Patents Assigned to Carlo Erba
  • Patent number: 5204364
    Abstract: The present invention relates to new N-imidazolyl and N-imidazolylmethyl derivatives of bicyclic compounds having the general formula (I) ##STR1## Wherein A is a .gtoreq.CR.sub.3 or >CHR.sub.3 group, in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a >C.dbd.CR.sub.4 R.sub.5 group, in which each of R.sub.4 and R.sub.5 independently is hydrogen or C.sub.1 -C.sub.5 alkyl;Z is --CH.sub.2 --, --O-- or --S--;n is zero or 1;each of R and R.sub.1 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is --COCH.sub.2 OH, --CH.sub.2 OR', --COOR', --CONR'R" or --CH.dbd.CH--COOR', in which each of R' and R" independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof; and wherein:a) when n is zero, then Z is --CH.sub.2 -- or --O--; whereas when n is one, then Z is --CH.sub.2 --, --O-- or --S--;b) when A is .gtoreq.CR.sub.3 or >CHR.sub.3 in which R.sub.3 is hydrogen, then n is one; andc) when, at the same time, A is >CHR.sub.3 in which R.sub.
    Type: Grant
    Filed: June 27, 1990
    Date of Patent: April 20, 1993
    Assignee: Farmitalia Carlo Erba, S.r.l.
    Inventors: Germano Carganico, Paolo Cozzi, Antonio Pillan, Patricia Salvati, Corrado Ferti
  • Patent number: 5202325
    Abstract: Compounds of the formula I ##STR1## wherein n is 1 or 2, R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group or R.sub.2 and R.sub.3 together represent a chemical bond, R.sub.4 represents a hydrogen atom, or a phenyl or C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an alkyl group and R.sub.6 represents a hydrogen or halogen atom, and the pharmaceutically acceptable salt thereof, are useful for the manufacture of a pharmaceutical composition useful in the treatment of emesis.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: April 13, 1993
    Assignee: Farmitalia Carlo Erba S r l.
    Inventors: Alessandro Rossi, Metilde Buonamici, Lorenzo Pegrassi, Enzo Brambilla
  • Patent number: 5200403
    Abstract: Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R.sup.2 is an organic group have beta-lactamase inhibition activity. A process for the preparation of the same and pharmaceutical compositions containing these compounds are provided.
    Type: Grant
    Filed: July 23, 1991
    Date of Patent: April 6, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Stephen Hanessian, Giuseppe Meinardi, Ettore Perrone
  • Patent number: 5196445
    Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 -C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3, and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 -alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in the preparation of pharmaceutical compositions active in the treatment of autoimmune diseases.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: March 23, 1993
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
  • Patent number: 5180758
    Abstract: 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: January 19, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Franco Francalanci
  • Patent number: 5178838
    Abstract: A chemical reagent vial has an elongated shape from the end portions of which extend two lugs, one of which is closed by a frangible membrane which can be broken by a projection of a funnel element which can be screw engaged on a set lug. The other lug having an outer surface at least a portion of which is conical and on which tightly abuts a conical surface of a hollow sleeve which, moreover, tightly engages with a thread of the lug thereon the sleeve is threaded, through the lug at least an outlet hole being formed, which is arranged between the two sealing regions of the sleeve on the lug.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: January 12, 1993
    Assignee: Farmitalia Carlo Erba S. R. L.
    Inventors: Nello Sala, Gilberto Passerini, Mario Buelli, Davide Conti, Rosario D. Lorenzo, Ivo Secondini, Simona Bravi
  • Patent number: 5174149
    Abstract: The present invention relates to devices and processes for the introduction of a liquid sample into an apparatus for gas chromatographic analysis. A sample is injected into a vaporization chamber positioned upstream of a gas chromatographic column. The vaporization chamber is equipped with a means to feed a carrier gas selectively into the chamber, the chamber being kept at a temperature at least equal to the boiling temperature of the solvent at the operating pressure. A separation is effectuated between the sample and its carrier solvent, the solvent vapor is exhausted through an exhaust duct. Thereafter, the flow of carrier gas is restored to the chamber and the separated solvent is exhausted from the chamber through a separate outline into a gas chromatographic column.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: December 29, 1992
    Assignee: Carlo Erba Strumentazione S.p.A.
    Inventors: Konrad Grob, Fausto Munari
  • Patent number: 5175182
    Abstract: The invention relates to acryloyl substituted pyrrole derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, --CN, --NO.sub.2, C.sub.1 -C.sub.4 alkyl, or a group ##STR2## R.sub.3 is hydrogen, halogen, --CN, or --NO.sub.2 ; each R.sub.4 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;A is a bond, a group ##STR3## or a group --NH--Het--CO--, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; andB is a group ##STR4## in which m is 1, 2 or 3 and each R.sub.5 is, independently, a C.sub.1 -C.sub.4 alkyl group, and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: December 29, 1992
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
  • Patent number: 5166152
    Abstract: Compounds having the general formula (I) ##STR1## wherein X represents an oxygen atom or a --S(O).sub.n --group, wherein n is zero, 1 or 2;R represents C.sub.1 -C.sub.6 alkyl, pyridyl or substituted or unsubstituted phenyl;R.sub.2, R.sub.3 and R.sub.4 are as defined herein; and Q represents hydrogen, carboxy, C.sub.2 -C.sub.7 alkoxycarbonyl or a --CON(R.sub.a)'R.sub.b group wherein R.sub.a and R.sub.b are as defined herein; and their pharmaceutically acceptable salts have immunomodulating activity and are useful in particular as immunostimulating agents, in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: November 24, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Gianfederico Doria, Anna M. Isetta, Mario Ferrari, Domenico Trizio
  • Patent number: 5155107
    Abstract: The present invention concerns steroidic 5.alpha.-reductase inhibitors having the formula: ##STR1## As a result of their 5.alpha.-reductase inhibiting activity, these compounds are useful in the treatment of androgen dependent conditions and diseases.
    Type: Grant
    Filed: February 5, 1991
    Date of Patent: October 13, 1992
    Assignee: Farmitalia Carlo Erba
    Inventors: Achille Panzeri, Enrico Di Salle, Marcella Nesi
  • 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: 5130472
    Abstract: The present invention relates to a new process for the preparation of Erbstatin and Erbstatin analogs, which can be represented by the following formula (I) ##STR1## wherein R is hydrogen, a lower alkyl or a lower alkanoyl group;n is an integer of 1 to 3;A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is hydrogen or a lower alkyl group, andR.sub.2 is a hydrogen or halogen atom.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: July 14, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Angelo Crugnola, Paolo Lombardi
  • Patent number: 5126333
    Abstract: A pharmaceutical composition comprising a drug and a dehydrated cyclodextrin having improved dissolution properties, and the process for the preparation thereof.
    Type: Grant
    Filed: August 2, 1990
    Date of Patent: June 30, 1992
    Assignee: Farmitalia Carlo Erba S.R.L.
    Inventors: Alessandro Martini, Clara Torricelli, Carlo Confalonieri, Roberto De Ponti
  • Patent number: 5124318
    Abstract: A sealed glass container containing therein a stable, injectable, sterile, pyrogen-free doxorubicin anti-tumor composition in a solution which consists essentially of a physiologically acceptable salt of doxorubicin dissolved in a physiologically acceptable solvent therefor, wherein said solution has not been reconstructed from a lyophilizate, and wherein said solution has a pH of from 2.5-3.5 and a concentration of said doxorubicin of from 0.1 to 100 mg/ml.
    Type: Grant
    Filed: January 25, 1990
    Date of Patent: June 23, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalonieri, Luciano Gambini, Roberto De Ponti
  • 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: 5122537
    Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: June 16, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Angelo Crugnola
  • Patent number: 5103029
    Abstract: 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: April 7, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Walter Cabri, Silvia de Bernardinis, Franco Francalanci, Sergio Penco
  • Patent number: 5100873
    Abstract: A peptide of formula (I):A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (I)wherein either:(i) A represents a hydrogen atom, a Boc group or an acetyl group, one of B and C represents a pMel or mMel residue, and the other of B and C represents a sigma bond or a Gly, Leu-Gly, E-Leu-Gly or Gln-E-Leu-Gly, E, or E-Gly residue with E=Arg(A), arg(A), Lys(A), lys(A), Orn(A) and orn(A); or(ii) A represents a hydrogen atom;B represents a Glp-Arg-Leu-Gly residue;C represents a pMel or mMel residue;D represents a sigma bond or an Asn or Thr residue;X represents a Gly or ala residue;Y represents a sigma bond or a His(R.sub.1);his(R.sub.1), Phe, phe, Ser, ser, Ala or ala residue,T represents a sigma bond or a Leu, leu, Phe or phe residue;W represents an OH, amino, pentylamino or phenethyl-amino group or a Met-R.sub.2, Leu-R.sub.2, Ile-R.sub.2 or Nle-R.sub.2 residue;R.sub.1 represents a hydrogen atom or a Tos, Dnp or Bzl group; andR.sub.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: March 31, 1992
    Assignee: Farmitalia Carlo Erba
    Inventors: Roberto de Castiglione, Mauro Galantino, Fabio Corradi, Luigia Gozzini, Marina Ciomei, Isabella Molinari
  • Patent number: 5091372
    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: September 26, 1990
    Date of Patent: February 25, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
  • Patent number: 5091373
    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: September 28, 1990
    Date of Patent: February 25, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini