Dr. Karl Thomae Gmbh

Karl Thomae Gmbh

Boehringer Ingelheim Kg

Dr. Karl Thomae Gesellschaft MIT Beschrankter Haftung

Rudolf Hammer

Wolfgang Eberlein

Wolfhard Engel

Gunter Trummlitz

Gunther Schmidt

Piero Del Soldato

Gerhard Mihm

Antonio Giachetti

Gu/ Nther Schmidt

Norbert Mayer

Gu/ Nter Trummlitz

Henri Doods

Erich Lehr

Joachim Mierau

Adriaan De Jonge

Piero D Soldato

Welfhard Engel

Franco Borsini

Gu/ Nther Trummlitz

The invention relates to the use of pramipexol as a pharmaceutical composition having an antidepressant activity.

Use of 2-amino-6-n-propyl-amino-4,5,6,7-tetrahydrobenzothiazole as a pharmaceutical composition having an antidepressant activity

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

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 invention relates to novel substituted 5,11-dihydro-6H-dibenz[b,e]azepin-6-one of the formula ##STR1## wherein A represents a (1-methyl-4-piperidinyl)-acetyl, (4-methyl-1-piperazinyl)-acetyl, or [(1-methyl-4-piperidinyl)-amino]-carbonyl group, and the acid addition salts thereof, which have valuable pharmacological properties, particularly an ulcer-inhibiting and secretion-inhibiting activity. The compounds of Formula I may be prepared using methods conventionally used for analogous compounds.

Substituted 5,11-dihydro-6H-dibenz[b,e]azepin-6-ones and pharmaceutical

Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR.sub.1 R.sub.2 --N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.

Condensed diazepinones, their compositions and methods of use as

The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydr o-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3, 2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.

Substituted dibenzodiazepinones

This invention relates to compounds of the formula ##STR1## wherein X is oxygen, --NH--, or--NCH.sub.3 --and

Dibenzodiazepinones, pharmaceutical compositions thereof and method of

New pyridobenzodiazepinones of the formula ##STR1## are described wherein X represents oxygen, --NH-- or --NCH.sub.3 -- and R represents 1-methyl-4-piperidinyl or 4-methyl-1-piperazinyl group optionally substituted by a methyl group, or a 3.alpha.- or 3.beta.-tropanyl group, and the nontoxic pharmaceutically acceptable acid addition salts thereof. The specification also describes processes for preparing these compounds, pharmaceutical compositions containing these compounds and new intermediate products used in preparing them. The compounds of formula I have antiulcerative effects and an inhibitory effect on gastric acid secretion, without the side effects such as dryness of the mouth and mydriasis which occur with other substances having an anticholinergic activity.

Pyridobenzodiazepinones, pharmaceutical compositions and method of use

This invention relates to compounds of the formula ##STR1## wherein R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl, 1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl, 2,3-dehydro-8-methyl-8-azabicyclo�3.2.1!oct-3-yl methyl, endo-8-methyl-8-azabicyclo�3.2.1!oct-3-yl-methyl, or exo-8-methyl-8-azabicyclo�3.2.1!oct-3-yl-methyl, each of which may optionally have one or two methyl substituents on the six-membered heterocyclic ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.

Pyridobenzodiazepinones, pharmaceutical compositions thereof and method

This invention relates to novel compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl having from 1 to 4 carbon atoms;

Thienobenzodiazepinones, pharmaceutical compositions thereof and method

Compounds of the formula ##STR1## wherein R is 1-methyl-4-piperididinyl, 4-methyl-1-piperazinyl, or 3 - or 3 -tropanyl, each of which may optionally have another methyl substituent attached to the heterocyclic ring;

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Milan, Italy

Rudolf Hammer