Boehringer Ingelheim Italia

Istituto De Angeli

Gruppo Lepetit

B.i. Italia

Marco Turconi

Arturo Donetti

Massimo Nicola

Rosamaria Micheletti

Antonio Giachetti

Annamaria Uberti

Ernesto Montagna

Enzo Cereda

Giovanni Battista Schiavi

Bruno Cavalleri

Giuseppe Bietti

Maura Bignotti

Enrica Dubini

Angelo Sagrada

Antoine Ezhaya

Grazia Maffione

Ettore Giraldo

Henri N Doods

Franco Borsini

Giovanni Tamborini

Rosamarie Micheletti

Pharmacologically active benzimidazolone derivatives as 5-HT.sub.1A and 5-HT.sub.2 receptors, useful in the treatment of CNS disorders, of formula: ##STR1## wherein the substituents are defined herein.

Benzimidazolone derivatives

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

Crystalline and pharmacologically active monohydrates of endo-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimi dazole-1-carboxamide hydrochloride and of endo-3-ethyl-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H -benzimidazole-1-carboxamide hydrochloride.

Crystalline forms of

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 amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Amidino and guanidino derivatives

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 the formula (I) ##STR1## wherein R represents H or C.sub.1-6 alkyl;

Benzofused-N-containing heterocycle derivatives

New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Indolyl derivatives and their use as 5-HT.sub.3, receptor antagonists

New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.

1,3-diazocycloalkenes as muscarinic receptor blocking agents

The present invention concerns new 2'-substituted-4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives having antibacterial activity. These compounds are compounds obtained by chemical modification of thiazolo[5,4-c]rifamycin SV.

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Voghera, Italy

Marco Turconi