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.
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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.