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:
June 21, 2021
Publication date:
May 12, 2022
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: New N-(2,6-diethylphenyl)-8-({4-[4-(dimethyl amino)piperidin-1-yl]-2-methoxyphenyl}amino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide phosphate of formula (II): Medicaments.
Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. 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 3, 2018
Date of Patent:
September 14, 2021
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Alessandra Badari, Elena Casale, Marcella Nesi, Francesca Quartieri
Abstract: The present invention relates to a new crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, process for its preparation, its utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing it.
Type:
Grant
Filed:
June 26, 2020
Date of Patent:
August 17, 2021
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ilaria Candiani, Giovanni Ottaiano, Attilio Tomasi
Abstract: The present invention relates to certain substituted heterocondensed pyridone analogues of formula (I) which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type enzyme, in particular cancer, cell proliferative disorders and immune-related disorders. 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:
May 16, 2019
Publication date:
July 8, 2021
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Elena CASALE, Francesco CASUSCELLI, Teresa DISINGRINI, Paola MAGNAGHI, Beatrice MALGESINI, Ilaria MOTTO, Stefano NUVOLONI
Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. 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.
Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. 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.
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 P ARP-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 in-flammation. 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.
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 12, 2019
Publication date:
December 3, 2020
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 a new crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, process for its preparation, its utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing it.
Type:
Application
Filed:
June 26, 2020
Publication date:
October 15, 2020
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ilaria CANDIANI, Giovanni OTTAIANO, Attilio TOMASI
Abstract: There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-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 in-flammation. 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.
Abstract: The present invention relates to a new crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, process for its preparation, its utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing it.
Type:
Grant
Filed:
May 18, 2017
Date of Patent:
August 11, 2020
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ilaria Candiani, Giovanni Ottaiano, Attilio Tomasi
Abstract: Substituted indazole derivatives of formula (I) or formula 2.(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 a deregulated protein kinase activity, like cancer.
Type:
Grant
Filed:
January 16, 2019
Date of Patent:
June 16, 2020
Assignees:
IGNYTA, INC., NERVIANO MEDICAL SCIENCES S.r.L.
Inventors:
Jonathan Lim, Elena Ardini, Maria Menichincheri
Abstract: There are provided substituted purine and 3-deazapurine analogues, which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. 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 19, 2017
Date of Patent:
June 16, 2020
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Elena Casale, Emiliana Corti, Paola Gnocchi, Marcella Nesi, Sten Christian Orrenius, Francesca Quartieri, Federico Riccardi Sirtori
Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. 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:
July 3, 2018
Publication date:
April 30, 2020
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Alessandra BADARI, Elena CASALE, Marcella NESI, Francesca QUARTIERI
Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. 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.
Abstract: Methods of treating neuroblastoma associated with a deregulated protein kinase activity are disclosed. The treatment may include administration of substituted indazole derivatives of formula (I) or formula 2.(I) and pharmaceutically acceptable salts therefor, as degined in the specification.
Type:
Grant
Filed:
July 31, 2018
Date of Patent:
February 18, 2020
Assignees:
IGNYTA, INC., NERVIANO MEDICAL SCIENCES, S.R.L.
Inventors:
Jonathan Lim, Elena Ardini, Maria Menichincheri
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:
Grant
Filed:
November 1, 2018
Date of Patent:
February 11, 2020
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Italo Beria, Michele Caruso, Daniele Donati, Paolo Orsini
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:
November 19, 2019
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 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:
June 20, 2018
Date of Patent:
November 19, 2019
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi