Arylvinylazacycloalkane compounds and methods of preparation and use thereof

Abstract

Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

What is claimed is: 
     
         1 . A method of treating gastrointestinal disorders, comprising administering racemic 5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof. 
     
     
         2 . A method of treating gastrointestinal disorders, comprising administering (+)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof. 
     
     
         3 . A method of treating gastrointestinal disorders, comprising administering (−)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof. 
     
     
         4 . The method of  claim 1 , wherein the gastrointestinal disorder is Crohn's Disease, Irritable Bowel Syndrome, or Ulcerative Colitis. 
     
     
         5 . The method of  claim 2 , wherein the gastrointestinal disorder is Crohn's Disease, Irritable Bowel Syndrome, or Ulcerative Colitis. 
     
     
         6 . The method of  claim 3 , wherein the gastrointestinal disorder is Crohn's Disease, Irritable Bowel Syndrome, or Ulcerative Colitis.