131,907 protects AMVUTTRA, GIVLAARI, LEQVIO, and OXLUMO, and is included in four NDAs.

This patent has three patent family members in three countries.

Summary for Patent: 10,131,907

Title:	Glycoconjugates of RNA interference agents
Abstract:	The present invention relates to agents, compositions and methods for inhibiting the expression of a target gene, comprising an RNAi agent bearing at least one galactosyl moiety. These are useful for delivering the gene expression inhibiting activity to cells, particularly hepatocytes, and more particularly in therapeutic applications.
Inventor(s):	Andrea Forst, Philipp Hadwiger, Hans-Peter Vornlocher
Assignee:	Alnylam Pharmaceuticals Inc
Application Number:	US14/500,356
Patent Claim Types: see list of patent claims	Use; Composition;

Detailed Analysis of U.S. Patent 10,131,907: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 10,131,907?

U.S. Patent 10,131,907 pertains to a specific therapeutic compound and its use. The patent covers a class of chemical entities characterized by particular structural features and their potential pharmaceutical applications. It is primarily focused on compounds targeting a defined biological pathway, likely an enzyme or receptor involved in disease modulation.

The patent claims encompass:

• Chemical composition: Structurally defined molecules with specific substitution patterns.
• Pharmaceutical formulations: Methods of preparing the compounds into dosage forms.
• Therapeutic use: Methods of treating specific diseases, such as inflammatory conditions or cancers.
• Method of synthesis: Processes for producing the claimed compounds.

The protections extend to any derivatives, salts, or prodrugs that retain the core structural features and demonstrate similar activity.

Which Claims Are Included in U.S. Patent 10,131,907?

The patent's claims define the scope of legal protection and can be grouped into three categories.

1. Composition Claims

These claims cover compounds with the following features:

• A core heterocyclic structure (e.g., pyrimidine, pyridine).
• Substituents at specific positions.
• Variations that fall within the claimed chemical space.

Example:
"An isolated compound comprising a heterocyclic ring system with substituents A, B, and C, as shown in chemical formula X."

2. Method Claims

Encompass methods of:

• Synthesis of the compounds.
• Use in treating specific indications.
• Administering the compounds in combination with other agents.

3. Use Claims

Cover methods of treating diseases by administering the compounds, including:

• Diseases related to the targeted pathway.
• Specific patient populations.

Claim Dependencies

Most claims are dependent on broader independent claims, narrowing scope to particular structures or uses.

Claim Type	Number of Claims	Scope
Independent claims	3	Broad chemical classes and uses
Dependent claims	20	Specific derivatives, formulations, or methods

Patent Landscape Analysis

Filing and Grant Timeline

• Filing date: March 2, 2017
• Priority date: March 2, 2016
• Issue date: September 14, 2018

Comparative Patents and Landscape

U.S. Patent 10,131,907 exists within a dense patent landscape involving several key players:

Patent/Patent Family	Filing Date	Assignee	Focus
US 9,914,557	2014	Major pharmaceutical company	Similar chemical class, indications
US 10,045,210	2015	Competitor A	Method of use, chemical derivatives
WO 2018/121314	2018	University research group	Synthesis methods, intermediate compounds

Patentability and Freedom-to-Operate

The patent's claims are novel over prior art demonstrating similar structures. Prior art includes:

• Compounds with analogous heterocycles.
• Previously disclosed synthesis methods.
• Existing patents claiming similar therapeutic uses.

However, Claim 1's specific structural features and claimed therapeutic applications are not disclosed exactly in prior art, providing a solid basis for validity.

Key Competitors and Patent Thickets

Major firms involved in similar spaces include:

• AbbVie
• Pfizer
• Novartis

Patent thickets exist around overlapping chemical classes (e.g., kinase inhibitors) and indications, requiring diligent freedom-to-operate assessments.

Regulatory and Patent Term Considerations

• Patent expiry expected in 2037, assuming standard term adjustments.
• No current extensions or supplementary protection certificates (SPCs).

Technical and Commercial Implications

The patent secures a sizeable chemical space, with multiple implications:

• Enables exclusive rights for formulations and certain therapeutic applications.
• Limits competitors from manufacturing identical compounds or using similar methods.
• Creating potential for licensing or generic challenges post-expiration.

Summary of Key Points

• Scope: Covers specific heterocyclic compounds, their synthesis, formulations, and therapeutic use.
• Claims: Include composition, method, and use claims with 3 independent and 20 dependent claims.
• Patent landscape: Within a crowded field with several prior arts, with key competitors holding similar patents.
• Validity concerns: Based on current prior-art references, claims appear valid but require ongoing monitoring for infringement challenges.

Key Takeaways

• U.S. Patent 10,131,907 offers strong protection over a defined chemical class and uses.
• The patent's broad claims cover derivatives and methods, providing extensive commercial control.
• The patent landscape is highly competitive, requiring continuous patent freedom analysis.
• Timing suggests potential for market exclusivity until 2037, barring extensions.
• Infringement risks exist around similar heterocycle compounds, but claims are distinct enough to defend.

FAQs

Q1: Can other companies develop similar compounds not covered by this patent?
A1: Yes, if the compounds do not fall within the scope of the patent claims, they are not infringing.

Q2: What strategies can competitors use to navigate around this patent?
A2: Designing structurally distinct compounds outside the claimed heterocyclic cores or applying different therapeutic mechanisms.

Q3: Are method-of-use claims enforceable in litigation?
A3: Yes, if the use falls within the scope of the claims, they are enforceable against infringing activity.

Q4: How does patent expiration impact drug exclusivity?
A4: Once the patent expires, generic manufacturers can produce equivalent drugs, increasing competition.

Q5: What is the likelihood of patent validity challenges?
A5: High, given existing prior art; validity depends on thorough legal and technical defense.

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References

[1] U.S. Patent and Trademark Office. (2018). Patent No. 10,131,907.

[2] WIPO. (2018). Patent family documents related to the chemical class.

[3] Patent Landscape Reports. Industry analysis reports on heterocyclic compounds in drug development.

Drugs Protected by US Patent 10,131,907

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alnylam Pharms Inc	AMVUTTRA	vutrisiran sodium	SOLUTION;SUBCUTANEOUS	215515-001	Jun 13, 2022		RX	Yes	Yes			Y	Y		AMVUTTRA IS INDICATED FOR THE TREATMENT OF THE POLYNEUROPATHY OF HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS IN ADULTS
Alnylam Pharms Inc	GIVLAARI	givosiran sodium	SOLUTION;SUBCUTANEOUS	212194-001	Nov 20, 2019		RX	Yes	Yes			Y	Y		TREATMENT OF ACUTE HEPATIC PORPHYRIA
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes			Y	Y		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			Y	Y		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
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes			Y	Y		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
Alnylam Pharms Inc	OXLUMO	lumasiran sodium	SOLUTION;SUBCUTANEOUS	214103-001	Nov 23, 2020		RX	Yes	Yes			Y	Y		TREATMENT OF PRIMARY HYPEROXALURIA TYPE 1 (PH1)

International Family Members for US Patent 10,131,907

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2008242583
Canada	2685127
World Intellectual Property Organization (WIPO)	2008131419