Dr. Karl Thomae Gmbh

Karl Thomae Gmbh

Other

Boehringer Ingelheim Kg

Boehringer Ingelheim Pharma Kg

Gerhard Mihm

Wolfgang Eberlein

Wolfhard Engel

Norbert Mayer

Henri Doods

Gunter Trummlitz

Klaus Rudolf

Adriaan De Jonge

Wolfgang Wienen

Michael Entzeroth

Norbert Hauel

Uwe Joerg Ries

Henning Priepke

Antonio Giachetti

Rudolf Hammer

Klaus Binder

Horst Dollinger

Franz Esser

Gerd Schnorrenberg

Rainer Zimmermann

Jean Marie Stassen

Klaus-Dieter Willim

Jurgen Krause

Heike Andrea Wieland

Harald Ziegler

Gunther Engelhardt

Gunther Schmidt

Jean-Marie Stassen

Gunther Trummlitz

Gu/ Nter Trummlitz

Volker Trach

Rainer Zimmerman

Jacobus C Antonius Van Meel

Wolfgang Weinen

Welfhard Engel

Adrian De Jonge

Richard Reichl

Novel disubstituted bicyclic heterocycles, of which the following are exemplary:

Disubstituted bicyclic heterocycles, the preparation thereof and their

The present invention relates to 5-membered heterocyclic condensed benzoderivatives of formula ##STR1## wherein R.sub.a to R.sub.c, A, X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. The compounds of the above formula I wherein R.sub.c denotes a cyano group are valuable intermediates for preparing the other compounds of formula I, and the compounds of the above formula I wherein R.sub.c denotes one of the following amidino groups and the tautomers and stereoisomers thereof have valuable pharmacological properties, particularly an antithrombotic activity.

Bicyclic heterocycles, the preparation thereof, and their use as

Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-�(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.

Amino acid derivatives, pharmaceutical compositions containing these

New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them. These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.

Condensed diazepinones, processes for preparing them and agents

Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.

Angiotensin-II inhibiting benzimidazoles, useful for the treatment of hypertension. Exemplary compounds are:

Benzimidazoles and pharmaceutical compositions containing them

Pharmaceutical compositions are described which contain 1,5,6,7-tetrahydro-4H-indazol-4-ones of the formula ##STR1## some of these substances themselves being new. The pharmaceutical compositions may be used as analgesics, antipyretics and antiphlogistics.

1,5,6,7-tetrahydro-4H-indazol-4-ones

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

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.

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Biberach, Germany

Gerhard Mihm