Details for Patent: 8,410,103

Which drugs does patent 8,410,103 protect, and when does it expire?

Patent 8,410,103 protects APRETUDE, CABENUVA KIT, and VOCABRIA, and is included in three NDAs.

This patent has one hundred and twenty-five patent family members in thirty-three countries.

Summary for Patent: 8,410,103

Title:	(3S,11aR)-N-[2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5- ,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide useful as anti-HIV agent
Abstract:	The present invention is directed to a substituted 2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2 -a]pyrido[1,2-d]pyrazine-5,7-dione useful as an anti-HIV agent, which has the formula: ##STR00001## as well as pharmaceutically acceptable salts thereof, compostions thereof, and methods of use thereof.
Inventor(s):	Johns; Brian Alvin (Research Triangle Park, NC), Kawasuji; Takashi (Osaka, JP), Taishi; Teruhiko (Osaka, JP), Taoda; Yoshiyuki (Osaka, JP)
Assignee:	Shionogi & Co., Ltd. (Osaka, JP) VIIV Healthcare Company (Research Triangle Park, NC)
Application Number:	13/352,686
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope and Claims of United States Patent 8,410,103

Introduction

United States Patent 8,410,103, issued on April 2, 2013, is a significant patent in the field of antiviral medications, particularly for the treatment of HIV. This patent is held by Shionogi & Co., Ltd. and ViiV Healthcare Company.

Inventors and Assignees

The inventors of this patent include Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, and Yoshiyuki Taoda. The assignees are Shionogi & Co., Ltd. and ViiV Healthcare Company, with the latter being based in Research Triangle Park, NC, and the former in Osaka, Japan[1][2].

Patent Description

The patent describes a novel compound with the formula (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide. This compound is useful as an HIV integrase inhibitor, which is crucial in the treatment and prevention of HIV infections[1][2].

Claims

The patent includes seven claims that cover the compound itself, its pharmaceutically acceptable salts, compositions containing the compound, and methods of use for treating or preventing HIV infections. Here are some key aspects of the claims:

• Compound Claims: The patent claims the specific chemical structure of the compound and its isomers.
• Salt Claims: It includes claims for pharmaceutically acceptable salts of the compound.
• Composition Claims: The patent covers pharmaceutical compositions that contain the compound, either alone or in combination with other antiretroviral agents.
• Method Claims: It claims methods for treating or preventing HIV infections using the compound[1].

Patent Expiration

The patent is set to expire on April 28, 2026. This expiration date is crucial for understanding when generic versions of the drug could potentially enter the market[2].

Related Patents

There are several related patents that extend the protection of this compound and its uses:

• Patent 10,927,129: Issued on February 23, 2021, this patent also covers the same compound and its use as an HIV integrase inhibitor, with an expiration date of April 28, 2026[2].
• Patent 11,224,597: Issued on January 18, 2022, this patent relates to pharmaceutical compositions of the compound, with an expiration date of September 15, 2031[2].
• Patent 11,389,447: This patent has an expiration date of June 30, 2027, and is part of the broader patent landscape protecting this compound and its uses[2].

Patent Landscape

The patent landscape surrounding this compound is complex and involves multiple patents and claims. Here are some key points:

• Drug Patent: The patent assigns exclusive legal rights to the inventors and assignees, protecting the proprietary chemical formulation. Patents typically expire 20 years from the date of filing, but can be extended or adjusted based on various factors[2].
• Drug Exclusivity: In addition to patent protection, the FDA may grant exclusivity periods that can run simultaneously with the patent. These periods can vary from 180 days to seven years, depending on the circumstances[2].

Patent Analytics

To fully understand the scope and claims of this patent, patent analytics can be employed. This involves analyzing the claims and scope concepts to identify gaps or opportunities in the intellectual property protection. Tools like Claim Coverage Matrix and Claim Charts can help in categorizing and analyzing large numbers of patent claims, making it easier to determine the coverage and value of the patent claims[3].

Impact on HIV Treatment

The compound described in this patent is a significant advancement in HIV treatment. As an HIV integrase inhibitor, it plays a crucial role in preventing the integration of HIV DNA into the host cell's genome, thereby inhibiting the replication of the virus. This makes it an essential component in antiretroviral therapy (ART) regimens.

"HIV integrase inhibitors are a class of antiretroviral drugs designed to block the action of integrase, a viral enzyme that integrates the genetic material of the virus into the host cell's DNA. This class of drugs has been a game-changer in the treatment of HIV, offering a new mechanism of action that can be used in combination with other antiretroviral agents to achieve viral suppression"[4].

Market and Generic Availability

Currently, there is no therapeutically equivalent generic version of the drug available in the United States. The expiration of the patent in 2026 will likely open the market to generic versions, assuming no further extensions or adjustments to the patent term[2].

Conclusion

United States Patent 8,410,103 is a critical patent in the field of HIV treatment, protecting a novel compound with significant antiviral activity. Understanding the scope and claims of this patent, along with its related patents and the broader patent landscape, is essential for pharmaceutical companies and researchers. The expiration of this patent in 2026 will mark an important milestone in the availability of generic versions of this crucial antiretroviral medication.

Key Takeaways

• Compound Description: The patent describes a specific compound with HIV integrase inhibitory activity.
• Claims: The patent includes claims for the compound, its salts, compositions, and methods of use.
• Expiration Date: The patent expires on April 28, 2026.
• Related Patents: Several related patents extend the protection of the compound and its uses.
• Patent Landscape: The patent landscape is complex, involving multiple patents and claims.
• Impact on HIV Treatment: The compound is a significant advancement in HIV treatment as an integrase inhibitor.

FAQs

Q: What is the main compound described in United States Patent 8,410,103?

A: The main compound is (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide.

Q: Who are the inventors and assignees of this patent?

A: The inventors include Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, and Yoshiyuki Taoda. The assignees are Shionogi & Co., Ltd. and ViiV Healthcare Company.

Q: What is the expiration date of this patent?

A: The patent is set to expire on April 28, 2026.

Q: What is the significance of this compound in HIV treatment?

A: The compound is an HIV integrase inhibitor, crucial in preventing the integration of HIV DNA into the host cell's genome, thereby inhibiting the replication of the virus.

Q: Are there any related patents that extend the protection of this compound?

A: Yes, there are several related patents, including Patent 10,927,129 and Patent 11,224,597, which extend the protection and uses of the compound.

Cited Sources

1. United States Patent and Trademark Office, "United States Patent US 8,410,103 B2," April 2, 2013.
2. Drugs.com, "Generic Cabenuva Availability," November 6, 2024.
3. SLWIP, "Patent Analytics," accessed December 20, 2024.
4. DrugBank Online, "Rilpivirine: Uses, Interactions, Mechanism of Action," March 14, 2013.

Drugs Protected by US Patent 8,410,103

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Viiv Hlthcare	APRETUDE	cabotegravir	SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	215499-001	Dec 20, 2021		RX	Yes	Yes	8,410,103		Y	Y
Viiv Hlthcare	CABENUVA KIT	cabotegravir; rilpivirine	SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212888-001	Jan 21, 2021		RX	Yes	Yes	8,410,103		Y	Y		TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
Viiv Hlthcare	CABENUVA KIT	cabotegravir; rilpivirine	SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212888-002	Jan 21, 2021		RX	Yes	Yes	8,410,103		Y	Y		TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
Viiv Hlthcare	VOCABRIA	cabotegravir sodium	TABLET;ORAL	212887-001	Jan 21, 2021		RX	Yes	Yes	8,410,103		Y	Y		TREATMENT OF HIV-1 IN AN ADULT IN COMBINATION WITH RILPIVIRINE
Viiv Hlthcare	VOCABRIA	cabotegravir sodium	TABLET;ORAL	212887-001	Jan 21, 2021		RX	Yes	Yes	8,410,103		Y	Y		TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG

Foreign Priority and PCT Information for Patent: 8,410,103

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2005-131161	Apr 28, 2005
Japan	2005-312076	Oct 27, 2005

International Family Members for US Patent 8,410,103

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1874117		C300676	Netherlands
European Patent Office	1874117		CA 2014 00032	Denmark
European Patent Office	1874117		PA2014021	Lithuania
European Patent Office	1874117		1490036-9	Sweden
European Patent Office	1874117		C20140020 00130	Estonia
European Patent Office	1874117		14C0041	France