January 14, 2008
These compounds may put you to sleep. M. Gold discloses novel compounds that inhibit cholinesterase and may lead to the development of novel drugs to treat sleep-related conditions such as insomnia, sleep apnea, and sleep problems related to shift work, abrupt altitude changes, or travel across time zones.
Sleep among mammals—including humans—involves the activity of the enzyme cholinesterase. Inhibiting the isozyme of cholinesterase that preferentially binds to acetylcholinesterase (as opposed to butyrylcholinesterase) may induce sleep. Like most drugs that act on the brain, these compounds must be able to cross the blood–brain barrier. The principal cholinesterase inhibitors disclosed by the inventor preferentially bind to the acetylcholinesterase and show evidence of being able to cross the blood–brain barrier. These compounds include galantamine and its salts and derivates. All of the compounds include the galantamine ring system (1).
Galantamine (or galanthamine) itself has been isolated from bulbs of the Caucasian snowdrop (Galanthus woronowii) and the common snowdrop (G. nivalis). Its chemical name is [4aS-(4aα,6β,8aR*)]-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef]benzazepin-6-ol and it has structure 2.
Future work in this area will likely include testing these compounds in animal models to determine their toxicity and efficacy as treatments for sleep disorders, as well as synthesizing and testing additional derivatives of these compounds. (Janssen Pharmaceutica N.V. [Belgium]. U.S. Patent 7,297,691, Nov 20, 2007; John Emanuele)
View patent information from CAS
What do you think of Patent Watch and Noteworthy Chemistry? Let us know.
Log In