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1. 发明授权

US11491158B2 N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors 有权
公开(公告)号：US11491158B2
公开(公告)日：2022-11-08
申请号：US17140471
申请日：2021-01-04
申请人： Nerviano Medical Sciences S.R.L.
发明人： Simona Bindi , Davide Carenzi , Ilaria Motto , Maurizio Pulici
IPC分类号： A61K31/519 , C07D487/04 , C07D513/04 , A61P37/00 , A61P25/28 , A61P35/00 , A61K31/4355 , A61K31/4365 , C07D491/048 , C07D495/04
摘要： 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.

2. 发明申请

US20220144813A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 有权
公开(公告)号：US20220144813A1
公开(公告)日：2022-05-12
申请号：US17352585
申请日：2021-06-21
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： Andrea Lombardi Borgia , Maria Menichincheri , Paolo Orsini , Achille Panzeri , Ettore Perrone , Ermes Vanotti , Marcella Nesi , Chiara Marchionni
IPC分类号： C07D405/14 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/12 , A61K31/496 , A61K45/06 , C07D403/12
摘要： 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.

3. 发明申请

US20220016122A1 SALT OF N-(2,6-DIETHYLPHENYL)-8-({4-[4-(DIMETHYLAMINO) PIPERIDIN-1-YL]-2-METHOXYPHENYL}AMINO)-1-METHYL-4,5-DIHYDRO-1H-PYRAZOLO[4,3-h]QUINAZOLINE-3-CARBOXAMIDE, ITS PREPARATION, AND FORMULATIONS CONTAINING IT 有权
公开(公告)号：US20220016122A1
公开(公告)日：2022-01-20
申请号：US17490318
申请日：2021-09-30
申请人： NERVIANO MEDICAL SCIENCES S.r.l.
发明人： Massimo ZAMPIERI , Marina CALDARELLI , Ilaria CANDIANI , Matteo D'ANELLO , Germano D'ARASMO
IPC分类号： A61K31/519 , A61P35/00 , C07D487/04
摘要： N-(2,6-diethylphenyl)-8-({4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl}amino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide phosphate of formula (II): Medicinal products containing the same which are useful in treating cancer, cell proliferative disorders, viral infections, autoimmune and neurodegenerative disorders.

4. 发明授权

US11091469B2 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 有权
公开(公告)号：US11091469B2
公开(公告)日：2021-08-17
申请号：US16912965
申请日：2020-06-26
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： Ilaria Candiani , Giovanni Ottaiano , Attilio Tomasi
IPC分类号： C07D405/12 , C07D405/14 , A61P35/00
摘要： 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.

5. 发明申请

US20210206759A1 HETEROCONDENSED PYRIDONES COMPOUNDS AND THEIR USE AS IDH INHIBITORS 有权
公开(公告)号：US20210206759A1
公开(公告)日：2021-07-08
申请号：US17056450
申请日：2019-05-16
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： Elena CASALE , Francesco CASUSCELLI , Teresa DISINGRINI , Paola MAGNAGHI , Beatrice MALGESINI , Ilaria MOTTO , Stefano NUVOLONI
IPC分类号： C07D471/04 , A61K31/519 , A61K45/06
摘要： 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.

6. 发明授权

US10556913B2 Asymmetric process for the preparation of thieno-indoles derivatives 有权
公开(公告)号：US10556913B2
公开(公告)日：2020-02-11
申请号：US16177551
申请日：2018-11-01
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： Italo Beria , Michele Caruso , Daniele Donati , Paolo Orsini
IPC分类号： C07D495/04
摘要： 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. The synthesis starts from the N-alkylation of 5-amino-4-halo-3-alkyl-1-benzothiophene-7-ol derivatives with enantiopure glycidyl 3-nosylate, followed by intramolecular 6-endo-tet cyclization using alkyl Grignard reagents; Mitsunobu activation of the secondary alcohol promotes internal spirocyclization, affording the 4,4a,5,6-tetrahydro-8H-cyclopropa[c]thieno[3,2-e]indol-8-one derivatives; finally, stereo-electronically controlled regioselective cyclopropane opening yields the key enantiopure 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates; which can be further derivatized following teachings disclosed in WO2013/149948 or WO2013/149946, to prepare the final thieno-indole derivatives of formula (Ia) or (Ib).Such compounds are disclosed to be alkylating compounds with cytotoxic activity, therefore useful as such in the treatment of a variety of cancers and in cell proliferative disorders, or, conjugated with different types of nucleophiles, in the preparation of Antibody Drug Conjugated derivatives.

7. 发明授权

US10385018B2 4-carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors 有权
公开(公告)号：US10385018B2
公开(公告)日：2019-08-20
申请号：US14438410
申请日：2013-10-23
申请人： NERVIANO MEDICAL SCIENCES S.r.l
发明人： Gianluca Mariano Enrico Papeo , Mikhail Yurievitch Krasavin , Paolo Orsini , Alessandra Scolaro
IPC分类号： C07D209/44 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/06 , C07D403/02 , C07D403/04 , C07D403/14 , C07D405/04 , C07D407/14 , C07D409/14 , C07D413/06 , C07D209/46 , A61K31/4035 , A61K31/4188 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377
摘要： 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.

8. 发明申请

US20190201406A1 N-(SUBSTITUTED-PHENYL)-SULFONAMIDE DERIVATIVES AS KINASE INHIBITORS 审中-公开
公开(公告)号：US20190201406A1
公开(公告)日：2019-07-04
申请号：US16312061
申请日：2017-06-19
申请人： Nerviano Medical Sciences S.R.L.
发明人： Simona Bindi , Davide Carenzi , Ilaria Motto , Maurizio Pulici
IPC分类号： A61K31/519 , A61P37/00 , A61P25/28 , A61P35/00 , A61K31/4355 , A61K31/4365 , C07D487/04 , C07D491/048 , C07D495/04
摘要： 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.

9. 发明申请

US20190169173A1 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 审中-公开
公开(公告)号：US20190169173A1
公开(公告)日：2019-06-06
申请号：US16301826
申请日：2017-05-18
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： Ilaria CANDIANI , Giovanni OTTAIANO , Attilio TOMASI
IPC分类号： C07D405/14 , A61P35/00
摘要： 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.

10. 发明授权

US10280176B2 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
公开(公告)号：US10280176B2
公开(公告)日：2019-05-07
申请号：US15467323
申请日：2017-03-23
申请人： Nerviano Medical Sciences S.R.L.
发明人： 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
IPC分类号： C07D487/14 , C07D487/04 , C07D401/10 , C07D403/14 , C07D413/14 , C07D231/56 , C07D239/72 , A61K31/519 , A61K31/551 , A61K31/5377
摘要： 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.

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