Details for Patent: 4,316,839

Summary for Patent: 4,316,839

Title:	Imidazodiazepine derivatives
Abstract:	Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonizing the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2 -one. Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
Inventor(s):	Gerecke; Max (Reinach, CH), Haefely; Willy (Reinach, CH), Hunkeler; Walter (Magden, CH), Kyburz; Emilio (Reinach, CH), Mohler; Hanns (Inzlingen, DE), Pieri; Lorenzo (Riehen, CH), Polc; Petar (Binningen, CH)
Assignee:	Hoffman-La Roche Inc. (Nutley, NJ)
Application Number:	06/193,775
Patent Claim Types: see list of patent claims	Compound;

Detailed Analysis of the Scope and Claims of United States Patent 4,316,839

Introduction

United States Patent 4,316,839, titled "Imidazodiazepine derivatives," was granted on February 23, 1982. This patent is significant in the field of pharmaceuticals, particularly for its contribution to the development of imidazodiazepine compounds. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background and Invention Overview

The patent pertains to imidazodiazepine derivatives, specifically compounds of the formula I and their pharmaceutically acceptable acid addition salts. These compounds are noted for their valuable pharmacodynamic properties, making them useful in the control or prevention of various illnesses[4].

Scope of the Invention

The scope of the invention encompasses several key aspects:

Chemical Structure

The patent describes imidazo[1,5-a][1,4]diazepine derivatives with a specific formula I, where various substituents (R1, R2, R3, R4, R5, R6) can be modified to produce different compounds. These substituents include groups such as cyano, lower alkanoyl, and alkyl groups, among others[4].

Pharmacodynamic Properties

The compounds are highlighted for their pharmacodynamic properties, which make them suitable for use in medicaments. The patent mentions their potential in controlling or preventing illnesses, although it does not specify particular diseases[4].

Manufacturing Process

The invention also includes methods for manufacturing these compounds and their intermediates. The process involves starting materials of a general formula and using known methods to synthesize the desired imidazodiazepine derivatives[4].

Claims of the Patent

The patent includes several claims that define the scope of the invention:

Claim 1: Compound Formula

The first claim defines the specific chemical structure of the imidazodiazepine derivatives, including the various substituents and their possible configurations[4].

Claim 2: Pharmaceutically Acceptable Acid Addition Salts

This claim covers the pharmaceutically acceptable acid addition salts of the compounds described in claim 1[4].

Claim 3: Medicaments

The patent claims medicaments containing the compounds or their acid addition salts, as well as the manufacture of such medicaments[4].

Claim 4: Use in Illness Control or Prevention

This claim pertains to the use of the compounds or their acid addition salts in the control or prevention of illnesses[4].

Patent Landscape

Prior Art

The patent references prior art, including Belgian Patent Specifications and U.S. Patents, which describe methods for preparing similar compounds. However, the specific imidazodiazepine derivatives and their pharmacodynamic properties are novel contributions of this patent[4].

International Patent Offices

To understand the global patent landscape, one would need to search international patent databases such as those provided by the European Patent Office (EPO), Japan Patent Office (JPO), and the World Intellectual Property Organization (WIPO)[1].

Related Patents

Other patents related to benzodiazepine derivatives, such as the process for preparing benzodiazepine-3-carboxylic acid alkyl derivatives (KR0167401B1), can provide insights into the broader field of benzodiazepine research[5].

Search Tools and Resources

For a comprehensive analysis, several search tools and resources are available:

USPTO Patent Public Search

This tool allows for searching existing patents and published patent applications, providing access to prior art and related patents[1].

Global Dossier

This service offers access to the file histories of related applications from participating IP Offices, which can be useful in understanding the global patent family of a specific application[1].

Patent and Trademark Resource Centers (PTRCs)

Local PTRCs can provide additional resources and training in patent search techniques, helping to identify related patents and prior art[1].

Economic and Research Implications

The Patent Claims Research Dataset by the USPTO can provide insights into the economic and research implications of patents like 4,316,839. This dataset includes detailed information on claims from U.S. patents and can help in analyzing the scope and impact of the patent[3].

Key Takeaways

• Chemical Structure: The patent describes specific imidazodiazepine derivatives with valuable pharmacodynamic properties.
• Manufacturing Process: The invention includes methods for synthesizing these compounds and their intermediates.
• Pharmaceutical Use: The compounds are useful in medicaments for controlling or preventing illnesses.
• Patent Landscape: The patent is part of a broader landscape of benzodiazepine research, with related patents and prior art available through various search tools.

FAQs

Q1: What is the main subject of United States Patent 4,316,839?

The main subject is imidazodiazepine derivatives, specifically their chemical structure, pharmacodynamic properties, and manufacturing process.

Q2: What are the potential uses of the compounds described in the patent?

The compounds are useful in medicaments for controlling or preventing various illnesses.

Q3: How can one search for related patents and prior art?

One can use tools like the USPTO Patent Public Search, Global Dossier, and local Patent and Trademark Resource Centers (PTRCs).

Q4: What resources are available for analyzing the economic and research implications of this patent?

The USPTO's Patent Claims Research Dataset provides detailed information on claims from U.S. patents and can help in analyzing the scope and impact of the patent.

Q5: Is the patent still in force?

No, the patent has expired, as indicated by its legal status.

Sources

1. USPTO - Search for patents: https://www.uspto.gov/patents/search
2. USPTO - Certificate Extending Patent Term: https://www.uspto.gov/sites/default/files/web/offices/pac/dapp/opla/term/certs/4316839.pdf
3. USPTO - Patent Claims Research Dataset: https://www.uspto.gov/ip-policy/economic-research/research-datasets/patent-claims-research-dataset
4. Google Patents - US4316839A: https://patents.google.com/patent/US4316839A/en
5. Google Patents - KR0167401B1: https://patents.google.com/patent/KR0167401B1/en

Drugs Protected by US Patent 4,316,839

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: 4,316,839

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Switzerland	8971/79	Oct 04, 1979
Switzerland	8972/79	Oct 04, 1979
Switzerland	10664/79	Nov 30, 1979
Switzerland	10665/79	Nov 30, 1979
Switzerland	5716/80	Jul 25, 1980

International Family Members for US Patent 4,316,839

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	227293
Australia	533641
Australia	6278280
Austria	7497
Brazil	8006404