Patents by Inventor Giuseppe Cassinelli

Giuseppe Cassinelli has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5470836
    Abstract: A compound of formula (I): ##STR1## wherein: R.sub.1 is a hydroxy group or an amino group optionally substituted with a C.sub.1 -C.sub.4 alkyl or phenyl-(C.sub.1 -C.sub.4) alkyl group,R.sub.2 is hydrogen or a hydroxy group,R.sub.3 is hydrogen or chlorine,R.sub.4 is hydrogen or a hydroxy or amino group,R.sub.5 is hydrogen or a hydroxy group, andR.sub.6 is hydrogen or a hydroxy group,or a non-toxic acid addition salt thereof, is useful in the parenteral treatment of visceral leishmaniasis or malaria, and a synergistic composition comprising a compound of formula (I) or a non-toxic acid addition salt thereof and sodium stibogluconate is useful in the treatment of visceral leishmaniasis.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: November 28, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Luigi Donno, Giuseppe Cassinelli
  • Patent number: 5356888
    Abstract: There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,R.sub.1 is hydrogen or halogen atom or an organic group,R.sub.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or acyloxy group,R.sub.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy, benzyl group or a methylene andR.sub.4 is chloro, fluoro, hydrogen atom or an organic group.The compounds I are elastase inhibitors. A process for their preparation is also provided, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 22, 1991
    Date of Patent: October 18, 1994
    Assignee: Farmitalia Carlo Erba
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Francesco Di Matteo, Piergiuseppe Orezzi, Giuseppe Cassinelli
  • Patent number: 5348952
    Abstract: Cephalosporins of the formula (I): ##STR1## wherein m is one or two; n is zero, one or two; A and B are organic residues; and R.sub.1 and R.sub.2 are halogen or hydrogen atoms or organic groups are endowed with elastase inhibitory activity. Two processes for their preparation starting from the corresponding 4-acyl cephem are also provided.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: September 20, 1994
    Assignee: Farmitalia Carlo Erba S.R.L.
    Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
  • Patent number: 5089489
    Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: February 18, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Paolo Carminati, Giuseppe Cassinelli
  • Patent number: 5077286
    Abstract: Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R.sup.1 is halogen atom, or an organic group, R.sup.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, R.sup.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, benzyl or a methylene group and R.sub.4 is an organic residue are disclosed. Compounds (Ia) and (Ib) are endowed with elastase inhibitory activity. A two-step process for their preparation starting from the corresponding 4-carboxy cephem or 3-carboxy penam is also provided.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: December 31, 1991
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
  • Patent number: 4954493
    Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl, or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.
    Type: Grant
    Filed: June 14, 1988
    Date of Patent: September 4, 1990
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Paolo Carminati, Giuseppe Cassinelli
  • 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: 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: 4487546
    Abstract: A device for transferring tubular fabrics, particularly panty hose, the opening or mouth of which is fitted on support hangers which are spaced apart from one another and hold the mouth at an open position, and for transferring such tubular fabrics onto a rigid body adjacent to and aligned with the hangers by inverting the tubular fabrics on such rigid body. The device includes a slide longitudinally movable on a fixed guide, jaws mounted on the slide and includes four discrete rotable elements in two pairs on two discrete planes, a pan projecting forwardly of the slide and freely axially movable relative thereto against the action of a spring, plungers supported from the jaws which project for insertion in the mouth or opening of the tubular fabric as the slide moves forward, followed by lifting such fabric out of the support hangers when the jaws are spread out.
    Type: Grant
    Filed: July 14, 1982
    Date of Patent: December 11, 1984
    Assignee: Savio & C. S.p.A.
    Inventor: Giuseppe Cassinelli
  • 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: 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: 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: 4366149
    Abstract: Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-3,4-ditrifluoroacetamido-L-lyxo-[or L-arabino-]hexopyranosyl chloride.
    Type: Grant
    Filed: October 29, 1981
    Date of Patent: December 28, 1982
    Inventors: Alberto Bargiotti, Giuseppe Cassinelli, Sergio Penco, Federico Arcamone, Annamaria Casazza
  • 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
  • Patent number: 4322412
    Abstract: There are disclosed compounds which exhibit anti-tumor activity. These compounds are of the formula I: ##STR1## wherein R.sub.1 is hydrogen, hydroxy or methoxy, R.sub.2 is hydrogen or hydroxy, and each of R.sub.3 and R.sub.4 independently is hydrogen or methyl, with the proviso that R.sub.3 and R.sub.4 are not simultaneously hydrogen, and pharmaceutically acceptable acid addition salts thereof. Also disclosed are processes for producing and using said compounds and therapeutic compositions containing same.
    Type: Grant
    Filed: July 14, 1980
    Date of Patent: March 30, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Salvatore Forenza, Maria C. Ripamonti, Daniela Ruggieri
  • Patent number: 4309503
    Abstract: Anthracycling 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 Macromonospora peucetica sp. nova and which has been deposited with the American Type Culture Collection under numbr No. 31366 ATCC.
    Type: Grant
    Filed: October 5, 1979
    Date of Patent: January 5, 1982
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
  • Patent number: 4276289
    Abstract: Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.
    Type: Grant
    Filed: March 17, 1980
    Date of Patent: June 30, 1981
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Giuseppe Cassinelli, Daniela Ruggieri, Federico Arcamone, Aurelio di Marco
  • Patent number: 4265885
    Abstract: 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 branched-chain aminodeoxy sugar to form the .alpha.-glycosidic linkage.
    Type: Grant
    Filed: October 5, 1979
    Date of Patent: May 5, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Alberto Bargiotti, Giuseppe Cassinelli, Federico Arcamone, Aurelio DiMarco
  • Patent number: 4254110
    Abstract: Antitumor anthracycline glycosides of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is formyl, hydroxymethyl or aminomethyl, and R.sub.3 is hydrogen, hydroxy or an acyloxy group; and pharmaceutically acceptable acid addition salts of said compounds in which one of R.sub.1 and R.sub. 2 is aminomethyl are prepared from daunorubicin, doxorubicin or 14-O-acyl derivatives of doxorubicin by deamination and C-3' epimerization effected with NaNO.sub.2 in a cold aqueous acidic medium, such as 1N aqueous acetic acid at 0.degree. C., to give compounds wherein one of R.sub.1 and R.sub.2 is formyl and the optional further steps of selective reduction, e.g., with NaCNBH.sub.3 in 4:1 dioxan:aqueous acetate buffer at pH 4.6 or with Na(CH.sub.3 COO).sub.3 BH in benzene under reflux, to form compounds in which one of R.sub.1 and R.sub.2 hydroxymethyl, or selective reductive amination, e.g., with NaCNBH.sub.3 in the presence of methanolic CH.sub.3 COONH.sub.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: March 3, 1981
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuseppe Cassinelli, Federico Arcamone, Aurelio di Marco