Patents Assigned to Nerviano Medical Sciences S.R.L.
  • Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors
    Patent number: 9199979
    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: Grant
    Filed: February 21, 2012
    Date of Patent: December 1, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Gabriella Traquandi, Chiara Marchionni, Alessandra Scolaro, Nicoletta Colombo
  • TRICYCLOPYRAZOLE DERIVATIVES
    Publication number: 20150329552
    Abstract: Compounds which are tricyclopyrazole derivatives 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: Application
    Filed: July 29, 2015
    Publication date: November 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
  • Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
    Patent number: 9181258
    Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one 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: October 4, 2012
    Date of Patent: November 10, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
  • SUBSTITUTED PYRIMIDINYL AND PYRIDINYL-PYRROLOPYRIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20150299192
    Abstract: The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
    Type: Application
    Filed: October 31, 2013
    Publication date: October 22, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Maria MENICHINCHERI, Mauro ANGIOLINI, Jay Aaron BERTRAND, Michele CARUSO, Paolo POLUCCI, Francesca QUARTIERI, Barbara SALOM, Matteo SALSA, Fabio ZUCCOTTO
  • FUNCTIONALIZED 9-BROMO-CAMPTOTHECIN DERIVATIVES
    Publication number: 20150291613
    Abstract: The present invention relates to new functionalized 9-bromo-camptothecin derivatives (I) 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 these functionalized 9-bromo-camptothecin derivatives in the preparation of conjugates.
    Type: Application
    Filed: October 29, 2013
    Publication date: October 15, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo BERIA, Michele CARUSO, Matteo SALSA, Daniela FAIARDI
  • 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: 20150274707
    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: May 20, 2015
    Publication date: October 1, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Natale Alvaro Barbugian, Romualdo Forino, Tiziano Fumagalli, Paolo Orsini
  • 4-CARBOXAMIDO-ISOINDOLINONE DERIVATIVES AS SELECTIVE PARP-1 INHIBITORS
    Publication number: 20150274662
    Abstract: There are provided substituted 4-carboxamido-isoindolinone 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 this 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.
    Type: Application
    Filed: October 23, 2013
    Publication date: October 1, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.r.L.
    Inventors: Gianluca Mariano Enrico Papeo, Mikhail Yurievitch Krasavin, Paolo Orsini, Alessandra Scolaro
  • Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
    Patent number: 9145418
    Abstract: The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one 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 compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: September 29, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Elena Casale, Marisa Montemartini, Claudia Piutti
  • Tricyclopyrazole derivatives
    Patent number: 9127015
    Abstract: Compounds which are tricyclopyrazole derivatives 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: November 24, 2010
    Date of Patent: September 8, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
  • Therapeutic combination comprising a Cdc7 inhibitor and an anti-neoplastic agent
    Patent number: 9119877
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: September 1, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Dario Ballinari, Antonella Ciavolella, Enrico Pesenti, Alessia Montagnoli
  • Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
    Patent number: 9114137
    Abstract: Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: August 25, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maurizio Pulici, Chiara Marchionni, Gabriella Traquandi, Alessandra Scolaro, Daniele Donati
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 9102662
    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: November 6, 2014
    Date of Patent: August 11, 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
  • PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE- AND FURANE-DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20150218138
    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: April 16, 2015
    Publication date: August 6, 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
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 9085558
    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: November 6, 2014
    Date of Patent: July 21, 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
  • 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
    Patent number: 9085565
    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: Grant
    Filed: October 30, 2014
    Date of Patent: July 21, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Natale Alvaro Barbugian, Romualdo Forino, Tiziano Fumagalli, Paolo Orsini
  • 3-Oxo-2,3-dihydro-1-indazole-4-carboxamide derivatives as PARP-1 inhibitors
    Patent number: 9073893
    Abstract: There are provided 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide 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 this 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.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: July 7, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Daniela Borghi, Michele Caruso, Helena Posteri, Mikhail Yurievitch Krasavin
  • SUBSTITUTED PYRROLES ACTIVE AS KINASES INHIBITORS
    Publication number: 20150166512
    Abstract: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. 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: July 24, 2013
    Publication date: June 18, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
  • Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
    Patent number: 9056854
    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: Grant
    Filed: November 3, 2014
    Date of Patent: June 16, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20150158876
    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: February 18, 2015
    Publication date: June 11, 2015
    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
  • TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
    Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo 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 these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    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