Patents Assigned to Nerviano Medical Sciences S.R.L.
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Bicyclo-pyrazoles active as kinase inhibitors
    Patent number: 9012487
    Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: April 21, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
  • Isoquinolin-1(2H)-one derivatives as PARP-1 inhibitors
    Patent number: 8993594
    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: October 23, 2013
    Date of Patent: March 31, 2015
    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
  • Resorcinol derivatives as HSP90 inhibitors
    Patent number: 8993556
    Abstract: The present invention relates to substituted resorcinol 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, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: March 31, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
  • FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER
    Publication number: 20150080316
    Abstract: The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa
  • Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8981089
    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: Grant
    Filed: August 21, 2013
    Date of Patent: March 17, 2015
    Assignee: 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
  • Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity
    Patent number: 8981092
    Abstract: Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: March 17, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Danilo Mirizzi, Giovanni Cervi, Matteo D'Anello, Gianluca Mariano Enrico Papeo, Ron Ferguson, Francesco Casuscelli
  • Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8975267
    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: Grant
    Filed: January 19, 2012
    Date of Patent: March 10, 2015
    Assignee: 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 INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
    Publication number: 20150065520
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8969366
    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: Grant
    Filed: August 27, 2013
    Date of Patent: March 3, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Chiara Marchionni, Fabio Zuccotto, Alessandra Badari, Mauro Angiolini, Davide Carenzi, Marina Caldarelli, Maurizio Pulici
  • SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
    Publication number: 20150057291
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: February 26, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
    Publication number: 20150057292
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: February 26, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • ALKYLATING AGENTS
    Publication number: 20150051154
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Application
    Filed: March 28, 2013
    Publication date: February 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
  • PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE- AND FURANE-DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20150051237
    Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • PROCESS FOR THE PREPARATION OF N-[5-(3,5-DIFLUORO-BENZYL)-1H-INDAZOL-3-YL]-4-(4-METHYL-PIPERAZIN-1-YL)-2-(TETRAHYDRO-PYRAN-4-YLAMINO)-BENZAMIDE
    Publication number: 20150051222
    Abstract: The present invention relates to a process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide. Novel solid forms of this compound, their utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing them are also object of the present invention.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Natale Alvaro BARBUGIAN, Romualdo FORINO, Tiziano FUMAGALLI, Paolo ORSINI
  • Use of CDK inhibitor for the treatment of glioma
    Patent number: 8946226
    Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: February 3, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Marina Ciomei, Francesco Fiorentini, Enrico Pesenti
  • 3,4-diarylpyrazoles as protein kinase inhibitors
    Patent number: 8946250
    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: Grant
    Filed: August 20, 2013
    Date of Patent: February 3, 2015
    Assignee: 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
  • Pharmaceutical composition of an anthracycline
    Patent number: 8940334
    Abstract: The present invention relates to pharmaceutical composition containing nemorubicin hydrochloride incorporated in microspheres. The compositions are useful for chemoembolization, particularly for loco regional treatment of tumors.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: January 27, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Cristina Geroni, Olga Valota, Alessandro Martini, Paolo Elia Cappella
  • Therapeutic combination comprising a PLK1 inhibitor and an antineoplastic agent
    Patent number: 8927530
    Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: January 6, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Juergen Moll, Mara Emanuela Casnaghi, Alessandro Luciano Croci
  • Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
    Patent number: 8916577
    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: Grant
    Filed: January 19, 2012
    Date of Patent: December 23, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni