| abstract |
It refers to compounds of the general formula 1 wherein X is a single bond or an ethynediyl group, where, in case X is a single bond, R1 is hydrogen, halogen, nitro, lower alkyl, halo-lower alkyl; alkoxycarbonyl, lower cycloalkyl, optionally substituted with oxygen, benzoyl, optionally substituted with lower alkyl, halo-lower alkyl, or halogen, phenyl, optionally substituted with halogen, hydroxy, lower alkyl, halo-lower alkyl, lower cycloalkyl, or alkoxy lower, halo-lower alkoxy, or cyano, styrenyl, phenylethyl, naphthyl, biphenyl, benzofuranyl, 5 or 6-link heterocyclic ring, optionally substituted with oxo, benzyloxy, benzoyl, methanesulfonyl, benzene lfonyl, or acetyl; if Xsea is an ethynediyl group, R1 is hydrogen, lower alkyl, optionally substituted with hydroxyl; halo-lower alkyl; lower cycloalkyl, optionally substituted with hydroxyl, lower alkyl, halo-alkyl or lower, lower alkoxy, halo-lower alkoxy, or halogen, lower cycloalkenyl, optionally substituted with lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, halogen , or oxo, lower alkenyl, phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy, halo, heterocyclic ring of 5 or 6 links, optionally substituted with lower alkyl, halogen, oxo, benzyloxy, benzoyl , methanesulfonyl, benzenesulfonyl, acetyl, pivaloyl, tert.butoxycarbonyl, or tert. butylcarbonyl; or benzofuranyl; R3 is phenyl, pyridine, thiophenyl or thiazolyl, which are optionally substituted with halogen, cyano, nitro, azido, hydroxyl, car boxyl, morpholin-4-carbonyl, carbamoyl, thiocarbamoyl, N-hydroxycarbamoyl, trimethylsilyl-ethynyl, or lower alkyl , lower alkynyl, lower alkoxy, halo-lower alkyl, 4-lower alkyl-piperazin-1-carbonyl, lower aminoalkylcarbonyl, which are optionally substituted by amino, lower aminoalkyl, acyl, oxo, hydroxyl, lower alkoxy, lower thioalkyl, or carboxyl which is optionally esterified or |