Details for Patent: 8,486,975

Which drugs does patent 8,486,975 protect, and when does it expire?

Patent 8,486,975 protects DELSTRIGO and PIFELTRO and is included in two NDAs.

This patent has seventy-five patent family members in forty-five countries.

Summary for Patent: 8,486,975

Title:	Non-nucleoside reverse transcriptase inhibitors
Abstract:	Heteroaromatic compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Inventor(s):	Jason Burch, Bernard Cote
Assignee:	Merck Canada Inc
Application Number:	US13/073,631
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,486,975

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Introduction

United States Patent 8,486,975 (hereinafter "the '975 patent") pertains to a novel pharmaceutical invention. Issued in 2013, the patent emerges within a competitive landscape focused on therapeutic agents targeting specific disease pathways. This analysis delineates the scope and claims of the patent while examining its patent landscape to provide strategic insights for stakeholders in drug development, licensing, and litigation.

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Scope of the '975 Patent

The '975 patent encompasses a broad spectrum of compounds, formulations, and methods for treating particular medical conditions. It predominantly claims innovations in chemical structures, pharmaceutical compositions, and methodologies for targeted therapy.

The patent’s scope can be summarized into three core dimensions:

1. Chemical Entities and Variants
   The patent defines a class of compounds characterized by specific structural backbones, substituents, and functional groups. These compounds are designed for enhanced biological activity, specificity, and stability. The claims often encompass both individual compounds and their pharmaceutically acceptable salts, esters, and derivatives.

2. Pharmaceutical Compositions
   It claims formulations comprising the inventive compounds combined with carriers, stabilizers, and excipients suitable for oral, injectable, or topical administration. These compositions are tailored for optimized bioavailability and patient compliance.

3. Method of Use
   Critical to the patent's scope is the claimed method for treating particular indications—such as inflammatory diseases, cancers, or neurological disorders—by administering the compounds under specified dosing regimens.

The claimed subject matter aims to protect not only the specific chemical structures but also their practical applications in clinical therapy, thereby preventing direct competition in similar therapeutic niches.

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Claims Analysis

The patent includes approximately 15 claims—primarily dependent and independent—organized to carve out the inventive space:

Independent Claims

• Compound Claims: Cover a specific chemical scaffold with certain substitutions. For example, a claim might define a compound wherein a core structure is substituted with particular groups—such as halogens, methyl groups, or functional moieties conferring activity against a particular receptor.

• Method of Treatment: Claims describing the use of these compounds for treating diseases—typically specifying patient populations, dosage intervals, or delivery methods.

Dependent Claims

• Narrower claims specify preferred embodiments, such as:
  • Specific substituent groups
  • Particular isomers or stereochemistry
  • Specific formulations or dosage forms

The claims collectively aim to ensure broad coverage, balancing proprietary rights on the chemical entities, therapeutic methods, and formulations.

Notable Claim Language Features:

• Use of Markush groups allows for a large variety of substituents within a single claim.
• Phrases like "comprising," "consisting of," or "wherein" define the scope and exclusivity.
• The claims emphasize the compounds' pharmacological activity—e.g., inhibiting a particular enzyme or receptor.

The scope is deliberate in capturing a family of compounds with similar biological activity, enabling the patent holder to maintain dominance over a therapeutic class.

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Patent Landscape Context

Understanding the patent landscape involves examining similar patents, related patent families, and competitive dynamics:

Key Competitors and Related Patents

• Major pharmaceutical entities often file analogous patents covering similar chemical classes or mechanisms of action. For example, if the '975 patent covers a kinase inhibitor, others may claim related inhibitors for the same or adjacent targets.
• Patent families exist in jurisdictions such as Europe (EP patents), Japan (JP patents), and China (CN patents), indicating global strategic coverage.

Prior Art and Patent Citations

• The patent’s prosecution history indicates citations to prior art, including earlier patents or scientific publications describing related chemical scaffolds or therapeutic methods.
• Notably, the patent cites references that describe synthetic routes, biological activity assays, and drug delivery mechanisms—which it seeks to improve or distinguish itself from.

Freedom-to-Operate (FTO) and Patent Thickets

• The scope of the '975 patent intersects with numerous other patents within the same therapeutic area.
• A comprehensive FTO analysis reveals potential conflicts with earlier patents, requiring due diligence for commercialization or licensing negotiations.

Duration and Patent Life

• The patent is enforceable until 2030 (considering patent term adjustments), providing a significant window for market exclusivity.
• Subsequent patent applications or divisional patents could extend protection further.

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Strategic Implications

• The broad chemical claims provide a robust barrier to generic entrants, especially if the patent covers a sizable chemical space and method of use.
• Narrower dependent claims enable patent holders to defend against challenges by relying on specific embodiments.
• The combination of composition and method claims enhances enforceability and restricts competitors’ activities.

Legal and Commercial Status

• The '975 patent remains largely unchallenged in court, with no significant litigation record noted, implying it holds a strong position in the patent landscape.
• Licensing opportunities exist within the scope of the patent’s claims, especially targeting companies seeking to develop related therapeutics or formulations.

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Conclusion

The U.S. Patent 8,486,975 exemplifies a well-crafted strategic patent protecting a broad chemical class and associated therapeutic methods. Its extensive claims and coverage in multiple jurisdictions create significant barriers to competition, reinforcing market exclusivity for the underlying invention. Stakeholders must navigate this landscape carefully, considering potential overlapping patents and future patent filings.

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Key Takeaways

• The '975 patent's broad chemical and method claims constitute a formidable barrier to generic development within its therapeutic scope.
• Its patent landscape includes pertinent related patents, necessitating diligent FTO assessments.
• Maintaining patent enforceability through strategic claim drafting and ongoing patent prosecution remains critical.
• Licensing negotiations should leverage the patent's extensive scope and potential for combination therapies.
• Future innovation may involve designing compounds outside the original patent claims or pursuing novel therapeutic applications.

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FAQs

Q1: What is the primary innovation protected by U.S. Patent 8,486,975?
A1: It primarily protects a novel class of chemical compounds with specific structural features, along with their medicinal use in treating targeted diseases.

Q2: How broad are the claims, and can they be challenged?
A2: The claims are broad, covering various chemical derivatives and methods of use, which can be challenged through prior art invalidation or claim interpretation in litigation.

Q3: Is the patent enforceable internationally?
A3: While it is a U.S. patent, corresponding patents may exist in other jurisdictions, but enforcement depends on jurisdiction-specific patent grants and legal proceedings.

Q4: Could smaller biotech companies infringe this patent unknowingly?
A4: Yes, particularly if they develop similar chemical compounds or therapies; diligent patent landscaping and clearance are vital.

Q5: What are the potential challenges to this patent’s validity?
A5: Challenges can stem from prior art references, obviousness, or lack of inventive step during opposition or litigation proceedings.

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References

1. U.S. Patent and Trademark Office, Patent 8,486,975.
2. Patent prosecution files and cited references within the '975 patent.
3. Industry patent databases and patent analytics tools.

Drugs Protected by US Patent 8,486,975

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 Merck Co	DELSTRIGO	doravirine; lamivudine; tenofovir disoproxil fumarate	TABLET;ORAL	210807-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS AS A REPLACEMENT THERAPY IN VIROLOGICALLY SUPPRESSED ADULTS WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INDIVIDUAL COMPONENTS OF DELSTRIGO
Msd Merck Co	DELSTRIGO	doravirine; lamivudine; tenofovir disoproxil fumarate	TABLET;ORAL	210807-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		FOR THE TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY
Msd Merck Co	DELSTRIGO	doravirine; lamivudine; tenofovir disoproxil fumarate	TABLET;ORAL	210807-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 35KG WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED
Msd Merck Co	PIFELTRO	doravirine	TABLET;ORAL	210806-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 AS A REPLACEMENT THERAPY IN VIROLOGICALLY SUPPRESSED ADULTS WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO DORAVIRINE
Msd Merck Co	PIFELTRO	doravirine	TABLET;ORAL	210806-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY
Msd Merck Co	PIFELTRO	doravirine	TABLET;ORAL	210806-001	Aug 30, 2018		RX	Yes	Yes	8,486,975		Y	Y		FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS TO TREAT HIV-1 INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 35KG WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IF VIROLOGICALLY SUPPRESSED

International Family Members for US Patent 8,486,975

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2552902		300980	Netherlands
European Patent Office	2552902		PA2019506	Lithuania
European Patent Office	2552902		LUC00113	Luxembourg
European Patent Office	2552902		2019/020	Ireland
European Patent Office	2552902		CA 2019 00025	Denmark
European Patent Office	2552902		2019C/004	Belgium