Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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:
July 6, 2016
Date of Patent:
March 21, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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:
November 23, 2016
Publication date:
March 16, 2017
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
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:
Grant
Filed:
March 28, 2013
Date of Patent:
February 7, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa
Abstract: The present disclosure is directed to a compound of formula (I) wherein L is null or a conditionally-cleavable moiety; W is null or a self-immolative system, comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid —peptidic and non peptidic—linker; RM is null or a reactive moiety that can be attached to one or more of L, W or Z groups, or RM is attached to oxygen when L, W and Z are all null; provided that at least one of L, W, Z and RM is not null; or a pharmaceutically acceptable salt thereof.
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:
Grant
Filed:
March 28, 2013
Date of Patent:
December 27, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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:
July 6, 2016
Publication date:
October 27, 2016
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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:
July 6, 2016
Publication date:
October 27, 2016
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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:
February 18, 2015
Date of Patent:
October 11, 2016
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
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:
June 3, 2016
Publication date:
September 29, 2016
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Natale Alvaro Barbugian, Romualdo Forino, Tiziano Fumagalli, Paolo Orsini
Abstract: There are provided substituted 3-phenyl-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.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
August 23, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L. a corporation
Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno[2,3-e]indole moiety tethered 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:
September 16, 2014
Publication date:
August 11, 2016
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Marina CALDARELLI, Michele CARUSO, Paolo ORSINI
Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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:
May 7, 2012
Date of Patent:
August 9, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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:
May 20, 2015
Date of Patent:
July 5, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Natale Alvaro Barbugian, Romualdo Forino, Tiziano Fumagalli, Paolo Orsini
Abstract: The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. 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.
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:
Grant
Filed:
January 30, 2015
Date of Patent:
April 12, 2016
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
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:
December 16, 2015
Publication date:
April 7, 2016
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
Abstract: The present invention relates to new morpholinyl anthracycline derivatives 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 compositions containing them.
Type:
Application
Filed:
April 23, 2014
Publication date:
March 17, 2016
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo BERIA, Michele CARUSO, Vittoria LUPI
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:
Grant
Filed:
April 3, 2012
Date of Patent:
March 15, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Francesco Casuscelli, Maria Gabriella Brasca, Marina Caldarelli, Giovanni Cervi, Teresa Disingrini, Francesca Quartieri
Abstract: The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus 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:
Grant
Filed:
April 5, 2012
Date of Patent:
March 15, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Maria Gabriella Brasca, Tiziano Bandiera, Jay Aaron Bertrand, Paola Gnocchi, Danilo Mirizzi, Marcella Nesi, Achille Panzeri
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:
February 9, 2016
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