Istituto De Angeli S.p.a.

Dr. Karl Thomae Gmbh

Boehringer Ingelheim Italia S.p.a.

Karl Thomae Gmbh

Boehringer Ingelheim Italia

Antonio Giachetti

Arturo Donetti

Enzo Cereda

Piero Del Soldato

Rosamaria Micheletti

Giuseppe Bietti

Wolfgang Eberlein

Wolfhard Engel

Gunter Trummlitz

Gerhard Mihm

Rudolf Hammer

Massimo Nicola

Marco Turconi

Ferdinando Pagani

Ernesto Montagna

Annamaria Uberti

Gunther Schmidt

Norbert Mayer

Adriaan De Jonge

Gu/ Nter Trummlitz

A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the radicals are defined in claim 1.

Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht

Pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid compounds which are useful for treating a human host suffering from anxiety.

Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-HT

New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2## wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.

Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT

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

Compounds of the formula ##STR1## wherein R is hydrogen or methyl;

Substituted heterocyclyl-phenylformamidines and salts thereof

There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a pharmaceutical material. The compound is characterized by a powerful activity against ulcers of the gastro-intestinal tract.

(+)-6-chloro-5,10-dihy

Formamidine derivatives and pharmaceutical use

Compounds of the formula ##STR1## wherein R represents substituents of various types;

Antiulcerogenic amidine derivatives of 2-substituted 4-phenylimidazole

Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; or R.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group; R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; and Het is a substituted or unsubstituted heterocycle containing two or three heteroatoms; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.

Guanidino-heterocyclyl-phenyl-amidines and salts thereof

Compounds of the formula ##STR1## wherein Het is a heterocycle containing 2 to 3 nitrogen atoms;

Substituted heterocyclyl-phenyl-(sulfonyl-or phosphonyl)-amidines

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

Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;

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Milan, Italy

Antonio Giachetti