Patents Assigned to Pharmacia S.p.A.
  • Patent number: 6172202
    Abstract: A process for the preparation of a conjugate between a poly (ethylene glycol) and a protein or glycoprotein, the process comprising specifically binding the domain to a specific binder, to shield the domain from the poly (ethylene glycol) in the following conjugating step, thereafter conjugating the poly (ethylene glycol) to the protein or glycoprotein, wherein conjugation of the poly (ethylene glycol) to the domain is avoided and thereafter releasing the specific binder from the domain without releasing the poly (ethylene glycol) from the protein or glycoprotein, wherein the protein or glycoprotein is other than a proteolytic enzyme selected from the group consisting of trypsin, urokinase, tissue plasminogen activator, plasmin, chymotrypsin, elastase and kallikrein.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: January 9, 2001
    Assignee: Pharmacia S.p.A.
    Inventors: Fabrizio Marcucci, Ruth Gregory
  • Patent number: 5972889
    Abstract: A conjugate of a polypeptide reactive with a fibroblast growth factor receptor and a cytotoxic agent is used for inhibiting the proliferation of epithelial lens cells, especially following extracapsular cataract surgery.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 26, 1999
    Assignee: Pharmacia S.p.A.
    Inventor: Yves Courtois
  • Patent number: 5912263
    Abstract: Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
    Type: Grant
    Filed: November 5, 1997
    Date of Patent: June 15, 1999
    Assignee: Pharmacia S.p.A.
    Inventors: Maria Menichincheri, Walter Ceccarelli, Marina Ciomei, Domenico Fusar Bassini, Nicola Mongelli, Ermes Vanotti
  • Patent number: 5843893
    Abstract: A conjugate of a polypeptide reactive with a fibroblast growth factor receptor and a cytotoxic agent is used for inhibiting the proliferation of epithelial lens cells, especially following extracapsular cataract surgery.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: December 1, 1998
    Assignee: Pharmacia S.p.A.
    Inventor: Yves Courtois
  • Patent number: 5840899
    Abstract: 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: November 24, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Franco Zarini
  • Patent number: 5840745
    Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: November 24, 1998
    Assignee: Pharmacia S. p. A.
    Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
  • Patent number: 5804209
    Abstract: The present invention relates to bioadhesive starches, to a process for their preparation and to pharmaceutical compositions containing them. It also relates to the use of such bioadhesive starches as carriers for the administration of a drug.
    Type: Grant
    Filed: February 9, 1996
    Date of Patent: September 8, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Roberto De Ponti, Alessandro Martini, Lorena Muggetti
  • Patent number: 5801167
    Abstract: The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.
    Type: Grant
    Filed: August 20, 1996
    Date of Patent: September 1, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Angelo Bedeschi, Franco Zarini, Walter Cabri, Ilaria Candiani, Sergio Penco, Laura Capolongo
  • Patent number: 5773522
    Abstract: A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein ?A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group ?A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.
    Type: Grant
    Filed: June 8, 1995
    Date of Patent: June 30, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Francesco Angelucci, Antonino Suarato
  • Patent number: 5753629
    Abstract: The present invention relates to compounds of formula (I) ##STR1## The compounds of the invention are useful as antitumor or antiviral agents.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: May 19, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Italo Beria, Enrico Pesenti, Laura Capolongo, Nicola Mongelli, Pier Giovanni Baraldi
  • Patent number: 5719159
    Abstract: The present invention provides compounds of formula (D wherein the symbol - - - represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain; B is a straight or branched C.sub.1 -C.sub.12 alkylene group optionally substituted by one or more aryl groups or fluorine atoms; W is a group R.sub.1 or (a) wherein R.sub.1 is a straight or branched C.sub. -C.sub.6 alkyl group unsubstituted or substituted by one or more fluorine atoms, provided that at least a fluorine atom is present in B or W. The compounds of the invention are useful as testosterone 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: February 17, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
  • Patent number: 5719135
    Abstract: The present invention relates to compound of formula (I) ##STR1## wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole;R.sub.1 is --H, --CN, --SO.sub.3 R.sub.4 --, --SO.sub.2 NHR.sub.5, ##STR2## --COOR.sub.6, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR3## --NR.sub.7 R.sub.8, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NH--C(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR4## --NHSO.sub.2 R.sub.9, --OR.sub.10, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR5## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n CH.sub.2 OH, --CH.sub.2 OPO(OH).sub.2 or --PO(OH).sub.2 ;R.sub.2 is C.sub.1 -C.sub.6 alkyl, halogen, or hydroxy;R.sub.3 is --H or C.sub.1 -C.sub.6 alkyl;R.sub.4 is --H, C.sub.1 -C.sub.6 alkyl or --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sub.5 is --H, C.sub.1 -C.sub.6 alkyl, --CH.sub.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: February 17, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Franco Buzzetti, Gabriella Maria Brasca, Antonio Longo, Dario Ballinari
  • Patent number: 5719177
    Abstract: Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: February 17, 1998
    Assignee: Pharmacia S.p.A.
    Inventors: Maria Menichincheri, Walter Ceccarelli, Marina Ciomei, Domenico Fusar Bassini, Nicola Mongelli, Ermes Vanotti
  • Patent number: 5663346
    Abstract: The present invention relates to compounds useful as tyrosine kinase inhibitors, having the following general formula (I) ##STR1## wherein one of the groups X.sup.1, X.sup.2, X.sup.3, X.sup.4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) ##STR2## each of R.sup.1 and R.sup.3 independently is hydrogen, amino, carboxy, cyano, --SO.sub.3 R.sup.4, --SO.sub.2 NHR.sup.5, ##STR3## --COOR.sup.6, --CONH(CH.sub.2).sub.o Ph, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR4## --N (CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NHC(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR5## --NHSO.sub.2 R.sup.7, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --OCH.sub.2 SO.sub.2 NH.sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR6## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n C.sub.2 OH, --CH.sub.2 OPO(OH).sub.2, --PO(OH).sub.2 ;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: February 9, 1996
    Date of Patent: September 2, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
  • Patent number: 5652125
    Abstract: The ability to improve the conversion of .epsilon.-rhodomycinone to daunorubicin can be conferred on a bacterial host transformed with a recombinant vector comprising a DNA coding for an appropriate protein useful for that conversion. Furthermore, the bacterial host may have a mutation that blocks the function of a gene of daunorubicin metabolism.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: July 29, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Claudio Scotti, Charles Richard Hutchinson, Anna Luisa Colombo, Silvia Filippini
  • Patent number: 5652250
    Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: July 29, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Franco Buzzetti, Angelo Crugnola, Antonio Longo, Maria Gabriella Brasca, Dario Ballinari
  • Patent number: 5637596
    Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: June 10, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Mario Varasi, Franco Heidempergher, Carla Caccia, Patricia Salvati
  • Patent number: 5621096
    Abstract: The invention provides a process for the preparation of the compound of formula I ##STR1## wherein R is carboxy group or a carboxylate anion, by enzymatic hydrolysis with a lipase or an acylase in an alcoholic solution, of a compound of the formula II ##STR2## wherein R.sub.1, represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and R.sub.2 is a hydrogen atom, an alkyl, alkenyl, phcnyl, phenylalkyl or phenylalkenyl group having from 1 to 18 carbon atoms or an alkoxy group.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: April 15, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Walter Cabri, Angelo Bedeschi
  • Patent number: 5585372
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 17, 1996
    Assignee: Pharmacia S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
  • Patent number: 5529932
    Abstract: Nucleic acid encoding the ribosome-inactivating protein SO-6 is provided.
    Type: Grant
    Filed: October 7, 1993
    Date of Patent: June 25, 1996
    Assignee: Pharmacia, S.p.A.
    Inventors: Rolando Lorenzetti, Luca Benatti, Maria Dian, Douglas Lappi, Maria B. Saccardo, Marco Soria