1192471-72-9

Upstream product

• 364-73-8 4-Bromo-1-fluoro-2-nitrobenzene 
• 1192471-71-8 4-bromo-1-isopropylsulfanyl-2-nitrobenzene 

Downstream Products

• 1352244-84-8 2-nitro-1-(propane-2-sulfonyl)-4-vinylbenzene 
• 1352244-13-3 2-(propane-2-sulfonyl)-5-vinylphenylamine 
• 1352244-12-2 5-bromo-2(propane-2-sulfonyl)phenylamine 
• 1352244-36-0 N₂-[5-bromo-2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-5-chloro-N₄-[2-(propane-2-sulfonyl)-5-vinylphenyl]pyrimidine-2,4-diamine 
• 1352244-33-7 N₄-[5-bromo-2-(propane-2-sulfonyl)phenyl]-5-chloro-N₂-[4-(4-methylpiperazin-1-yl)-3-vinylphenyl]pyrimidine-2,4-diamine 
• 1352244-21-3 (2,5-dichloropyrimidin-4-yl)-[2-(propane-2-sulfonyl)-5-vinylphenyl]amine 
• 1352244-19-9 [5-bromo-2-(propane-2-sulfonyl)phenyl]-(2,5-dichloropyrimidin-4-yl)amine 
• 1192471-73-0 3-{[4-(Isopropylsulfonyl)-3-nitrophenyl]ethynyl}aniline 

Relevant academic research and scientific papers

Pyrimidina-1,5(1,3)-dibenzenacycloheptaphane derivative as mutant epidermal growth factor receptor inhibitor

The present invention relates to a pyrimidinyl monobenzocycloheptazole derivative represented by chemical formula I, a solvate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient, capable of effectively inhibiting the growth and drug resistance of cancer cells caused by the mutation of tyrosine kinase domain in epidermal growth factor receptor (Chem. I). .

Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.13,7.1 9,13]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles

A novel set of 2,4,8,22-tetraazatetracyclo[14.3.1.13,7.1 9,13]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles were prepared as potential anaplastic lymphoma kinase (ALK) inhibitors, designed to rigidly lock an energy-minimized bioactive conformation of the diaminopyrimidine (DAP) scaffold, a well-documented kinase platform. From 13 analogues prepared, macrocycle 2m showed the most promising in vitro ALK enzymatic (IC50 = 0.5 nM) and cellular (IC50 = 10 nM) activities. In addition, macrocycle 2m exhibited a favorable kinase selectivity preference for inhibition of ALK relative to the highly homologous insulin receptor (IR) kinase (IR/ALK ratio of 173). The inclusive in vitro biological results for this set of macrocycles validate this scaffold as a viable kinase template and further corroborate recent DAP/ALK solid state studies indicating that the inverted "U" shaped conformation of the acyclic DAPs is a preferred bioactive conformation.

MACROCYCLIC COMPOUNDS AS ALK, FAK AND JAK2 INHIBITORS

The present invention provides compounds of Formula I or a pharmaceutically acceptable salt forms thereof, wherein R1, R2, R3, R4, R5, A and X are as defined herein, methods of treatment and uses thereof.

MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS

The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, w