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-three patent family members in forty-four countries.

Summary for Patent: 8,486,975

Title:	Non-nucleoside reverse transcriptase inhibitors
Abstract:	Heteroaromatic compounds of Formula I: ##STR00001## are HIV reverse transcriptase inhibitors, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 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):	Burch; Jason (Redwood City, CA), Cote; Bernard (Notre-Dame-de-I'lle-Perrot, CA)
Assignee:	Merck Canada Inc. (Kirkland, Quebec, CA)
Application Number:	13/073,631
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope and Claims of United States Patent 8,486,975

Introduction

United States Patent 8,486,975, titled "Non-nucleoside reverse transcriptase inhibitors," is a significant patent in the field of HIV treatment. This patent, issued to Merck Canada Inc., covers crucial compounds and methods for the treatment and prophylaxis of HIV-mediated diseases.

Inventors and Assignees

The patent was invented by Jason Burch and Bernard Cote and is assigned to Merck Canada Inc.[2][5].

Issue and Expiration Dates

The patent was issued on July 16, 2013, and its original expiration date is October 7, 2031. However, due to a patent term extension, the expiration date has been extended to August 30, 2032[2][5].

Claims and Scope

Non-Nucleoside Reverse Transcriptase Inhibitors

The patent covers a class of compounds known as non-nucleoside reverse transcriptase inhibitors (NNRTIs), which are essential for the treatment of HIV. These compounds are designed to inhibit the reverse transcriptase enzyme, a critical component in the HIV replication process[1].

Chemical Compounds

The patent describes specific heteroaromatic compounds, including detailed chemical formulas and structures. For example, compounds like 3-chloro-5-[4-(1,1-difluoroethyl)-1-[(4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-2-oxopyridin-3-yl]oxybenzonitrile are outlined[1].

Pharmaceutical Compositions

The patent also includes claims related to pharmaceutical compositions containing these compounds, either alone or in combination with other antiretroviral drugs. This is evident in the trade names PIFELTRO® (doravirine) and DELSTRIGO® (doravirine, lamivudine, and tenofovir disoproxil fumarate)[2].

Patent Term Extension

The patent has been granted a term extension under 35 U.S.C. 156 due to the regulatory review period (RRP) associated with the FDA approval process. The extension period was determined to be 328 days, although a longer period of 1,092 days (3.0 years) was calculated based on the RRP. However, only the portion of the RRP occurring after the patent's issue date was considered[2].

Regulatory Review Period

The FDA determined the regulatory review period for PIFELTRO and DELSTRIGO, which started on September 9, 2011, and continued until the patent's issue date on July 16, 2013. This period is crucial for calculating the patent term extension[2][4].

Exclusivity and Market Rights

In addition to the patent protection, the FDA has granted exclusivity rights for these drugs. For instance, the exclusivity for PIFELTRO and DELSTRIGO runs concurrently with the patent and has specific expiration dates, such as January 27, 2025, for new patient populations[5].

Patent Landscape

Broad vs. Narrow Patents

The scope of this patent is significant because it covers a broad range of compounds and their uses. Broad patents, like this one, offer more protection against infringers as they are harder to design around compared to narrow patents[3].

Number of Claims and Scope

The patent includes multiple claims, with independent claims defining the broadest scope of protection. Dependent claims serve as narrower fallback positions. The number of claims can indicate the complexity and value of the technology but does not necessarily reflect the breadth of the patent's scope[3].

Patent Technology Centers

The USPTO organizes patents into technology centers and art units, which help in examining and categorizing patents. This patent falls under the biotechnology and organic chemistry category, reflecting its technical area[3].

Impact on HIV Treatment

Clinical Significance

The compounds covered by this patent are crucial in the treatment of HIV, offering effective non-nucleoside reverse transcriptase inhibitors. Drugs like doravirine have shown significant efficacy in clinical trials, making them valuable additions to the antiretroviral therapy arsenal[2].

Market Dominance

The patent and exclusivity rights granted to Merck Canada Inc. provide a competitive edge in the market for HIV treatments. This dominance is further reinforced by the patent term extension, ensuring exclusive rights for a longer period[2][5].

Challenges and Considerations

Regulatory Approval

The regulatory approval process, which includes the RRP, is a critical factor in determining the patent term extension. Delays in this process can impact the effective patent life and exclusivity period[2][4].

Generic Competition

The expiration of the patent and exclusivity rights will eventually open the market to generic competition. However, the current patent term extension and exclusivity periods delay this competition, allowing Merck to maintain market exclusivity for a longer period[5].

Key Takeaways

• Patent Scope: The patent covers a broad range of non-nucleoside reverse transcriptase inhibitors and their pharmaceutical compositions.
• Patent Term Extension: The patent has been extended by 328 days due to the regulatory review period.
• Exclusivity: FDA-granted exclusivity rights run concurrently with the patent, providing additional market protection.
• Clinical Impact: The compounds are significant in HIV treatment, with drugs like doravirine showing high efficacy.
• Market Dominance: The patent and exclusivity rights ensure Merck's competitive edge in the HIV treatment market.

FAQs

What are non-nucleoside reverse transcriptase inhibitors (NNRTIs)?

NNRTIs are a class of antiretroviral drugs that inhibit the reverse transcriptase enzyme, crucial for HIV replication.

What are the trade names of the drugs covered by this patent?

The trade names are PIFELTRO® (doravirine) and DELSTRIGO® (doravirine, lamivudine, and tenofovir disoproxil fumarate).

Why was the patent term extended?

The patent term was extended due to the regulatory review period associated with the FDA approval process.

What is the significance of FDA-granted exclusivity?

FDA-granted exclusivity provides sole marketing rights to the manufacturer, running concurrently with the patent and delaying generic competition.

When does the patent and exclusivity expire?

The patent expires on August 30, 2032, and the exclusivity for new patient populations expires on January 27, 2025.

Cited Sources

1. US8486975B2 - Non-nucleoside reverse transcriptase inhibitors - Google Patents
2. NOTICE OF FINAL DETERMINATION - Regulations.gov
3. The Ways We've been Measuring Patent Scope are Wrong: - Boston University Law
4. Determination of Regulatory Review Period for Purposes of Patent Extension - Federal Register
5. Generic Pifeltro Availability - Drugs.com

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			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			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			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			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			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			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