January 6, 2014

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The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2014 ACS

Patent Number: WO 2013177349
Title: Preparation of quinazolinediones as tankyrase inhibitors for the treatment of cancer
Inventor(s): Keenan, Richard M.; Miller, Aaron Bayne; Qin, Donghui
Patent Assignee(s): GlaxoSmithKline LLC, USA
Source: PCT Int. Appl., 81pp. CODEN: PIXXD2
Language: English

Abstract:
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).

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.

 View the full-text here.

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