1190071-58-9

Upstream product

• 622386-07-6 tert-butyl 4-(pyrazin-2-yl)piperazine-1-carboxylate 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 622386-08-7 5'-bromo-2,3,5,6-tetrahydro-1,2'-bipyrazinyl-4-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

CDK4/6 INHIBITOR

Disclosed is a series of compounds acting as CDK4/6 inhibitors. Specifically disclosed are compounds as represented by formula (I), pharmaceutically acceptable salts or isomers thereof, pharmaceutical compositions containing same, and the use thereof in the preparation of drugs for treating cancers.

SUBSTITUTED 2-HYDROGEN-PYRAZOLE DERIVATIVE SERVING AS ANTICANCER DRUG

Disclosed is a substituted 2H-pyrazole derivative serving as a selective CDK4/6 inhibitor. Specifically, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt thereof which serves as a selective CDK4/6 inhibitor.

HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY

Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

4-(pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6

Identification and structure-guided optimization of a series of 4-(pyrazol-4-yl)-pyrimidines as selective CDK4/6 inhibitors is reported herein. Several potency and selectivity determinants were established based on the X-ray crystallographic analysis of representative compounds bound to monomeric CDK6. Significant selectivity for CDK4/6 over CDK1 and CDK2 was demonstrated with several compounds in both enzymatic and cellular assays.