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Upstream product

• 109-01-3 1-methyl-piperazine 
• 6336-45-4 vinylboronic acid dibutyl ester 
• 477846-54-1 1-(2-bromo-4-nitrobenzene)-4-methylpiperazine 
• 701-45-1 2-bromo-1-fluoro-4-nitrobenzene 
• 7486-35-3 tri-n-butyl(vinyl)tin 

Downstream Products

• 1352244-23-5 4-(4-methylpiperazin-1-yl)-3-vinylphenylamine 
• 1352244-32-6 4-bromo-2-(5-chloro-2-[4-(4-methylpiperazin-1-yl)-3-vinylphenylamino]pyrimidin-4-ylamino)benzoic acid methyl ester 
• 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 
• 1352244-34-8 N-(4-bromo-2-{5-chloro-2-[4-(4-methylpiperazin-1-yl)-3-vinylphenylamino]pyrimidin-4-ylamino}phenyl)-N-methylmethanesulfonamide 
• 1395028-50-8 3-ethyl-4-(4-methylpiperazin-1-yl)aniline 

Relevant academic research and scientific papers

TRICYCLIC INHIBITORS OF KINASES

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

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.