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CAPLUS COPYRIGHT 2014 ACS
||Preparation of quinazolinediones as tankyrase inhibitors for the treatment of cancer
||Keenan, Richard M.; Miller, Aaron Bayne; Qin, Donghui
||GlaxoSmithKline LLC, USA
||PCT Int. Appl., 81pp. CODEN: PIXXD2
The invention relates to quinazolinediones of formula I and their prepn., useful as modulators, notably inhibitors, of tankyrases (TNKS1 and TNKS2) in the treatment of cancer, fibrosis, and other hyperproliferative diseases. Compds. of formula I, in which R1, R2, and R3 are independently H, halo, C1-4 alkyl, and C1-4 alkoxy, provided that at least one of R1, R2, and R3 is not H; R4 is H and Me; or pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by a multistep process (procedure given). Invention compds. were evaluated for the tankyrase inhibitory activity. From the assay, it was detd. that II exhibited pIC50 values of 8.1 (TNKS1) and 7.1 (TNKS2).
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