427878-70-4Relevant articles and documents
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0230; 0233, (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.
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α mitogen-activated protein kinase inhibitors
Hynes Jr., John,Dyckman, Alaric J.,Lin, Shuqun,Wrobleski, Stephen T.,Wu, Hong,Gillooly, Kathleen M.,Kanner, Steven B.,Lonial, Herinder,Loo, Derek,McIntyre, Kim W.,Pitt, Sidney,Ding, Ren Shen,Shuster, David J.,Yang, XiaoXia,Zhang, Rosemary,Behnia, Kamelia,Zhang, Hongjian,Marathe, Punit H.,Doweyko, Arthur M.,Tokarski, John S.,Sack, John S.,Pokross, Matthew,Kiefer, Susan E.,Newitt, John A.,Barrish, Joel C.,Dodd, John,Schieven, Gary L.,Leftheris, Katerina
, p. 4 - 16 (2008/09/18)
A novel structural class of p38 mitogen-activated protein (MAP) kinase inhibitors consisting of substituted 4-(phenylamino)-pyrrolo[2,1-f][1,2,4] triazines has been discovered. An initial subdeck screen revealed that the oxindole-pyrrolo[2,1-f][1,2,4]tria