AU2015101722A4 — Oncogenic ros1 and alk kinase inhibitor

USPTO Abstract

The present invention provides a compound suitable for treating cancer, in particular NSCLC, which exceptionally inhibits activity of oncogenic ROS1 kinase and ALK kinase. Further, the invention provides a composition, in particular a pharmaceutical composition, comprising said compound. Further, a method for targeting cancer cells harboring an abnormality in ROS1 gene or ALK gene by contacting a cell with said compound is provided. The compound of the invention has certain structural components such as a quinoline moiety in the backbone and at least one phenyl-containing moiety in a side chain with a hydrophobic substituent attached to the backbone via an up to 6-membered linking group as well as a further hydrophobic moiety. The presence of said structural components allows for an advantageous interaction with the ROS1 kinase domain and, further, with the ALK kinase domain. Hence, said compound represents a highly promising opportunity for patients bearing ROS1 - or ALK-dependent cancer. Concentration (pLM) Fig. 1A S .0 15 20 2:5 Concentration (pM) Fig. 1B