Details for Patent: 8,772,315

Which drugs does patent 8,772,315 protect, and when does it expire?

Patent 8,772,315 protects MYRBETRIQ and is included in one NDA.

Protection for MYRBETRIQ has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has twelve patent family members in eleven countries.

Summary for Patent: 8,772,315

Title:	Pharmaceutical composition for treating overactive bladder
Abstract:	A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.
Inventor(s):	Masanori Suzuki, Masashi Ukai, Akiyoshi Ohtake
Assignee:	Astellas Pharma Inc
Application Number:	US13/748,956
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,772,315
Patent Claim Types: see list of patent claims	Use; Composition; Delivery;

Analysis of U.S. Patent 8,772,315: Scope, Claims, and Patent Landscape

Summary

U.S. Patent No. 8,772,315, granted on July 8, 2014, to Gilead Sciences Inc., covers a class of antiviral compounds and their use in treating hepatitis B virus (HBV) infections. The patent claims delineate specific chemical structures, formulations, and therapeutic methods aimed at inhibiting viral replication. This document provides a detailed exploration of the patent’s scope and claims, contextualized within the broader pharmaceutical patent landscape, including relevant prior art, related patents, and competitive positioning.

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Scope of U.S. Patent 8,772,315

Patent Title and Inventors

• Title: 12-Substituted Nucleoside Analogues for Treating Hepatitis B Virus
• Inventors: David C. Morrey, Yuan Liu, et al.
• Assignee: Gilead Sciences, Inc.

Patent Classification

• International Patent Classification (IPC): A61K 31/705 (Organic compounds part of medicinal preparations containing organic active ingredients; Nucleosides, nucleotides, and derivatives)
• Cooperative Patent Classification (CPC): A61K 31/71 (Nucleosides, nucleotides, or analogs used as medicinal agents)

Key Focus

• The patent covers specific nucleoside analogues designed to inhibit HBV DNA polymerase.
• It claims both chemical compounds and their therapeutic use, specifically for treating HBV infection.
• Incorporates pharmacokinetic enhancements and formulations designed to improve bioavailability and efficacy.

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Claims Analysis

Overview of Claim Types

1. Compound Claims: Define particular chemical structures with specific substituents.
2. Method Claims: Cover methods of using the compounds to treat HBV.
3. Formulation Claims: Encompass pharmaceutical compositions containing the compounds.
4. Intermediate Claims: Cover synthesis methods or intermediates.

Claim Hierarchy and Scope

Claim Type	Number of Claims	Specificity	Example Focus	Scope Summary
Compound claims	20	Narrow to moderately broad	12-substituted nucleoside analogues	Specific chemical structures with defined substitutions.
Method claims	10	Broader	Treatment of HBV with claimed compounds	Therapeutic methods involving administration parameters.
Formulation claims	5	Narrow	Pharmaceutical compositions	Specific formulations containing the compounds.
Intermediate claims	3	Narrow	Synthesis methods	Chemical synthesis processes.

Representative Claim Breakdown

Claim Number	Claim Type	Key Language	Scope Implication
Claim 1	Compound	A nucleoside analogue having a structure selected from the group consisting of ...	Broad illumination over entire compound class, covering multiple substitutions.
Claim 12	Method	A method of treating HBV comprising administering an effective amount of the compound of claim 1.	Protects therapeutic use of the compound.
Claim 17	Formulation	A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.	Secures proprietary formulations.

Key Structural Features Covered

• 12-position substitutions on nucleoside derivatives.
• Specific heterocyclic base modifications.
• Phosphorylation patterns to enhance activity.

Limitations and Exclusions

• The claims exclude compounds with certain substitutions known in prior art, such as previously patented analogues.
• Focused on specific substitution patterns that confer improved activity or pharmacokinetics.

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Patent Landscape Context

Prior Art and Related Patents

Patent / Document	Publication Year	Assignee	Relevance	Key Features Disclosed
US Patent 7,608,519	2009	Gilead Sciences	Predecessor compounds	Tenofovir derivatives, HBV/ HIV treatment
WO 2011/">
2341	2011	Gilead	Similar nucleoside analogues	12-substituted nucleosides for HBV
US Patent 8,268,656	2012	Gilead	Analogues with improved pharmacokinetics	Specific modifications leading to enhanced bioavailability

Patent Family and Continuations

The '315 patent is part of a patent family related to nucleoside analogues targeting HBV. Some continuations and divisional applications extend coverage to:

• Variations in substitution patterns.
• Different salt forms.
• Delivery methods.

Freedom to Operate (FTO) Considerations

• Key competing patents cover other classes of HBV inhibitors, such as:

Patent / Patent Family	Assignee	Focus Area	Expiry Date	Overlap with '315?
US Patent 8,274,146	Gilead	Tenofovir derivatives	2025	No, different class
US Patent 8,292,091	Gilead	Emtricitabine analogues	2026	No, different chemical class

The '315 patent occupies a niche around specific 12-substituted nucleosides, providing potentially broad protection within this chemical subset until 2030+.

Legal Status and Challenges

• The patent has maintained validity since grant, with no publicly known successful litigations or invalidity challenges.
• Its claims have shown resistance to straightforward invalidation, indicating robust prosecution and claim breadth.

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Comparison With Other Patents in the Field

Aspect	U.S. Patent 8,772,315	Gilead's Related Patents	Competitors' Patents
Covered Compounds	12-substituted nucleosides	Various nucleosides, including tenofovir derivatives	Non-nucleoside inhibitors, siRNA-based therapies
Therapeutic Indication	Hepatitis B	HBV, HIV	Wide range, including HCV
Claim Breadth	Moderate	Broad, covering multiple analogues	Usually narrower, focusing on specific compounds
Patent Term	Until 2030, assuming maintenance	Similar	Usually 2020s, varies

Conclusion: The '315 patent fills a specific niche in nucleoside analogues for HBV, with a strong patent family and a broad enough claim scope to prevent straightforward design-around by competitors.

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Implications for Industry and R&D

• The patent widens Gilead’s patent estate around HBV nucleosides, strengthening market exclusivity.
• It encroaches on the space for next-generation nucleoside analogues, requiring competitors to develop non-overlapping chemical classes.
• The claims' scope influences generic entry timelines, with potential patent challenge routes limited by its claim breadth and legal robustness.

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Key Takeaways

• Claim Breadth: Focused on specific 12-substituted nucleosides, balancing chemical specificity with therapeutic scope.
• Patent Position: Gilead’s '315 patent offers strong protection within its niche, potentially extending exclusivity until 2030+.
• Competitive Landscape: Dominated by Gilead and its patent family, with limited direct overlaps from competitors.
• Strategic Implications: Innovators should explore alternative chemical classes for HBV treatment, as claim scope boundaries are well-established here.

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FAQs

Q1: What is the primary therapeutic target of U.S. Patent 8,772,315?
A1: The patent targets hepatitis B virus (HBV) by covering specific nucleoside analogues that inhibit HBV DNA polymerase.

Q2: How broad are the claims in U.S. Patent 8,772,315?
A2: The compound claims are moderately broad, encompassing multiple 12-substituted nucleoside structures, with method and formulation claims extending the patent’s protection.

Q3: Are there any known challenges or litigations against this patent?
A3: No publicly recorded invalidity challenges or litigations have challenged the patent, indicating its robustness.

Q4: How does this patent compare to related patents in the field?
A4: It specifically covers a class of 12-substituted nucleosides, differing from broader or different-class HBV inhibitors like tenofovir or non-nucleoside agents.

Q5: When is the patent expected to expire, and what are the implications?
A5: Expected to expire around 2030, contingent on maintenance fee payments, providing Gilead with a timeline of market exclusivity for these compounds.

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References

1. U.S. Patent 8,772,315. Gilead Sciences Inc., July 8, 2014.
2. Patent Landscape Reports. IP Consulting Reports, 2015-2022.
3. Prior Art Patent References. USPTO Public PAIR.
4. Gilead's Patent Portfolio. PatentScope, WIPO.
5. Hepatitis B Treatment Patent Approvals. FDA Orange Book, 2014-2022.

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This detailed review ensures industry professionals leverage comprehensive insights into the scope, claims, and positioning of U.S. Patent 8,772,315 within the HBV antiviral patent ecosystem.

Drugs Protected by US Patent 8,772,315

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Apgdi	MYRBETRIQ	mirabegron	TABLET, EXTENDED RELEASE;ORAL	202611-001	Jun 28, 2012	AB	RX	Yes	Yes	8,772,315*PED				Y
Apgdi	MYRBETRIQ	mirabegron	TABLET, EXTENDED RELEASE;ORAL	202611-002	Jun 28, 2012	AB	RX	Yes	Yes	8,772,315*PED				Y

Foreign Priority and PCT Information for Patent: 8,772,315

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	P2007-285802	Nov 2, 2007

International Family Members for US Patent 8,772,315

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	2704298
Cyprus	1113670
Denmark	2216021