Patents Assigned to Pharmacia Italia S.p.A.
  • Patent number: 6906199
    Abstract: It is described a process for preparing, in high yields and purity and without the need of carrying out several steps and/or isolating many intermediates which could lead to undesired by-products, a distamycin derivative of formula wherein R is a bromine or chlorine atom; or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful in therapy as antitumor agents.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: June 14, 2005
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Francensco Caldarelli, Lucio Ceriani, Ilaria Candiani
  • Publication number: 20050059156
    Abstract: The present invention relates to a quantitative, highly sensitive analytical procedure capable to control at part per billion (ppb) detection level the possible presence of undesired chemical contaminants, especially ?-lactam antibiotics, in anthracycline products.
    Type: Application
    Filed: August 5, 2004
    Publication date: March 17, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Vincenzo Rizzo, Mario Arangio, Giuseppe Razzano, Maristella Colombo, Federico Sirtori
  • Publication number: 20050048594
    Abstract: High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
    Type: Application
    Filed: July 9, 2004
    Publication date: March 3, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Claudio Dalvit, Elena Ardini, Maria Flocco, Gianpaolo Fogliato, Nicola Mongelli, Marina Veronesi
  • Publication number: 20050043346
    Abstract: Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: August 5, 2004
    Publication date: February 24, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Ermes Vanotti, Roberto D'Alessio, Marcellino Tibolla, Mario Varasi, Alessia Montagnoli, Corrado Santocanale, Katia Martina, Maria Menichincheri
  • Publication number: 20050043323
    Abstract: Pyrimidylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: August 5, 2004
    Publication date: February 24, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Ermes Vanotti, Roberto D'Alessio, Marcellino Tibolla, Mario Varasi, Alessia Montagnoli, Corrado Santocanale, Paolo Orsini, Antonio Pillan
  • Publication number: 20050032869
    Abstract: Pyrazolyl-indole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: July 1, 2004
    Publication date: February 10, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Daniela Berta, Barbara Forte, Sergio Mantegani, Mario Varasi, Paola Vianello
  • Publication number: 20050032839
    Abstract: Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: July 1, 2004
    Publication date: February 10, 2005
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Daniele Fancelli, Barbara Forte, Jurgen Moll, Mario Varasi, Paola Vianello
  • Patent number: 6849616
    Abstract: Estramustine phosphate is an anti-mitotic chemotherapeutic drug with proven efficacy against cancer. The invention describes methods which potentiate the therapeutic benefit of intravenous estramustine phosphate. The invention provides for intravenous estramustine phosphate to be administered at a high dosage exceeding 1300 mg as a single dose. Efficacious enhancement of estramustine phosphate pharmacokinetics is thereby achieved. Further provided, estramustine phosphate may be intravenously administered for use in combinational regimens with other chemotherapeutic agent. The therapeutic advantages achieved using the intravenous estramustine phosphate formulation are applicable to treatment of a variety of cancers including prostate cancer, breast cancer, lung cancer, colorectal cancer, pancreatic cancer, ovarian cancer, melanoma, and other cancers.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: February 1, 2005
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Michael S. Kopreski, Beryl Asp, Bo Fredholm, Per-Olv Gunnarsson
  • Patent number: 6838547
    Abstract: The present invention refers to distamycin and derivatives thereof, such as bromo- or chloro-acryloyl derivatives of distamycin, which are conjugated with glutathione, to a process for their preparation and to pharmaceutical compositions thereof. The compounds of the invention are endowed with a remarkable antitumor activity and are thus useful in therapy in the treatment of cancer.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: January 4, 2005
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Italo Beria, Paolo Cozzi, Maria Cristina Geroni
  • Publication number: 20040229930
    Abstract: The present invention features formulations of indolinones. The formulation is suitable for parenteral or oral administration, wherein the formulation comprises an indolinone, and a pharmaceutically acceptable carrier therefor. The formulations and the compounds themselves are useful for the treatment of protein kinase related disorders.
    Type: Application
    Filed: September 10, 2003
    Publication date: November 18, 2004
    Applicant: Pharmacia Italia S.p.A.
    Inventor: Paolo Gatti
  • Patent number: 6800635
    Abstract: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from s solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline forms I and II in a solvent at a temperature below 30° C.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: October 5, 2004
    Assignee: Pharmacia Italia, S.p.A.
    Inventors: Attilio Tomasi, Stefania Magenes, Giuliano Ramella, Mario Ungari, Marco Pandolfi
  • Patent number: 6784198
    Abstract: 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: August 31, 2004
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Paolo Pevarello, Raffaella Amici, Manuela Villa, Barbara Salom, Anna Vulpetti, Mario Varasi
  • Publication number: 20040092744
    Abstract: A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/diethyl ether mixture comprising raw cabergoline, followed by recovery and drying of the resulting crystals.
    Type: Application
    Filed: October 31, 2003
    Publication date: May 13, 2004
    Applicant: Pharmacia Italia, S.p. A.
    Inventors: Attilio Tomasi, Stefania Magenes, Mario Ungari, Giuliano Ramella, Gianfranco Pallanza
  • Patent number: 6730664
    Abstract: A pharmaceutical formulation which comprises a parenterally acceptable carrier or diluent, estramustine phosphate and a sulfoalkyl ether cyclodextrin. The formulation can be administered according to a combined chemotherapy regimen in association with one or more chemotherapeutic agents. The formulation also enables estramustin phosphate to be administered with no side effects at the site of injection.
    Type: Grant
    Filed: March 15, 2002
    Date of Patent: May 4, 2004
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Lorena Muggetti, Paolo Colombo, Alessandro Martini, Giovanni Buzzi
  • Publication number: 20040072855
    Abstract: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from s solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline forms I and II in a solvent at a temperature below 30° C.
    Type: Application
    Filed: October 31, 2003
    Publication date: April 15, 2004
    Applicant: Pharmacia Italia, S.p.A.
    Inventors: Attilio Tomasi, Stefania Magenes, Giuliano Ramella, Mario Ungari, Marco Pandolfi
  • Publication number: 20040009993
    Abstract: The invention provides novel pyrido[2,3-d]pyrimidin-7(8H)-ones derivatives active as telomerase inhibitors, the use of the derivatives as therapeutic agents, such as antitumoral agents, processes for preparation of the derivatives, and to pharmaceutical compositions comprising the derivatives.
    Type: Application
    Filed: December 4, 2002
    Publication date: January 15, 2004
    Applicant: Pharmacia Italia S.p.A.
    Inventors: Mauro Angiolini, Dario Ballinari, Domenico Fusar Bassini, Luisella Bonomini, Markus Gude, Maria Menichincheri, Jurgen Moll, Jean-Yves Trosset
  • Patent number: 6673806
    Abstract: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from a solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline Forms I and II in a solvent at a temperature below about 30° C.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: January 6, 2004
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Attilio Tomasi, Stefania Magenes, Giuliano Ramella, Mario Ungari, Marco Pandolfi
  • Patent number: 6673805
    Abstract: The present invention relates to novel stable solution formulations comprising oxaliplatin alone or in combination with irinotecan (CPT-11), an effective stabilizing amount of lactic acid and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method for manufacturing such formulations ready for administration and their use in the antitumor therapy are also within the scope of the invention.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: January 6, 2004
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Sara Lauria, Alessandro Martini, Cristina Ciocca
  • Patent number: 6596845
    Abstract: Compounds which are cinnamoyl distamycin derivatives of formula (I), wherein n is 2, 3, or 4; R0 is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which are the same or different, are selected from hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms; and C1-C4 alkoxy; X is a halogen atom; Y and Z are the same or different and are selected, independently for each heterocyclic ring of the polyheterocyclic chain, from N and CH; B is selected from (a), (b), (c), (d), (e), (f), (g)and (h) wherein R3, R4, R5, R6 and R7 are, independently from each other, hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; provided that at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrrole; are useful as antitumor agents.
    Type: Grant
    Filed: December 4, 2000
    Date of Patent: July 22, 2003
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Giulia Pennella, Romeo Romagnoli
  • Patent number: 6586428
    Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: July 1, 2003
    Assignee: Pharmacia Italia, S.p.A.
    Inventors: Maria Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato