| 摘要 |
<p>Phenyl-(5-trifluoromethyl-pyrimidin-2-yl)-amine compounds (I) and their salts, diastereomers or enantiomers are new. Phenyl-(5-trifluoromethyl-pyrimidin-2-yl)-amine compounds of formula (I) and their salts, diastereomers or enantiomers are new. R 1> : 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, 3-7C-cycloalkyl or phenyl ring (all optionally substituted by OH, NR 3>R 4>, CN, halo, CF 3, 1-6C-alkoxy, OCF 3 and/or 1-6C-alkyl); R 2> : 1-10C-alkyl, 3-10C-alkenyl, 3-10C-alkynyl or 3-7C-cycloalkyl ring (all optionally substituted by halo, OH, NR 3>R 4>, CN, CF 3, OCF 3, 1-6C-alkoxy, 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, or 3-8C-cycloalkyl, -O-CH 2-phenyl, C n-alkoxycarbonyl (optionally substituted by halo, OH, 1-6C-alkyl, 1-6C-alkoxy, NR 3>R 4>, CF 3 and/or OCF 3)), preferably alcohol group of formula (A); R1a : CH 3, C 2H 5, propyl or isopropyl; R1b, R1c : H, CH 3 or C 2H 5; either R 3>, R 4> : H, 1-6C-alkyl, 2-6C-alkenyl, 3-8C-cycloalkyl, phenyl ring, 3-8 membered heterocycle ring, and/or a monocyclic heteroaryl ring (optionally substituted by OH, NR 5>R 6>, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3); or R 3>R 4>N : 5-7-membered ring optionally containing 1 or 2 further heteroatoms in addition to N, and optionally substituted by OH, NR 5>R 6>, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3; and R 5>, R 6> : H or 1-6C-alkyl (optionally substituted by OH, CN, halo, CF 3, 1-6C-alkoxy and/or OCF 3). An independent claim is included for the preparation of (I). [Image] [Image] ACTIVITY : Cytostatic; Virucide; Cardiovascular-Gen.; Vasotropic; Antiarteriosclerotic. MECHANISM OF ACTION : Cyclin-dependent kinase inhibitor; Vascular endothelial growth factor receptor kinase-2 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 insects cells. The results showed that (2R,3R)-3-[2-(4-methanesulfonyl-phenylamino)-5-trifluoromethyl-pyrimidin-4-yloxy]-butan-2-ol exhibited an IC 5 0 value of 9 nM.</p> |
