| 摘要 |
<p>Disclosed are compounds of the general formula , Iwherein R - hydrogen, lower alkyl, lower alkoxy group, halogen or trifluoromethyl; R1 û hydrogen or halogen, or R and R1 together may represent a group -CH=CH-CH=CH-; R2 and R2' independently one fromanother represent hydrogen, halogen, trifluoromethyl, lower alkoxy or cyanogroup; or R2 and R2' together may represent a group -CH=CH-CH=CH-, possibly substituted by one or two substituents selected of the lower alkyl of lower alkoxygroup; every R3 - hydrogen, lower alkyl or together form cycloalkyl group; R4 - hydrogen, -N(R5)2, -N(R5)(CH2)nOH, -N(R5)S(O)2-lower alkyl, -N(R5)S(O)2-phenyl, -N=CH-N(R5)2, -N(R5)C(O)R5 or cyclic tertiary amine -or ,R5 independently one from another represent hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 -hydrogen, hydroxy group, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyanogroup, -(CH2)nO(CH2)nOH, -CHO or 5- or 6-membered heterocyclic group, possibly, related through alkylene group, X - -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)- or -N(R5)(CH2)m-; n = 0-4; and m = 1 or 2, and also pharmaceutically acceptable salts thereof with acids. Compounds of the formula I reveal a high affinity to the receptor NK-1. They can be used for treating diseases relating to antagonsists or receptor NK-1.</p> |
