871839-91-7Relevant articles and documents
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology
Boga, Sobhana Babu,Deng, Yongqi,Zhu, Liang,Nan, Yang,Cooper, Alan B.,Shipps, Gerald W.,Doll, Ronald,Shih, Neng-Yang,Zhu, Hugh,Sun, Robert,Wang, Tong,Paliwal, Sunil,Tsui, Hon-Chung,Gao, Xiaolei,Yao, Xin,Desai, Jagdish,Wang, James,Alhassan, Abdul Basit,Kelly, Joseph,Patel, Mehul,Muppalla, Kiran,Gudipati, Subrahmanyam,Zhang, Li-Kang,Buevich, Alexei,Hesk, David,Carr, Donna,Dayananth, Priya,Black, Stuart,Mei, Hong,Cox, Kathleen,Sherborne, Bradley,Hruza, Alan W.,Xiao, Li,Jin, Weihong,Long, Brian,Liu, Gongjie,Taylor, Stacey A.,Kirschmeier, Paul,Windsor, William T.,Bishop, Robert,Samatar, Ahmed A.
, p. 761 - 767 (2018/06/25)
The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were identified as potent inhibitors of ERK1/2 with excellent kinase selectivity and dual mechanism of action but suffered from poor pharmacokinetics (PK). The challenge of PK was overcome by the discovery of a novel 3(S)-thiomethyl pyrrolidine analog 7. Lead optimization through focused structure-activity relationship led to the discovery of a clinical candidate MK-8353 suitable for twice daily oral dosing as a potential new cancer therapeutic.
SPIROCYCLIC COMPOUNDS
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, (2017/07/31)
Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
COMPOUNDS THAT ARE ERK INHIBITORS
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, (2009/10/18)
Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
