January 6, 2014

CAS databases provide millions of journal article references from more than 10,000 major scientific journals worldwide, patent and patent family references from 63 patent authorities around the world, and other reputable web sources.

The following patent record is from the CAplusSM database.


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

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.

Recent News

    December 19, 2014 | CAS Expands Coverage of
    Reactions from Dissertations in CASREACT
    December 18, 2014
| Additional Experimental Spectra 
    Now Available in CAS REGISTRY on SciFinder and
    in STN
    October 7, 2014
 | CAS and Obiter Research form a
    multi-year collaboration to provide SciFinder to their
    research team
                                                                     More News >> 

 Media Contact

 Name: Rhonda Ross
 Phone: 614-447-3624                                       
 Email: cas-pr@cas.org