Dr. Karl Thomae Gmbh

Karl Thomae Gmbh

Karl Thomae Gesellschaft MIT Beschrankter Haftung

Adriaan De Jonge

Wolfgang Eberlein

Wolfhard Engel

Gerhard Mihm

Norbert Mayer

Gunter Trummlitz

Klaus Rudolf

Antonio Giachetti

Rudolf Hammer

Gunther Trummlitz

Jacobus C Van Meel

Hendricus C Innemee

Petrus B Timmermans

Pieter A Van Zwieten

Novel condensed diazepinone of general formula I are described, ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A.sup.1, A.sup.2 and R.sup.1 to R.sup.10 are as defined in herein useful as vagal pacemakers for treating bradycardia and bradyarrhythmia. The novel diazepinones also have spasmolytic properties on peripheral organs, antiemetic properties and are capable of promoting cerebral blood flow.

Condensed diazepinones, processes for preparing them and pharmaceutical

New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.

Substituted pyrido(2,3-B) (1,4) benzodiazepin-6-ones, and medicaments

New condensed diazepinones of general formula I are described ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A, R.sup.1 to R.sup.10 and Z are defined as in the specification.

(.+-.)-1-[4-[Ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]-N, N-dimethyl-4-piperidine carboxamide and (+)-1-[4-[ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]N,N-d imethyl-4-piperidinecarboxamide, as well as the physiologically acceptable acid addition salts of these compounds are suitable for the treatment of bradycardia and bradyarrhythmia.

Agent for treating bradycardia and bradyarrhythmia

There are described new condensed diazepinones of general formula ##STR1## wherein  .circle.B represents one of the divalent groups ##STR2## and D represents the groups ##STR3## and X.sup.1, X.sup.2 represents a .dbd.CH-- group or, if  .circle.B assumes the meaning of the divalent group S, U or W, they may also represent an N atom, A.sup.1 and A.sup.2 in general represent lower alkylene groups, Z represents a C--C bond or the groups, --O--, --S--, --CH.sub.2 --, or --(CH.sub.2).sub.2 --; R represents hydrogen or methyl, R.sup.1 and R.sup.2 generally represent alkyl groups which, together with the nitrogen atom between them, may also form a saturated monocylic, heterocyclic group, R.sub.3 represents alkyl, chlorine or hydrogen, R.sub.4 represents hydrogen or methyl, R.sup.5 and R.sup.6 represent hydrogen, halogen or alkyl, R.sub.7 represents hydrogen, chlorine or methyl, R.sup.8 represents hydrogen or lower alkyl, R.sup.9 represents hydrogen, halogen, lower alkyl and R.sup.10 represents hydrogen or methyl and R.sup.12 represents branched or unbranched alkyl. The compounds of general formula I and the acid addition salts thereof may be resolved into their isomers. The compounds of formula I and their salts may be used as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia.

Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom and

5,11-dihydro-6H-pyrido(2,3-B)(1,4)benzodiazepin-6-ones substituted in

The method of treating glaucoma with compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, hydroxy-(alkyl of 1 to 4 carbon atoms), benzyl, halo-benzyl, methyl-benzyl, methoxy-benzyl or allyl;

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Adriaan De Jonge