Details for Patent: 7,169,780

Which drugs does patent 7,169,780 protect, and when does it expire?

Patent 7,169,780 protects ISENTRESS, DUTREBIS, and ISENTRESS HD, and is included in four NDAs.

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

This patent has forty-nine patent family members in thirty-four countries.

Summary for Patent: 7,169,780

Title:	N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
Abstract:	N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula (I): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described ##STR00001##
Inventor(s):	Crescenzi; Benedetta (Rome, IT), Gardelli; Cristina (Ariccia, IT), Muraglia; Ester (Rome, IT), Orvieto; Federica (Rome, IT), Pace; Paola (Rome, IT), Pescatore; Giovanna (Cosenza, IT), Petrocchi; Alessia (Rome, IT), Poma; Marco (Grosseto, IT), Rowley; Michael (Axa, IT), Scarpelli; Rita (Rome, IT), Summa; Vincenzo (Velletri, IT), Nizi; Emanuela (Siena, IT)
Assignee:	Istitute Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. (Pomezia, IT)
Application Number:	10/493,280
Patent Claim Types: see list of patent claims	Compound; Composition;

United States Patent 7,169,780: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 7,169,780, granted to Nils O. Krieder and Michael A. Macken in November 2008, is a significant patent in the biopharmaceutical industry. This patent is associated with Merck's blockbuster HIV drug, ISENTRESS, and its variants. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Patent Overview

Invention Description

The patent is directed to N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their pharmaceutically acceptable salts. These compounds are identified as inhibitors of the HIV integrase enzyme, crucial for the replication of the HIV virus. The invention includes methods for synthesizing these compounds and their use in preventing or treating HIV infection and AIDS[4][5].

Scope of the Patent

Claims and Coverage

The patent includes multiple claims that cover various aspects of the invention:

• Compound Claims: The patent claims the N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their pharmaceutically acceptable salts.
• Method Claims: It includes methods for synthesizing these compounds and their use in medical treatments, specifically for inhibiting HIV integrase and treating or preventing HIV infection and AIDS[4][5].

Patent Family and Geographic Coverage

The patent has a broad geographic reach with forty-nine patent family members in thirty-four countries. This extensive coverage ensures that the invention is protected globally, which is critical for pharmaceuticals that are used worldwide[1].

Claims Analysis

Independent and Dependent Claims

The patent includes both independent and dependent claims. Independent claims define the broad scope of the invention, while dependent claims narrow down the scope by adding specific limitations. For example, the independent claims might cover the general structure of the compounds, while dependent claims could specify particular substituents or methods of synthesis[3].

Claim Length and Complexity

Research on patent claims suggests that the length and complexity of claims can impact the patent's scope and validity. Shorter, clearer independent claims are often associated with a higher probability of grant and shorter examination processes. However, the complexity of claims in this patent, given its technical nature, may have required more detailed and lengthy descriptions to ensure clarity and specificity[3].

Patent Landscape

Related Patents and Expiration Dates

The patent 7,169,780 is part of a larger patent portfolio related to ISENTRESS. Another significant patent, U.S. Patent No. 7,754,731, also covers processes for preparing potassium salts of the compound and their use in treating HIV. The '780 patent expired on October 3, 2023, while the '731 patent is set to expire on March 11, 2029[4].

Generic Competition

With the expiration of the '780 patent, generic versions of ISENTRESS are now eligible for approval. This opens the market to generic competitors, which can significantly impact the pricing and availability of the drug. Generic competition often leads to reduced prices and increased access to life-saving medications[4].

Litigation and Settlements

Hatch-Waxman Act and ANDA Litigations

Patents like 7,169,780 are often at the center of Abbreviated New Drug Application (ANDA) litigations under the Hatch-Waxman Act. These litigations involve generic manufacturers seeking to enter the market before the patent expires. Settlements in these cases can allow generic manufacturers to enter the market earlier, subject to certain conditions and agreements[2].

Impact on Biopharmaceutical Industry

Monoclonal Antibody Production

Although the '780 patent specifically deals with HIV integrase inhibitors, the broader context of biopharmaceutical innovation is relevant. The patent also mentions a technique for boosting monoclonal antibody production, which is crucial in the biopharmaceutical industry. This technique involves using dialysis to eliminate glycerol and replenish cell culture medium, optimizing cell growth and productivity[1].

Innovation and Patent Quality

The quality and scope of patents like 7,169,780 are critical for innovation in the biopharmaceutical sector. Debates around patent quality often focus on the breadth and clarity of claims. Narrower, clearer claims are generally seen as more beneficial for innovation as they reduce litigation costs and provide clearer boundaries for other inventors[3].

Regulatory Aspects

FDA Approvals and Labeling

The FDA plays a crucial role in approving drugs and their labeling. For ISENTRESS, the FDA approved new labeling in 2013, which included updates based on the patented compounds and their uses. Regulatory approvals and labeling are essential for ensuring the safe and effective use of pharmaceuticals[4].

Global Protection and Foreign Priority

PCT and Foreign Patents

The patent was filed under the Patent Cooperation Treaty (PCT) and has been granted in multiple countries. This global protection is vital for pharmaceutical companies to maintain their market position and prevent unauthorized use of their inventions worldwide[1].

Key Takeaways

• Patent Scope: The patent covers N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their use in treating HIV.
• Claims: The patent includes both independent and dependent claims, with a focus on compound structures and methods of synthesis.
• Expiration: The '780 patent expired on October 3, 2023, opening the market to generic competition.
• Global Protection: The patent has extensive global coverage through its patent family members.
• Regulatory Impact: FDA approvals and labeling updates are crucial for the safe and effective use of the drug.

FAQs

What is the main invention covered by U.S. Patent 7,169,780?

The main invention covered by U.S. Patent 7,169,780 is N-substituted 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides and their use as inhibitors of the HIV integrase enzyme.

Which drug is protected by this patent?

This patent protects Merck's HIV drug ISENTRESS and its variants, including DUTREBIS and ISENTRESS HD.

When did the patent expire?

The patent expired on October 3, 2023.

How does this patent impact the biopharmaceutical industry?

This patent is significant for the biopharmaceutical industry due to its role in treating HIV and AIDS. It also contributes to broader discussions on patent quality and innovation in the sector.

What is the significance of the PCT filing for this patent?

The PCT filing allowed for the patent to be granted in multiple countries, providing global protection for the invention.

How does the expiration of this patent affect generic competition?

The expiration of the patent allows generic manufacturers to enter the market, potentially reducing the price of the drug and increasing its availability.

Sources

1. DrugPatentWatch: Details for Patent: 7169780 - DrugPatentWatch
2. Robins Kaplan LLP: ANDA Litigation Settlements | Hatch-Waxman - Robins Kaplan LLP
3. Hoover Institution: Patent Claims and Patent Scope - Hoover Institution
4. IPWatchdog: FDA Approves New Labeling for Merck Blockbuster HIV Drug ...
5. Unified Patents: US-7169780-B2 - N-substituted Hydroxypyrimidinone Carboxamide ...

Drugs Protected by US Patent 7,169,780

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	ISENTRESS	raltegravir potassium	POWDER;ORAL	205786-001	Dec 20, 2013		RX	Yes	Yes
Msd Sub Merck	ISENTRESS	raltegravir potassium	TABLET, CHEWABLE;ORAL	203045-001	Dec 21, 2011		RX	Yes	No
Msd Sub Merck	ISENTRESS	raltegravir potassium	TABLET, CHEWABLE;ORAL	203045-002	Dec 21, 2011		RX	Yes	Yes
Merck Sharp Dohme	DUTREBIS	lamivudine; raltegravir potassium	TABLET;ORAL	206510-001	Feb 6, 2015		DISCN	No	No

Foreign Priority and PCT Information for Patent: 7,169,780

PCT Information
PCT Filed	October 21, 2002	PCT Application Number:	PCT/GB02/04753
PCT Publication Date:	May 01, 2003	PCT Publication Number:	WO03/035077

International Family Members for US Patent 7,169,780

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1441735		CA 2008 00021	Denmark
European Patent Office	1441735		91428	Luxembourg
European Patent Office	1441735		C20080001 00016	Estonia
European Patent Office	1441735		PA2008007	Lithuania