Dr. Karl Thomae Gmbh

Karl Thomae Gmbh

Other

Norbert Mayer

Wolfgang Eberlein

Gerhard Mihm

Wolfhard Engel

Gunter Trummlitz

Henri Doods

Adriaan De Jonge

Klaus Rudolf

Rudolf Hammer

Gunther Engelhardt

Antonio Giachetti

Gunther Trummlitz

Willy Roth

Volker Trach

Helmut Ballhause

Alex Prox

Welfhard Engel

Adrian De Jonge

Richard Reichl

Claus A Landgraf

Kurt Schumacher

Condensed diazepinones of general formula I ##STR1## in which

Condensed diazepinones and medicaments containing these compounds

New diazepinones of formula I ##STR1## wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human and veterinary medicine.

Condensed diazepinones, processes for preparing them and pharmaceutical

Novel compounds of the general formula ##STR1## which have antitussive activity, wherein R.sub.1 -R.sub.4 are as defined herein.

Substituted 6-benzyl-2H-3,4,5,6-tetrahydro-(1,3)-oxazines

5,11-Dihydro-6H-pyrido[2,3-b][1,4]-benzo-diazepinones substituted in the 11-position corresponding to general formula I ##STR1## wherein R.sup.1 and R.sup.2 represent hydrogen atoms or alkyl groups having 1 to 3 carbon atoms, A.sup.1 is a straight-chained or branched alkylene group with 1 to 5 carbon atoms, A.sup.2 is a methylene group or, if R.sup.1 is hydrogen and R.sup.2 is methyl, A.sup.2 may also be an ethylene group, and the physiologically acceptable acid addition salts thereof are suitable for treating bradycardia and bradyarrhythmia and spasm in the colon, bladder and bronchi.

Use of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-ones

A method for treating abstructive respiratory passage disorders which comprises the use of 5,11-dihydro-11-[[(1-methyl-4-piperidinyl)-amino]carbonyl]-6H-dibenz[b,e]a zepin-6-one; 5,11-dihydro-11-[(1-methyl-4-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, alone or in combination.

Agents for the treatment of acute and chronic obstructive respiratory

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.

Novel condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, A.sup.1, A.sup.2 and R.sup.1 -R.sup.10 are as defined herein. The condensed diazepinones are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia and they have spasmolytic effects on peripheral organs, particularly the colon, bladder and bronchi.

A method for treating shock in a patient, which comprises administering to the patient a therapeutically effective amount of a diazepinone of the general formula: ##STR1## wherein A represents a 5,11-dihydro-6H-pyrido[2,3-b] [1,4] benzodiazepin-6-one group bound in the 11-position; a 5,10-dihydro-11H-dibenzo [b,e] [1,4] diazepin-11-one group bound in the 5-position; a 5,11-dihydro-10H-pyrido [3-2b] [1-4] benzodiazepin-10-one group bound in the 5-position; a 4,9-dihydro-10H-thieno [3,4-b] [1,5] benzodiazpin-10-one group bound in the 4-position, unsubstituted or substituted at the 1- or 3-position or both in the 1- and 3-position by an alkyl group having from 1 to 4 carbon atoms, or in the 3-positionby chlorine, fluorine or bromine; a 6-11-dihydro-5H-pyrido [2,3-b] [1,5] benzodiazepin-5-one group bound in the 11-position; or a 1-methyl-1,4,9,10-tetrahydropyrrolo-[3,2-b] [1,5] benzodiazepin-10-one group bound in the 4-position, unsubstituted or substituted at the 3-position by methyl or methyl or chlorine;

Use of diazepinones for treating disorders of the microcirculation

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

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Norbert Mayer