N-(4-PIPERIDINYL) (DIHYDROBENZOFURAN OR DIHYDRO-2H-BENZOPYRAN)CARBOXAMIDE DERIVATIVES, METHOD AND INTERMEDIATES FOR THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS BASED ON THEM

摘要

N-(4-piperidinyl) (dihydrobenzofuran or dihydro-2H-benzopyran)carboxamide derivatives, method and intermediates based on them. These derivatives have the structure of formula (I), wherein A is a radical of formula -CH2-CH2- (a-1), -CH2-CH2-CH2- (a-2), or -CH2-CH2- CH2-CH2- (a-3), wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C1-6 alkyl radical; R1 is hydrogen or halogen; R2 is hydrogen, amino, mono or dialkylamino or alkylcarbonylamino; R3 is hydrogen or alkyl L is cycloalkyl, cycloalkanone, alkenyl or L is -Alk-R4 (b-1), -Alk-X-R5 (b-2), -Alk-Y-C(=O)-R7 (b-3) or -Alk-Y-C(=O)-NR9R10 (b-4), wherein Alk is alkanediyl and R4 is H, CN, alkylsulphonylamino cycloalkyl, cycloalkanone aryl, diarylmethyl or Het, R5 is H, alkyl, hydroxyalkyl, cycloalkyl, aryl or Het, X is O, S, SO2 or NR6, wherein R6 is H, alkyl or aryl, R7 is H, alkyl, cycloalkyl, aryl, arylalkyl in alkyl, diarylmethyl, alkoxy or OH, Y is NR8 or bound whilst R8 is H, alkyl or aryl, R9 and R10 are H, alkyl, cycloalkyl, aryl or aralkyl in alkyl, or R9 and R10 together with N are pyrolidinyl or piperidinyl circle, or R9 and R10 together with N are piperazinyl or 4-morpholine residue, and their N-oxides, salts and stereochemical isomers.