3-(ACYLAMINOMETHYL)IMIDAZOL[1,2-A]PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY

摘要

3-(ACYLAMINOMETHYL)IMIDAZO¢1,2-a!PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY A compound which is a 3-(acylaminomethyl)-imidazo¢1,2-a!pyridine derivative of formula (I) (I) in which R1 denotes hydrogen; linear or branched C1-C4 alkyl; or benzyl: R2 denotes linear or branched C1-C6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl: or R1 and R2 together denote a C3-C5 aliphatic chain: and either a) X1 and X2 both denote hydrogen, X3 denotes halogen; C1-C3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula -COOR in which R denotes hydrogen or C1-C6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula -CONR3R4 in which R3 and R4 independently denote hydrogen or C1-C4 alkyl or together denote a chain of formula -(CH2)2-Z-(CH2)2- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula -CH2-, -NH- or -N(C1-C4 alkyl)-; alkylamino of formula NHR5 in which R5 denotes C2-C6 alkyl; or dialkylamino of formula -NR6R7 in which R6 and R7 independently denote C2-C6 alkyl or together denote a chain of formula -(CH2)2-Z-(CH2)2- in which z denotes a direct bond, oxygen, sulphur, or a divalent group of formula -CH2-, -NH- or -N(C1-C4 alkyl)-: and Y denotes hydrogen; halogen; methyl; trifluoromethyl; optionally esterified carboxy of formula -COOR8 in which R8 denotes hydrogen or C1-C6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula -CONR9R10 in which R9 and R10 independently hydrogen or C1-C4 alkyl; or optionally mono- or dialkylated amino of formula -NR11R12 in which R11 and R12 independently denote hydrogen or C1-C4 alkyl: with the exclusion, in case (a), of compounds in which X3 denotes halogen; alkyl; or methylthio and Y denotes hydrogen; halogen; or methyl: or b) X1, X2 and X3 independently denote hydrogen; halogen; C1-C4 alkyl; methoxy; methylthio; ethylthio; methylsulphonyl; nitro; amino; methylamino; dimethylamino; acetylamino; or diacetylamino: and Y denotes hydrogen; chlorine; or methyl: with the exclusion, in case (b), of compounds in which X1 and X2 both denote hydrogen: or a pharmacologically acceptable acid addition salt is useful in therapy.