Details for Patent: 6,878,717

Summary for Patent: 6,878,717

Title:	HIV replication inhibiting pyrimidines
Abstract:	This invention concerns the use of compounds of formula: ##STR1## the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a.sup.1 =-a.sup.2 -a.sup.3 =a.sup.4 - forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R.sup.1 is hydrogen, aryl, formyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy-carbonyl, substituted C.sub.1-6 alkyl, or substituted C.sub.1-6 alkyloxyC.sub.1-6 alkylcarbonyl; each R.sup.2 independently is hydroxy, halo, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, --S(.dbd.O).sub.p R.sup.6, --NH--S(.dbd.O).sub.p R.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl or C.sub.3-7 cycloalkyl; or L is --X--R.sup.3 wherein R.sup.3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is --NR.sup.1 --, --NH--NH--, --N.dbd.N--, --O--, --C(.dbd.O)--, --CHOH--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2 --; Q is hydrogen, C.sub.1-6 alkyl, halo, polyhalo-C.sub.1-6 alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C.sub.3-7 cycloalkyl, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, --S(.dbd.O).sub.p R.sup.6, --NH--S(.dbd.O).sub.p R.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
Inventor(s):	De Corte; Bart (Southampton, PA), De Jonge; Marc Rene (5045 CA Tilburg, NL), Heeres; Jan (Vosselaar, BE), Ho; Chih Yung (Lansdale, PA), Janssen; Paul Adriaan Jan (B2350 Vosselaar, BE), Kavash; Robert W. (Maple Glen, PA), Koymans; Lucien Maria Henricus (B-2300 Turnhout, BE), Kukla; Michael Joseph (Maple Glen, PA), Ludovici; Donald William (Quakertown, PA), Van Aken; Koen Jeanne Alfons (B-2300 Turnhout, BE)
Assignee:
Application Number:	09/430,966
Patent Claim Types: see list of patent claims	Use; Compound;

United States Patent 6,878,717: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 6,878,717, titled "HIV replication inhibiting pyrimidines," is a significant patent in the field of pharmaceuticals, particularly in the treatment of HIV. This patent, issued on April 12, 2005, is part of a broader portfolio of intellectual property related to antiretroviral therapies.

Background and Inventors

The patent was invented by a team of researchers including Bart De Corte, Chih Yung Ho, Robert W. Kavash, Michael Joseph Kukla, and Donald William Ludovici, among others. These inventors were affiliated with Janssen Pharmaceutica, Inc., a company known for its innovative pharmaceutical products[1][4].

Scope of the Patent

The patent covers a class of compounds known as pyrimidines, which are designed to inhibit HIV replication. Specifically, it includes claims related to the active ingredients, pharmaceutical formulations, and methods of using these compounds to treat HIV.

Claims Overview

The patent includes a total of 32 claims, which can be categorized into several key areas:

• Claims 1-5, 9, 11, 15, 21, 22, and 26-32: These claims pertain to the specific chemical structures of the pyrimidine compounds, their pharmaceutical formulations, and combinations with other retroviral compounds[1].

Active Ingredients and Formulations

The patent focuses on etravirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI), which is a crucial component in the treatment of HIV. The claims cover various aspects of etravirine, including its chemical structure, synthesis methods, and pharmaceutical formulations[4].

Methods of Use

In addition to the compounds and formulations, the patent also claims methods of using these pyrimidines to treat HIV. This includes dosing regimens and combinations with other antiretroviral drugs[1].

Patent Landscape

The patent landscape surrounding U.S. Patent 6,878,717 is complex and involves several related patents and applications.

Related Patents

• U.S. Patent 7,037,917: This patent is a continuation of U.S. Patent 6,878,717 and claims priority to earlier applications. It also covers etravirine and related compounds, ensuring a broader protection for the inventors and assignees[1].
• Other Patents in the Family: The patent is part of a larger family of patents that cover various aspects of HIV treatment, including other antiretroviral compounds and formulations.

Ownership and Assignments

The patent is owned by Janssen Pharmaceutica, Inc., and has undergone several assignments and recordations in the U.S. Patent and Trademark Office. The chain of title includes assignments from the inventors to Janssen Pharmaceutica, Inc., and subsequent assignments to Janssen Pharmaceutica N.V.[1].

Inventorship and Contribution

Determining the true and only inventors is crucial in U.S. patent law. For U.S. Patent 6,878,717, the inventors listed have contributed to the conception and reduction to practice of the patentable subject matter. This involves both the idea or subject matter of the patent claims and the actual implementation or testing of these ideas[2].

Patent Scope and Claims Analysis

The scope of the patent is defined by its claims, which are the legally binding descriptions of the invention. The claims in U.S. Patent 6,878,717 are detailed and specific, ensuring broad protection for the inventors while also providing clear boundaries for what is considered infringing.

Claim Dependency

The claims in the patent are structured in a way that some claims depend on others. This dependency is crucial for understanding the full scope of the patent and how different claims interact with each other[3].

Economic and Legal Implications

The issuance and maintenance of U.S. Patent 6,878,717 have significant economic and legal implications.

Market Impact

The patent has played a critical role in the development and marketing of etravirine, a drug that has improved the treatment options for HIV patients. The exclusivity provided by the patent has allowed Janssen Pharmaceutica to recoup its investment in research and development.

Legal Challenges

Patents in the pharmaceutical sector often face legal challenges, including disputes over inventorship, patent validity, and infringement. The patent has likely been subject to various legal reviews and challenges, given its importance in the HIV treatment landscape[5].

Maintenance and Extension

The patent's term and maintenance are critical for its continued validity. The first maintenance fee payment for U.S. Patent 6,878,717 was due in 2009, and subsequent fees would have been required to maintain the patent's validity. There was also a terminal disclaimer filed to ensure that the patent did not extend beyond the expiration date of the full statutory term defined by earlier related patents[1].

Conclusion and Key Takeaways

• Inventors and Assignees: The patent was invented by a team of researchers affiliated with Janssen Pharmaceutica, Inc.
• Scope and Claims: The patent covers pyrimidine compounds, specifically etravirine, and includes claims related to active ingredients, formulations, and methods of use.
• Patent Landscape: The patent is part of a larger family of patents related to HIV treatment and has undergone several assignments and recordations.
• Economic and Legal Implications: The patent has significant economic and legal implications, including market impact and potential legal challenges.
• Maintenance and Extension: The patent's term and maintenance are crucial for its continued validity.

Key Takeaways

• U.S. Patent 6,878,717 is a critical patent in the treatment of HIV, covering etravirine and related compounds.
• The patent's scope is defined by its detailed claims, which include chemical structures, formulations, and methods of use.
• The patent is owned by Janssen Pharmaceutica, Inc., and has undergone several legal and administrative processes.
• The economic and legal implications of the patent are significant, influencing both the market and legal landscapes.

Frequently Asked Questions (FAQs)

What is the main subject matter of U.S. Patent 6,878,717?

The main subject matter of U.S. Patent 6,878,717 is the class of compounds known as pyrimidines, specifically etravirine, which are designed to inhibit HIV replication.

Who are the inventors of U.S. Patent 6,878,717?

The inventors of U.S. Patent 6,878,717 include Bart De Corte, Chih Yung Ho, Robert W. Kavash, Michael Joseph Kukla, and Donald William Ludovici, among others.

What is the significance of the claims in U.S. Patent 6,878,717?

The claims in U.S. Patent 6,878,717 are crucial as they define the scope of the patent, including the chemical structures of the pyrimidine compounds, their pharmaceutical formulations, and methods of use.

How does U.S. Patent 6,878,717 fit into the broader patent landscape?

U.S. Patent 6,878,717 is part of a larger family of patents related to HIV treatment and is closely related to other patents such as U.S. Patent 7,037,917.

What are the economic implications of U.S. Patent 6,878,717?

The patent has significant economic implications, including the exclusivity it provides for Janssen Pharmaceutica to market etravirine, which helps in recouping research and development investments.

Cited Sources

1. IN THE UNITED STATES PATENT AND TRADEMARK OFFICE - Application for Extension of U.S. Patent No. 7,037,917[1].
2. Determining Inventorship for US Patent Applications - Oregon State University[2].
3. Patent Claims Research Dataset - USPTO[3].
4. US6878717B2 - HIV replication inhibiting pyrimidines - Google Patents[4].
5. AI VISUALIZE, INC. v. NUANCE COMMUNICATIONS, INC. - Court of Appeals for the Federal Circuit[5].

Drugs Protected by US Patent 6,878,717

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 6,878,717

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	PCT/EP 99/07417	Sep 24, 1999

International Family Members for US Patent 6,878,717

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1002795		PA2008016	Lithuania
European Patent Office	1002795		CA 2009 00004	Denmark
European Patent Office	1002795		300373	Netherlands
European Patent Office	1002795		91528	Luxembourg
European Patent Office	1002795		PA2008016,C1002795	Lithuania