40422-90-0Relevant articles and documents
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl) phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials
Marsilje, Thomas H.,Pei, Wei,Chen, Bei,Lu, Wenshuo,Uno, Tetsuo,Jin, Yunho,Jiang, Tao,Kim, Sungjoon,Li, Nanxin,Warmuth, Markus,Sarkisova, Yelena,Sun, Frank,Steffy, Auzon,Pferdekamper, Annemarie C.,Li, Allen G.,Joseph, Sean B.,Kim, Young,Liu, Bo,Tuntland, Tove,Cui, Xiaoming,Gray, Nathanael S.,Steensma, Ruo,Wan, Yongqin,Jiang, Jiqing,Chopiuk, Greg,Li, Jie,Gordon, W. Perry,Richmond, Wendy,Johnson, Kevin,Chang, Jonathan,Groessl, Todd,He, You-Qun,Phimister, Andrew,Aycinena, Alex,Lee, Christian C.,Bursulaya, Badry,Karanewsky, Donald S.,Seidel, H. Martin,Harris, Jennifer L.,Michellys, Pierre-Yves
, p. 5675 - 5690 (2013/08/23)
The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.
NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF
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Page/Page column 121; 122, (2013/10/22)
The present invention relates to compounds of formula (I): wherein R6 is -CONH2 or a -C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
