Patents Assigned to Carlo Erba S.p.A.
  • Patent number: 4447432
    Abstract: There are provided azino rifamycin compounds of the formula (I): ##STR1## Y.dbd.H or CH.sub.3 CO; R.sub.1 linear or branched C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl- R.sub.2 =linear or branched C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 chloroalkyl, C.sub.3 -C.sub.4 alkenyl, Cycloalkyl having 3 to 7 C atoms in the ring, cycloalkyl alkyl having 3 to 6 C atoms in the ring, phenyl, or C.sub.7 -C.sub.8 aralkyl, unsubstituted or mono-substituted by a halogen atom in the aryl group; or NR.sub.1 R.sub.2 =a cyclic moiety having 5 to 8 C atoms, unsubstituted or substituted by 1 or 2 CH.sub.3 groups, morpholino.The compounds inhibit the growth of gram positive bacteria and Mycobacterium tuberculosis.Oxidized compounds, preparative methods and pharmaceutical compositions are also described and claimed.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: May 8, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giovanni Franceschi, Leonardo Marsili, Aurora Sanfilippo, Sergio Vioglio
  • Patent number: 4444773
    Abstract: Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha. and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen or halogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R" are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents pyridyl optionally substituted by alkyl. The compounds have antiinflammatory, antiulcerogenic and anti-gastric secretory activity.
    Type: Grant
    Filed: July 14, 1982
    Date of Patent: April 24, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Carlo Passarotti, Giuliana Arcari, Ada Buttinoni
  • Patent number: 4438105
    Abstract: Starting from the known 4'-deoxy-4'-iodo-N-trifluoroacetyldaunorubicin, two new anthracycline glycosidic antibiotics, the 4'-deoxy-4'-iodo-daunorubicin and 4'-deoxy-4'-iodo-doxorubicin, have been prepared by known procedures. Both the new glycosides have been found to be endowed with outstanding antitumoral activity.
    Type: Grant
    Filed: April 14, 1982
    Date of Patent: March 20, 1984
    Assignee: Farmaitalia Carlo Erba S.p.A
    Inventors: Antonino Suarato, Sergio Penco, Federico Arcamone, Anna M. Casazza
  • Patent number: 4428952
    Abstract: Substituted Pyrrolo [2,1-b] and Pyrido [2, 1 b] Quinazolines are provided, together with pharmaceutical compositions, containing them. The compounds have pharmaceutical utility, and are particularly useful for the treatment of or prevention of the formation of gastrointestinal ulcers.
    Type: Grant
    Filed: June 10, 1982
    Date of Patent: January 31, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Carlo Passarotti, Giuliana Arcari
  • Patent number: 4421851
    Abstract: Anthracycline glycosides W, X, Y and Z which are prepared by the fermentation of mutant F.I. 416 of Streptomyces peucetius var. caesius. The new compounds are useful against both gram positive and gram negative bacteria and as antitumor agents.
    Type: Grant
    Filed: November 16, 1981
    Date of Patent: December 20, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
  • Patent number: 4411834
    Abstract: Anthracycline antibiotics of the formula: ##STR1## wherein R is --CO--CH.sub.2 OH, --CHOH--CH.sub.3, --CO--CH.sub.3 or --CH.sub.2 --CH.sub.3 having antitumor and antibacterial activity are prepared by culturing a new mutant strain of microorganism designated as Micromonospora peucetica sp. nova and which has been deposited with the American Type Culture Collection under number No. 31366 ATCC.
    Type: Grant
    Filed: September 2, 1981
    Date of Patent: October 25, 1983
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
  • Patent number: 4406901
    Abstract: Ethers of substituted hydroxymethylpyrazines, such as, for instance, the compound 2-methoxymethyl-5-methylpyrazine-4-oxide. The compounds exhibit elevated lipid-lowering activity, especially anti-lipolytic activity (decrease of plasma-free fatty acids), triglyceride-lowering activity, cholesterol-lowering activity, and plasma-phospholipid-lowering activity.
    Type: Grant
    Filed: November 16, 1981
    Date of Patent: September 27, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Cozzi, Antonio Pillan, Leone Bertone, Pier P. Lovisolo
  • Patent number: 4400377
    Abstract: A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp; Y is selected from the group consisting of Thr, Met, Leu, Nle, Val; W is selected from the group consisting of Met, Nle, Leu.
    Type: Grant
    Filed: March 5, 1982
    Date of Patent: August 23, 1983
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Gerhard Zetler, Alessandro Rossi, Chiara De Paolis
  • Patent number: 4393052
    Abstract: Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosy l chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyrano syl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifl uoroacetyl-L-lyxo-hexopyranosyl chloride.
    Type: Grant
    Filed: October 29, 1981
    Date of Patent: July 12, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Alberto Bargiotti, Giuseppe Cassinelli, Sergio Penco, Federico Arcamone, Annamaria Casazza
  • Patent number: 4388314
    Abstract: Heteromonocyclic and heterobicyclic derivatives of unsaturated 7-ayclamide-3-cephem-4-carboxylic acid are disclosed, and process for preparing same. These compounds are suitable for treating infections caused by Gram-positive and Gram-negative microorganisms.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: June 14, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuliano Nannini, Ettore Perrone, Dino Severino, Giuseppe Meinardi, Gisella Monti, Alberta Bianchi, Angelo Forgione, Carlo Confalonieri
  • Patent number: 4382940
    Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;X represents an oxygen or sulphur atom or an NH or NCH.sub.3 group;R.sub.3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 together represent a 3- or 4-membered carbon atom chain;Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR.sub.5 wherein R.sub.5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R.sub.5 and R.sub.3 together represent a 2- or 3-membered carbon atom chain;R.sub.6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; andR.sub.
    Type: Grant
    Filed: December 1, 1980
    Date of Patent: May 10, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Luigi Bernardi, Germano Bosisio, Sergio Mantegani, Alessandro Rossi, Aldemio Temperilli
  • Patent number: 4370474
    Abstract: Anthracycline glycosides W, X, Y and Z which are prepared by the fermentation of mutant F.I. 416 of Streptomyces peucetius var. caesius. The new compounds are useful against both gram positive and gram negative bacteria and as antitumor agents.
    Type: Grant
    Filed: November 15, 1979
    Date of Patent: January 25, 1983
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
  • Patent number: 4361577
    Abstract: .omega.-Nor-cycloalkyl-13,14-dehydro-prostaglandin compounds, specifically 5c-9-oxo-11.alpha.,15S-dihydroxy-20,19,18-tirnor-17-cyclohexyl-prost-5-en- 13-ynoic acid, the esters and salts thereof, having antiulcer and luteolytic activity, are disclosed.
    Type: Grant
    Filed: February 2, 1979
    Date of Patent: November 30, 1982
    Assignee: Carlo Erba - S.p.A.
    Inventors: Carmelo Gandolfi, Renato Pellegata, Roberto Ceserani, Maria M. Usardi
  • Patent number: 4358448
    Abstract: Derivatives of N-substituted thiazolyl oxy-imino-substituted cephalosporins, such as, for instance, the compound 7.beta.-[2-(2-imino-3-hydroxy-4-thiazolinyl)-2-methoxy-imino-acetamino]-3- [(tetrazolo[1,5-b]pyridazin-6-yl)-thiomethyl]-3-cephem-4-carboxylic acid, are disclosed. The disclosed compounds have high anti-bacterial activity against Gram-positive and Gram-negative bacteria normally susceptible to cephalosporins.
    Type: Grant
    Filed: November 12, 1980
    Date of Patent: November 9, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Ettore Perrone, Giuliano Nannini, Marco Alpegiani, Franco Giudici, Giuseppe Meinardi
  • Patent number: 4350627
    Abstract: There is disclosed biologically active peptides of the formula ##STR1## where X is a hydrogen atom, an N-terminus protecting group (any of an acyl-type protecting group, an aromatic urethane-type protecting group, an alkyl-type protecting group, or an alkyl urethane type protecting group), or a residue of a natural L-amino acid or a dipeptide formed of two natural L-amino acids, wherein the free amino group may be replaced by any of the foregoing N-terminus protecting groups;Y is a hydrogen atom or a protecting group for the phenolic hydroxyl group of tyrosine;A is a D-amino acid residue with a lower (thio) alkyl side chain;B is a neutral L-amino acid residue, a glycine residue, or an N-methyl amino acid residue;C is a direct bond or an amino acid or di-or tripeptide residue; andW is OH, OR, NH.sub.2, NHR, N(R).sub.2, NH-NH.sub.
    Type: Grant
    Filed: December 3, 1980
    Date of Patent: September 21, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Roberto de Castiglione, Fiorenzo Faoro, Giuseppe Perseo, Silvano Piani, Francesco Santangelo
  • Patent number: 4345070
    Abstract: A new process for the preparation of the known 4'-deoxydaunorubicin and 4'-deoxydoxorubicin is disclosed. The used starting material is 4'-eip-N-trifluoroacetyldaunorubicin which is converted into 4'-deoxy-4'-iodo-N-trifluoroacetyl-daunorubicin from which 4'-deoxy-daunorubicin can be reductively obtained and eventually transformed, by known methods, into 4'-deoxy-doxorubicin.
    Type: Grant
    Filed: June 5, 1981
    Date of Patent: August 17, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Antonino Suarato, Sergio Penco, Federico Arcamone
  • Patent number: 4345068
    Abstract: Disclosed is a process for preparing the known antitumor glycosides: 4'-epidaunorubicin, 3',4'-diepidaunorubicin, and their doxorubicin analogs by oxidizing the C-4' hydroxyl group of N-protected daunorubicin to form certain novel intermediates having a 4'-keto configuration, followed by reduction of the keto group with NaBH.sub.4 and mild alkaline hydrolysis to remove the N-protecting acyl groups.
    Type: Grant
    Filed: June 30, 1980
    Date of Patent: August 17, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Antonio Suarato, Sergio Penco, Federico Arcamone
  • Patent number: 4342775
    Abstract: 3-(1-imidazolyl)-derivatives of 2,3-dihydro-4H-1-benzopyran, such as, for instance, the compound 3-(1-imidazolyl)-2,3-dihydro-4H-1-benzopyran-4-one, are disclosed, as well as method of making same, and pharmaceutical compositions containing same. Also disclosed is a method of using such compounds to inhibit blood platelet aggregation, to increase total serum HDL cholesterol, to increase the ratio between .alpha.-lipoprotein and .beta.-lipoprotein total cholesterol, and/or of reducing total serum cholesterol or serum triglycerides.
    Type: Grant
    Filed: February 12, 1981
    Date of Patent: August 3, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Cozzi, Nicola Mongelli, Antonio Pillan, Maria Bergamaschi, Pier P. Lovisolo
  • Patent number: 4341780
    Abstract: Substituted pyrido [1,2-a] pyrimidines and pharmaceutical compositions containing them, suitable for use as anti-allergy, anti-ulcer, and anti-diabetic agents.
    Type: Grant
    Filed: May 27, 1981
    Date of Patent: July 27, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Piero Sberze, Marcellino Tibolla, Maria L. Corno
  • Patent number: 4337248
    Abstract: Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxyca rbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta -N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparo momycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbo nyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.
    Type: Grant
    Filed: June 4, 1980
    Date of Patent: June 29, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carlo Battistini, Giuseppe Cassinelli, Giovanni Franceschi, Rosanna Mazzoleni, Federico Arcamone