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1. (WO2017148925) RADIOLABELED MACROCYCLIC EGFR INHIBITOR

Pub. No.:    WO/2017/148925    International Application No.:    PCT/EP2017/054611
Publication Date: Sat Sep 09 01:59:59 CEST 2017 International Filing Date: Wed Mar 01 00:59:59 CET 2017
IPC: A61K 51/04
C07D 498/06
A61K 101/02
Applicants: ONCODESIGN SA
Inventors: HOFLACK, Jan Marie Cyriel Jozef
BERTHET, Cyril
BLOM, Petra Marcella Françoise
VERCOUILLIE, Johnny
ROBIC, Caroline
CATOEN, Sarah
Title: RADIOLABELED MACROCYCLIC EGFR INHIBITOR
Abstract:
The present invention relates to 18-Fluor radiolabeled macrocyclic quinazoline compounds, which are suitable as positron emission tomography (PET) tracers for imaging epidermal growth factor receptors (EGFR), and their use in in vivo diagnosis, preclinical and clinical tumour imaging, patient stratification on the basis of mutational status of EGFR, and assessing tumour response to therapeutic treatments. The present invention also describes precursor compounds and methods of preparing the radiotracers. The invention is relevant to any cancer that is influenced or driven by deregulated EGFR, such as, but not limited to, non-small cell lung cancer (NSCLC), pancreatic, hepatocellular, oesophageal, gastric, colorectal, prostate, cervical, renal, ovarian, breast cancers, head and neck squamous cell carcinoma, and malignant glioma.