Patents Assigned to Societa' Farmaceutici Italia
  • Patent number: 4018776
    Abstract: A process is disclosed for preparing a cephalosporin of structure: ##STR1## where R is selected from the class consisting of hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, tetrazolyl-1-methyl;R.sup.1 is selected from the class consisting of hydroxy, alkoxy having from 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxy-benzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, p-halophenacyloxy; andZ is selected from the class consisting of hydrogen, hydroxy, --O--Alkyl, --O--CO--Alkyl, --Br, --I, --NH.sub.2, --O--COCH.sub.3, --O--CO--NH.sub.2, and an --S-mononuclear nitrogen heterocyclic ring,Wherein a compound of structure: ##STR2## where R, R.sup.1 and Z have the above meanings, is reacted with iodine in a suitable aqueous solvent at a temperature between 5.degree. and 80.degree.
    Type: Grant
    Filed: August 4, 1975
    Date of Patent: April 19, 1977
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Maurizio Foglio, Paolo Masi, Antonino Suarato, Giovanni Franceschi
  • Patent number: 4012381
    Abstract: A process is disclosed for preparing derivatives of 7-amino-cephalosporanic acid and 7-amino-desacetoxycephalosporanic acid of structure: starting from a 3-acylamino-2.beta.-thiohydrazoazetidinone of structure: ##STR1## wherein the compound (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed with water in an acid medium, and the resultant 3-amino-2.beta.-thiohydrazoazetidinone of structure: ##STR2## is reacted in a suitable solvent and at a temperature between -100.degree. and +120.degree. C with a compound selected from the class consisting of inorganic basic or weakly acid oxides and inorganic and organic bases, to finally give the desired compound (V) which is isolated and purified in known manner.2.beta.-thiohydrazoazetidinones are also disclosed as intermediates.
    Type: Grant
    Filed: June 12, 1975
    Date of Patent: March 15, 1977
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Maurizio Foglio, Giovanni Franceschi, Paolo Masi, Antonino Suarato
  • Patent number: 4012284
    Abstract: 1. A process for the preparation of a new antibiotic F.I. 1762, which comprises cultivating the Streptomyces 1762 under aerobic conditions in a liquid nutrient medium containing a carbon source, a nitrogen source and mineral salts, at a temperature between 25.degree. and 37.degree. C, over a period of time from 3 to 7 days, and extracting the formed antibiotic from the fermentation broth at a pH between 8 and 9 by means of a water-immiscible solvent, isolating and purifying the antibiotic F.I. 1762.
    Type: Grant
    Filed: October 6, 1964
    Date of Patent: March 15, 1977
    Assignee: Societa' Farmaceutici Italia, S.p.A.
    Inventors: Aurelio Di Marco, Graziana Canevazzi, Arpad Grein, Piergiuseppe Orezzi, Marcello Gaetani
  • Patent number: 3996228
    Abstract: Pyrimidinoaminoethyl ergoline derivatives of the formula: ##STR1## wherein R is hydrogen or methyl; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl having 1 to 3 carbon atoms, methoxy and phenyl;R.sub.3 is hydrogen, halogen, alkyl and alkoxy each having 1 to 3 carbon atoms, phenyl, nitro, amino, cyano, acylamino, carboxamido and carbalkoxy each having 1 to 3 carbon atoms, trifluoromethyl or --SO.sub.2 --Y wherein Y is hydroxyl, amino or methyl and R.sub.
    Type: Grant
    Filed: December 9, 1974
    Date of Patent: December 7, 1976
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Giuliana Arcari, Luigi Bernardi, Germano Bosisio, Alfredo Glasser, Aldemio Temperilli
  • Patent number: 3975389
    Abstract: New derivatives of caffeine are disclosed having the formula: ##SPC1##Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, chlorine, bromine, an alkyl or an alkoxy radical containing from 1 to 4 carbon atoms. They are made by transforming 8-.alpha. hydroxyethyl caffeine into the corresponding 8-.alpha.-chloroethyl caffeine by the action of a suitable chlorinating agent such as thionyl chloride, reacting the product so obtained in a suitable solvent such as anhydrous dimethylformamide at a temperature from 40.degree. to 110.degree. C and for a period of time from 1 to 5 hours with the sodium or potassium salt of a nicotinic acid of the formula: ##SPC2##Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the above-mentioned meanings, and crystallizing the resulting product from a suitable solvent, such as ethanol. These new compounds have broncholitic activity.
    Type: Grant
    Filed: September 23, 1974
    Date of Patent: August 17, 1976
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Giuliana Arcari, Pietro De Micheli, Fulvio Luini, Ugo Scarponi
  • Patent number: 3972883
    Abstract: Ergoline derivatives are disclosed having the general formula ##SPC1##Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2##WhereinY is hydrogen, a lower alkyl radical having from 1 to 4 carbon atoms or phenyl;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, methyl or halogen; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, halogen, a lower alkyl radical having from 1 to 4 carbon atoms, carbethoxy, or a lower alkyloxy radical having from 1 to 4 carbon atoms.Novel processes for the preparation of these compounds are also disclosed.
    Type: Grant
    Filed: January 28, 1974
    Date of Patent: August 3, 1976
    Assignee: Societa Farmaceutici Italia S.p.A.
    Inventors: Giuliana Arcari, Luigi Bernardi, Germano Bosisio, Alfredo Glasser, Innocenzio Sinatra
  • Patent number: 3966739
    Abstract: Esters of 1-methyl-lumilysergol-10-methylether having the formula: ##SPC1##Wherein R is selected from the group consisting of 2-furanoyl and the pyrrole group of the formula: ##SPC2##Wherein Y is selected from the group consisting of hydrogen, lower alkyl having from 1 to 6 carbon atoms and phenyl; R.sub.1 is selected from the group consisting of hydrogen, methyl and carbonyl; R.sub.2 is selected from the group consisting of hydrogen, methyl, halogen and carbonyl, provided that only one of R.sub.1 and R.sub.2 can be carbonyl; R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, halogen, alkyl, alkoxy having from 1 to 6 carbon atoms and carboethoxy; the pharmaceutically acceptable addition salts thereof with an organic acid and a process for the preparation thereof. The compounds possess adrenolytic, hypotensive, sedative and antiserotoninic activities.
    Type: Grant
    Filed: March 7, 1972
    Date of Patent: June 29, 1976
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Luigi Bernardi, Germano Bosisio, Gian Carlo Fregnan
  • Patent number: 3963760
    Abstract: Anthracycline derivatives of the formula ##SPC1##Wherein R.sub.1, R.sub.2, R.sub. 3 and R.sub.4 are independently selected from the group consisting of hydrogen, chlorine, bromine and methoxy, with the proviso that at least one of the substituents is methoxy, and wherein R.sub.5 is selected from the group consisting of hydrogen, OH OR and OCOR; R being an alkyl group of 1 to 4 carbon atoms are prepared, in a single step, by selectively demethylating a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above by treating same with an aluminum halide in the presence of a suitable solvent at a temperature of 0.degree. to 50.degree.C.
    Type: Grant
    Filed: September 15, 1975
    Date of Patent: June 15, 1976
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Luigi Bernardi, Bianca Patelli
  • Patent number: 3957785
    Abstract: Novel 8.beta.-pyrimidino-aminomethyl-10.alpha.-ergoline and 10.alpha.-methoxyergoline derivatives which possess a high and prolonged adrenolytic activity and a low toxicity, and some of which also possess hypotensive and analgesic activity are prepared by reacting a pyrimidine anion with an ergoline derivative in an aprotic solvent.
    Type: Grant
    Filed: July 31, 1974
    Date of Patent: May 18, 1976
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Giuliana Arcari, Luigi Bernardi, Germano Bosisio, Maurizio Foglio, Alfredo Glasser, Aldemio Temperilli