Preparation of Hymenialdisine Derivatives and potential Application to Treatment of Inflammatory Diseases, Alzheimer's, and Cancer

 

Introduction

 

Cyclin-dependent kinases and NF-kB regulate a large number of genes and biochemical pathways. Deviations in their activity are associated with diseases, including those linked to immune, inflammatory, and anti-apoptotic responses. Many areas of drug discovery are focused on discovery of reagents that inhibit their activities.

Naturally occurring compounds that are identified through marine biology represent a broad spectrum of potentially useful compounds. The multi-ring indolazepine derivatives described here are closely related to hymenialdisine compounds that have been isolated from marine sponges and are known to be potent kinase and NF-kB inhibitors.

 

Description of Technology

 

This technology consists of indolazepines, which are hymenialdisine-related compounds that inhibit NF-kB and cyclin-dependent kinases. These compounds have the potential for anti-inflammatory activity and inhibition of cancer cells. This invention describes in vitro biological activity and methods for synthesis and production of these unique indolazepine compounds.

 

Key Benefits

  • More potent inhibition of cyclin-dependent kinase and NF-KB activity: Will potentially lead to an effective inhibitor which has improved efficacy over hymenialdisine and other inhibitory molecules.
  • Method for synthesis: Will provide the ability to produce pure, active material.

 

Applications

 

These compounds can potentially be used on their own, or in combination with complementary drugs or compounds in the treatment of a wide variety of medical conditions including inflammatory disorders such as arthritis, asthma, Alzheimer's, and cancers.

 

Patent Status

 

US 7335769 (issued Feb 26, 2008)
US 7193079 (issued Mar 20, 2007)
US 2004/0235820 A1 (filed Apr 28, 2004)

 

Inventors

 

Jetze Tepe

 

Tech ID

 

TEC2003-0052

 

Alternative contact due to temporary leave:

 

Nina (Isi) Davis, Technology Marketing Manager, email: davisnin@msu.edu, phone (direct): (517)884-1829. 

 

Patent Information:

For Information, Contact:

Randy Ramharack
Technology Manager
Michigan State University
ramharac@msu.edu
Inventors:
Jetze Tepe