公开(公告)号：US20130053347A1

公开(公告)日：2013-02-28

申请号：US13695609

申请日：2010-05-03

申请人： Veronique Mathieu ,  Gwendoline Van Goietsenoven ,  Jacques Dubois ,  Florence Lefranc-Kiss ,  Laurent Ingrassia ,  Robert Kiss

发明人： Veronique Mathieu ,  Gwendoline Van Goietsenoven ,  Jacques Dubois ,  Florence Lefranc-Kiss ,  Laurent Ingrassia ,  Robert Kiss

IPC分类号： C07F9/6574 ,  G01N33/566 ,  A61P35/00 ,  A61K31/675

CPC分类号： C07D491/056

摘要： The present invention relates to the biology and mechanism of action of the naturally occurring compound Narciclasine, especially as an anti-cancer agent for brain tumors. The invention provides new insights on the target molecule of Amaryllidaceae isocarbostyril derivatives as for example Narciclasine and provides new prodrugs of these Amaryllidceae isocabostyril constituents for treating cancer, specifically cancers or tumors located in the brain.

摘要翻译： 本发明涉及天然存在的化合物Narciclasine的生物学和作用机理，特别是作为脑肿瘤的抗癌剂。 本发明提供了关于芳香樟科异卡泊霉素衍生物如Narciclasine的靶分子的新见解，并提供了这些用于治疗癌症，特别是位于脑中的癌症或肿瘤的这些芳樟脑异卡培司他尔的新前药。

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。

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。

公开(公告)号：US20060149045A1

公开(公告)日：2006-07-06

申请号：US10538993

申请日：2003-12-18

申请人： Jean-Claude Braekman ,  Eric Quaquebeke ,  Laurent Ingrassia ,  Janique Dewelle ,  Robert Kiss ,  Francis Darro

发明人： Jean-Claude Braekman ,  Eric Quaquebeke ,  Laurent Ingrassia ,  Janique Dewelle ,  Robert Kiss ,  Francis Darro

IPC分类号： C07J41/00 ,  C07J17/00 ,  C07J43/00

CPC分类号： C07J17/00 ,  A61K31/57 ,  A61K31/575 ,  C07J7/00 ,  C07J9/00 ,  C07J41/00 ,  C07J43/00

摘要： The present invention relates to novel steroid compounds of Formula (IB) having anti-tumor activity. The present invention also relates to a method for the preparation of said steroid compounds. The invention further relates to a pharmaceutical composition comprising an effective amount of said steroid compounds. Furthermore, the present invention concerns the use of said steroid compounds as a medicament and in the preparation of a medicament for the treatment of cancer. The present invention also relates to the use of a steroid compound or a pharmaceutical composition comprising said steroid compound according to the invention in the treatment of cancer.

摘要翻译： 本发明涉及具有抗肿瘤活性的式（IB）的新型类固醇化合物。 本发明还涉及一种制备所述类固醇化合物的方法。 本发明还涉及包含有效量的所述类固醇化合物的药物组合物。 此外，本发明涉及所述类固醇化合物作为药物和制备用于治疗癌症的药物的用途。 本发明还涉及包含根据本发明的所述类固醇化合物的类固醇化合物或药物组合物在治疗癌症中的用途。