| 摘要 |
1. Compounds of general formula I, or racemic mixtures thereof, or individual optical isomers thereof, or pharmaceutically acceptable salts and/or hydrates thereof, wherein: X is the amino group R'R''N, optionally substituted or unsubstituted with identical substituents R' and R'', or a substituted oxy group; the R'R''N group is a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; the amino group substituents R' and R'' are hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, heteroaroyl, alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, alkoxycarbonyl, aryloxycarbonyl, araloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, heterocyclylaminocarbonyl, alkylaminothiocarbonyl, arylaminothiocarbonyl, heteroarylaminothiocarbonyl, heterocyclylaminothiocarbonyl, optionally substituted aminosulphonyl, the R'R''N group may be a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; and the substituted oxy group is a hydroxy group in which hydrogen is substituted with alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, hetaryl and heterocyclyl, or acyl, or an aminocarbonyl group or an oxycarboyl group; R1a and R1b are hydrogen and alkyl, or R1a and R1b together form a -(CH2)n- polymethylene chain, wherein n=2-5; R1c and R1d are hydrogen and alkyl, or R1c and R1d together form a -(CH2)n- polymethylene chain, wherein n=2-5; R2 is an acyl group, a thioacyl group, a substituted oxycarbonyl group, a substituted amidine group, a substituted aminocarbonyl group, a substituted aminothiocarbonyl group or a sulphonyl group; R3 is hydrogen, C1-C6 alkyl, an alkoxy group, halogen, CF3, CN. |
