United States Patent 11,091,440: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 11,091,440, titled "Malate Salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and Crystalline Forms Thereof for the Treatment of Cancer," is a critical patent held by Exelixis, Inc. This patent is part of a broader portfolio related to the drug CABOMETYX®, used in the treatment of various cancers. Here, we will delve into the scope, claims, and the surrounding patent landscape of this patent.
Patent Overview
Inventors and Applicants
The patent was invented by Adrian St. Clair Brown, Ely (GB); Peter Lamb, Oakland, CA (US); and William P. Gallagher, Princeton, NJ (US), with Exelixis, Inc., Alameda, CA (US) as the applicant[4].
Filing and Issue Dates
The patent application was filed on January 14, 2021, and the patent was issued on August 17, 2021[4].
Expiration Date
The patent is set to expire on January 15, 2030[5].
Claims and Scope
Claim Structure
The patent includes several claims, with a focus on the malate salt of a specific cyclopropane-1,1-dicarboxamide compound and its crystalline forms. Claims 1-3 are particularly relevant, as they cover the compound, its crystalline forms, and methods for their preparation and use in treating cancer[5].
Claim 1: Compound and Crystalline Forms
Claim 1 specifically describes the malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide and its crystalline forms. This claim is foundational, as it defines the core invention protected by the patent[4].
Claim 2: Methods of Preparation
Claim 2 outlines the methods for preparing the malate salt and its crystalline forms. This includes various chemical processes and conditions necessary to produce the compound[4].
Claim 3: Pharmaceutical Compositions
Claim 3 covers pharmaceutical compositions containing the malate salt and its crystalline forms. This claim is crucial for the therapeutic application of the compound in treating cancer[4].
Patent Landscape
Related Patents
The patent is part of a family of patents related to CABOMETYX®, including U.S. Patent Nos. 7,579,473, 8,497,284, 8,877,776, 11,091,439, 11,098,015, and 11,298,349. These patents collectively protect various aspects of the drug, including its chemical structure, preparation methods, and therapeutic uses[2][5].
Malate Salt Patents
The '440 patent is one of the "Malate Salt Patents," which also includes U.S. Patent Nos. 11,091,439 and 11,098,015. These patents share an identical specification and cover different claims related to the malate salt and its crystalline forms[1].
Infringement and Validity Disputes
Litigation Background
Exelixis has been involved in several patent infringement lawsuits against generic drug manufacturers, including MSN Laboratories Private Ltd. and MSN Pharmaceuticals Inc. These lawsuits involve allegations of infringement of the '440 patent, among others[2].
Obviousness and Written Description Challenges
The validity of the '440 patent has been challenged on grounds of obviousness under 35 U.S.C. § 103 and lack of written description under 35 U.S.C. § 112. Defendants have argued that the claimed invention would have been obvious to a person of ordinary skill in the art and that the specification does not adequately describe the claimed subject matter[1][2].
Patent Analytics and Claim Coverage
Claim Coverage Matrix
To manage the complex patent landscape, companies like Exelixis can use patent analytics tools to create a Claim Coverage Matrix. This matrix helps in identifying which patents and claims are actively protecting the intellectual property and where gaps or opportunities exist[3].
Scope Concepts and Claim Charts
Using tools like ClaimScape® software, companies can categorize patents by claims and scope concepts, generating interactive claim charts. These charts are useful for technical experts to determine the applicability of scope concepts to target products or methods, highlighting gaps in current coverage and future design opportunities[3].
Expert Opinions and Depositions
Expert Testimony
In the litigation involving the '440 patent, expert opinions from Dr. Salvatore Lepore and Dr. Jonathan Steed have been crucial. These experts have provided testimony on the alleged obviousness of the patents under dispute[2].
Regulatory Context
FDA Approval and Orange Book Listing
CABOMETYX®, the drug protected by the '440 patent, is listed in the FDA’s Orange Book, which is a publication of approved drug products with therapeutic equivalence evaluations. Generic manufacturers seeking to produce a generic version of CABOMETYX® must navigate the patent landscape and address any patent infringement claims[5].
Key Takeaways
- Patent Scope: The '440 patent covers the malate salt of a specific cyclopropane-1,1-dicarboxamide compound, its crystalline forms, and methods for their preparation and use in treating cancer.
- Related Patents: Part of a family of patents related to CABOMETYX®, including other Malate Salt Patents.
- Litigation: Involved in infringement lawsuits against generic drug manufacturers.
- Validity Challenges: Faces challenges on grounds of obviousness and lack of written description.
- Patent Analytics: Utilizes tools like Claim Coverage Matrix and Claim Charts to manage patent landscape.
- Regulatory Context: Listed in the FDA’s Orange Book, affecting generic drug approvals.
FAQs
What is the main subject matter of U.S. Patent 11,091,440?
The main subject matter is the malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide and its crystalline forms, used in the treatment of cancer.
Who are the inventors of the '440 patent?
The inventors are Adrian St. Clair Brown, Peter Lamb, and William P. Gallagher.
What is the expiration date of the '440 patent?
The patent is set to expire on January 15, 2030.
Which other patents are related to the '440 patent?
The '440 patent is related to other Malate Salt Patents (U.S. Patent Nos. 11,091,439 and 11,098,015) and other patents covering CABOMETYX®, such as U.S. Patent Nos. 7,579,473, 8,497,284, 8,877,776, and 11,298,349.
What are the common challenges to the validity of the '440 patent?
The patent faces challenges on grounds of obviousness under 35 U.S.C. § 103 and lack of written description under 35 U.S.C. § 112.
Cited Sources:
- U.S. District Court Opinion: Generally, an obviousness-type double patenting analysis entails two steps... (D.I. 124, r 6)[1].
- Finnegan IP Health Blog: On October 29, 2019, May 11, 2020, and February 23, 2022, Exelixis, Inc. (“Exelixis”) filed three separate complaints for patent infringement against MSN Laboratories Private Ltd. and MSN Pharmaceuticals Inc.[2].
- Schwegman Patent Analytics: Patent analytics shows you which patents and claims are actively protecting your intellectual property, and where gaps or opportunities exist[3].
- United States Patent 11,091,440: Malate Salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and Crystalline Forms Thereof for the Treatment of Cancer[4].
- RPX Insight: CABOMETYX® is covered by, inter alia, claims 1-5 of the '776 Patent, claims 1, 3 and 4 of the '439 Patent, claims 1-3 of the '440 Patent[5].
