Fluorination of bioactive compounds

Lead Research Organisation: University of Southampton
Department Name: School of Chemistry

Abstract

This is a synthetic organic chemistry project, dealing with the synthesis of fluorinated bioactive compounds. The project fits in a larger research program in our group, and the choice of modifications is guided byour recent work in how physical properties of organic molecules can be modified by targeted fluorination, and how these effects can be explained and predicted (key papers: Angew. Chem. Int.Ed.2012, 51, 6176 (VIP); Chem. Eur. J. 2014, 20, 106;J. Am. Chem. Soc.2015, 137, 1230; Chem. Eur. J. 2015, 21, 17808; Angew. Chem. Int. Ed.2015, in press (VIP)).

Publications

10 25 50

Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/N509747/1 01/10/2016 30/09/2021
1795539 Studentship EP/N509747/1 29/09/2016 30/09/2019 David Evans
 
Description We have identified bioactive compounds for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; or liver damage arising from fibrosis
Exploitation Route Further development of the discovered bioactive
Sectors Other

 
Description Further development of the discovered bioactives
Sector Pharmaceuticals and Medical Biotechnology,Other
 
Title FLUORINATED BILE ACID DERIVATIVES 
Description Compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; or liver damage arising from fibrosis. 
IP Reference WO2020025942 
Protection Patent application published
Year Protection Granted 2020
Licensed Commercial In Confidence
Impact in progress