Boehringer Biochemia Robin S.p.a.

Boehringer Mannheim Italia

Beehringer Biochemia Robin S.p.a.

Odoardo Tofanetti

Carmelo A Gandolfi

Sergio Tognella

Silvano Spinelli

Marco Frigerio

Andrea Zaliani

Carlo Riva

Franco Zunino

Roberto Di Domenico

Alessandro Pasini

Raimondo Russo

Ernesto Menta

Giorgio Cignarella

Bruno Lumachi

Ennio Cavalletti

Piervitto Cipolla

PierVitto Cipolla

Sergio Tongnella

Roberto Assereto

Michele Tedeschi

Daniele Castoldi

Mauro Germini

Sengio Tognella

Amino anthracenediones-bis platinum complexes, useful as antitumoral

Aralkyl-1,4-dihydropyridines, a method for their preparation and

Compounds of formula I, and pharmaceutical compositions containing compounds of formula I ##STR1## wherein: R.sub.1 is:

2-(aminoalkylthio)methyl-1,4-dihydropyridine, a method for the

Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;

2-thiomethyl-substituted-1,4-dihydropyridines, and pharmaceutical

2-thiomethyl-substituted-1,4-dihydropyridines, method for their

Compounds of formula I ##STR1## wherein R.sub.1 is a cyano, nitro, acetyl, benzoyl or alkoxycarbonyl group;

2-selenomethyl-1,4-dihydropyridines having calcium-antagonistic

Cyclic amino-thioacetal amides of formula I ##STR1## wherein X is O, S, p is 1 or 2, R and R.sub.1 are optionally esterified hydrogen or carboxy, A is a single bond, methylene or ethylene, m is zero or 1, n is an integer 1 to 7 and y is a imidazole or .beta.-pyridylmethyl residue. Compounds I have valuable therapeutic properties.

Cyclic amino-thioacetal amides, a process for the preparation thereof

Compounds of formula I ##STR1## wherein R.sub.1 is a cyano, nitro, benzoyl, acetyl, amido or alkoxycarbonyl group;

2-methylthiomethyl-dihydropyridines and pharmaceutical compositions

Compounds of formula I wherein R.sub.1 is an alkoxy carbonyl, aminocarbonyl, acetyl, benzyl, cyano or nitro group; R.sub.2 is as optionally substituted phenyl, aryl, hetaryl residue; R.sub.3 is an alkoxy-carbonyl group, X is an oxygen or sulphur atom, R.sub.4 is hydrogen, an optionally substituted alkyl, cycloalkyl, alkenyl group, Y is a single bond oxygen, sulphur or substituted nitrogen atom. Compounds of formula I are prepared by acylation from a 2-mercaptomethyl-1,4-dihydropyridine and are useful in therapy.

2-(acylthio)methyl dihydropyridines, and pharmaceutical compositions

Pyridines of formula I ##STR1## wherein R.sub.1 is acetyl, benzoyl, cyano, nitro, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or a heterocyclic group; and .phi. is a sulphurated residue such as alkylthio, cycloakylthio, arylthio, heteroarylthio, aminoalkylthio. Compounds I are useful in therapy in cardiovascular field.

2-thiomethyl-substituted-pyridine and -3,5-dicarboxylates having

Pharmaceutical compositions containing unit or separate dosages of 2.5 to 5 grams of reduced glutathione (GSH) and known anti-tumor agents, to be used simultaneously, separately or sequentially in anti-tumor therapy. Compounds of the invention, that can be used both in mono- or polychemotherapy, reach surprising results against tumors, thus avoiding the onset of dangerous side-effects, such as nephrotoxicity induced by cisplatinum, and increasing the long term survival rates.

Pharmaceutical compositions having antineoplastic activity

2-Substituted thiazolidines compounds having formula I ##STR1## wherein X is a CH.sub.2, O or S, R is hydroxy or an acyloxy, alkyloxy, alkenyloxy or alkinyloxy group, R.sub.1 is hydrogen or a group of formula ##STR2## R.sub.2 is hydrogen or a free or esterified carboxy group, R.sub.a and R.sub.b are hydrogen or methyl, p is zero or 1, R.sub.3 is hydrogen, a C.sub.1 -C.sub.2 alkylsulphonyl group, a phenyl or p-Cl phenyl, p-methylsulphonyl group or an acyl group; are useful as mucus regulating, antitussive and antibronchospastic agents.

Antitussive and mucus regulating 2-substituted thiazolidines

Thiazolidines of formula I ##STR1## wherein R is H, C.sub.1 -C.sub.4 -alkyl, allyl or propargyl;

2-sulphinyl-acetyl-1,3-thiazolidines, their preparation and

Compounds of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is acetyl, benzoyl, cyano, nitro, carboxy, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or hetaryl residue; R.sub.3 is a carboxy or alkoxycarbonyl group; A is a cyclopropyl group or a group of formula --CH.dbd.CH-- and R.sub.4 is a phenyl or heteroaryl group, optionally mono, di or tri-substituted, are useful in radical scavenging therapy.

2-substituted -1,4-dihydropyridines and pharmaceutical compositions

Dihydropyridines of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is a CN, NO.sub.2, COCH.sub.3, COPh group, a carboalkoxy or carboamide group; R.sub.2 is an aromatic or heteroaromatic, mono- or bicyclic eventually substituted phenyl group; R.sub.3 is a carboalkoxy group; while A is a halogen atom or an ammonium or phosphonium residue. The compounds I are useful as antihypertensive, antitumoral, antimetastatic, antithrombotic, and/or antiischemic agent.

Growing community of inventors

Milan, Italy

Odoardo Tofanetti