N-SUBSTITUTED INDOLE-3-GLYOXYLAMIDES AND MEDICINAL PREPARATION ELICITING ANTI-ASTHMATIC, ANTI-ALLERGIC AND IMMUNODEPRESSIVE/IMMUNOMODULATING EFFECT, METHOD FOR PREPARING COMPOUNDS (VARIANTS) AND METHOD FOR PREPARING MEDICINAL PREPARATION

摘要

FIELD: organic chemistry, medicine, pharmacy.;SUBSTANCE: invention relates to N-substituted indole-3-glyoxylamides of the general formula (I); ;eliciting anti-asthmatic, anti-allergic and immunodepressive/immunomodulatingb effect wherein R means hydrogen atom, (C₁-C₆)-alkyl wherein alkyl group comprises optionally one phenyl substituent that, in turn, comprises optionally at least one substituent taken among the group including halogen atom, methoxy-group, ethoxy-group, (C₁-C₆)-alkyl; R₁ means phenyl cycle comprising at least one substituent taken among the group including (C₁-C₆)-alkoxy-group, hydroxy-group, nitro-group, (C₁-C₆)-alkoxycarbonylamino-group or one fluorine atom; or R₁ represents pyridine residue of the formula (II):; ;wherein carbon atoms 2, 3 and 4 in pyridine residue have optionally similar or different substituents R₅ and R₆ wherein R₅ and R₆ mean (C₁-C₆)-alkyl or halogen atom; or R₁ represents allylaminocarbonyl-2-methylprop-1-yl group; or R and R₁ in common with nitrogen atom to which they are bound form piperazine cycle of the formula (III):; ;wherein R₇ means phenyl or pyridinyl; R₂ means (C₁-C₆)-alkyl that comprises optionally phenyl residue that, in turn, is substituted optionally with halogen atom, methoxy-group or ethoxy-group; or (C₁-C₆)-alkyl group relating to R₂ is substituted optionally with 2-, 3- or 4-pyridyl residue; R₃ and R₄ are similar or different substituents and mean hydrogen atom, hydroxy-group, (C₁-C₆)-alkoxy-group, (C₁-C₃)-alkoxycarbonylamino-group or (C₁-C₃)-alkoxycarbonylamino-(C₁-C₃)-alkyl; or R₃ represents cyclopentyloxycarbonylamino-group; Z means oxygen atom (O) being alkyl, alkoxy-group or alkylamino-group mean both regulated unbranched groups, such as methyl, ethyl, n-propyl, n-butyl, n-hexyl and branched alkyl group, such as isopropyl or tert.-butyl group; halogen atom means fluorine, chlorine, bromine or iodine and alkoxy-group means methoxy-, propoxy-, isopropoxy-, isobutoxy- or pentoxy-group, and also their pharmaceutically acceptable salts with acids. Compounds with indicated activity can be used for preparing a medicinal preparation.;EFFECT: improved preparing methods, valuable medicinal properties of compounds and preparation.;7 cl, 2 sch, 5 tbl, 34 ex