900174-43-8

The invention relates to a ceritinib intermediate and a method for preparing ceritinib. A ceritinib intermediate compound is 4-isopropoxy-5-guanidyl-2-N-substituted piperidine-4-base toluene nitrate (VII). The method includes carrying out substation reaction on 2-nitro-4,5-dimethyl chlorobenzene and isopropyl alcohol in the presence of alkali to generate compounds III; carrying out condensation onthe compounds III and halogenated acetaldehyde di-acetal and carrying out reduction ring formation by ammonia-ammonium chloride-sodium borohydride to obtain compounds IV; carrying out amino protection to obtain compounds V; carrying out catalytic hydrogenation in solvents and carrying out nitro reduction to obtain amino so as to obtain compounds VI; carrying out reaction on the compounds VI and cyanamide to obtain compounds VII. The ceritinib can be prepared from the compounds VII by the aid of the method. The ceritinib intermediate and the method have the advantages of inexpensive and easilyavailable raw materials, simplicity and convenience in operation, high elementary reaction selectivity, low wastewater quantity and green environmental protection.

The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions.

The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.