Lipid absorption inhibiting di:hydro-pyridine derivs. - which are 6-amino-4,5-di:aryl-4,5-di:hydro-pyridine-3-carboxylic acid ester(s)

摘要

New 6-amino-4,5-diaryl-4,5-dihydro pyridine-3-carboxylic acid ester derivs. are the tautomeric cpds. of formula (Ia,b) and their pharmaceutically innocuous salts (where R1 and R2 are aryl or heteroaryl (thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxozolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinolyl, isoquinolyl, indolyl, benzimidazolyl, quinazolyl or quinoxalyl) opt. carrying 1, 2 or 3 substits. selected from phenyl, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylene, dioxyalkylene, halogen, CF3, OCF3, OH, amino, alkylamino, dialkylamino, alkylarylamino, NO2, CN, N3, COOH, carbalkoxy, carboxamido, sulphonamido and S(O)m-alkyl (m is 0, 1 or 2), the alkyl and alkoxy substituents opt. in turn being substd. by alkoxy, COOH, carbalkoxy, halogen, NH2, alkylamino or dialkylamino; R3 is an open-chain or cyclic, saturated or unsaturated hydrocarbon residue opt. substd. by OH, alkoxy, halogen, aryl or a group -N(R')(R") (in which R' and R" are H, alkyl or aralkyl); and R4 is H, alkyl, aralkyl or a group -N(R"')(R"") (in which R" and R"" are H, aralkyl, alkyl or alkyl substd. by halogen or alkoxy, or -N(R"'(R"") is a 4-to-7-membered aliphatic (sic) ring opt. contg. as a ring member an O- or S-atom or an NH or NR5' group, R5' being a residue as defined for R1 and R2 above)). (Ia,b) have lipid absorption inhibiting activity; in particular, they lower elevated serum cholesterol levels and reduce hypertriglyceridaemia. They are therefore suitable for use in the treatment of hyperlipoproteinoemias, atherosclerosis, adipositas and metabolic disorders induced thereby. (Ia,b) are also useful as diuretics, saluretics, antiarrhythmics and cardiotonics.