Detailed Analysis of the Scope and Claims of United States Patent 3,562,257
Introduction
United States Patent 3,562,257, filed by Hiroshi Kngita, Hirozumi Inoue, Muneyoshi Ikezaki, and Satoshi Takeo, and assigned to Tanabe Seiyaku Co., Ltd., Japan, pertains to novel benzothiazepine derivatives and their preparation. This patent is significant in the pharmaceutical industry, particularly for its applications in developing antidepressants, tranquilizers, and coronary vasodilators.
Scope of the Patent
The patent covers a specific class of benzothiazepine derivatives with a defined chemical structure. Here are the key components of the scope:
Chemical Structure
The benzothiazepine derivatives are of the formula:
[ 2-R_1, 3-(R_2-O-), 5-(R_3-N(-R_4)-Y-), X-2,3-Dihydro-1,5-benzodiazepin-4(5H)-one ]
Where:
- ( R_1 ) is a phenyl group which may be substituted with 1 to 3 lower alkyl groups, lower alkoxy groups, or halogen atoms.
- ( R_2 ) is a hydrogen atom or a lower alkanoyl group.
- ( R_3 ) and ( R_4 ) are each a lower alkyl group.
- ( X ) is a hydrogen atom or a halogen atom.
- ( Y ) is an alkylene group of 2 or 3 carbon atoms[1].
Applications
These derivatives are useful as antidepressants, tranquilizers, and coronary vasodilators. This broad range of therapeutic applications underscores the significance of this patent in the pharmaceutical sector.
Claims of the Patent
The patent includes several claims that define the specific compounds and their preparation methods:
Compound Claims
The patent claims various benzothiazepine derivatives with specific substitutions at the R1, R2, R3, R4, X, and Y positions. For example, one of the claimed compounds is 2-phenyl-3-hydroxy-5-(γ-dimethylamino-n-propyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one[1].
Method Claims
The patent also claims the methods for preparing these compounds. These methods involve several steps, including the reaction of specific precursors under controlled conditions. For instance, the reaction between 2-phenyl-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one and β-dimethylaminoethyl chloride is described in detail[1].
Patent Landscape Analysis
To understand the broader context and impact of this patent, a patent landscape analysis is essential.
Importance of Patent Landscape Analysis
A patent landscape analysis helps in identifying the critical and relevant patent information in a given technology area, which is crucial for competitive innovation. It reduces redundant search efforts, accelerates time to commercialization, and protects teams from defensive litigation[3].
Related Patents and Technologies
The benzothiazepine derivatives covered in this patent are closely related to other pharmaceutical compounds, such as diltiazem, which is a well-known calcium-channel blocker and vasodilator. Diltiazem, also a benzothiazepine derivative, is used in the management of angina pectoris and hypertension[4].
Competitive Environment
The pharmaceutical industry is highly competitive, with numerous companies and research institutions actively developing new drugs. The filing of over 3.1 million patent applications worldwide in 2016 highlights the intensity of innovation in this field. This patent, therefore, represents a significant contribution to the existing body of knowledge and intellectual property in the area of benzothiazepine derivatives[3].
Preparation Methods
The patent provides detailed descriptions of the preparation methods for the claimed compounds. Here is an overview of one such method:
Example Preparation
For the preparation of 2-phenyl-3-hydroxy-5-(γ-dimethylamino-n-propyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, the process involves:
- Adding sodium hydride to a solution of 2-phenyl-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one in dioxane.
- Stirring the mixture at room temperature and then at about 40°C.
- Adding β-dimethylaminoethyl chloride dropwise to the mixture.
- Stirring the resultant mixture at 55 to 65°C for several hours.
- Evaporating the solvent and recrystallizing the product[1].
Impact and Applications
The compounds described in this patent have significant therapeutic applications:
Therapeutic Uses
As mentioned, these benzothiazepine derivatives are useful as antidepressants, tranquilizers, and coronary vasodilators. This versatility makes them valuable in treating a range of medical conditions.
Market Significance
The market for these types of pharmaceuticals is substantial. For example, diltiazem, a related compound, has seen significant consumption in both Germany and the USA, with thousands of kilograms used annually[4].
Key Takeaways
- Chemical Structure: The patent covers benzothiazepine derivatives with a specific chemical structure.
- Applications: These compounds are useful as antidepressants, tranquilizers, and coronary vasodilators.
- Preparation Methods: Detailed methods for preparing these compounds are provided.
- Patent Landscape: The patent is part of a broader landscape of pharmaceutical innovation, with significant competitive and market implications.
- Related Compounds: The patent is related to other benzothiazepine derivatives like diltiazem.
FAQs
What are the primary therapeutic applications of the benzothiazepine derivatives described in US Patent 3,562,257?
The primary therapeutic applications are as antidepressants, tranquilizers, and coronary vasodilators.
How are the benzothiazepine derivatives prepared according to the patent?
The preparation involves several chemical reactions, including the use of sodium hydride and β-dimethylaminoethyl chloride, followed by specific temperature and stirring conditions.
What is the significance of this patent in the pharmaceutical industry?
This patent is significant because it contributes to the development of new therapeutic compounds and provides detailed preparation methods, which can accelerate innovation and commercialization.
How does this patent relate to other known benzothiazepine derivatives like diltiazem?
The patent covers compounds that are structurally related to diltiazem, which is a well-known calcium-channel blocker and vasodilator.
What is the importance of performing a patent landscape analysis in this context?
A patent landscape analysis helps in identifying relevant patent information, reducing redundant search efforts, accelerating time to commercialization, and protecting against defensive litigation.
Sources
- United States Patent 3,562,257 - Benzothiazepine derivatives.
- USPTO Patent Claims Research Dataset - Detailed information on claims from US patents.
- How to perform a patent landscape analysis in 5 key steps - IP Checkups.
- Diltiazem | C22H26N2O4S | CID 39186 - PubChem.
