Abstract: There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.
Type:
Grant
Filed:
June 24, 1985
Date of Patent:
December 15, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Ettore Perrone, Marco Alpegiani, Franco Zarini, Costantino D. Bruna, Giovanni Franceschi
Abstract: Anthracycline glycosides of general formula (I) ##STR1## wherein R is hydrogen or hydroxy, and pharmaceutically acceptable salts thereof, are anti-tumor agents.
Type:
Grant
Filed:
March 24, 1986
Date of Patent:
August 4, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Alberto Bargiotti, Michele Caruso, Antonino Suarato, Sergio Penco, Fernando Giuliani
Abstract: Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.
Type:
Grant
Filed:
October 16, 1985
Date of Patent:
June 23, 1987
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
Abstract: Anthracycline glycosides of the general formula (A): ##STR1## wherein X is hydrogen or hydroxy and R is hydrogen or a methyl or a hydroxymethyl group; and their pharmaceutically acceptable salts; are useful as antitumor agents.
Type:
Grant
Filed:
March 17, 1986
Date of Patent:
June 9, 1987
Assignee:
Farmitalia Carlo ERBA S.p.A.
Inventors:
Alberto Bargiotti, Pierangelo Zini, Sergio Penco, Fernando Giuliani
Abstract: 2H-Benzofuran-3-one derivatives, process for their preparation and pharmaceutical compositions containing them. The compounds and compositions are useful in the treatment of allergies.
Type:
Grant
Filed:
July 19, 1979
Date of Patent:
June 2, 1987
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Ciriaco Romeo, Maria L. Corno
Abstract: The present invention relates to the preparation of sterile and stable freeze-dried forms of Cisplatinum containing from 10 to 50 mg of active ingredient, which can be obtained on an industrial scale and which have particular characteristics of facility and rapidity of dissolution which permit them to be used in a more advantageous and rational manner in antitumor chemotherapy, as compared with the freeze-dried forms of Cisplatinum presently on the market.These particular characteristics are achieved as the result of employing special ingredients in respect of formulation (concentration of the solution to be freeze-dried, introduction of alcohols, adjustment of the pH of the solution to an appropriate value), and as the result of using a manufacturing technique having as its final stage the freeze-drying of Cisplatinum in a water-alcoholic medium.
Type:
Grant
Filed:
May 28, 1985
Date of Patent:
June 2, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Gaetano Battelli, Diego Oldani, Alessandro Rigamonti
Abstract: The invention discloses a method for extracting phenylalanine from the broths obtained by enzymatic processes; this method consists in flocculating and filtering the broth, concentrating the filtrate followed by filtering off the resulting cinnamic acid, decolorating and concentrating the filtrate to obtain phenylalanine crystals at a very pure degree.
Type:
Grant
Filed:
February 10, 1986
Date of Patent:
May 26, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Onorino G. Rosa, Carlo Varesio, Ernesto Oppici
Abstract: The present invention relates to new condensed benzopyrone derivatives having a 5-tetrazolyl substituent thereon, and to pharmaceutical compositions containing them. The compounds are useful in the treatment of allergic conditions.
Type:
Grant
Filed:
January 14, 1986
Date of Patent:
May 12, 1987
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Ada Buttinoni
Abstract: Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate 4-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with an oxidating agent and a organic or inorganic base.Also described are novel penam compounds useful as antibacterials which are prepared by the described process.
Abstract: There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.
Abstract: A process for the preparation of the N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester (aspartame) which is characterized by adding phosphoric acid and a lower alkyl alcohol to the reaction mixture containing N-formyl .alpha.-L-aspartyl- and .beta.-L-aspartyl-L-phenyl-alanine methyl ester and only one of the resultant deformylated isomers, i.e. aspartame phosphate precipitates.The .alpha.-isomer phosphate is collected by filtration and converted to free aspartame by treatment with a base.
Type:
Grant
Filed:
May 25, 1984
Date of Patent:
April 7, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Ernesto Oppici, Franco Dallatomasina, Pietro Giardino
Abstract: A water-swellable, water-insoluble polymer is loaded with a biologically active substance or substance convertible into a biologically active substance in vivo by preparing and grinding a mixture of a said substance with a water-swellable, water-insoluble polymer in a weight ratio of the said substance:polymer of from 1:0.1 to 1:100. The thus-loaded polymer is useful as a pharmaceutical composition.
Abstract: There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.
Type:
Grant
Filed:
April 13, 1983
Date of Patent:
December 30, 1986
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Luigi Bernardi, Enzo Brambilla, Laura Chiodini, Enrico di Salle, Daniela Ruggieri, Osvaldo Sapini, Aldemio Temperilli
Abstract: A water-swellable, water-insoluble polymer is loaded with methylhydroxyprogesterone acetate (MAP) by:(a) preparing and grinding a mixture of a said polymer and MAP; or(b)(i) preparing a mixture of a said polymer which is stable under the heating to which the mixture is subjected in step (ii) and MAP and (ii) heating the mixture up to the melting temperature of MAP; or(c) swelling a said polymer with a MAP solution capable thereof and drying the resulting swollen polymer/MAP system.The MAP loaded polymer is useful as a pharmaceutical composition.
Abstract: A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an inert solvent at a temperature of from 110.degree. to 150.degree. C. for a period of from 2 hours to a few days.
Type:
Grant
Filed:
August 6, 1984
Date of Patent:
December 23, 1986
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Carlo Battistini, Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile
Abstract: 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.
Type:
Grant
Filed:
August 22, 1984
Date of Patent:
December 2, 1986
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Franco Faustini, Roberto d'Alessio, Achille Panzeri, Enrico di Salle
Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein R.sub.1 is carboxy, esterified carboxy or an amide of formula ##STR2## in which R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, A is C.sub.2 -C.sub.6 alkylene and R.sub.a and R.sub.b are hydrogen or C.sub.1 -C.sub.6 alkyl or R.sub.a and R.sub.b taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;each of R.sub.3 to R.sub.8 is independently hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 alkenyloxy or C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.
Type:
Grant
Filed:
March 4, 1986
Date of Patent:
November 25, 1986
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
Abstract: Penem derivatives are disclosed characterized by a substituted pyridiniomethyl group in the 2-position of the penem nucleus. The compounds of the present application exhibit better antibacterial activity than other known penem derivatives.
Type:
Grant
Filed:
June 10, 1985
Date of Patent:
November 18, 1986
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
Abstract: Carboxy-thiazolo[3,2-a]pyrimidine derivatives, and pharmaceutical compositions containing them. The compounds and compositions possess anti-allergic activity.
Type:
Grant
Filed:
June 21, 1985
Date of Patent:
September 2, 1986
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Maria L. Corno
Abstract: A new antitumor anthracycline glycoside, 4-demethoxy-13-dihydrodaunorubicin, is disclosed.The new compound is prepared by reduction of the side-chain ketone function of the known 4-demethoxydaunorubicin, with sodium borohydride in aqueous solution at room temperature.
Type:
Grant
Filed:
November 5, 1984
Date of Patent:
August 5, 1986
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Sergio Penco, Federico Arcamone, Anna Maria Casazza