Ciba-geigy Corporation

Ernst Schweizer

Jorg Frei

Atso Ilvespaa

Jaroslav Stanek

Andre Gagneux

Jean J Gallay

Ernst Aufderhaar

Denis V Varsanyi

Jean-Jacques Gallay

1-Phenyl-3-azabicyclo[3.1.0]hexane-2,4-diones of the formula ##STR1## wherein R.sub.1 is hydrogen, R.sub.2 is hydrogen, sulfo or acyl and R.sub.3 is hydrogen, or R.sub.1 is a saturated or unsaturated aliphatic, cycloaliphatic or cycloaliphatic-aliphatic carbon radical of up to and including 18, preferably of up to and including 12, carbon atoms, R.sub.2 is hydrogen, lower alkyl, sulfo or acyl and R.sub.3 is hydrogen or lower alkyl, and to salts thereof, and salts thereof, have valuable pharmacological properties and are effective aromatase inhibitors. They can therefore be used for the treatment of hormonal diseases, in particular mammary carcinomas.

Substituted azabicycloalkanes, the use thereof, pharmaceutical

The invention relates to a process for the manufacture of novel benzazole derivatives of the formula I ##STR1## in which R.sub.1 represents an optionally 4-substituted piperazino group or a group of the formula R.sub.2 --alk--X.sub.2 --,

Process for the manufacture of novel benzazole derivatives,

The compounds of the formula ##STR1## in which R represents the radical of the formula ##STR2## in which R.sub.1 represents lower alkyl and

Antidiabetic iminosulphonamides

6-[(4-Substituted piperazin-l-yl)thiocarbonylamino]benzazoles and their

The invention relates to guanidine derivatives, particularly to substituted guanidines of the formula ##STR1## having hypoglycaemic activity, for the oral treatment of hyperglycaemia in mammals, especially for the oral treatment of Diabetes mellitus.

Guanidine compounds, pharmaceutical compositions and use

Novel hydroxylalkyl dithiocarbamate of the formula ##STR1## wherein R.sub.1 represents a phenyloxyphenyl or phenylaminophenyl radical which is unsubstituted or substituted by lower alkyl, halogen, trifluoromethyl, nitro and/or cyano, and alk represents lower alkylene, are useful as anthelmintic agents.

Process for the production of novel hydroxyalkyl dithiocarbamates

The present invention relates to new dithiocarbamic acid esters having the formula ##STR1## wherein R.sub.1 represents a phenyloxyphenyl or phenylaminophenyl radical which is unsubstituted or substituted by lower alkyl, halogen, trifluoromethyl, nitro or cyano, R.sub.2 represents hydrogen or lower alkyl, and alk represents lower alkylidene or lower alkylene, and also to salts of compounds of the formula (I), wherein R.sub.2 represents hydrogen, with pharmaceutically acceptable bases. These new compounds possess a strong anthelminthic activity and are useful for the treatment of warm-blooded animals infected with parasitic helminths. A specific embodiment is the N-[4-(4-nitroanilino)-phenyl]-dithiocarbamic acid-(2-carboxyethyl)-ester.

Dithiocarbamic acid esters

Cpmpounds of the class of 5-substituted and 5,6-disubstituted 2-amino-4-(hydroxyamino) and 2,4-bis-(hydroxyamino)pyrimidines and their pharmaceutically acceptable acid addition salts possess valuable biological properties, in particular antibacterial and antimalarial activity and potentiate the action of antibacterial sulphanilamide derivatives. Specific embodiments are 2-amino-4-(hydroxyamino)-5-(3,4,5-trimethoxybenzyl)-pyrimidine, and 2-amino-4-(hydroxyamino)-5-(p-chlorophenyl)-6-ethyl pyrimidine and its hydrochloride.

Substituted 2-amino-4-(hydroxyamino)-pyrimidines

Compounds of the class of 1-heteroarylsulphonyl-2-imino-imidazolidines which are substituted in the 3-position by an aliphatic or cycloaliphatic hydrocarbon radical, especially a cycloalkyl radical, and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties. In particular, they possess hypoglycaemic activity and can be used for the treatment of hyperglycaemia in mammals. A specific embodiment is 1-[5-(2-butyramido-ethyl)-2-thienylsulphonyl]-2-imino-5-cyclohexyl-imidazo lidine.

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Arlesheim, Switzerland

Ernst Schweizer