July 29, 2013

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 2013063214
Title: Preparation of pyrazolo[4,3-c]pyridines as ERK inhibitors for cancer treatment

Lim, Jongwon; Kelley, Elizabeth Helen; Methot, Joey L.; Zhou, Hua; Petrocchi, Alessia; Mansoor, Umar Faruk; Fischer, Christian; O'Boyle, Brendan M.; Guerin, David Joseph; Bienstock, Corey E.; Boyce, Christopher W.; Daniels, Matthew H.; Falcone, Danielle; Ferguson, Ronald D., II; Fevrier, Salem; Huang, Xianhai; Lipford, Kathryn Ann; Sloman, David L.; Wilson, Kevin; Zhou, Wei; Witter, David; Maletic, Milana M.; Siliphaivanh, Phieng

Patent Assignee(s): Merck Sharp & Dohme Corp., USA
Source: PCT Int. Appl., 323pp. CODEN: PIXXD2
Language: English

Disclosed are the ERK inhibitors of formula I (wherein X is S or O; R1 is H, halo, CN, (un)substituted heteroaryl, etc.; R2 is H, (C1-6)alkyl, (un)substituted aryl, etc.; R3 is H, (C1-6)alkyl, (un)substituted aryl, etc.; R4 is H, halo, (C1-C6)alkyl, OH and NH2) and the pharmaceutically acceptable salts thereof.  Also disclosed are methods of treating cancer using the compds. of formula I an of synthesizing compds. of formula I. Example compd. II was prepd. from intermediate III and 1-(tert-butoxycarbonyl)piperidine-3-carboxylic acid in the presence of diphenylphosphoryl azide and TEA.  In an active mouse ERK2 activity assay, II had an IC50 of 3.13 nM.

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

    October 28, 2015 | CAS and Influential Research
    Leaders in Japan Share Common Business
    Challenges in Driving Economic Development
    through Scientific Research

    September 1, 2015 | BizInt Smart Charts and New
    STN Collaboration Extends and Optimizes Intellectual
    Property Search Workflow

    August 7, 2015 | CAS Announces the 2015 SciFinder
    Future Leaders in Chemistry and First-Ever Alumni

                                                                    More News >> 

Media Contact

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