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1. 发明申请

WO2019011715A1 PYRAZOLO-QUINAZOLINE DERIVATIVES AS CHOLINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2019011715A1
公开(公告)日：2019-01-17
申请号：PCT/EP2018/067896
申请日：2018-07-03
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BADARI, Alessandra , CASALE, Elena , NESI, Marcella , QUARTIERI, Francesca
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
摘要： 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.

2. 发明申请

WO2015110467A1 PROCESS FOR THE PREPARATION OF SUBSTITUTED N-(5-BENZENESULFONYL-1H-INDAZOL-3-YL)-BENZAMIDES 审中-公开
标题翻译：制备取代的N-（5-苯并呋喃-1H-吲哚-3-基） - 苯甲酸的方法
公开(公告)号：WO2015110467A1
公开(公告)日：2015-07-30
申请号：PCT/EP2015/051133
申请日：2015-01-21
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： ARCARI, Alessandro , D'ARASMO, Germano , LOMBARDI BORGIA, Andrea
IPC分类号： C07D405/14 , C07D231/56 , C07D405/12
CPC分类号： C07D231/56 , C07D405/12 , C07D405/14
摘要： The present invention relates to a process for the preparation of substituted N-(5-benzenesulfonyl-1 H-indazol-3-yl)-benzamides and to the useful intermediate compounds of such process. Such derivatives are described and claimed in WO2008/074749, which also discloses processes for their preparation. The process of the present invention allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis starts from 5-iodo-1 H-indazol-3-ylamine and comprises, as the key steps, the coupling of an activated benzoic acid with a 5-phenylsulfanyl-1 H-indazol-3-ylamine scaffold and the subsequent oxidation of the sulfur atom, followed by further functional group transformations, which furnish the desired products. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, IGF-1R or ALK inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
摘要翻译：本发明涉及制备取代的N-（5-苯磺酰基-1H-吲唑-3-基） - 苯甲酰胺的方法和该方法的有用的中间体化合物。在WO2008 / 074749中描述和要求保护这些衍生物，其也公开了它们的制备方法。本发明的方法允许以高产率和纯度和有限数量的步骤获得所需的产物。合成从5-碘-1H-吲唑-3-基胺开始，并且作为关键步骤包括活化的苯甲酸与5-苯基硫烷基-1H-吲唑-3-基胺支架的偶联和随后的氧化的硫原子，随后进一步的官能团转化，其提供所需的产物。根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予IGF-1R或ALK抑制活性。因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

3. 发明申请

WO2014067960A3 FUNCTIONALIZED 9-BROMO-CAMPTOTHECIN DERIVATIVES 审中-公开
公开(公告)号：WO2014067960A3
公开(公告)日：2014-05-08
申请号：PCT/EP2013/072633
申请日：2013-10-29
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BERIA, Italo , CARUSO, Michele , SALSA, Matteo , FAIARDI, Daniela
IPC分类号： C07D491/22 , A61K31/4745 , A61P35/00
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.

4. 发明申请

WO2014019908A2 SUBSTITUTED PYRROLES ACTIVE AS KINASES INHIBITORS 审中-公开
标题翻译：取代的吡咯作为激酶抑制剂
公开(公告)号：WO2014019908A2
公开(公告)日：2014-02-06
申请号：PCT/EP2013/065598
申请日：2013-07-24
申请人： NERVIANO MEDICAL SCIENCES S.R.L.
发明人： BRASCA, Maria Gabriella , BINDI, Simona , CALDARELLI, Marina , NESI, Marcella , ORRENIUS, Sten Christian , PANZERI, Achille
IPC分类号： C07D401/04 , C07D473/00 , C07D487/04 , A61P35/00 , A61K31/4355 , A61K31/52 , A61K31/519 , A61K31/53 , A61K31/40
CPC分类号： C07D403/04 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/53 , A61K45/06 , C07D401/04 , C07D473/00 , C07D487/04 , C07F5/04 , C07F7/083
摘要： 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.
摘要翻译：本发明涉及调节蛋白激酶活性的取代的吡咯化合物，因此可用于治疗由蛋白激酶活性失调引起的疾病，特别是Jak家族激酶。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或含有它们的药物组合物治疗疾病的方法。

5. 发明申请

WO2013014038A1 3-OXO-2,3-DIHYDRO-1H-INDAZOLE-4-CARBOXAMIDE DERIVATIVES AS PARP-1 INHIBITORS 审中-公开
标题翻译：作为PARP-1抑制剂的3-氧代-2,3-二氢-1H-吲唑-4-羧酰胺衍生物
公开(公告)号：WO2013014038A1
公开(公告)日：2013-01-31
申请号：PCT/EP2012/064054
申请日：2012-07-18
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PAPEO, Gianluca Mariano Enrico , BORGHI, Daniela , CARUSO, Michele , POSTERI, Helena , KRASAVIN, Mikhail Yurievitch
发明人： PAPEO, Gianluca Mariano Enrico , BORGHI, Daniela , CARUSO, Michele , POSTERI, Helena , KRASAVIN, Mikhail Yurievitch
IPC分类号： C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , A61K31/454 , A61K31/4545 , A61K31/4439 , A61P35/00 , A61P9/00 , A61P25/00 , A61P29/02
CPC分类号： C07D401/04 , A61K31/4188 , A61K31/454 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： There are provided 3-oxo-2,3-dihydro-lH-indazole-4-carboxamide 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.
摘要翻译：提供了选择性抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的3-氧代-2,3-二氢-1H-吲唑-4-甲酰胺衍生物。因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。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，以及利用包含这些化合物的药物组合物治疗疾病的方法。

6. 发明申请

WO2012152763A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂活化的取代的吲哚酚衍生物
公开(公告)号：WO2012152763A1
公开(公告)日：2012-11-15
申请号：PCT/EP2012/058389
申请日：2012-05-07
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , LOMBARDI BORGIA, Andrea , CIOMEI, Marina , DONATI, Daniele , NESI, Marcella
发明人： LOMBARDI BORGIA, Andrea , CIOMEI, Marina , DONATI, Daniele , NESI, Marcella
IPC分类号： C07D231/56 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/416 , A61P35/00
CPC分类号： A61K31/416 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D231/56 , C07D295/155 , C07D295/185 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C12N9/12 , C12Y207/10001
摘要： 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.
摘要翻译：本发明涉及调节蛋白激酶活性的取代吲唑化合物，因此可用于治疗由脱蛋白激酶活性引起的疾病，如癌症。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的方法。

7. 发明申请

WO2012016993A1 DERIVATIVES OF PYRAZOLOPHENYL-BENZENESULFONAMIDE COMPOUNDS AND USE THEREOF AS ANTITUMOR AGENTS 审中-公开
标题翻译：吡唑并苯基芳香胺化合物的衍生物及其作为抗菌剂的用途
公开(公告)号：WO2012016993A1
公开(公告)日：2012-02-09
申请号：PCT/EP2011/063325
申请日：2011-08-02
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella , SCOLARO, Alessandra , DONATI, Daniele
发明人： PULICI, Maurizio , MARCHIONNI, Chiara , TRAQUANDI, Gabriella , SCOLARO, Alessandra , DONATI, Daniele
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D451/04 , C07D471/04 , A61P35/00 , A61K31/4439
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。

8. 发明申请

WO2012013557A1 ISOXAZOLO-QUINAZOLINES AS MODULATORS OF PROTEIN KINASE ACTIVITY 审中-公开
标题翻译：作为蛋白激酶活性的调节剂的ISOXAZOLO-QUINAZOLINES
公开(公告)号：WO2012013557A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/062453
申请日：2011-07-20
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , CALDARELLI, Marina , BERIA, Italo , COLOMBO, Nicoletta , PIUTTI, Claudia , SALSA, Matteo , TRAQUANDI, Gabriella
发明人： CALDARELLI, Marina , BERIA, Italo , COLOMBO, Nicoletta , PIUTTI, Claudia , SALSA, Matteo , TRAQUANDI, Gabriella
IPC分类号： C07D498/02 , A61K31/517 , A61P35/00
CPC分类号： A61K31/519 , A61K45/06 , A61N5/10 , C07D498/02 , C07D498/04
摘要： 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.
摘要翻译：本发明涉及调节蛋白激酶活性的取代异恶唑并喹唑啉，因此可用于治疗由失调蛋白激酶活性引起的疾病，特别是人MPS1和PERK。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。

9. 发明申请

WO2011092120A1 6,7- DIHYDROIMIDAZO [1,5-A] PYRAZIN-8 (5H) - ONE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译： 6,7-二氢吲哚并[1,5-A]吡嗪-8（5H） - 一种衍生物作为蛋白激酶调节剂
公开(公告)号：WO2011092120A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/050846
申请日：2011-01-21
申请人： NERVIANO MEDICAL SCIENCES S.r.l. , MIRIZZI, Danilo , ORRENIUS, Sten Christian , TRIFIRO', Paolo
发明人： MIRIZZI, Danilo , ORRENIUS, Sten Christian , TRIFIRO', Paolo
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04
摘要： There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).
摘要翻译：提供了本说明书中定义的式（I）的6,7-二氢咪唑并[1,5-a]吡嗪-8（5H） - 酮化合物或其药学上可接受的盐的3,5-二取代衍生物，其中调节蛋白激酶的活性。因此，这些化合物可用于治疗由失调的蛋白激酶活性引起的疾病。特别地，用本发明的式（I）化合物治疗的这些疾病是由选自下组的失调的蛋白激酶活性引起的和/或与其相关的，所述蛋白激酶活性选自癌症，病毒感染，HIV预防艾滋病发展感染的个体，细胞增殖性疾病，自身免疫和神经变性疾病。本发明还涉及制备式（I）化合物的方法，其组合文库，包含它们的药物组合物，以及使用包含式（I）化合物的药物组合物治疗疾病的方法。

10. 发明申请

WO2011029775A1 [1,2,4]TRIAZOLO [1,5-c]PYRIMIDINE DERIVATIVES AS Hsup90 MODULATORS 审中-公开
标题翻译： [1,2,4]三唑并[1,5-c]嘧啶衍生物作为Hsup90调节剂
公开(公告)号：WO2011029775A1
公开(公告)日：2011-03-17
申请号：PCT/EP2010/062930
申请日：2010-09-03
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , CASALE, Elena , CASUSCELLI, Francesco , DALVIT, Claudio , POLUCCI, Paolo , ZUCCOTTO, Fabio
发明人： CASALE, Elena , CASUSCELLI, Francesco , DALVIT, Claudio , POLUCCI, Paolo , ZUCCOTTO, Fabio
IPC分类号： C07D487/04 , A61P25/28 , A61P35/00 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) 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, 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活性的式（I）的[1,2,4]三唑并[1,5-c]嘧啶衍生物。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，治疗疾病的方法和包含这些化合物的药物组合物。

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