Details for Patent: 7,858,643

Which drugs does patent 7,858,643 protect, and when does it expire?

Patent 7,858,643 protects XALKORI and is included in two NDAs.

This patent has fifty-two patent family members in forty-five countries.

Summary for Patent: 7,858,643

Title:	Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
Abstract:	Enantiomerically pure compound of formula 1 ##STR00001## are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
Inventor(s):	Cui; Jingrong Jean (San Diego, CA), Funk; Lee Andrew (Oceanside, CA), Jia; Lei (San Diego, CA), Kung; Pei-Pei (San Diego, CA), Meng; Jerry Jialun (San Diego, CA), Nambu; Mitchell David (San Diego, CA), Pairish; Mason Alan (San Diego, CA), Shen; Hong (San Diego, CA), Tran-Dube; Michelle (La Jolla, CA)
Assignee:	Agouron Pharmaceuticals, Inc. (San Diego, CA)
Application Number:	11/212,331
Patent Claim Types: see list of patent claims	Compound; Composition;

Detailed Analysis of the Scope and Claims of United States Patent 7,858,643

Introduction

United States Patent 7,858,643, titled "Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors," was granted on December 28, 2010. This patent is crucial in the field of pharmaceuticals, particularly in the development of cancer treatments.

Inventors and Assignee

The patent was invented by Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, and Michelle Tran-Dube. The assignee of this patent is Agouron Pharmaceuticals, Inc., which is now a part of Pfizer Inc.[2][4].

Scope of the Patent

This patent covers enantiomerically pure aminoheteroaryl compounds that act as potent inhibitors of protein kinases, specifically targeting the c-MET (hepatocyte growth factor receptor) kinase. These compounds are designed to treat abnormal cell growth, such as cancer, in mammals.

Chemical Structure and Synthesis

The patent describes the chemical structure of the compounds, which include various heteroaryl groups and specific substitutions. The synthesis methods for these compounds are also detailed, involving several chemical reactions and purification steps[1][4].

Biological Activity

The compounds are characterized by their high inhibitory activity against c-MET kinase, with some having a Ki (inhibition constant) of less than 5 μM, 2 μM, 1 μM, 500 nM, 200 nM, or 100 nM. This high potency makes them promising candidates for cancer therapy[1].

Claims of the Patent

The patent includes several claims that define the scope of protection:

Compound Claims

• Claims cover the enantiomerically pure compounds of a specific formula, including various substitutions and modifications.
• These compounds are defined by their chemical structure and stereochemistry[1][4].

Method Claims

• Methods for synthesizing these compounds are claimed, including specific reaction steps and conditions.
• Methods for using these compounds in the treatment of abnormal cell growth, particularly cancer, are also included[1][4].

Composition Claims

• Compositions containing the enantiomerically pure compounds, either as salts or in combination with other therapeutic agents, are claimed.
• These compositions are intended for use in pharmaceutical formulations[1][4].

Patent Landscape Analysis

Competitor Identification

Patent landscape analysis helps identify key competitors in the field of protein kinase inhibitors. Companies like Pfizer Inc., through its subsidiary Agouron Pharmaceuticals, are major players. This analysis also reveals other inventors and assignees working on similar technologies[3].

Patent Expiration Dates

The patent 7,858,643 is set to expire on October 8, 2029. Understanding the expiration dates of related patents, such as 7,230,098 (expiring August 26, 2025) and 8,217,057 (expiring November 6, 2029), is crucial for strategic planning and potential generic drug development[2].

Technological Trends

The patent landscape in this area shows a trend towards developing highly specific and potent kinase inhibitors. This trend is driven by the need for more effective cancer treatments with fewer side effects. The analysis also highlights mergers and acquisitions, licensing activities, and litigation in the sector[3].

Market Developments

Patent landscape studies reveal market developments such as new product launches, partnerships, and regulatory approvals. For instance, the approval of Xalkori (crizotinib), which targets c-MET and ALK kinases, is a significant market development in this field[2].

Tools and Strategies for Patent Landscape Analysis

Data Sources

Data for patent landscape analysis can be collected from various sources, including the United States Patent and Trademark Office (USPTO), the World Intellectual Property Organization (WIPO), and the European Patent Office (EPO)[3].

Search Strategies

A well-defined search strategy is essential, involving the use of specific keywords, patent class codes, and collaboration with technical and market experts. This ensures that all relevant patents and technical literature are included in the analysis[3].

Report Generation

The final step involves generating a comprehensive report with statistical figures and graphs. This report should be easy to interpret and provide valuable insights into the patent landscape, including patent trends, competitor activities, and market developments[3].

Key Takeaways

• Compound Specificity: The patent covers highly specific enantiomerically pure aminoheteroaryl compounds with potent inhibitory activity against c-MET kinase.
• Therapeutic Use: These compounds are intended for the treatment of abnormal cell growth, particularly cancer.
• Expiration Dates: The patent expires on October 8, 2029, which is crucial for planning generic drug development and licensing strategies.
• Market Trends: The patent landscape analysis reveals trends towards more specific and potent kinase inhibitors, driven by the need for effective cancer treatments.
• Competitor Analysis: Identifying key competitors and their activities is essential for strategic planning and market positioning.

FAQs

What is the main subject of United States Patent 7,858,643?

The main subject of this patent is enantiomerically pure aminoheteroaryl compounds that act as protein kinase inhibitors, specifically targeting the c-MET kinase.

Who are the inventors and assignee of this patent?

The inventors include Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, and Michelle Tran-Dube. The assignee is Agouron Pharmaceuticals, Inc., now part of Pfizer Inc.

What is the significance of the expiration date of this patent?

The expiration date (October 8, 2029) is significant for planning generic drug development, licensing strategies, and understanding the competitive landscape in the pharmaceutical industry.

How does patent landscape analysis help in this field?

Patent landscape analysis helps in identifying competitors, understanding technological trends, and making informed decisions about research and development investments, licensing strategies, and market positioning.

What are some of the key trends in the patent landscape for protein kinase inhibitors?

Key trends include the development of highly specific and potent kinase inhibitors, driven by the need for more effective cancer treatments with fewer side effects.

Cited Sources

1. United States Patent and Trademark Office, "Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors," US7858643B2, December 28, 2010.
2. Drugs.com, "Generic Xalkori Availability," November 6, 2024.
3. Sagacious Research, "Navigating Technological Domains with Patent Landscape Analysis."
4. Google Patents, "Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors," US7858643B2.

Drugs Protected by US Patent 7,858,643

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pf Prism Cv	XALKORI	crizotinib	CAPSULE, PELLETS;ORAL	217581-001	Sep 7, 2023		RX	Yes	No			Y	Y
Pf Prism Cv	XALKORI	crizotinib	CAPSULE, PELLETS;ORAL	217581-002	Sep 7, 2023		RX	Yes	No			Y	Y
Pf Prism Cv	XALKORI	crizotinib	CAPSULE, PELLETS;ORAL	217581-003	Sep 7, 2023		RX	Yes	Yes			Y	Y
Pf Prism Cv	XALKORI	crizotinib	CAPSULE;ORAL	202570-001	Aug 26, 2011		RX	Yes	No			Y	Y
Pf Prism Cv	XALKORI	crizotinib	CAPSULE;ORAL	202570-002	Aug 26, 2011		RX	Yes	Yes			Y	Y

International Family Members for US Patent 7,858,643

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1786785		PA2013005	Lithuania
European Patent Office	1786785		CA 2013 00009	Denmark
European Patent Office	1786785		92155	Luxembourg
European Patent Office	1786785		C300587	Netherlands
European Patent Office	1786785		C20130007 00075	Estonia