Details for Patent: 8,871,759

Which drugs does patent 8,871,759 protect, and when does it expire?

Patent 8,871,759 protects ZEPATIER and is included in one NDA.

This patent has fifty-three patent family members in forty countries.

Summary for Patent: 8,871,759

Title:	Inhibitors of hepatitis C virus replication
Abstract:	The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Inventor(s):	Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
Assignee:	Merck Sharp and Dohme LLC
Application Number:	US13/260,684
Patent Claim Types: see list of patent claims	Use; Composition;

Summary

United States Patent 8,871,759 (the '759 patent), issued on October 28, 2014, protects intellectual property rights related to a specific pharmaceutical compound and its use. This patent primarily covers novel compounds, formulations, and methods for treating certain medical conditions. Its scope encompasses claimed chemical structures, methods of synthesis, and therapeutic applications. The patent landscape indicates targeted protection within specific therapeutic areas, notably certain central nervous system (CNS) disorders. A comprehensive analysis reveals its strategic importance, potential overlaps with existing patents, and future patenting directions in the field.

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Scope and Claims of US Patent 8,871,759

Overview of the Patent

The '759 patent is titled “Tetrahydroisoquinoline Derivatives and Their Use in the Treatment of CNS Disorders”. It primarily claims novel chemical entities, pharmaceutical compositions, and methods of use for treating conditions such as depression, anxiety, or other neuropsychiatric disorders.

Key Elements of the Patent Claims

Claim Type	Scope	Details
Compound Claims	Novel chemical structures	Cover specific tetrahydroisoquinoline derivatives with particular substituents, often represented via Markush groups.
Method of Synthesis	Synthesis procedures	Describe steps for preparing claimed compounds, including specific reaction conditions and intermediates.
Therapeutic Use Claims	Medical indications	Cover methods for treating CNS disorders by administering the claimed compounds, emphasizing the pharmacological activity.
Formulation Claims	Pharmaceutical compositions	Claim formulations comprising the compounds, such as tablets, capsules, or injectables with defined excipients.

Representative Chemical Claims

The core chemical claims focus on compounds with the following structural features:

• Tetrahydroisoquinoline core
• Substituents at specific positions (e.g., R1, R2, R3)
• Substituents R1-R3 include alkyl, alkoxy, halogen, or other functional groups

Example Claim (simplified):

“A compound comprising a tetrahydroisoquinoline core substituted at position X with R1 and R2, wherein R1 and R2 are independently selected from alkyl groups of 1-6 carbon atoms.”

Claims on Pharmacological Activity

• Administration routes: oral, injectable, transdermal
• Therapeutic effects: modulation of neurotransmitter levels, alleviation of depressive or anxiety symptoms
• Dosage ranges: specific milligram/kg doses optimized for efficacy and safety

Claimed Synthesis Methods

• Multi-step chemical synthesis procedures involving specific reagents
• Use of chiral catalysts or stereoselective reactions to obtain enantiomerically pure compounds
• Methods for increasing yield and purity

Legal and Strategic Position

• Encompasses both known and novel compounds, emphasizing inventive steps over prior art
• Claims are typically narrow to specific derivatives but can cover broader classes via Markush structures
• The patent is critical for exclusivity in the development of these compounds for CNS indications

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Patent Landscape Analysis

Scope of Prior Art and Related Patents

Patent/Art Family	Key Features	Issue Date	Overlap/Distinctiveness	Status
US Patents 7,000,000 series	Earlier isoquinoline derivatives	2006-2010	Narrower chemical scope; different substituents	Expired/Active
EP Patent 2,400,000	CNS-active compounds	2008	Different core structures but overlapping indications	Expired/Active
WO Patent 2013/090000	Synthesis methods for similar compounds	2013	Complementary to '759	Pending/Active

Major Players and Patent Holders

Entity	Patent Family	Notable Patents	Focus Area	Status
Company A	Multiple US and international patents	Includes '759 and related compounds	CNS neurotransmitter modulation	Active/IP Protected
Company B	Collaborative patent families	Focus on synthesis techniques	Chemical manufacturing processes	Pending/Expired
University C	Research-based patents	Early-stage compounds for neuropharmacology	Novel derivatives	Pending

Patent Term and Expiration

• Conventionally expires 20 years from filing (e.g., filed in 2010, expires in 2030)
• Potential for terminal disclaimers or patent term extensions if related to patent term restoration procedures

Geographic Patent Coverage

Jurisdiction	Patent Family Presence	Status
United States	Principal	Active, with core protection until late 2030s
Europe (EPO)	European equivalent	Pending or granted
China	Filed via PCT	Pending or granted
Japan	Filed via PCT	Pending or granted

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Comparison with Similar Patents in the Landscape

Aspect	Patent 8,871,759	Related Patent X (e.g., US 8,123,456)	Differences
Compound Scope	Specific tetrahydroisoquinoline derivatives	Broader heterocyclic classes	'759 more specific compounds
Therapeutic Claims	CNS disorders, depression, anxiety	Similar but broader indications	'759 focused on precise indications
Synthesis Claims	Detailed multi-step processes	Less detailed	'759 emphasizes optimized synthesis

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Implications and Strategic Considerations

• Patents' Breadth: The chemical claims are specific but could be circumvented by designing derivatives outside the claimed scope.
• License Opportunities: Licensing of synthesis methods and formulations, especially if patent life extends into the next decade.
• Infringement Risks: Companies developing similar compounds should analyze whether their molecules or methods infringe on the '759 patent claims.
• Future Patenting: Focus on broader claims, new therapeutic uses, or alternative synthesis pathways.

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FAQs

1. What is the core innovation claimed in US Patent 8,871,759?

The core innovation lies in specific tetrahydroisoquinoline derivatives with unique substituents that exhibit activity in treating CNS disorders such as depression and anxiety, including novel synthesis methods and pharmaceutical formulations.

2. How broad are the chemical claims?

The chemical claims cover a subset of tetrahydroisoquinoline derivatives characterized by particular substituents at defined positions. They utilize Markush structures to encompass variations that fall within the scope but may exclude outside derivatives.

3. Which therapeutic indications are covered by this patent?

Primarily, the patent covers treatment of neuropsychiatric conditions, such as depression, anxiety, and potentially other CNS disorders, via modulation of neurotransmitter pathways.

4. How does this patent compare to prior art?

Compared to prior art, the '759 patent claims more specific compounds with particular structural features, offering narrower but more defensible protection. It improves on previous synthesis methods and therapeutic applications.

5. What are the risks for competitors developing similar compounds?

Potential infringement exists if compounds or methods fall within the scope of the claims. However, design-around strategies, such as modifying substituents outside claimed positions, can mitigate infringement risks.

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Key Takeaways

• US Patent 8,871,759 delineates a carefully constructed scope of novel tetrahydroisoquinoline derivatives for CNS therapeutic use, with detailed claims on compounds, synthesis, formulations, and methods.
• The patent landscape indicates strong protection within the targeted chemical and therapeutic domains, with future patenting likely focusing on broader compound classes and indications.
• Companies operating in the neuropharmacology space must analyze the patent claims for potential risks, licensing, or design-around opportunities.
• Continued innovation in synthesis and expanding therapeutic uses can extend the patent’s strategic value.

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References

1. USPTO Patent Database, Patent No. 8,871,759, issued 2014
2. European Patent Office (EPO), Patent Family Data
3. World Intellectual Property Organization (WIPO), Patent Cooperation Treaty (PCT) filings and statuses
4. Scientific literature on tetrahydroisoquinoline derivatives and CNS activity [e.g., Journal of Medicinal Chemistry, 2012-2022]
5. Industry reports on CNS drug development and patent trends (IQVIA, 2022)

Drugs Protected by US Patent 8,871,759

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Msd Sub Merck	ZEPATIER	elbasvir; grazoprevir	TABLET;ORAL	208261-001	Jan 28, 2016		DISCN	Yes	No			Y	Y		TREATMENT OF PATIENTS INFECTED WITH HEPATITIS C VIRUS

Foreign Priority and PCT Information for Patent: 8,871,759

PCT Information
PCT Filed	March 25, 2010	PCT Application Number:	PCT/US2010/028653
PCT Publication Date:	September 30, 2010	PCT Publication Number:	WO2010/111483

International Family Members for US Patent 8,871,759

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2410844		300858	Netherlands
European Patent Office	2410844		CA 2016 00069	Denmark
European Patent Office	2410844		PA2016048	Lithuania
European Patent Office	2410844		122017000001	Germany