| abstract |
A benzamidine derivative of formula 1 or the pharmaceutically acceptable salts thereof: ** Formula ** wherein R1 is methyl; ethyl; propyl; isopropyl; butyl; t-butyl; pentyl; cyclopentyl; hexyl; cyclohexyl; phenyl; aminomethyl; aminoethyl; Not me; isobutylamide; guanidine; 1-propylpiperidine; 2-morpholinomethyl; NR6R7; CH2NR6R7; ** Formula ** where A is C1 ~ C6 alkyl and n is an integer from 2 to 6; pyridinyl; 4-hydroxypiperidinomethyl; cyclohexylaminomethyl; R2 is hydrogen; methyl; ethyl; isopropyl; propyl; butyl; isobutyl; methoxymethyl; hydroxymethyl; 2-methylpropyl; pentyl; chloromethyl; chloroethyl; cyclopentyl; cyclopentylmethyl; cyclohexyl; benzyl; vinyl; R3 and R4, each independently, are hydrogen; halogen; hydroxy; cyclohexylamino; methoxy; C1-C4 alkanoyloxy; C1-C7 aliphatic alkoxy which is substituted with carboxy, esterified carboxy or amidated carboxy; R5 is hydrogen or hydroxy; R6 and R7, each independently, are hydrogen; methyl; ethyl; propyl; benzyl; pyridin-3-yl; pyridin-4-yl; 2- morpholinoethyl; 4-pyridinylcarbonyl; 3-pyridinylcarbonyl; isobutylcarbonyl; ethanesulfonyl; methoxyethyl; hydroxyethyl; hydroxyacetyl; methoxyacetyl; Y is oxygen; sulfur; NR6; CH2; X1 and X3, each independently, are oxygen; sulfur; amine; methylamine; X2 is propylene; pentylene; hexylene; heptylene; ethylene-O-ethylene; 3-hydroxy-3-methylpentylene; methylethylene-NHethylene; ethylene-NH-ethylene; propylene which is interrupted by piperazine; butylene carbonyl; 2-butenyl; methylene-phenylene-methylene; methylene-pyridylene-methylene; 1,2-ethylene-1,4-phenylene-1,2-ethylene; 1,3-propylene-1,4-phenylene-1,3-propylene; 1,2-ethylene-naphthalene-1,2-ethylene; with the proviso that if X1 and X3 are oxygen, X2 is pentyl and R3 and R4 are hydrogen, the compound of formula 1, wherein R1 is methyl and R2 is isopropyl, is excluded. |