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:
August 6, 2018
Publication date:
November 29, 2018
Applicant:
NERVIANO MEDICAL SCIENCES S.r.l.
Inventors:
Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, 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:
June 20, 2018
Publication date:
October 11, 2018
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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:
February 22, 2017
Date of Patent:
September 25, 2018
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
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:
November 23, 2016
Date of Patent:
September 11, 2018
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 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:
Grant
Filed:
May 18, 2017
Date of Patent:
September 11, 2018
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
Abstract: The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation.
Type:
Application
Filed:
July 12, 2016
Publication date:
August 2, 2018
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo BERIA, Michele CARUSO, Daniele DONATI, 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:
July 6, 2016
Date of Patent:
July 24, 2018
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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:
Grant
Filed:
April 23, 2014
Date of Patent:
November 28, 2017
Assignee:
Nerviano Medical Sciences S.r.l.
Inventors:
Italo Beria, Michele Caruso, Vittoria Lupi
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:
May 18, 2017
Publication date:
September 7, 2017
Applicant:
NERVIANO MEDICAL SCIENCES S.r.l.
Inventors:
Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
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:
May 18, 2017
Publication date:
September 7, 2017
Applicant:
NERVIANO MEDICAL SCIENCES S.r.l.
Inventors:
Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
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:
July 29, 2015
Date of Patent:
July 11, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Teresa Disingrini, Sergio Mantegani, Mario Varasi
Abstract: The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.
Type:
Grant
Filed:
October 30, 2014
Date of Patent:
July 4, 2017
Assignees:
Genentech, Inc., Nerviano Medical Sciences S.R.L.
Inventors:
Italo Beria, Michele Caruso, John A. Flygare, Vittoria Lupi, Rita Perego, Paul Polakis, Andrew Polson, Matteo Salsa, Susan D. Spencer, Barbara Valsasina, Robert L. Cohen
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:
Grant
Filed:
July 24, 2013
Date of Patent:
June 27, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
Abstract: The present invention relates to 6-amino-7-deaza-purine derivatives 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:
Grant
Filed:
May 7, 2014
Date of Patent:
June 20, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Mauro Angiolini, Laura Buffa, Maria Menichincheri, Ilaria Motto, Paolo Polucci, Gabriella Traquandi, Fabio Zuccotto
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:
February 22, 2017
Publication date:
June 8, 2017
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 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:
April 16, 2015
Date of Patent:
June 6, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
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:
June 3, 2016
Date of Patent:
May 16, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Natale Alvaro Barbugian, Romualdo Forino, Tiziano Fumagalli, Paolo Orsini
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:
September 6, 2016
Date of Patent:
May 2, 2017
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: 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:
December 16, 2015
Date of Patent:
April 11, 2017
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
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:
Grant
Filed:
October 31, 2013
Date of Patent:
March 28, 2017
Assignee:
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