| 摘要 |
<p>The invention relates to a new application of benzacetaminederivatives as medicamentous formulations, to theirpharmaceutically acceptable adjunctive salts and to theirstereochemical isomers. The derivatives have the formulawhere R1 and R2 mean, separately from each other, hydrogen, C1-C6alkyl or C3-C6 cycloalkyl; R1 and R2 together with the nitrogenatom to which thy are bound may form pyrrolidine, piperidinyl,morpholine, piperazinyl or 4-C1-4 alkylpiperazinyl group; X is Oor S; R3 is hydrogen or C1-C6 alkyl; R4, R5 and R6, separatelyfrom each other are hydrogen, halogen, C1-C6 alkyl, C1-C6alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl,C1-C4 alkyloxycarbonyl, C1-C4 alkylcarbonyl, aminocarbonyl andhydroxy; R7 is hydrogen or halogen, and R8, R9 & R10,independently, are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkyloxy,nitro, hydroxy, trifluoromethoxy, 2,2,2-trifluoroethoxy,(trifluoromethyl)carbonyl, aminocarbonyl, (cyclopropyl) carbonylor C1-C6 alkyl-C(=Y)-radical, where Y is O, =N-OH, =N-OCH3, =N-NH2or =N-N(CH3)2 provided that: 1) R1 is different from n-propyl,when R2, R3, R4, R5, R6, R7, R9 & R10 are hydrogen, R8 means4-ethoxy and X is oxygen, and 2) X is different from sulphur, whenR1, R2, R3, R6, R7 R9 & R10 are hydrogen and R4 & R5 aredimethoxy. The invention also relates to new benzacetaminederivatives, to pharmaceutical composition containing them and tomethods for their preparation.18 claims</p> |
