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
