ANALOGIFREMGANGSMAATE FOR FREMSTILLING AV TERAPEUTISK AKTIVE PYRIDO (2,3-B)(1,4)BENZODIAZEPIN-6-ON-DERIVATER

• Main Authors: EBERLEIN, WOLFGANG, JONGE, ADRIAAN DE, TRUMMLITZ, GUENTER, MAYER, NORBERT, MIHM, GERHARD, ENGEL, WOLARD
• Format: Patent
• Language: Norwegian
• Published: 22.10.1990
• Edition: 5
• 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

Substituted pyrido[2,3-b]-1,4-benzodiazepin-6-ones of the formula I in which R denotes an alkyl group having 1 to 4 C atoms, a chlorine atom or a hydrogen atom; R represents a hydrogen atom or a methyl group; R and R each denote a hydrogen atom, a fluorine, chlorine or bromine atom or an alkyl group having 1 to 4 C atoms, but with the proviso that at least one of the radicals R , R , R and R is different from hydrogen, R and R represent alkyl radicals having up to 6 carbon atoms and which are identical or different from one another or together with the nitrogen atom between them form a 4- to 7-membered, saturated, monocyclic, heteroaliphatic ring which can optionally be interrupted by an oxygen atom or by the N-CH3 group, Z is either a single bond or an oxygen atom, or a methylene or 1,2- ethylene group and A is a methylene group in position 2 or 3 of the heteroaliphatic ring, or when linked in position 3 is also a single bond, and their salts with inorganic or organic acids are described. The compounds of the formula I have favourable effects on the heart rate and are suitable for use in human and veterinary medicine as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in view of a lack of gastric acid secretion- inhibiting, salivation-inhibiting and mydriatic effects, as well as excellent absorption.