Patents Assigned to Nerviano Medical Sciences S.R.L.
  • PYRAZOLYL-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20140051708
    Abstract: The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: April 3, 2012
    Publication date: February 20, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Maria Gabriella Brasca, Marina Caldarelli, Giovanni Cervi, Teresa Disingrini, Francesca Quartieri
  • ISOQUINOLIN-1(2H)-ONE DERIVATIVES AS PARP-1 INHIBITORS
    Publication number: 20140045846
    Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 13, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
  • [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS
    Publication number: 20140045836
    Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
  • PLK inhibitor salts
    Patent number: 8648078
    Abstract: The present invention relates to novel crystalline, water-soluble salts of a plk inhibitor. Such crystal salts are for example L-tartrate, succinate, phosphate, mesylate, maleate, L-malate, hydrochloride, fumarate (half mole of counterion), fumarate, citrate (half mole of counterion), benzenesulfonate and L-aspartate (half mole of counterion). New crystal forms of the base as well as solvates and hydrates of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 11, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Massimo Zampieri, Italo Beria, Annalisa Airoldi, Ilaria Candiani, Riccardo Frigerio
  • Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and platinum derivatives
    Patent number: 8642580
    Abstract: Compounds which are ?-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.
    Type: Grant
    Filed: June 20, 2001
    Date of Patent: February 4, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: M. Cristina Geroni, Paolo Cozzi, Italo Beria
  • Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
    Patent number: 8623876
    Abstract: Substituted pyrrolo-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 dysregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: January 7, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
  • 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS
    Publication number: 20140005150
    Abstract: 3,4-diarylpyrazole 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: August 20, 2013
    Publication date: January 2, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
  • SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130344031
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Application
    Filed: August 27, 2013
    Publication date: December 26, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20130345245
    Abstract: Pyrimidinylpyrrolopyridinone 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: August 27, 2013
    Publication date: December 26, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Chiara Marchionni, Fabio Zuccotto, Alessandra Badari, Mauro Angiolini, Davide Carenzi, Marina Caldarelli, Maurizio Pulici
  • Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8614220
    Abstract: Pyrazolo-quinazoline 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: Grant
    Filed: December 17, 2007
    Date of Patent: December 24, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri, Barbara Valsasina
  • PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20130338148
    Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) 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: August 21, 2013
    Publication date: December 19, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
  • THIAZOLYLPHENYL-BENZENESULFONAMIDO DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130324551
    Abstract: Thiazolylphenyl-benzenesulfonamido 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: February 21, 2012
    Publication date: December 5, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Gabriella Traquandi, Chiara Marchionni, Alessandra Scolaro, Nicoletta Colombo
  • Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8598172
    Abstract: Dihydropteridin-6-one 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: Grant
    Filed: November 26, 2008
    Date of Patent: December 3, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Helena Posteri, Gabriele Fachin
  • Isoquinolin-1 (2H)-one derivatives as PARP-1 inhibitors
    Patent number: 8592416
    Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: November 26, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
  • CDK inhibitor salts
    Patent number: 8586598
    Abstract: The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: November 19, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Massimo Zampieri, Annalisa Airoldi, Maria Gioia Fornaretto, Maria Gabriella Brasca
  • TRICYCLIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20130302416
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 14, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • [1,2,4]triazolo [1,5-c]pyrimidine derivatives as Hsp90 modulators
    Patent number: 8580783
    Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: November 12, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
  • TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20130296305
    Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 7, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
    Patent number: 8557845
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
    Patent number: 8557857
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: October 15, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello