United States Patent 5,457,105: A Detailed Analysis of Scope and Claims
Introduction
United States Patent 5,457,105, titled "Quinazoline derivatives useful for treatment of neoplastic disease," is a significant patent in the field of pharmaceuticals, particularly in the treatment of cancer. This patent, granted in 1995, outlines the synthesis, properties, and therapeutic applications of various quinazoline derivatives.
Background
Quinazolines are a class of heterocyclic compounds that have been extensively studied for their pharmacological properties. The patent in question focuses on specific quinazoline derivatives that have shown promise in treating neoplastic diseases, which include various types of cancers.
Scope of the Patent
General Formula and Structure
The patent describes quinazoline derivatives of a general formula, where the variable "m" can be 1, 2, or 3, and each R1 substituent can include hydroxy, amino, carboxy, carbamoyl, and other functional groups[1][5].
Synthesis
The synthesis of these quinazoline derivatives involves several steps, including the condensation of appropriate starting materials and subsequent modification to introduce the desired substituents. The patent provides detailed methods for synthesizing these compounds, ensuring reproducibility and consistency in their preparation.
Pharmacological Properties
The quinazoline derivatives described in this patent are pharmacologically active, particularly in inhibiting the activities of various receptor tyrosine kinases (RTKs). RTKs are enzymes that play critical roles in cell signaling pathways, and their dysregulation is often associated with cancer. By inhibiting these enzymes, the quinazoline derivatives can potentially halt or slow the progression of neoplastic diseases[1][2].
Claims of the Patent
Composition of Matter Claims
The patent includes claims for the quinazoline derivatives themselves, as well as their pharmacologically acceptable salts and compositions containing these compounds. These claims are broad, covering a wide range of possible substituents and modifications to the core quinazoline structure[1].
Method of Use Claims
In addition to the composition of matter claims, the patent also includes method of use claims. These claims describe the therapeutic applications of the quinazoline derivatives, specifically their use in treating neoplastic diseases such as various types of cancer. The methods include administering the compounds to patients in need of such treatment[1].
Specific Examples
The patent provides several specific examples of quinazoline derivatives, along with their synthesis and biological activity data. These examples help to illustrate the scope of the invention and demonstrate the efficacy of the compounds in inhibiting RTKs and treating cancer[1].
Patent Landscape
Related Patents
The patent landscape surrounding quinazoline derivatives is extensive. Several other patents, such as US009187459B2 and CA2557433, also describe quinazoline derivatives and their therapeutic uses. These patents often overlap in their claims but may differ in specific substituents, synthesis methods, or the particular RTKs targeted[2][4].
Prior Art
The prior art cited in the patent includes various earlier patents and publications that describe other quinazoline derivatives and their pharmacological properties. This prior art helps to establish the novelty and non-obviousness of the inventions claimed in US5457105A[1][5].
International Patent Cooperation
The invention described in US5457105A is part of a broader international patent strategy. Similar patents have been filed and granted in other jurisdictions, such as the European Patent Office (EPO), under publications like EP0566226A1. This international cooperation reflects the global interest in these compounds for cancer treatment[5].
Impact and Significance
Therapeutic Applications
The quinazoline derivatives described in this patent have significant therapeutic potential. By inhibiting RTKs, these compounds can be used to treat a variety of cancers, offering new treatment options for patients. The specificity and efficacy of these compounds make them valuable additions to the arsenal of cancer therapies.
Commercial and Research Implications
The patent has commercial and research implications, as it provides a foundation for further development and commercialization of these compounds. Pharmaceutical companies can use this patent as a starting point for developing new drugs, and researchers can build upon the disclosed methods and compounds to explore new therapeutic avenues.
Key Takeaways
- Quinazoline Derivatives: The patent focuses on quinazoline derivatives with specific substituents that inhibit RTKs.
- Therapeutic Use: These compounds are useful in treating neoplastic diseases, particularly various types of cancer.
- Scope of Claims: The patent includes claims for the composition of matter, method of use, and specific examples of the quinazoline derivatives.
- Patent Landscape: The patent is part of a broader landscape that includes related patents and international cooperation.
- Impact: The patent has significant therapeutic, commercial, and research implications.
FAQs
What are the primary therapeutic applications of the quinazoline derivatives described in US5457105A?
The primary therapeutic applications are in the treatment of neoplastic diseases, including various types of cancer, by inhibiting receptor tyrosine kinases (RTKs).
How are the quinazoline derivatives synthesized according to the patent?
The synthesis involves condensation of appropriate starting materials followed by modification to introduce the desired substituents.
What is the significance of the variable "m" in the general formula of the quinazoline derivatives?
The variable "m" can be 1, 2, or 3, indicating the flexibility in the structure of the quinazoline ring.
Are there other patents related to quinazoline derivatives?
Yes, several other patents, such as US009187459B2 and CA2557433, also describe quinazoline derivatives and their therapeutic uses.
What is the current legal status of US5457105A?
The patent has expired, as indicated by its lifetime status.
Sources
- US5457105A - Quinazoline derivatives useful for treatment of neoplastic disease - Google Patents
- US009187459B2 - Quinazoline-7-ether compounds and methods of use - Google Patents
- Mastering Patent Claim Construction - Digital Commons @ Touro Law
- CA2557433 - Quinazoline derivatives and therapeutic use thereof - Canadian Patents Database
- EP0566226A1 - Quinazoline derivatives - Google Patents
