GERHARD SIEMEISTER,JULIA SCHULZE,PHILIP LIENAU,ROLF JAUTELAT,ULRICH LÜCKING
申请号：
BRPI0920112
公开号：
BRPI0920112A2
申请日:
2009.10.09
申请国别(地区):
BR
年份:
2015
代理人:
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.
