Farmitalia Carlo Erba

Farmitalia Carlo Erba S.r.l.

Societa' Farmaceutici Italia

Other

Giuseppe Cassinelli

Federico Maria Arcamone

Sergio Merli

Giovanni Rivola

Arpad Grein

Marco Alpegiani

Ettore Perrone

Piergiuseppe Orezzi

Alberto Bargiotti

Giovanni Franceschi

Aurelio Di Marco

Pierluigi Bissolino

Sergio Penco

Paolo Carminati

Daniela Ruggieri

Annamaria Casazza

Aurelio DIMarco

Carlo Battistini

Teresa Bordoni

Rosanna Mazzoleni

Salvatore Forenza

Maria C Ripamonti

Francesco Di Matteo

Luigi Donno

A compound of formula (I): ##STR1## wherein: R.sub.1 is a hydroxy group or an amino group optionally substituted with a C.sub.1 -C.sub.4 alkyl or phenyl-(C.sub.1 -C.sub.4) alkyl group, R.sub.2 is hydrogen or a hydroxy group, R.sub.3 is hydrogen or chlorine, R.sub.4 is hydrogen or a hydroxy or amino group, R.sub.5 is hydrogen or a hydroxy group, and R.sub.6 is hydrogen or a hydroxy group, or a non-toxic acid addition salt thereof, is useful in the parenteral treatment of visceral leishmaniasis or malaria, and a synergistic composition comprising a compound of formula (I) or a non-toxic acid addition salt thereof and sodium stibogluconate is useful in the treatment of visceral leishmaniasis.

Paromomycin or its derivatives or salts thereof in combination with

There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,

1,1-dioxo-cephem-4-carbothiolic acid derivatives

.beta.-lactam derivatives of the cephem sulphone type

6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.

6-substituted penem esters as anti-inflammatory and anti-degenerative

Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R.sup.1 is halogen atom, or an organic group, R.sup.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, R.sup.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, benzyl or a methylene group and R.sub.4 is an organic residue are disclosed. Compounds (Ia) and (Ib) are endowed with elastase inhibitory activity. A two-step process for their preparation starting from the corresponding 4-carboxy cephem or 3-carboxy penam is also provided.

Beta-lactam derivatives of the 4-acylcephem sulphone and 3-acylpenam

6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl, or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.

##STR1## are prepared by a biosynthetic process based on the addition of sodium salt of 1,3-N,N-dimethylbarbituric acid and 2-thiobarbituric acid respectively during the fermentation process of different micro-organisms such as Streptomyces peucetius and its mutants. The novel compounds are provided with good antibacterial and antitumour activity.

Biosynthetic anthracyclines related to daunorubicin

4'-Deoxy-13(S)-dihydro-4'-iododoxorubicin having the formula (II): ##STR1## and pharmaceutically acceptable salts thereof are anti-tumor agents.

New antitumor agent obtained by microbial stereoselective reduction of

Anthracycline glycosides W, X, Y and Z which are prepared by the fermentation of mutant F.I. 416 of Streptomyces peucetius var. caesius. The new compounds are useful against both gram positive and gram negative bacteria and as antitumor agents.

Antitumor antibiotics

Anthracycline antibiotics of the formula: ##STR1## wherein R is --CO--CH.sub.2 OH, --CHOH--CH.sub.3, --CO--CH.sub.3 or --CH.sub.2 --CH.sub.3 having antitumor and antibacterial activity are prepared by culturing a new mutant strain of microorganism designated as Micromonospora peucetica sp. nova and which has been deposited with the American Type Culture Collection under number No. 31366 ATCC.

Preparation of II-deoxy anthracycline antibiotics

Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosy l chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyrano syl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifl uoroacetyl-L-lyxo-hexopyranosyl chloride.

Antitumor anthracycline glycosides, their preparation, intermediates

11-Deoxy-carminomycin compounds

Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-3,4-ditrifluoroacetamido-L-lyxo-[or L-arabino-]hexopyranosyl chloride.

Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxyca rbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta -N-benzyloxycarbonylparomomycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparo momycin; 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2',5',3'',4''-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.

Paromomycin containing compounds and method of use

There are disclosed compounds which exhibit anti-tumor activity. These compounds are of the formula I: ##STR1## wherein R.sub.1 is hydrogen, hydroxy or methoxy, R.sub.2 is hydrogen or hydroxy, and each of R.sub.3 and R.sub.4 independently is hydrogen or methyl, with the proviso that R.sub.3 and R.sub.4 are not simultaneously hydrogen, and pharmaceutically acceptable acid addition salts thereof. Also disclosed are processes for producing and using said compounds and therapeutic compositions containing same.

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Voghera, Italy

Giuseppe Cassinelli