The present invention relates to a compound of formula (I) or pharmaceutically acceptable salts, stereoisomers, diastereoisomers, enantiomers, polymorphs, racemic mixtures, solvates or isomers and mixtures thereof. The invention also relates to a process for the stereoselective preparation of such compounds. The compounds of formula (I) are useful as medicaments, in particular for inhibiting crown
protein 1 expression in the induction of
immunosuppression or in the treatment and / or prevention of diseases or disorders selected from the group consisting of
transplant rejection, autoimmune diseases, inflammatory diseases, infectious diseases and
lymphoproliferative disorders. The present invention also relates to a vector comprising a crown
protein 1
promoter element wherein the crown
protein 1
promoter element starts directly upstream of the
transcription start site (TSS) of the crown protein 1
gene and spans a sequence segment of at least about 700 bp in the
genome in the
vertebrate genome. The invention also relates to a method for identifying immunomodulatory compounds that alter the activity of the crown protein 1
promoter using said vector. The invention also relates to BRD3 as an upstream target responsible for driving crown protein-1 expression and activity in immune cells, and to compounds that selectively target the
bromodomain of BRD3 and thereby deplete crown protein 1 levels, in particular compounds of formula (I). # imgabs0 #