427878-70-4Relevant articles and documents
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
-
, (2018/03/25)
The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
Development of a practical synthesis of a p38 kinase inhibitor via a safe and robust amination
Shi, Zhongping,Kiau, Susanne,Lobben, Paul,Hynes Jr., John,Wu, Hong,Parlanti, Luca,Discordia, Robert,Doubleday, Wendel W.,Leftheris, Katerina,Dyckman, Alaric J.,Wrobleski, Stephen T.,Dambalas, Konstantinos,Tummala, Srinivas,Leung, Simon,Lo, Ehrlic
, p. 1618 - 1625 (2013/02/23)
The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)- hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38α MAP kinase inhibitors
Wrobleski, Stephen T.,Lin, Shuqun,Hynes Jr., John,Wu, Hong,Pitt, Sidney,Shen, Ding Ren,Zhang, Rosemary,Gillooly, Kathleen M.,Shuster, David J.,McIntyre, Kim W.,Doweyko, Arthur M.,Kish, Kevin F.,Tredup, Jeffrey A.,Duke, Gerald J.,Sack, John S.,McKinnon, Murray,Dodd, John,Barrish, Joel C.,Schieven, Gary L.,Leftheris, Katerina
, p. 2739 - 2744 (2008/12/21)
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38α MAP kinase inhibitors. The synthesis, structure-activity relationships (SAR), and in vivo activity of selected analogs from this class o