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:
April 13, 1979
Date of Patent:
December 30, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
Abstract: New 2-oxa-bicyclic prostaglandin compounds, and pharmaceutical and veterinary compositions containing them, having pharmaceutical utility for example as anti-aggregating, vasodilating, and cytoprotective agents. Processes for preparing the compounds are also disclosed.
Type:
Grant
Filed:
February 26, 1979
Date of Patent:
October 28, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Carmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Ceserani, Maria M. Usardi
Abstract: There is disclosed a process for the manufacture of azetidinones related to nocardicin having the formula ##STR1## wherein R is a saturated or unsaturated alkyl having from 1 to 6 carbon atoms, .alpha.-aminobenzyl, benzyl, free or substituted phenyl, or a free or substituted heterocyclic;R.sub.1 is hydrogen, alkyl having from 1 to 4 carbon atoms, trimethylsilyl, trichloroethyl, benzhydryl or benzyl; andR.sub.2 is a free or substituted phenyl, or a free or substituted heterocyclic, using the same starting compound, but with the possibility of proceeding to the final compound via two somewhat different routes. A number of novel intermediates are also disclosed.
Type:
Grant
Filed:
June 30, 1978
Date of Patent:
October 28, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Maurizio Foglio, Giovanni Franceschi, Paolo Lombardi, Cosimo Scarafile, Federico Arcamone
Abstract: Substituted morpholine derivatives, such as, for instance, the compound 2-[.alpha.-(2-methoxy-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:
January 8, 1979
Date of Patent:
October 21, 1980
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Piero Melloni, Arturo D. Torre, Giovanni C. Carniel, Alessandro Rossi
Abstract: Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.
Type:
Grant
Filed:
November 13, 1978
Date of Patent:
September 16, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giuliana Arcari, Luigi Bernardi, Giovanni Falconi, Ugo Scarponi
Abstract: Compounds having the formula: ##STR1## wherein R is H or OH, and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyldaunorubicin, a known compound.
Abstract: Compounds having the formula: ##STR1## wherein (a) when R.sup.1 is --COCH.sub.3 or --COCH.sub.2 OH, R.sup.2 is --OH, R.sup.3 is --OCH.sub.3 and R.sup.4 is --H;(b) when R.sup.2 is --COCH.sub.3 or --COCH.sub.2 OH; R.sup.1 is --OH, R.sup.3 is --H and R.sup.4 is --OCH.sub.3 ;and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyl daunorubicin, a known compound.
Type:
Grant
Filed:
April 27, 1979
Date of Patent:
August 5, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Sergio Penco, Fausto Gozzi, Francesco Angelucci, Federico Arcamone
Abstract: [14-.sup.14 C]-daunorubicin and doxorubicin are prepared by reacting 9-desacetyl-9-formyl-N-trifluoroacetyl daunorubicin with [.sup.14 C]-diazomethane to form [14-.sup.14 C]-N-trifluoroacetyl daunorubicin from which the protecting group is removed by mild alkaline hydrolysis to afford [14-.sup.14 C]-daunorubicin which is then, in the form of the hydrochloride, reacted with bromine to form the corresponding labelled 14-bromo derivative, which, upon treatment with sodium formate leads to [14-.sup.14 C]-doxorubicin.
Type:
Grant
Filed:
February 14, 1978
Date of Patent:
July 8, 1980
Assignee:
Societa Farmaceutici Italia (Farmitalia Carlo Erba S.p.A.)
Inventors:
Gian P. Vicario, Sergio Penco, Federico Arcamone
Abstract: 7.beta.-acylamino-7.alpha.-methoxy-3-pyrazinylthiomethyl-cephalosporins and their intermediates having high resistance toward .beta.-lactamase enzymes, as well as good antibacterial activity and processes for preparation thereof.
Type:
Grant
Filed:
March 10, 1978
Date of Patent:
June 3, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giorgio Palamidessi, Maurizio Foglio, Franco Zarini, Giovanni Franceschi, Aurora Sanfilippo, 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 1, 1978
Date of Patent:
March 4, 1980
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 a hydrogen atom or a trifluoroacetyl group are useful in treating certain mammalian tumors.
Type:
Grant
Filed:
May 1, 1978
Date of Patent:
March 4, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Paolo Masi, Antonino Suarato, Luigi Bernardi, Federico Arcamone
Abstract: N-acyl derivatives of the known antitumor antibiotic carminomycin, particularly N-trifluoroacetyl carminomycin, have a much lower toxicity than carminomycin.
Type:
Grant
Filed:
January 26, 1978
Date of Patent:
February 12, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Antonino Suarato, Paolo Masi, Luigi Bernardi, Federico Arcamone
Abstract: Disclosed is 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 amino-deoxy sugar to form the .alpha.-glycosidic linkage.
Type:
Grant
Filed:
December 14, 1977
Date of Patent:
January 15, 1980
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giuseppe Cassinelli, Federico Arcamone, Aurelio Di Marco
Abstract: Substituted 2-vinyl chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and a styryl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.
Type:
Grant
Filed:
July 24, 1978
Date of Patent:
January 15, 1980
Assignee:
Carlo Erba S.p.A.
Inventors:
Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
Abstract: Substituted 2-vinyl-chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and a styryl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.
Type:
Grant
Filed:
July 24, 1978
Date of Patent:
January 15, 1980
Assignee:
Carlo Erba S.p.A.
Inventors:
Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
Abstract: Substituted 2-vinyl chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and a pyridyl-vinyl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.
Type:
Grant
Filed:
July 24, 1978
Date of Patent:
December 4, 1979
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
Abstract: Substituted 2-vinyl chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and an unsubstituted furyl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.
Type:
Grant
Filed:
July 24, 1978
Date of Patent:
December 4, 1979
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Giriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
Abstract: Heteromonocyclic and heterobicyclic derivatives of unsaturated 7-acylamido-3-cephem-4-carboxylic acid are disclosed which exhibit antibacterial activity against Gram-positive and Gram-negative microorganisms and can be used to treat infections caused by such microorganisms.
Type:
Grant
Filed:
January 11, 1978
Date of Patent:
October 30, 1979
Assignee:
Carlo Erba S.p.A.
Inventors:
Giuliano Nannini, Ettore Perrone, Dino Severino, Giuseppe Meinardi, Gisella Monti, Alberta Bianchi, Angelo Forgione, Carlo Confalonieri