Patents Assigned to Farmitalia Carlo Erba S.p.A.
  • Patent number: 5391735
    Abstract: The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2-hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.
    Type: Grant
    Filed: April 12, 1994
    Date of Patent: February 21, 1995
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Arturo D. Torre, Ettore Lazzari, Giuseppe Mazzini
  • Patent number: 5138042
    Abstract: Anthracycline glycosides useful as antitumor agents of formula XV: ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: August 11, 1992
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Francesco Angelucci, Sergio Penco, Ermes Vanotti, Federico Arcamone
  • Patent number: 5124317
    Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs, e.g. doxorubicin, in the treatment of both human and animal tumors.
    Type: Grant
    Filed: April 3, 1990
    Date of Patent: June 23, 1992
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalconieri, Luciano Gambini, Roberto De Ponti
  • Patent number: 5051416
    Abstract: A method is provided for treating a warm-blooded animal having a susceptible bacterial infection which comprises administering orally to said animal a non-toxic, antibacterially effective amount of acetoxymethyl ester of (5R,6S)-2(5R,6S)-2-carbamoyloxymethyl-6-[1(R)-hydroxyethyl]-2-penem-3-carb oxylic acid.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: September 24, 1991
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Maurizio Foglio, Giovanni Franceschi, Aurora Sanfilippo
  • Patent number: 5043440
    Abstract: Process for preparing compounds according to formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom or a protective group and R.sub.3 represents a C.sub.1 -C.sub.10 alkyl or an aryl group, by oxidation of compounds according to formula (II) ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 have the above-mentioned meanings, in a two-phase system comprising:a) an organic phase including a 4-acylazetidinone compound (II) and an "onium" salt dissolved in a medium immiscible with water,b) an aqueous solution including an alkali or alkaline-earth metal salt of an organic or inorganic peracid.4-Acyloxyazetidinones (I) are useful intermediates in the synthesis of anti-bacterial compounds.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: August 27, 1991
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Marco Ricci, Maria Altamura, Daniele Bianchi, Walter Cabri, Norberto Gatti
  • Patent number: 5037970
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolysis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: August 6, 1991
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Francesco Angelucci, Sergio Penco, Ermes Vanotti, Federico Arcamone
  • Patent number: 4946831
    Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs, e.g. doxorubicin, in the treatment of both human and animal tumors.
    Type: Grant
    Filed: July 27, 1989
    Date of Patent: August 7, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalonieri, Luciano Gambini, Roberto De Ponti
  • Patent number: 4942155
    Abstract: The novel compounds are provided with good antibacterial and antitumour activity.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 17, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
  • Patent number: 4939282
    Abstract: A new process for the preparation of 6-deoxyanthracyclinones of general formula I: ##STR1## wherein R represents a hydrogen atom, a hydroxy group or a lower alkoxy group is described. The process provides a total synthesis of the 6-deoxyanthracyclinones of formula I using 1,2,3,6-tetrahydro-phthalate as starting material. The obtained racemic mixture of the compounds of formula I, if desired, can be submitted to optical resolution by the conventional method of conversion to diastereomeric derivatives using a chiral resolving agent. Alternatively, the racemic mixture can be used as such for the condensation with a suitably protected halosugar derivative to obtain alpha glycosidic derivatives of formula XV: ##STR2## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group.
    Type: Grant
    Filed: June 19, 1984
    Date of Patent: July 3, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Francesco Angelucci, Sergio Penco, Ermes Vanotti, Federico Arcamone
  • Patent number: 4904650
    Abstract: The invention relates to 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
    Type: Grant
    Filed: July 26, 1988
    Date of Patent: February 27, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Franco Buzzetti, Natale Barbugian, Paolo Lombardi, Enrico di Salle
  • Patent number: 4895836
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: January 23, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniel Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari
  • Patent number: 4895933
    Abstract: 4'-Deoxy-13(S)-dihydro-4'-iododoxorubicin having the formula (II): ##STR1## and pharmaceutically acceptable salts thereof are anti-tumor agents.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: January 23, 1990
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Teresa Bordoni, Sergio Merli, Giovanni Rivola
  • Patent number: 4882315
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: November 21, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Laura Chiodini, Mauro Gobbini, Sergio Mantegani, Daniel Ruggieri, Aldemio Temperilli, Gabriella Traquandi, Patrizia Ferrari
  • Patent number: 4873233
    Abstract: The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or fluorine;R.sub.5 is (a) hydrogen or C.sub.1 -C.sub.6 alkyl; (b) phenyl unsubstituted or substituted by one or two substituents independently chosen from C.sub.1 -C.sub.6 alkyl, halogen and amino; (c) an acyl group; or (d) a hydroxy protecting group; and the pharmaceutically acceptable salts thereof,which are useful in therapy, in particular as anti-cancer agents.
    Type: Grant
    Filed: September 12, 1988
    Date of Patent: October 10, 1989
    Assignee: Farmitalia Carlo Erba S.p.a.
    Inventors: Vittoria Villa, Enrico di Salle, Paolo Lombardi
  • Patent number: 4861793
    Abstract: Pharmaceutical compounds of the formula ##STR1## wherein R is H or CH.sub.3, R.sub.1 is H or OCH.sub.3, R.sub.2 is a C.sub.1 -C.sub.4 hydrocarbon group and X is an organic group. Also disclosed is a process for the preparation of these compounds. The compounds have dopamine agonist or antagonist activity.
    Type: Grant
    Filed: March 31, 1987
    Date of Patent: August 29, 1989
    Assignee: Farmitalia Carlo Erba, S.p.A
    Inventors: Luigi Bernardi, Laura Chiodini, Aldemio Temperilli
  • Patent number: 4861870
    Abstract: Disclosed is a process for purifying an impure anthracyclinone glycoside by selective adsorption of a slightly acidic aqueous solution of an impure glycoside on at least one resin and subsequent de-absorption of the purified glycoside by elution with acidic water or a mixture of water and a polar solvent.
    Type: Grant
    Filed: February 2, 1987
    Date of Patent: August 29, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Ernesto Oppico, Carlo Varesio, Onorino G. Rosa
  • Patent number: 4843073
    Abstract: t-Alkyl ergoline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 =H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 23, 1987
    Date of Patent: June 27, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Aldemio Temperilli, Enzo Brambilla, Mauro Gobbini, Maria A. Cervini
  • Patent number: 4839346
    Abstract: New anthracycline glycosides having formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy and either R.sup.2 or R.sup.3 is hydrogen with the other amino-methyl are described. The new compounds and their pharmaceutically acceptable addition salts are useful as antitumour agents.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: June 13, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Alberto Bargiotti, Teresa Bordoni, Pierangelo Zini, Sergio Penco
  • Patent number: 4801588
    Abstract: Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: January 31, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Aldemio Temperilli, Rosanna Eccel, Enzo Brambilla, Patricia Salvati
  • Patent number: 4797411
    Abstract: The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl;each of R.sub.1 and R.sub.2 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;n is an integer of 1 to 5; and either(a) A is >C.dbd.O and B is --O--, --NH-- or --CH.sub.2 --; or(b) A is --CH.sub.2 --and B is --O--, --NH--, --CH.sub.2 -- or >C.dbd.O; or(c) A is --O-- and B is >C.dbd.O or --CH.sub.2 --; or(d) A is --NH-- and B is >C.dbd.O or --CH.sub.2 --,and their pharmaceutically acceptable salts.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: January 10, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Angelo Crugnola, Enrico di Salle, Paolo Lombardi