United States Patent 9,693,989 B2: A Detailed Analysis of Scope and Claims
Introduction
The United States Patent 9,693,989 B2, titled "N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases," is a significant patent in the pharmaceutical industry. This patent, granted to inventors Lyssikatos et al., pertains to novel compounds and their use in treating various hyperproliferative diseases, including cancer and inflammation.
Background of the Invention
The patent is focused on type I receptor tyrosine kinases, a family of receptors that include EGFR (ErbB1 or HER1), ErbB2, ErbB3, and ErbB4. These receptors are implicated in the development and progression of several hyperproliferative diseases. The invention aims to provide compounds that inhibit these kinases, thereby offering therapeutic benefits[1][4].
Scope of the Patent
Compounds of Formula I
The patent describes compounds of Formula I, which are defined by specific structural elements including B, G, A, E, R¹, R², R³, m, and n. These compounds are designed to inhibit type I receptor tyrosine kinases and are useful in treating hyperproliferative diseases such as cancer and inflammation[1][4].
Pharmaceutical Compositions
The patent also covers pharmaceutical compositions containing these inhibitors. These compositions can include various forms such as salts, solvates, and prodrugs, which are pharmacologically acceptable. The invention encompasses methods for preparing these compounds and compositions[1].
Claims of the Patent
Method of Treating Diseases
A key aspect of the patent is the method of treating diseases mediated by type I receptor tyrosine kinases. This involves administering an effective amount of a compound of Formula I, or its metabolite, solvate, or pharmacologically acceptable salt or prodrug, to a warm-blooded animal[1].
Inhibition of Kinase Production
The patent also claims methods for inhibiting the production of type I receptor kinases by administering the aforementioned compounds. This inhibition is crucial for the therapeutic effect in treating hyperproliferative diseases[1].
Definitions and Structural Elements
Alkyl Groups
The patent defines various structural elements, including alkyl groups, which are saturated linear or branched-chain monovalent hydrocarbon radicals of one to twelve carbon atoms. These alkyl groups can be optionally substituted with one or more substituents[1].
Other Structural Elements
Other structural elements such as B, G, A, E, R¹, R², R³, m, and n are also defined in detail. These definitions are critical for understanding the scope of the compounds covered by the patent[1].
Patent Landscape and Exclusivity
Patent Expiration
The patent US 9,693,989 B2 is part of a broader patent landscape that includes several related patents. For instance, one of the related patents, US 8,648,087, is set to expire in April 2031, while another, US 7452895, has already expired as of November 2024[5].
Challenges and Oppositions
The patent landscape for Tukysa, a drug that utilizes these compounds, is complex and involves multiple patents and ongoing legal events. The patents protecting Tukysa are open to challenges, and the generic launch date is estimated to be April 27, 2038, based on the current patent exclusivities[5].
Impact on Pharmaceutical Industry
Investment and Development
The pharmaceutical industry invests billions of dollars in developing and bringing groundbreaking therapeutics to market. Robust and predictable patent protection is crucial for supporting these commercialization strategies. However, the current legal landscape, particularly the Federal Circuit’s stance on genus claims, poses challenges to the validity of many existing pharmaceutical and biologic patents[3].
Market Expansion
The market for therapeutic antibodies and other biologics is expanding rapidly, with estimates suggesting it will reach $300 billion by 2025. This expansion underscores the importance of strong patent protection to protect innovations in this field[3].
Legal Considerations
Patent Disclosure Laws
The Federal Circuit’s application of patent disclosure laws, specifically Section 112(a), has led to a more rigid stance on genus claims. This has resulted in many existing antibody and pharmaceutical patents being deemed invalid under current law. The scope of patent claims is critical, as claims that are too narrow can be easily designed around, while claims that are too broad may not be commensurate with what is taught in the patent application[3].
Patent Term Extensions
The USPTO applies statutory limitations when calculating patent term extensions. For instance, in the case of Tukysa, the applicant has sought various extensions, but the actual period of extension is subject to several regulatory and statutory considerations[2].
Key Takeaways
- Compounds and Uses: The patent covers N4-phenyl-quinazoline-4-amine derivatives and related compounds as inhibitors of type I receptor tyrosine kinases for treating hyperproliferative diseases.
- Pharmaceutical Compositions: The patent includes pharmaceutical compositions containing these inhibitors in various forms.
- Patent Landscape: The patent is part of a complex landscape involving multiple related patents and ongoing legal events.
- Legal Considerations: The patent's validity and scope are influenced by current legal stances on genus claims and patent disclosure laws.
- Market Impact: Strong patent protection is crucial for the commercialization of pharmaceuticals and biologics in an expanding market.
FAQs
What are the main compounds covered by US Patent 9,693,989 B2?
The main compounds covered are N4-phenyl-quinazoline-4-amine derivatives and related compounds designed to inhibit type I receptor tyrosine kinases.
What diseases are these compounds used to treat?
These compounds are used to treat hyperproliferative diseases, including cancer and inflammation.
What is the current status of the patent?
The patent is active and set to expire in April 2031, based on related patent US 8,648,087.
How does the Federal Circuit’s stance on genus claims affect pharmaceutical patents?
The Federal Circuit’s increasingly rigid stance on genus claims has led to many existing pharmaceutical and biologic patents being deemed invalid under current law, highlighting the need for precise and commensurate patent claims.
What is the estimated generic launch date for Tukysa based on its patent exclusivities?
The estimated generic launch date for Tukysa is April 27, 2038, based on its current patent exclusivities.
Sources
- United States Patent and Trademark Office. US9693989B2 - N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases.
- Federal Register. Volume 88 Issue 228 (Wednesday, November 29, 2023).
- DigitalCommons@NYLS. Eviscerating Patent Scope.
- Google Patents. US9693989B2 - N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases.
- Pharsight. Tukysa patent expiration.
