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公开(公告)号：US20090232907A1
公开(公告)日：2009-09-17
申请号：US12313179
申请日：2008-11-17
申请人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
发明人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
IPC分类号： A61K33/24 , A61K31/4188 , A61K31/4166 , A61K31/473
CPC分类号： A61K31/4166 , A61K31/4188 , A61K31/473 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.
摘要翻译： 新的脲基取代的萘二甲酰亚胺衍生物，其药学上可接受的盐和溶剂合物可用于制备用于治疗细胞增殖性疾病如癌症的药物组合物。 本发明还提供了单独使用本文所述的化合物和抗肿瘤剂组合治疗特定类型的癌症例如前列腺，食管，胶质母细胞瘤，胶质瘤，NSCLC，头颈部和乳腺的方法。
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2.发明申请Compositions and methods for treatment of glioblastoma, gliosarcoma, NSCLC, and head and neck cancer 审中-公开用于治疗胶质母细胞瘤，神经胶质瘤，NSCLC和头颈部癌症的组合物和方法公开(公告)号：US20090186915A1
公开(公告)日：2009-07-23
申请号：US12313187
申请日：2008-11-17
申请人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
发明人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
IPC分类号： A61K31/473 , A61P35/00
CPC分类号： A61K31/473 , A61K31/47 , A61K31/53 , A61K2300/00
摘要： Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.
摘要翻译： 新的脲基取代的萘二甲酰亚胺衍生物，其药学上可接受的盐和溶剂合物可用于制备用于治疗细胞增殖性疾病如癌症的药物组合物。 本发明还提供了单独使用本文所述的化合物和抗肿瘤剂组合治疗特定类型的癌症例如前列腺，食管，胶质母细胞瘤，胶质瘤，NSCLC，头颈部和乳腺的方法。
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3.发明申请ISOCARBOSTYRIL ALKALOID DERIVATIVES HAVING ANTI-PROLIFERATIVE AND ANTI-MIGRATORY ACTIVITIES 审中-公开具有抗增生活性和抗活性活性的异烟碱碱性阿片碱衍生物公开(公告)号：US20100076005A1
公开(公告)日：2010-03-25
申请号：US12445405
申请日：2007-10-12
申请人： Laurent Ingrassia , Lise Wlodarczak , Stephanie Thomas , Eric Van Quaquebeke , Laurent Van den Hove , Robert Kiss , Francis Darro
发明人： Laurent Ingrassia , Lise Wlodarczak , Stephanie Thomas , Eric Van Quaquebeke , Laurent Van den Hove , Robert Kiss , Francis Darro
IPC分类号： A61K31/4355 , C07D491/02 , A61P35/04
CPC分类号： C07D491/06
摘要： Isocarbostyril alkaloid derivatives having an anti-proliferative and anti-migratory activities are disclosed. In particular, compounds of formula (I) or (II), as well as stereoisomers, tautomers, racemates, prodrugs, metabolites thereof, pharmaceutically acceptable salt and/or solvate are encompassed which are useful in the treatment and prophylaxis of cancer. Methods of preparation are also disclosed.
摘要翻译： 公开了具有抗增殖和抗迁移活性的异卡波斯特尔生物碱衍生物。 特别地，包括可用于治疗和预防癌症的式（I）或（II）的化合物以及立体异构体，互变异构体，外消旋体，前药，其代谢物，药学上可接受的盐和/或溶剂合物。 还公开了制备方法。
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4.发明授权公开(公告)号：US07741337B2
公开(公告)日：2010-06-22
申请号：US12093086
申请日：2006-11-09
IPC分类号： A61K31/473 , C07D221/18
CPC分类号： C07D405/12 , C07D221/18 , C07D401/12 , C07D417/12
摘要： The present invention is directed to azonafide derivatives obtained by reacting azonafide with aldehydes, acyl halides, thioacyl halides, monoisocyanates, isothiocyanates, sulfonyl halides, monohalogenoalkanes, monohalogenoalkenes or monohalogenoalkynes, and are useful as active ingredients of pharmaceutical compositions for the prevention and treatment of cell proliferative disorders, in particular several forms of cancer.
摘要翻译： 本发明涉及通过使azonafide与醛，酰卤，硫代酰卤，单异氰酸酯，异硫氰酸酯，磺酰卤，单卤代烷烃，单卤代烯烃或单卤代炔反应得到的azonafide衍生物，可用作预防和治疗细胞的药物组合物的活性成分 增殖性疾病，特别是几种形式的癌症。
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5.发明申请NAPTHALIMIDE DERIVATIVES, METHODS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS THEREFROM 审中-公开NAPTHALIMIDE衍生物，其生产方法及其药物组合物公开(公告)号：US20070117836A1
公开(公告)日：2007-05-24
申请号：US11556571
申请日：2006-11-03
IPC分类号： A61K31/473 , C07D221/04
CPC分类号： C07D221/14 , C07D405/12
摘要： Novel substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods for making such derivatives.
摘要翻译： 新型取代萘酰亚胺衍生物，其药学上可接受的盐和溶剂合物可用于制备用于治疗细胞增殖性疾病如癌症的药物组合物。 本发明还提供了制备这种衍生物的方法。
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6.发明申请Azonafide Derivatives, Methods for Their Production and Pharmaceutical Compositions Therefrom 失效Azonafide衍生物，其生产方法和药物组合物公开(公告)号：US20080292585A1
公开(公告)日：2008-11-27
申请号：US12093086
申请日：2006-11-09
IPC分类号： A61K38/21 , C07D221/18 , A61P35/00 , A61K31/473
CPC分类号： C07D405/12 , C07D221/18 , C07D401/12 , C07D417/12
摘要： Azonafide derivatives are obtained by reacting azonafide with aldehydes, acyl halides, thioacyl halides, monoisocyanates, isothiocyanates, sulfonyl halides, monohalogenoalkanes, monohalogenoalkenes or monohalogenoalkynes, and are useful as active ingredients of pharmaceutical compositions for the prevention and treatment of cell proliferative disorders, in particular several forms of Cancer.
摘要翻译： 唑酮衍生物是通过使唑酮与醛，酰基卤，硫代酰卤，单异氰酸酯，异硫氰酸酯，磺酰卤，单卤代烷烃，单卤代烯烃或单卤代炔反应而得到的，并且可用作预防和治疗细胞增殖性疾病的药物组合物的活性成分 几种形式的癌症。
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7.发明申请TARGETING OF ALPHA-1 OR ALPHA-3 SUBUNIT OF NA+, K+-ATPASE IN THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开NA +，K + -ATPASE在治疗增殖性疾病中的ALPHA-1或ALPHA-3亚型的靶向公开(公告)号：US20100068198A1
公开(公告)日：2010-03-18
申请号：US12513663
申请日：2006-11-09
申请人： Tatjana Mijatovic , Eric Van Quaquebeke , Nancy Denève , Laurent Van den Hove , Francis Darro , Robert Kiss
发明人： Tatjana Mijatovic , Eric Van Quaquebeke , Nancy Denève , Laurent Van den Hove , Francis Darro , Robert Kiss
IPC分类号： A61K39/395 , C07H21/00 , C07K16/18 , A61K31/7088 , A61P35/00
CPC分类号： C12N15/1137 , C12N2310/14 , C12Y306/03009
摘要： Targeting of select subunits of the Na+,K+-ATPase is described, and especially the alpha-1 subunit and/or the alpha-3 subunit. Antisense agents, agents capable of causing RNA interference that can reduce the expression of Na+,K+-ATPase, and antibodies and antibody fragments and derivatives specific for Na+,K+-ATPase are useful as reagents and pharmaceutical formulations for the treatment of proliferative diseases, such as tumours and cancers. Methods and kits are also described.
摘要翻译： 描述了Na +，K + -ATP酶的选择亚基的靶向，特别是α-1亚基和/或α-3亚基。 反义剂，能够引起可以降低Na +，K + -ATP酶以及针对Na +，K + -ATP酶特异性的抗体和抗体片段和衍生物的抗体和抗体的RNA干扰的试剂可用作治疗增殖性疾病的试剂和药物制剂，例如 作为肿瘤和癌症。 还描述了方法和试剂盒。
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8.发明申请公开(公告)号：US20090221628A1
公开(公告)日：2009-09-03
申请号：US12313186
申请日：2008-11-17
申请人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
发明人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van Den Hove , Francis Darro , Robert Kiss
IPC分类号： A61K31/435 , A61P35/00
CPC分类号： A61K31/435 , A61K45/06 , A61K2300/00
摘要： Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.
摘要翻译： 新的脲基取代的萘二甲酰亚胺衍生物，其药学上可接受的盐和溶剂合物可用于制备用于治疗细胞增殖性疾病如癌症的药物组合物。 本发明还提供了单独使用本文所述的化合物和抗肿瘤剂组合治疗特定类型的癌症例如前列腺，食管，胶质母细胞瘤，胶质瘤，NSCLC，头颈部和乳腺的方法。
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9.发明申请5-Urea Substituted Naphthalimide Derivatives, Methods of Production and Pharmaceutical Compositions for Treating Cancer 审中-公开5-尿素取代萘酰亚胺衍生物，生产方法和药物组合物治疗癌症公开(公告)号：US20090118321A1
公开(公告)日：2009-05-07
申请号：US12227090
申请日：2007-05-07
申请人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van den Hove , Francis Darro , Robert Kiss
发明人： Eric Van Quaquebeke , Gentiane Simon , Mohamed El Yazidi , Jerome Tuti , Laurent Van den Hove , Francis Darro , Robert Kiss
IPC分类号： A61K31/473 , C07D221/06 , A61P35/00
CPC分类号： C07D221/14
摘要： Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods for making such derivatives through hydrolysis of known compounds.
摘要翻译： 新的脲基取代的萘二甲酰亚胺衍生物，其药学上可接受的盐和溶剂合物可用于制备用于治疗细胞增殖性疾病如癌症的药物组合物。 本发明还提供了通过已知化合物的水解制备此类衍生物的方法。
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公开(公告)号：US20070123473A1
公开(公告)日：2007-05-31
申请号：US10582121
申请日：2004-12-17
申请人： Jean-Claude Braekman , Laurent Ingrassia , Prosper Nshimyumukiza , Eric Van Quaquebeke , Janique Dewelle , Laurent Van Den Hove , Robert Kiss , Francis Darro
发明人： Jean-Claude Braekman , Laurent Ingrassia , Prosper Nshimyumukiza , Eric Van Quaquebeke , Janique Dewelle , Laurent Van Den Hove , Robert Kiss , Francis Darro
IPC分类号： A61K31/704 , A61K31/58 , C07J43/00
CPC分类号： C07J43/00
摘要： Glycosylated steroid compounds having anti-migratory activity and methods for their preparation are disclosed. Pharmaceutical compositions having an effective amount of the glycosylated steroid compounds are also disclosed. The glycosylated steroid compounds may be used as a medicament. Preparation of medicaments containing the glycosylated steroid compounds for treatment of diseases associated with cell migration, in particular, cancer, are disclosed. The glycosylated steroid compounds or pharmaceutical compositions containing the glycosylated steroid compounds may be used in the treatment of diseases associated with cell migration, in particular for the treatment of cancer.
摘要翻译： 公开了具有抗迁移活性的糖基化类固醇化合物及其制备方法。 还公开了具有有效量的糖基化类固醇化合物的药物组合物。 糖基化类固醇化合物可以用作药物。 公开了含有用于治疗与细胞迁移相关的疾病，特别是癌症的糖基化类固醇化合物的药物的制备。 含有糖基化类固醇化合物的糖基化类固醇化合物或药物组合物可用于治疗与细胞迁移有关的疾病，特别是用于治疗癌症。
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