Gruppo Lepetit S.p.a.

Giorgio Tarzia

Gianbattista Panzone

Adriano Malabarba

Luigi Mariani

Aldo Trani

Pietro Ferrari

Emilio Occelli

Luigi Fontanella

Domenico Barone

Adele Giunta

The present invention is directed to an amide derivative of the glycopeptide, teicoplanin. This compound is an antibiotic that is active against gram positive bacteria. This compound is produced by subjecting teicoplanin to an amidation reaction.

Amides of teicoplanin compounds

The present invention is directed to teicoplanin derivatives in which position 63 of the glycopeptide core is substituted with a substituted alkylamide.

Substituted alkylamides of teicoplanin compounds

The present invention is directed to new de-(acetylglucosaminyl)-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria. The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.

De-(acetylglucosaminyl-di(dehydro)-deoxy teicoplanin derivatives

The present invention is directed to new de-(acetylglucosaminyl-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria. The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.

De-(acetylglucosaminyl)-di(dehydro)-deoxy teicoplanin derivatives

The present invention refers to new s-triazolo[3,4-a]phthalazine derivatives, to the process for their preparation and to the pharmaceutical compositions containing them.

6-substituted-s-triazolo[3,4-a]phthalazine derivatives

The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.

3,6-disubstituted triazolo [3,4-A]phthalazine derivatives

1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(3H)-one derivatives of the formula ##STR1## wherein R is (C.sub.1-4)alkyl, R.sub.1 stands for hydrogen, methyl, ethyl, phenyl, bromo, chloro or nitro, R.sub.2 is hydrogen or (C.sub.1-4)alkyl, R.sub.3 represents hydrogen, chloro, fluoro, bromo, trifluoromethyl and methoxy, and X is ##STR2## wherein n is zero or 1, or --NH--R.sub.4 wherein R.sub.4 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, or phenyl group. The novel compounds are useful as anticonvulsant and anti-anxiety agents. Also encompassed by the present invention are the process for preparing the novel pyrrolodiazepines and the pharmaceutical compositions containing them.

1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(3H)-one derivatives a process

1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-ones of the formula ##STR1## wherein R is lower alkyl, R.sub.1 stands for hydrogen, methyl, ethyl or phenyl, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen, chloro, fluoro, bromo, trifluoromethyl or methoxy are described with anticonvulsant and anti-anxiety activity. Also described is the process for preparing the above compounds and pharmaceutical preparations containing them.

1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-one derivatives

A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.

Pyrrolo-diazepine derivatives and their pharmaceutical compositions

Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;

Aminopyrrole derivatives

Pharmacologically active 2,4,5-trisubstituted oxazoles of the general formula ##STR1## wherein A is cyclohexyl, thienyl or a group of the formula ##STR2## in which R represents one to three substituents each independently selected from the group consisting of hydrogen, lower alkyl, halo, halo-lower alkyl, lower alkoxy, nitro, cyano, amino, carbamoyl, acetamino or carboxy; one of the R.sub.1 and R.sub.2 groups is a lower alkyl group and the other is an amido group, ##STR3## wherein R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, hydroxy, amino, lower alkylideneamino, cycloalkylideneamino, benzylideneamino and R.sub.4 is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen atom may also form a 5- to 7-membered hetero ring which may contain one other hetero atom selected from N, O and S. The compounds have antiinflammatory activity.

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Rome, Italy

Giorgio Tarzia