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公开(公告)号：US20050043346A1
公开(公告)日：2005-02-24
申请号：US10912323
申请日：2004-08-05
申请人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Katia Martina , Maria Menichincheri
发明人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Katia Martina , Maria Menichincheri
IPC分类号： A61K31/444 , A61K31/4745 , A61K45/06 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4745 , A61K45/06 , A61K2300/00
摘要： Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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： 公开了式（I）的吡啶基吡咯衍生物及其药学上可接受的盐，以及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。
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公开(公告)号：US07279575B2
公开(公告)日：2007-10-09
申请号：US10912319
申请日：2004-08-05
申请人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Paolo Orsini , Antonio Pillan
发明人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Paolo Orsini , Antonio Pillan
IPC分类号： C07D239/02 , A01N43/54 , A61K31/505
CPC分类号： C07D471/04 , A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： Pyrimidylpyrrole derivatives of formula (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 disregulated protein kinase activity, like cancer.
摘要翻译： 公开了式（I）的嘧啶基吡咯衍生物及其药学上可接受的盐，如本说明书中定义的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。
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公开(公告)号：US20050043323A1
公开(公告)日：2005-02-24
申请号：US10912319
申请日：2004-08-05
申请人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Paolo Orsini , Antonio Pillan
发明人： Ermes Vanotti , Roberto D'Alessio , Marcellino Tibolla , Mario Varasi , Alessia Montagnoli , Corrado Santocanale , Paolo Orsini , Antonio Pillan
IPC分类号： A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/506 , A61K31/513 , A61K31/52 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： Pyrimidylpyrrole derivatives of formula (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 disregulated protein kinase activity, like cancer.
摘要翻译： 公开了本说明书中定义的式（I）的嘧啶基吡咯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。
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公开(公告)号：US20140045846A1
公开(公告)日：2014-02-13
申请号：US14061100
申请日：2013-10-23
申请人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
发明人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
IPC分类号： C07D217/24 , C07D401/12
CPC分类号： C07D217/24 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , Y10T436/145555
摘要： There are provided substituted isoquinolin-1(2H)-one 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 the present 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
摘要翻译： 提供了选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的取代的异喹啉-1（2H） - 酮衍生物。 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。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。
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公开(公告)号：US08993594B2
公开(公告)日：2015-03-31
申请号：US14061100
申请日：2013-10-23
申请人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
发明人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
IPC分类号： C07D217/24 , A61K31/472 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04
CPC分类号： C07D217/24 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , Y10T436/145555
摘要： There are provided substituted isoquinolin-1(2H)-one 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 the present 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
摘要翻译： 提供了选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的取代的异喹啉-1（2H） - 酮衍生物。 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。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。
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6.发明申请THERAPEUTIC COMBINATION COMPRISING A CDC7 INHIBITOR AND AN ANTI-NEOPLASTIC AGENT 有权包含CDC7抑制剂和抗神经药物的治疗组合公开(公告)号：US20120276093A1
公开(公告)日：2012-11-01
申请号：US13509625
申请日：2010-11-17
IPC分类号： A61K31/506 , A61K33/24 , A61K31/655 , A61K31/513 , A61K31/7068 , A61P35/00 , A61K31/704 , A61K31/7048 , A61K31/517 , A61K31/69 , A61K31/5377 , A61K39/395 , A61K31/519
CPC分类号： A61K45/06 , A61K31/40 , A61K31/495 , A61K31/506 , A61K2300/00
摘要： The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
摘要翻译： 本发明提供治疗组合，其包含（a）如说明书中所述的式（I）化合物和（b）一种或多种抗肿瘤剂，其选自烷基化或烷基化样试剂，抗代谢药 ，拓扑异构酶I抑制剂，拓扑异构酶11抑制剂，生长因子或生长因子受体的抑制剂，抗有丝分裂剂，蛋白酶体抑制剂，抗凋亡蛋白的抑制剂和针对细胞表面蛋白的抗体， 其中活性成分在每种情况下以虱子形式存在，或以药学上可接受的盐或其任何水合物的形式存在。
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公开(公告)号：US20120157454A1
公开(公告)日：2012-06-21
申请号：US13320969
申请日：2010-05-19
申请人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
发明人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
IPC分类号： A61K31/472 , A61K31/4725 , C07D413/12 , A61K31/5377 , G01N21/64 , A61P35/00 , A61P9/00 , A61P25/00 , A61P29/00 , C07D217/24 , C07D401/12
CPC分类号： C07D217/24 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , Y10T436/145555
摘要： There are provided substituted isoquinolin-1(2H)-one 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 the present 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
摘要翻译： 提供了选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的取代的异喹啉-1（2H） - 酮衍生物。 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。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。
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8.发明授权Therapeutic combination comprising a Cdc7 inhibitor and an anti-neoplastic agent 有权包含Cdc7抑制剂和抗肿瘤剂的治疗组合公开(公告)号：US09119877B2
公开(公告)日：2015-09-01
申请号：US13509625
申请日：2010-11-17
IPC分类号： A61K31/40 , A61K31/495 , A61K45/06 , A61K31/506
CPC分类号： A61K45/06 , A61K31/40 , A61K31/495 , A61K31/506 , A61K2300/00
摘要： The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
摘要翻译： 本发明提供治疗组合，其包含（a）如说明书中所述的式（I）化合物和（b）一种或多种抗肿瘤剂，其选自烷基化或烷基化样试剂，抗代谢药 拓扑异构酶I抑制剂，拓扑异构酶II抑制剂，生长因子或生长因子受体的抑制剂，抗有丝分裂剂，蛋白酶体抑制剂，抗凋亡蛋白的抑制剂和针对细胞表面蛋白的抗体， 其中活性成分在每种情况下以虱子形式存在，或以药学上可接受的盐或其任何水合物的形式存在。
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公开(公告)号：US08592416B2
公开(公告)日：2013-11-26
申请号：US13320969
申请日：2010-05-19
申请人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
发明人： Gianluca Mariano Enrico Papeo , Jay Aaron Bertrand , Giovanni Cervi , Barbara Forte , Rosita Lupi , Alessia Montagnoli , Alessandra Scolaro , Fabio Zuccotto , Paolo Orsini , Helena Posteri
IPC分类号： C07D217/24 , C07D401/04 , A61K31/472
CPC分类号： C07D217/24 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , Y10T436/145555
摘要： There are provided substituted isoquinolin-1(2H)-one 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 the present 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
摘要翻译： 提供了选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的取代的异喹啉-1（2H） - 酮衍生物。 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。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。
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10.发明申请THERAPEUTIC COMBINATION COMPRISING A PARP-1 INHIBITOR AND AN ANTI-NEOPLASTIC AGENT 审中-公开包含PARP-1抑制剂和抗神经药物的治疗组合公开(公告)号：US20130129841A1
公开(公告)日：2013-05-23
申请号：US13813321
申请日：2011-07-25
IPC分类号： A61K31/454 , A61K31/7068 , A61K45/00 , A61K31/4545 , A61K31/4188 , A61K31/337 , A61K33/24 , A61K31/5377
CPC分类号： A61K31/454 , A61K31/337 , A61K31/4188 , A61K31/4545 , A61K31/5377 , A61K31/7068 , A61K33/24 , A61K45/00 , A61K45/06 , A61K2300/00
摘要： The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an antimitotic agent and radiation wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
摘要翻译： 本发明提供治疗组合，其包含（a）如说明书中所述的式（I）化合物和（b）一种或多种抗肿瘤剂，其选自烷基化或烷基化样试剂，抗代谢药 ，拓扑异构酶I抑制剂，拓扑异构酶II抑制剂，抗有丝分裂剂和放射剂，其中活性成分以游离形式或以药学上可接受的盐或其水合物的形式存在于各种情况下。
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