Gruppo Lepetit

Amedeo Omodei-Sale'

Pietro Consonni

Giulio Galliani

Giorgio Pifferi

Umberto Guzzi

Emilio Toja

Duccio Favara

Domenica Selva

New acyl -1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylendioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy; a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenactyl;

New acyl-1H-1,2,4-triazole derivatives

New .beta.-lactam acetic acid derivatives I ##STR1## wherein R represents alkyl, alkyl substituted with amino, protected amino, mono- or di-alkylamino, hydroxy, protected hydroxy or alkoxy, and alkenyl, and their salts are useful as intermediates for preparing 1-azabicyclo [3.2.0]hept-2-ene antibiotics II ##STR2## The process for preparing the .beta.-lactam acetic acid derivatives I as well as the overall process which starting from the acids I leads to the antibiotics II are also claimed.

Novel .beta.-lactam acetic acid derivatives

3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 stands for hydrogen, hydroxy, methoxy, ethoxy, or mono- or di-methylamino, and R.sub.4 represents hydrogen or (C.sub.1-4)alkyl. Also described and claimed are their use as antiinflammatory agents and the pharmaceutical compositions containing them.

Antiinflammatory 3H-naphtho[1,2-d]imidazoles

Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group. Also described is a process for their manufacture. Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredients are also claimed.

1,2,4-Triazole derivatives, and their use as antifertility agents

Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group. Also described is a process for their manufacture. Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredient are also claimed.

1,2,4-Triazole derivatives as antifertility agents and pharmaceutical

New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids. The compounds possess an outstanding antireproductive utility.

Antireproductive tricyclic ortho-fused nitrogen containing compounds

3,2-Benzoxazepines of the formula ##STR1## and their preparation. In formula (I), R respesents hydrogen or lower alkyl; R.sup.1 represents hydrogen, lower alkyl, lower alkenyl, hydroxy-lower alkyl, carbamyloxy-lower alkyl, acyl, amidino, carbamyl, mono- or di-substituted carbamyl; R.sup.2 may be in position 7 or 8 of the benzoxazepine ring and represents hydrogen, nitro, amino, acetamino or halo. The compounds are prepared by reacting 1,2,4,5-tetrahydro-3,2-benzoxazepine with a reactant which reacts with a secondary amino group to give substitution in the 2-position. The compounds have anti-inflammatory and central nervous system activity.

3,2-Benzoxazepine derivatives

A new class of 2,3-benzoxazepine compounds of the formula ##SPC1## In the formula, R is heterocyclic acyl or heterocyclic acetyl. The compounds have central nervous system and anti-inflammatory activity.

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Voghera, Italy

Amedeo Omodei-Sale'