Substd. 2-amino-3,4-di:hydropropyridine derivs. - lipid absorption inhibitors, diuretics, saluretics, antiarrhythmics and cardiotonics, reduce high cholesterol levels in serum

• Main Authors: THOMAS,.DR.,GUENTHER, MEYER,.DR.,HORST, GARTHOFF,BERNWARD,DR, TOWART,ROBERTSON,DR, SITT,RUEDIGER,DR, ROSENTRETER,.DR.,ULRICH
• Format: Patent
• Language: English; German
• Published: 19.06.1981
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Substd. 2-amino-3,4-dihydropyridine derivs. of formula (I) and their pharmaceutically acceptable salts are new. (R is H, alkyl (opt. substd. by OH, halogen, alkoxy or NR8R9), opt. substd. aralkyl or aryl (opt. contg. 1 or 2 halo, alkyl, alkoxy, alkyl mercapto or CF3 substits); R8 and R9 are each H, alkyl or aralkyl; R1 and R2 are each aryl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, quinolyl, isoquinolyl, indolyl, benzimidazolyl, quinazolyl or quinoxalyl, all of these gps. opt. contg. 1,2 or 3 phenyl, alkyl, alkenyl, alkinyl, alkoxy, alkenoxy, alkinoxy, alkylene, dioxyalkylene, halo, CF3, OCF3, SCF3, OH, amino, alkylamino, dialkylamino, alkylarylamino, NO2, CN, azido, carboxy, carbalkoxy, carbonamido, sulphonamido and/or SOM-alkyl (M=0,1 or 2) substits., the alkyl and alkoxy substits. being opt. substd. by alkoxy, carboxy, carbalkoxy, halo, amino alkylamino or dialkylamino. R3 and R4 are each H, alkyl, aralkyl, alkenyl or alkinyl, the alkyl and alkenyl gps. being opt. linear, branched or cyclic and opt. substd. by COR5; or R3 and R4 together with the N-atom to which they are attached, form a 4-7 membered ring opt. interrupted by O,S, NH or NR6; R5 is alkyl, aralkyl or aryl; and R6 is as R1 and R2. (I) are very effective in the treatment of metabolic disturbances, esp. causing a reduction of increased cholesterol levels in serum with simultaneous reduction of hyperhiglyerinaemia. (I) can therefore be used to treat hyperlipoproteinaemia, atherosi atherosclerosis, adipositas, and attendant metabolic disorders. (I) are esp. suitable for use as lipid absorption inhibitors, diuretics, saluretics, antiarrhythmics and cardiotonics. Suitable daily doses are 1.0-500 (pref. 5-100) mg/kg.