SULFOXIMINE SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS MEDICINE

摘要

Sulfoximine substituted anilino-pyrimidine compounds (I) and their salts, diastereomers and enantiomers, are new. Sulfoximine substituted anilino-pyrimidine compounds of formula (I) and their salts, diastereomers and enantiomers, are new. X : O or NH; R1 : methyl, ethyl, propyl or isopropyl; R2, R3 : H, methyl or ethyl; and R4 : 1-6C-alkyl or 3-7C-cycloalkyl ring. Independent claims are included for the preparations of (I). [Image] ACTIVITY : Cytostatic; Virucide; Cardiovascular-Gen.; Vasotropic; Antiarteriosclerotic. MECHANISM OF ACTION : Cyclin-dependent kinase inhibitor. The ability of (I) to inhibit cyclin-dependent kinase was tested in recombinant cyclin-dependent kinase-1 and B-type cyclin-glutathione-S-transferase-fusion proteins purified from baculovirus infected insect cells. The results showed that (RS)-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]amino}-5-(trifluoromethyl) pyrimidin-2-yl]amino}phenyl)-S-methylsulfoximide exhibited an IC 5 0 value of 3 nM.