On September 18, 2014, Amans, Dominique; Atkinson, Stephen John; Harrison, Lee Andrew; Hirst, David Jonathan; Law, Robert Peter; Lindon, Matthew; Preston, Alexander; Seal, Jonathan Thomas; Wellaway, Christopher Roland published a patent.Application of 596114-50-0 The title of the patent was Preparation of acylaminotetrahydroquinoline derivatives for use as bromodomain inhibitors. And the patent contained the following:
Title compounds I [A = NH, O, S, SO, etc.; V = (un)substituted Ph, heteroaromatic, or pyridone; W and Z independently = CH or N; X or Y independently = C or N; R1 = alkyl; R2 = alkyl, cycloalkyl, heterocyclyl, CH2CF3, or CH2OMe; R3 = alkyl, CH2F, CH2OH, or CH2OC(O)Me; R4 = absent, H, OH, halo, CN, CO2H, etc.; R5 = absent, H, halo, OH, or alkoxy], and their pharmaceutically acceptable salts, are prepared and disclosed as bromodomain inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in BRD4 BD2 TR-FRET assays, e.g., II demonstrated a pIC50 value of ≥7.0. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Application of 596114-50-0
The Article related to quinoline acylaminotetrahydro preparation bromodomain inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 596114-50-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia