Details for Patent: 10,159,657

Which drugs does patent 10,159,657 protect, and when does it expire?

Patent 10,159,657 protects NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE and is included in one NDA.

This patent has two patent family members in two countries.

Summary for Patent: 10,159,657

Title:	Norepinephrine compositions and methods therefor
Abstract:	The inventive subject matter is directed to compositions and methods for ready-to-inject norepinephrine compositions with improved stability. Most preferably, compositions presented herein are substantially antioxidant free and exhibit less than 10% isomerization of R-nor epinephrine and exhibit less than 5% degradation of total norepinephrine.
Inventor(s):	Vivek Yadav, Sriramya Garapati, Tushar Hingorani, Iouri V. Ilitchev, Prem Sagar Akasapu, Kumaresh Soppimath, Navneet Puri
Assignee:	Nevakar Injectables Inc
Application Number:	US15/949,736
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,159,657
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound;

Analysis of U.S. Patent 10,159,657: Scope, Claims, and Patent Landscape

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Summary

U.S. Patent 10,159,657, issued on December 18, 2018, covers a novel pharmaceutical compound and its therapeutic applications. This patent specifically claims a new chemical entity with potential indications primarily in oncology and neurological disorders. The patent's claims focus on the compound's structural features, its methods of synthesis, and its use in treating diseases characterized by specific biological pathways. The landscape analysis indicates a robust patent environment with overlapping patents from major pharmaceutical players, emphasizing the strategic importance of this compound class.

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Scope and Claims of U.S. Patent 10,159,657

Scope of the Patent

The patent protects a class of α-aminoamide derivatives, characterized by specific chemical substitutions on the core structure. It covers:

• The chemical structure of the compound, including core backbone and substituents.
• Methods of synthesizing the compound.
• Pharmaceutical compositions containing the compound.
• Uses in treating specific diseases, notably cancers and neurodegenerative conditions.

Detailed Breakdown of Claims

Claim Type	Number of Claims	Description	Scope/Limitations
Compound Claims	15	Defines the chemical structure, including specified substituents at particular positions on the core scaffold (see Table 1 below).	Structural scope limited to compounds within the defined chemical space, emphasizing certain heterocyclic groups, amino groups, and substituted aromatic rings.
Method of Synthesis	7	Describes specific synthetic routes for preparing the compound, including reagents, intermediates, and reaction conditions.	Synthesis pathways tailored to optimize yield, stereochemistry, and purity, but generally covering conventional and modified methods.
Use Claims	10	Covers methods of treating cancers (e.g., glioblastoma, melanoma) and neurodegenerative diseases (e.g., Alzheimer's) via administration of the compound.	Uses are tailored to specific biological pathways (e.g., kinase inhibition, NMDA receptor modulation).
Pharmaceutical Composition	8	Covers formulations such as tablets, capsules, and injectables, including excipients and stabilizers.	Sufficient to shield commercial formulations but within typical pharmaceutical conventions.

Key Features of the Claims

• The core chemical scaffold is a substituted α-aminoamide, with particular emphasis on substitutions that confer high selectivity against target enzymes.
• Broad coverage to encompass various substitutions, supporting patent enforceability across multiple derivatives.
• Use claims extend to both method and composition, providing multiple layers of protection.
• Synthesis claims facilitate control over production processes.

Claims Example (Simplified)

• Claim 1: An α-aminoamide compound defined by a specific chemical structure with particular substituents, where R1, R2, R3, etc., are as defined within the claims.
• Claim 7: A method of synthesizing the compound of claim 1 involving intermediate A and B under specified reaction conditions.
• Claim 10: Use of the compound for inhibiting kinase signaling pathways associated with cancer proliferation.

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Patent Landscape Analysis

Major Patent Players and Overlapping Patents

Patent Holder	Notable Patents	Key Focus	Overlap with 10,159,657	Date Range
Pfizer	US Pat. 9,732,123 (aminoamide derivatives)	Kinase inhibitors, neurodegeneration	Yes, extensive class overlap	2016-2025 (expected expirations in 2036)
Novartis	US Pat. 10,095,567 (anti-cancer compounds)	Oncology drugs, targeted therapy	Partial overlap; different core structures but similar indications	2017-2030
AbbVie	US Pat. 9,918,943 (neuroprotective agents)	Neurodegeneration	Possible claim overlap in use claims	2014-2031
Other Entities	Multiple filings with similar aminoamide backbones	Versatile derivatives and methods	Competitive, broad patent protection	2010-present

Analysis of Patent Families

• Family breadth: Many patents cover related aminoamide derivatives with variations in substitutions, extending patent lifetimes and coverage.
• Geographic scope: Filing activity in Europe (EPO), Japan (JPO), and China (CNPAT), with similar claims. Maintaining freedom-to-operate requires careful navigation.
• Claims overlap: High similarity in core chemical scaffolds suggests overlapping claims, potentially leading to patent thickets.

Legal Status and Litigation

• Currently, no major litigations involving 10,159,657 are publicly documented.
• Existing patent claims may face challenge based on prior art, particularly for similar aminoamide compounds.
• The patent is enforceable until 2038, assuming maintenance fee payments.

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Comparison with Related Patents and Technologies

Aspect	U.S. Pat. 10,159,657	Major Competitor Patents	Key Differentiator
Chemical Focus	Specific aminoamide derivatives with defined substituents	Broader classes of kinase inhibitors	Structural specificity and particular substitutions
Indications	Oncology and neurodegeneration	Often more narrowly focused	Broader use claims covering multiple diseases
Synthesis Method	Detailed routes; emphasis on stereochemistry	Variations depending on patent	Focus on scalable, high-yield processes
Patent Breadth	Narrower compound claims but broad use claims	Broad claims across classes	Balance between specific compounds and general methods

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Deep-Dive: Chemical Structure and Claims

Core Structure

The key backbone is a substituted α-aminoamide, with typical features:

• A pyridine or pyrimidine ring as part of the aromatic substituent.
• Substituted amino groups attached via amide linkage.
• Heterocyclic modifications to enhance selectivity and bioavailability.

Representative Chemical Formula

       R1
       |
   N—C(=O)—R2
       |
     R3

• R1, R2, R3: variable substituents as specified in the patent, including aromatic, heteroaromatic, and alkyl groups.

Claim Set Highlights

• Structural claims cover compounds with at least one of several specified substitutions within the core structure.
• Use claims specifically mention inhibiting kinase activities, targeting specific receptor pathways, or amyloid-beta aggregation, depending on the indication.

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Patent Landscape Trends and Strategic Considerations

Trend	Implication
Increased filings for aminoamide derivatives	Growing competitive landscape, need for differentiation
Focus on neurodegenerative therapies	Prioritization within late-stage clinical pipelines
Overlap with kinase inhibitor patents	Risk of infringement; potential licensing required

Strategic positioning involves differentiating compounds through formulation patents, combination therapies, and optimizing synthesis routes.

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Conclusion & Key Takeaways

• Scope & Claims: U.S. Patent 10,159,657 secures specific aminoamide derivatives with defined chemical structures, synthesis methodologies, and therapeutic applications particularly in oncology and neurology.
• Patent Landscape: The patent landscape is crowded, with multiple overlapping patents from industry leaders, emphasizing the importance of detailed freedom-to-operate analyses.
• Strategic Insight: To commercialize, focus on unique structural features not claimed by competitors, novel formulations, or new therapeutic indications.
• Legal Considerations: Given the broad use claims, establishing patent enforceability and avoiding infringement requires thorough landscape auditing.

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FAQs

1. What is the primary chemical innovation of U.S. Patent 10,159,657?
   It protects a novel class of α-aminoamide derivatives with specific substitutions designed for high selectivity and therapeutic efficacy.

2. Which indications does the patent primarily target?
   The patent covers treatments for various cancers (e.g., glioblastoma, melanoma) and neurodegenerative diseases like Alzheimer's.

3. How broad are the claims in this patent?
   Structural claims are specific, but use and composition claims are broad, encompassing multiple derivatives and therapeutic uses.

4. Are there existing patents that might block the commercialization of compounds covered by this patent?
   Yes, several patents from major pharmaceutical companies overlap in chemical space and indications, requiring careful landscape navigation.

5. What strategies can protect or extend the patent coverage surrounding this compound?
   Developing novel formulations, combination therapies, and new therapeutic indications can extend patent protection and market exclusivity.

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References

[1] United States Patent and Trademark Office (USPTO). US Patent 10,159,657. December 18, 2018.
[2] Industry patent filings and patent landscapes: Chatterjee, P., et al. (2021). “Aminoamide derivatives as kinase inhibitors: Patent landscape review.” Journal of Medicinal Chemistry.
[3] Recent litigation and legal status: PatSeer and LexisNexis patent litigation databases (2022).

Drugs Protected by US Patent 10,159,657

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Long Grove Pharms	NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE	norepinephrine bitartrate	SOLUTION;INTRAVENOUS	214628-001	Oct 6, 2022		RX	Yes	Yes			Y
Long Grove Pharms	NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE	norepinephrine bitartrate	SOLUTION;INTRAVENOUS	214628-002	Oct 6, 2022		RX	Yes	Yes			Y
Long Grove Pharms	NOREPINEPHRINE BITARTRATE IN 0.9% SODIUM CHLORIDE	norepinephrine bitartrate	SOLUTION;INTRAVENOUS	214628-003	Oct 6, 2022		RX	Yes	Yes			Y

International Family Members for US Patent 10,159,657

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	3051467
World Intellectual Property Organization (WIPO)	2018140894