1-OXO-3-(1H-INDOLE)-3-IL-1,2,3,4-TETRAHYDROISOXYNOLINES, METHODS FOR THE PRODUCTION THEREOF, COMBINATORIC LIBRARY AND FOCUSED LIBRARY

摘要

The invention relates to novel 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines and to the cis- and trans-isomers thereof exhibiting protein kinase inhibiting properties, to methods for the production thereof and to combinatoric and focused libraries for separating leader compounds. 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines correspond to general formulas 1 and 2, wherein R1, R2 and R4, independently from each other are, a cyclic system substituent selected from hydrogen and alkyl, R3 is an aminogroup substituent selected from alkyl, cycloalkyl or alkyl, possibly substituted with an aryl, heteroaryl, heterocyclyl, alkoxy, amine, alkylamine and dialkylamine group, R5 and R6 are, independently from each other, an amino group substituent selected from hydrogen, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl or alkyl, possibly substituted with aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, amino, alkylamine, dialkylamine, aryl alkylamine, or R5 and R6 forms, together with a nitrogen atom with which they are bound, a possibly substituted azaheterocycle. A method for obtaining compounds of general formula 1 consists in interacting corresponding indole-3-ilmethylenamines and homophtalic anhydrides in an organic solvent medium. A method for obtaining compounds of general formula 2 consists in treating the compounds of formula 1 with thionyl chloride or with 1,1'-carbonyldiimidazole in such a way that the respective derivatives are obtain and interact with respective amines of general formula 6 in the organic solvent medium.