1445894-87-0

Upstream product

• 1369906-03-5 4-bromo-1-nitro-2-(propan-2-yloxy)benzene 
• 1692-15-5 4-pyridylboronic acid 
• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 625-98-9 3-chlorofluorobenzene 
• 40422-90-0 4-chloro-1-nitro-2-(propan-2-yloxy)benzene 
• 700-37-8 4-chloro-2-fluoro-nitrobenzene 

Downstream Products

• 1462951-47-8 N-[4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)phenyl]formamide 
• 1462947-68-7 7-(2-methoxyphenyl)-2-{[4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)phenyl]-amino}thieno[3,2-d]pyrimidine-6-carboxamide 
• 1462950-47-5 4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)aniline 
• 1462950-48-6 1-methyl-4-[4-nitro-3-(propan-2-yloxy)phenyl]pyridinium iodide 
• 1462952-26-6 methyl 7-(2-methoxyphenyl)-2-{[4-(1-methylpiperidin-4-yl)-2-(propan-2-yloxy)phenyl]amino}thieno[3,2-d]pyrimidine-6-carboxylate 
• 1462951-24-1 2-{4-[4-nitro-3-(propan-2-yloxy)phenyl]-3,6-dihydropyridin-1(2H)-yl}ethanol 
• 1462951-21-8 2-{4-[4-amino-3-(propan-2-yloxy)phenyl]piperidin-1-yl}ethanol 
• 1462951-23-0 1-(2-hydroxyethyl)-4-[4-nitro-3-(propan-2-yloxy)phenyl]pyridinium iodide 
• 1032903-33-5 5-chloro-N₂-(2-isopropoxy-4-(piperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1445894-89-2 2-methylpropan-2-yl 4-[4-amino-3-(propan-2-yloxy)phenyl]piperidine-1-carboxylate 

Relevant academic research and scientific papers

NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF

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.

NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF

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.

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

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.