| abstract |
The invention provides a composition of matter which: ? (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or ? (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 % by weight of an atropisomer of formula (2A); wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by: formula (2A) and formula (2B) or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R<sup>1</sup> is trifluoromethyl; R<sup>2</sup> is hydrogen; R<sup>3</sup> is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar<sup>1</sup> is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R<sup>5</sup> as defined herein; and R<sup>4</sup>; R<sup>5 </sup> when present, R<sup>6</sup> and R<sup>7</sup> independently selected from various substituents as defined herein. Also provided are individual atropisomers thereof as well as of various compounds having a five-membered heteroaromatic ring containing 1 or 2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, with three rings Ar1, X and Y, and substituents R1-R7 all being defined as in formulas (1A) or (1B) below; pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers. Formula (1A), formula (1B). |