Patents Assigned to Carlo Erba S.p.A.
  • Patent number: 4285966
    Abstract: The present invention relates to 15-epi-derivatives of prostacyclin and its analogs, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.
    Type: Grant
    Filed: October 30, 1978
    Date of Patent: August 25, 1981
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Cesarani
  • Patent number: 4277491
    Abstract: Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them having numerous pharmaceutical or veterinary utilities including, for example, hypotensive, vasodilatory, anti-aggregating, luteolytic, and cytoprotective activities. Processes for preparing the compounds are also disclosed.
    Type: Grant
    Filed: December 1, 1978
    Date of Patent: July 7, 1981
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4276289
    Abstract: Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.
    Type: Grant
    Filed: March 17, 1980
    Date of Patent: June 30, 1981
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Giuseppe Cassinelli, Daniela Ruggieri, Federico Arcamone, Aurelio di Marco
  • Patent number: 4271160
    Abstract: Substituted morpholine derivatives, such as, for instance the compound 2-[.alpha.-(3,4-methylendioxy-phenoxy)-benzyl]-morpholine are disclosed.The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.
    Type: Grant
    Filed: June 20, 1980
    Date of Patent: June 2, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Arturo Della Torre, Giovanni C. Carniel, Alessandro Rossi
  • Patent number: 4271184
    Abstract: Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them having numerous pharmaceutical or veterinary utilities including, for example, hypotensive, vasodilatory, antiaggregating, luteolytic, and cytoprotective activities. Processes for preparing the compounds and compositions are also disclosed.
    Type: Grant
    Filed: November 30, 1979
    Date of Patent: June 2, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4271183
    Abstract: Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them having numerous pharmaceutical or veterinary utilities including, for example, hypotensive, vasodilatory, anti-aggregating, luteolytic, and cytoprotective activities. Processes for preparing the compounds and compositions are also disclosed.
    Type: Grant
    Filed: April 13, 1979
    Date of Patent: June 2, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4268451
    Abstract: Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is a hydrogen atom or a trifluoroacetyl group are useful in treating certain mammalian tumors.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: May 19, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Masi, Antonino Suarato, Luigi Bernardi, Federico Arcamone
  • Patent number: 4267116
    Abstract: Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is hydrogen or a trifluoroacetyl group are useful in treating certain mammalian tumors.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: May 12, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Masi, Antonino Suarato, Luigi Bernardi, Federico Arcamone
  • Patent number: 4267327
    Abstract: 2-Hydroxymethyl-pyrazine derivatives are disclosed, such as, for instance, the compound 2-hydroxymethyl-5-methylpyrazine-4-oxide. The compounds exhibit an elevated lipid lowering activity, and can be used to control triglyceride and cholesterol levels.
    Type: Grant
    Filed: February 26, 1979
    Date of Patent: May 12, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Cozzi, Osvaldo Magni, Leone Bertone, Romano Angelucci, Pier P. Lovisolo
  • Patent number: 4265885
    Abstract: A new class of antitumor glycoside antibiotics of the formula (IA): ##STR1## wherein R is hydrogen or hydroxy; and X is ##STR2## These compounds are prepared, using novel intermediates, by condensing the appropriate aglycone and branched-chain aminodeoxy sugar to form the .alpha.-glycosidic linkage.
    Type: Grant
    Filed: October 5, 1979
    Date of Patent: May 5, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Alberto Bargiotti, Giuseppe Cassinelli, Federico Arcamone, Aurelio DiMarco
  • Patent number: 4262016
    Abstract: Bicyclic Prostaglandins and pharmaceutical and veterinary compositions containing them, having numerous pharmaceutical and veterinary utilities, including for example hypotensive, vasodilatory, anti-aggregating, and anti-thrombotic activities. Methods for preparing the compounds and compositions are also disclosed.
    Type: Grant
    Filed: June 18, 1979
    Date of Patent: April 14, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4259244
    Abstract: Bicyclic prostaglandins having numerous pharmaceutical and veterinary utilities including, for example, use as hypotensive, vasodilatory, anti-aggregating, cytoprotective, and bronchodilatory agents. Pharmaceutical and veterinary compositions comprising the compounds in combination with pharmaceutically and/or veterinarily acceptable carriers and/or diluents are also disclosed.
    Type: Grant
    Filed: April 13, 1979
    Date of Patent: March 31, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4254110
    Abstract: Antitumor anthracycline glycosides of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is formyl, hydroxymethyl or aminomethyl, and R.sub.3 is hydrogen, hydroxy or an acyloxy group; and pharmaceutically acceptable acid addition salts of said compounds in which one of R.sub.1 and R.sub. 2 is aminomethyl are prepared from daunorubicin, doxorubicin or 14-O-acyl derivatives of doxorubicin by deamination and C-3' epimerization effected with NaNO.sub.2 in a cold aqueous acidic medium, such as 1N aqueous acetic acid at 0.degree. C., to give compounds wherein one of R.sub.1 and R.sub.2 is formyl and the optional further steps of selective reduction, e.g., with NaCNBH.sub.3 in 4:1 dioxan:aqueous acetate buffer at pH 4.6 or with Na(CH.sub.3 COO).sub.3 BH in benzene under reflux, to form compounds in which one of R.sub.1 and R.sub.2 hydroxymethyl, or selective reductive amination, e.g., with NaCNBH.sub.3 in the presence of methanolic CH.sub.3 COONH.sub.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: March 3, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Federico Arcamone, Aurelio di Marco
  • Patent number: 4254137
    Abstract: Bicyclic prostaglandins and pharmaceutical and veterinary compositions containing them, having numerous pharmaceutical and veterinary utilities, including for example hypotensive, vasodilatory, anti-aggregating, and anti-thrombotic activities. Methods for preparing the compounds and compositions are also disclosed.
    Type: Grant
    Filed: June 18, 1979
    Date of Patent: March 3, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4252948
    Abstract: Pyridazinyl-ergoline compounds having neuroleptic activity are obtained by reacting an 8.beta.-tosylmethyl ergoline with the sodium derivative of an aminopyridazine or a mercaptopyridazine in a dipolar aprotic solvent.
    Type: Grant
    Filed: March 19, 1979
    Date of Patent: February 24, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Luigi Bernardi, Carlo Elli, Giovanni Falconi, Alberto Bonsignori
  • Patent number: 4252941
    Abstract: Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR" R"' (wherein R" and R"' both represent alkyl groups having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, or a phenyl group;R.sub.3 represents a fluorine atom, a cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, or sulphonamido group, an alkoxy group having from 1 to 4 carbon atoms, an acyl group having from 2 to 4 carbon atoms, or a benzoyl group;R.sub.
    Type: Grant
    Filed: September 4, 1979
    Date of Patent: February 24, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Sergio Mantegani, Giuliana Arcari, Anna M. Caravaggi, Germano Bosisio
  • Patent number: 4251531
    Abstract: 3,4-Dihydro-quinazoline derivatives, such as 6-carboxy-2-(2'-ethoxy-phenyl)-3,4-dihydro-4-oxo-quinazoline, are disclosed. The compounds possess anti-allergy properties and can be used for the treatment of allergic conditions.
    Type: Grant
    Filed: November 2, 1976
    Date of Patent: February 17, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
  • Patent number: 4251513
    Abstract: 9-Desacetyl-9-ethylen oxide daunorubicin hydrochloride is an effective antitumor antibiotic.
    Type: Grant
    Filed: February 14, 1978
    Date of Patent: February 17, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Sergio Penco, Francesco Angelucci, Federico Arcamone
  • Patent number: 4250188
    Abstract: 2-Oxa-bicyclic prostaglandins, a method for their preparation and pharmaceutical and veterinary compositions containing them are disclosed.
    Type: Grant
    Filed: November 1, 1979
    Date of Patent: February 10, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4247687
    Abstract: A process is disclosed for preparing 4'-deoxy-neomycin B, having the formula: ##STR1## Chlorination with sulphuryl chloride in pyridine gives the corresponding 4'-6'-dichloro analog which is selectively dechlorinated at position 4' with tributyltin hydride. The 6'-chloro group is then subjected to azidolysis to introduce an azido group. De-O-benzoylation of the resulting 6'-azido derivative, followed by hydrogenolysis, gives 4'-deoxy neomycin B. The new compound displays an antibacterial activity with a higher grade and broader spectrum when compared with those of neomycin B and paromomycin I.
    Type: Grant
    Filed: June 12, 1979
    Date of Patent: January 27, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventor: Stephen Hanessian