851435-00-2

Upstream product

• 175137-46-9 5-cyclopropyl-2H-pyrazol-3-ylamine 
• 3934-20-1 2,6-Dichloropyrimidine 
• 175137-46-9 3-amino-5-cyclopropyl-1H-pyrazole 

Downstream Products

• 1266476-83-8 N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-methylsulfonylphenyl)-pyrimidin-4-amine 
• 1266476-85-0 2-[4-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]phenyl]acetonitrile 
• 1266477-49-9 3-[[4-[(5-cyclopropyl-2H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]benzenesulfonamide 
• 1425932-87-1 N⁴-(5-cyclopropyl-1H-pyrazol-3-yl)-N²-((1-tosyl-1H-indol-4-yl)methyl)pyrimidine-2,4-diamine 
• 1425932-85-9 N⁴-(5-cyclopropyl-1H-pyrazol-3-yl)-N²-((1-tosyl-1H-indol-6-yl)methyl)pyrimidine-2,4-diamine 

Relevant academic research and scientific papers

SERINE/THREONINE PAK1 INHIBITORS

Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

2, 4-DIAMINE-PYRIMIDINE DERIVATIVE AS SERINE/THREONINE KINASE INHIBITORS

Compounds having the formula I wherein A, Rla, Rlb, R2, R3, R4, R5, R6, R7, Rs, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders

PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS

The present invention relates to compounds II useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.

Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases

The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput screening identified a promising hit in the 4- aminopyrazolylpyrimidine chemotype. Initial optimization of the series led to more potent Trk inhibitors. Further optimization using two strategies resulted in significant improvement of physical properties and led to the discovery of 10z (AZ-23), a potent, orally bioavailable Trk A/B inhibitor. The compound offers the potential to test the hypothesis that modulation of Trk activity will be of benefit in the treatment of cancer and other indications in vivo.

PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES

Compounds of formula (I): and their use in the inhibition of Trk activity are described.