公开(公告)号：US09199979B2

公开(公告)日：2015-12-01

申请号：US13985698

申请日：2012-02-21

申请人： Maurizio Pulici ,  Gabriella Traquandi ,  Chiara Marchionni ,  Alessandra Scolaro ,  Nicoletta Colombo

发明人： Maurizio Pulici ,  Gabriella Traquandi ,  Chiara Marchionni ,  Alessandra Scolaro ,  Nicoletta Colombo

IPC分类号： C07D401/00 ,  C07D417/00 ,  C07D417/04 ,  C07D417/14 ,  A61K31/44 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496

CPC分类号： C07D417/04 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K45/06 ,  C07D417/14 ,  A61K2300/00

摘要： 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.

摘要翻译： 公开了说明书中定义的式（I）的噻唑基苯基 - 苯磺酰胺衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

公开(公告)号：US20150291613A1

公开(公告)日：2015-10-15

申请号：US14439020

申请日：2013-10-29

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： Italo BERIA ,  Michele CARUSO ,  Matteo SALSA ,  Daniela FAIARDI

IPC分类号： C07D491/147 ,  A61K45/06 ,  C07K5/08 ,  A61K38/06 ,  A61K31/4745 ,  A61K31/496

CPC分类号： C07D491/147 ,  A61K31/4745 ,  A61K31/496 ,  A61K38/06 ,  A61K45/06 ,  C07D491/22 ,  C07K5/08

摘要： 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.

摘要翻译： 本发明涉及具有细胞毒活性并且可用于治疗疾病如癌症，细胞增殖病症和病毒感染的新的功能化的9-溴 - 喜树碱衍生物（I）。 本发明还提供了制备这些化合物的方法，包含它们的药物组合物和使用这些化合物治疗疾病的方法或含有它们的药物组合物。 本发明还涉及这些官能化的9-溴 - 喜树碱衍生物在制备缀合物中的用途。

公开(公告)号：US09145418B2

公开(公告)日：2015-09-29

申请号：US14349516

申请日：2012-10-04

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： Francesco Casuscelli ,  Elena Casale ,  Marisa Montemartini ,  Claudia Piutti

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K45/06 ,  A61N5/10

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10

摘要： 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.

摘要翻译： 本发明涉及调节蛋白激酶活性的式（I）的取代的3,4-二氢吡咯并[1,2-a]吡嗪-1（2H） - 酮衍生物，因此可用于治疗由失调的 蛋白激酶活性。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。

公开(公告)号：US09114137B2

公开(公告)日：2015-08-25

申请号：US13752807

申请日：2011-08-02

申请人： Maurizio Pulici ,  Chiara Marchionni ,  Gabriella Traquandi ,  Alessandra Scolaro ,  Daniele Donati

发明人： Maurizio Pulici ,  Chiara Marchionni ,  Gabriella Traquandi ,  Alessandra Scolaro ,  Daniele Donati

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  A61K31/4439 ,  C07D403/04 ,  C07D451/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/506 ,  A61K45/06

CPC分类号： A61K31/4439 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/506 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D451/04 ,  C07D471/04

摘要： 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.

摘要翻译： 描述了式（I）的取代的吡唑并苯基 - 苯磺酰胺化合物，其中m，R 1，R 2，R 3和R 4在描述中定义，其调节蛋白激酶的活性。这些化合物可用于治疗由失调蛋白激酶 活动，如癌症和细胞增殖性疾病。

公开(公告)号：US20150218138A1

公开(公告)日：2015-08-06

申请号：US14688207

申请日：2015-04-16

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： Ermes Vanotti ,  Marina Caldarelli ,  Alessandra Cirla ,  Barbara Forte ,  Antonella Ermoli ,  Maria Menichincheri ,  Antonio Pillan ,  Alessandra Scolaro

IPC分类号： C07D409/14 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/4725 ,  A61K31/4545 ,  A61N5/10 ,  A61K31/506 ,  A61K31/496 ,  C07D409/04 ,  C07D405/04 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D409/14 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04

摘要： 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.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中G，W，R 2，R 3，R 4，R 5和R 6如说明书中所定义。 本发明的另外的目的是制备式（I）化合物，包含它们的药物组合物和治疗细胞增殖性疾病的方法的方法和中间体。 事实上，式（I）化合物在治疗中可用于治疗与抑制性蛋白激酶活性相关的疾病，如癌症。

公开(公告)号：US08993556B2

公开(公告)日：2015-03-31

申请号：US13264888

申请日：2010-04-16

申请人： Maria Gabriella Brasca ,  Elena Casale ,  Ron Ferguson ,  Paolo Polucci ,  Fabio Zuccotto

发明人： Maria Gabriella Brasca ,  Elena Casale ,  Ron Ferguson ,  Paolo Polucci ,  Fabio Zuccotto

IPC分类号： C07D231/14 ,  C07D261/14 ,  C07D261/18 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  A61K31/42 ,  A61K31/454 ,  A61K31/439 ,  A61K31/496 ,  A61K31/5377

CPC分类号： C07D231/14 ,  C07D261/14 ,  C07D261/18 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02

摘要： The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.

摘要翻译： 本发明涉及抑制热休克蛋白HSP90活性的取代间苯二酚衍生物。 因此，本发明的化合物可用于治疗增殖性疾病如癌症和神经变性疾病。 本发明还提供了制备这些化合物的方法，包含它们的药物组合物，治疗疾病的方法和包含这些化合物的药物组合物。

公开(公告)号：US08981092B2

公开(公告)日：2015-03-17

申请号：US13747859

申请日：2013-01-23

申请人： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

发明人： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

IPC分类号： C07D241/38 ,  A61K31/4985 ,  C07D487/04 ,  A61K45/06

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, 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.

摘要翻译： 公开了3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物。 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

公开(公告)号：US20150065520A1

公开(公告)日：2015-03-05

申请号：US14534617

申请日：2014-11-06

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： C07D405/12

CPC分类号： C07D405/14 ,  A61K31/496 ,  A61K45/06 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12

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.

公开(公告)号：US20150051237A1

公开(公告)日：2015-02-19

申请号：US14531261

申请日：2014-11-03

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： Ermes Vanotti ,  Marina Caldarelli ,  Alessandra Cirla ,  Barbara Forte ,  Antonella Ermoli ,  Maria Menichincheri ,  Antonio Pillan ,  Alessandra Scolaro

IPC分类号： C07D403/04

CPC分类号： C07D409/14 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04

摘要： 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.

公开(公告)号：US20150051222A1

公开(公告)日：2015-02-19

申请号：US14528475

申请日：2014-10-30

申请人： NERVIANO MEDICAL SCIENCES S.R.L.

发明人： Natale Alvaro BARBUGIAN ,  Romualdo FORINO ,  Tiziano FUMAGALLI ,  Paolo ORSINI

IPC分类号： C07D405/14

CPC分类号： A61K31/496 ,  A61P35/00 ,  C07B2200/13 ,  C07D405/12 ,  C07D405/14

摘要： 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.