Details for Patent: 4,935,437

Summary for Patent: 4,935,437

Title:	(Substituted aralkyl) heterocyclic compounds
Abstract:	A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.
Inventor(s):	Edwards; Philip N. (Bramhall, GB2), Large; Michael S. (Stoke-on-Trent, GB2)
Assignee:	Imperial Chemical Industries plc (London, GB2)
Application Number:	07/204,743
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Detailed Analysis of the Scope and Claims of United States Patent 4,935,437

Introduction

United States Patent 4,935,437, titled "(Substituted-aralkyl)heterocyclic compounds," was granted on June 19, 1990, to inventors Philip N. Edwards and Michael S. Large of Imperial Chemical Industries plc. This patent is significant in the field of organic chemistry and pharmaceuticals, particularly for its application in the development of therapeutic agents.

Inventors and Assignee

The inventors of this patent are Philip N. Edwards and Michael S. Large, both from England. The patent is assigned to Imperial Chemical Industries plc, a major chemical company based in London, England[2].

Patent Overview

This patent describes a class of (substituted-aralkyl)heterocyclic compounds, their synthesis, and their potential therapeutic applications. The compounds are characterized by specific substituents and structural elements that confer them with desirable pharmacological properties.

Chemical Structure and Substituents

The patent details compounds of the formula I, where various substituents such as azido, carbamoyl, cyano, formyl, hydroxy, or nitro radicals are present. These compounds also include 1-6C hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl, or alkylsulphonyl radicals, among others. The specific arrangement and nature of these substituents are crucial for the compounds' biological activity[2].

Synthesis Methods

The patent outlines several methods for synthesizing these compounds. These methods involve various chemical reactions, including the use of halogenating agents, dehydrohalogenation, and hydrogenation. For example, a compound with a 1-hydroxyethylene radical can be converted into a compound with an ethylene radical through a series of reactions involving halogenation, dehydrohalogenation, and hydrogenation[1].

Therapeutic Applications

The compounds described in this patent have potential therapeutic applications, particularly in the treatment of disorders related to metabolism and as antineoplastic agents. The patent falls under the classification A61P3/00, which pertains to drugs for disorders of the metabolism, and A61P35/00, which pertains to antineoplastic agents[1].

Claims

The patent includes nine claims that define the scope of the invention. These claims specify the structural requirements of the compounds, including the types of substituents and the methods of synthesis. The claims are designed to protect the unique chemical structures and their therapeutic uses, ensuring that the inventors and the assignee have exclusive rights to these compounds and their applications[2].

Prior Art and References

The patent references several prior art documents, including U.S. patents and scientific publications. These references highlight the state of the art in the field at the time of the invention and distinguish the novel aspects of the patented compounds. For example, references include patents by Iizuka et al., Tanouchi et al., and publications in the Journal of Medicinal Chemistry[2].

Patent Landscape

The patent landscape for this invention involves a detailed analysis of the claims and their scope. Here are some key points:

• Claim Coverage: The claims cover a broad range of (substituted-aralkyl)heterocyclic compounds with specific substituents and structural elements. This broad coverage ensures that any similar compounds developed in the future would likely infringe on these claims.
• Scope Concepts: Analyzing the scope concepts of these claims helps in understanding the value and applicability of the patent. For instance, the claims related to antineoplastic agents would be highly valuable given the ongoing research and development in cancer treatment[3].
• Gaps and Opportunities: A thorough analysis of the patent claims and the broader patent landscape can identify gaps in current coverage and highlight future design opportunities. This could involve identifying areas where the current claims do not provide adequate protection or where new compounds could be developed without infringing on existing patents.

Industrial and Commercial Significance

This patent is significant in the pharmaceutical industry due to its potential applications in treating various metabolic disorders and cancer. The compounds described could serve as leads for the development of new drugs, and the synthesis methods outlined provide a roadmap for their production.

Example of Application

One of the compounds described in this patent, anastrozole, is a well-known aromatase inhibitor used in the treatment of breast cancer. The synthetic route for anastrozole mentioned in this patent highlights the practical application of the invention in producing therapeutically important compounds[5].

Key Takeaways

• Chemical Structure: The patent describes (substituted-aralkyl)heterocyclic compounds with specific substituents.
• Synthesis Methods: Various chemical reactions are outlined for synthesizing these compounds.
• Therapeutic Applications: The compounds have potential uses in treating metabolic disorders and as antineoplastic agents.
• Claims and Scope: The patent includes nine claims that define the structural requirements and therapeutic uses of the compounds.
• Patent Landscape: The analysis of claims and scope concepts helps in understanding the value and applicability of the patent.

FAQs

What is the main subject of United States Patent 4,935,437?

The main subject of this patent is the description and synthesis of (substituted-aralkyl)heterocyclic compounds and their potential therapeutic applications.

Who are the inventors of this patent?

The inventors are Philip N. Edwards and Michael S. Large, both from England.

What is the assignee of this patent?

The assignee is Imperial Chemical Industries plc, based in London, England.

What are the potential therapeutic applications of the compounds described in this patent?

The compounds have potential applications in treating disorders related to metabolism and as antineoplastic agents.

How are the compounds described in this patent synthesized?

The synthesis involves various chemical reactions, including halogenation, dehydrohalogenation, and hydrogenation.

What is an example of a compound described in this patent that has significant therapeutic use?

An example is anastrozole, an aromatase inhibitor used in the treatment of breast cancer.

Sources

1. US4935437A - (Substituted aralkyl) heterocyclic compounds - Google Patents
2. United States Patent (19) - Googleapis.com
3. Patent Analytics | Intellectual Property Law - SLWIP
4. US 2002/0103141 A1 - Patent Application Publication - Google Patents
5. US20090247765A1 - Process for preparing pure anastrozole - Google Patents

Drugs Protected by US Patent 4,935,437

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
No data available in table

Foreign Priority and PCT Information for Patent: 4,935,437

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	8714013	Jun 16, 1987

International Family Members for US Patent 4,935,437

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0296749		97C0023	France
European Patent Office	0296749		09C0055	France
European Patent Office	0296749		SPC/GB96/004	United Kingdom
European Patent Office	0296749		97C0032	Belgium
European Patent Office	0296749		C970012	Netherlands