Istituto De Angeli S.p.a.

Boehringer Ingelheim Italia S.p.a.

Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

B.i. Italia

Boehringer Ingelheim Italia

Istituto De Angeli

Rosamaria Micheletti

Arturo Donetti

Massimo Nicola

Marco Turconi

Antonio Giachetti

Enzo Cereda

Ernesto Montagna

Annamaria Uberti

Piero Del Soldato

Giuseppe Bietti

Giuseppe Bianchi

Patrizia Ferrari

Alberto Cerri

Mauro Gobbini

Marco Torri

Giovanni Battista Schiavi

Simona Sputore

Silvia Armaroli

Maria Pia Zappavigna

Giorgio Fedrizzi

Alessandra Benicchio

Marco Pozzi

Piero Enrico Scotti

Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms. 

Azaheterocyclyl derivatives of androstanes and androstenes as medicaments for cardiovascular disorders

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 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

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

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 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

Rosamaria Micheletti