Patent ID: 9040259
Filing Date: 2015-05-26
Classification: A61P,C07D,C07K,C12N,C12P

Abstract:
1. A method of generating analogues of FKBP-ligands which incorporate a non-natural starter unit, said method comprising: (a) generating a recombinant strain in which at least the rapK homologue has been deleted or inactivated; and (b) feeding a non-natural starter unit to said strain, wherein said starter unit is selected from the group consisting of 2-norbornane carboxylic acid, 2-(cis/trans)-hydroxycyclohexane carboxylic acid, 3-(cis/trans)-hydroxycyclohexane carboxylic acid, 4-(cis/trans)-hydroxycyclohexane carboxylic acid, 2-(cis/trans)-methylcyclohexane carboxylic acid, 4-(cis/trans)-methylcyclohexane carboxylic acid, 3-(cis/trans)methoxycyclohexane carboxylic acid, 4-(cis/trans)methoxycyclohexane carboxylic acid, 4-oxo cyclohexane carboxylic acid, 2-oxo cyclohexane carboxylic acid, 4-trans-n-pentylcyclohexane carboxylic acid, 2-trans-aminocyclohexane carboxylic acid, 4-cis-aminocyclohexane carboxylic acid, 4-(cis/trans)-aminomethylcyclohexane carboxylic acid, cyclopentane carboxylic acid, cyclobutane carboxylic acid, 1-methylcyclohexane carboxylic acid, 3-trans-hydroxy-4-cis-fluorocyclohexane carboxylic acid and 4-trans-hydroxy-3-cis-fluorocyclohexane carboxylic acid, 3-cis-hydroxy-4-trans-fluorocyclohexane carboxylic acid and 4-cis-hydroxy-3-trans-fluorocyclohexane carboxylic acid, 3-cis-hydroxy-4-trans-chlorocyclohexane carboxylic acid and 4-cis-hydroxy-3-trans-chlorocyclohexane carboxylic acid, 3-trans-hydroxy-4-cis-chlorocyclohexane carboxylic acid and 4-trans-hydroxy-3-cis-chlorocyclohexane carboxylic acid, 3-trans-cyclohexeneoxide carboxylic acid, 3-cis-cyclohexeneoxide carboxylic acid, 3,4-cis-dihydroxycyclohexane carboxylic acid and 3,4-trans-dihydroxycyclohexane carboxylic acid, cyclohexaneacetic acid, cyclohexanepropionic acid and 4-cis/trans-tert-butylcyclohexane carboxylic acid, and simple esters or salts thereof.