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16 条记录 (耗时 0.035 秒)

    15-O-Desmethylmacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies
    3.
    发明申请
    15-O-Desmethylmacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies 审中-公开
    15-O-去甲基衍生物及其在治疗癌症或B细胞恶性肿瘤中的应用

    公开(公告)号：US20090209507A1

    公开(公告)日：2009-08-20

    申请号：US12294253

    申请日：2007-03-30

    申请人： Sabine Gaisser ,  Christine Martin ,  Ming Zhang ,  Barrie Wilkinson ,  Nigel Coates ,  Mohammed Nur-E-Alam ,  William Vousden

    发明人： Sabine Gaisser ,  Christine Martin ,  Ming Zhang ,  Barrie Wilkinson ,  Nigel Coates ,  Mohammed Nur-E-Alam ,  William Vousden

    IPC分类号： A61K31/395 ,  C07D225/06 ,  A61P35/00 ,  C12P17/10 ,  C12N5/10

    CPC分类号： C07D225/06

    摘要： The present invention relates to 15-O-desmethylmacbecin analogues according to the formula (IA) or (IB) herein, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R3 represents H or CONH2 that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.

    摘要翻译： 本发明涉及根据本文的式（IA）或（IB）的15-O-去甲基蒿酸类似物或其药学上可接受的盐：其中：R 1和R 2都表示H或一起表示一个键（即C 4至 C5是双键）; 并且R 3表示可用的H或CONH 2，例如。 在治疗癌症，B细胞恶性肿瘤，疟疾，真菌感染，中枢神经系统疾病和神经变性疾病，依赖于血管生成的疾病，自身免疫疾病和/或作为癌症的预防性预处理。 本发明还提供了这些化合物的制备方法及其在医药中的用途，特别是用于治疗和/或预防癌症或B细胞恶性肿瘤的方法。

    18 ,21-Didesoxymacbecin Derivatives for the Treatment of Cancer
    6.
    发明申请
    18 ,21-Didesoxymacbecin Derivatives for the Treatment of Cancer 审中-公开
    18，21-Didesoxymacbecin衍生物治疗癌症

    公开(公告)号：US20090253667A1

    公开(公告)日：2009-10-08

    申请号：US12296542

    申请日：2007-05-09

    申请人： Christine Martin ,  Ming Zhang ,  Nigel Coates ,  William Vousden ,  Steven Moss ,  Sabine Gaisser

    发明人： Christine Martin ,  Ming Zhang ,  Nigel Coates ,  William Vousden ,  Steven Moss ,  Sabine Gaisser

    IPC分类号： A61K31/395 ,  C12P17/10 ,  C12N1/00 ,  C07D225/06

    CPC分类号： C07D225/06

    摘要： The present invention relates to 18,21-didesoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pre-treatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.

    摘要翻译： 本发明涉及有用的18,21-二氧杂氧化锍类似物。 在治疗癌症，B细胞恶性肿瘤，疟疾，真菌感染，中枢神经系统疾病和神经变性疾病，依赖于血管生成的疾病，自身免疫性疾病和/或作为癌症的预防性预处理。 本发明还提供了这些化合物的制备方法及其在医药中的用途，特别是用于治疗和/或预防癌症或B细胞恶性肿瘤的方法。

    C21-Deoxy Ansamycin Derivatives as Antitumor Agents
    10.
    发明申请
    C21-Deoxy Ansamycin Derivatives as Antitumor Agents 审中-公开
    C21-Deoxy Ansamycin衍生物作为抗肿瘤剂

    公开(公告)号：US20100210597A1

    公开(公告)日：2010-08-19

    申请号：US12526605

    申请日：2008-03-03

    申请人： Steven Moss ,  Christine Martin ,  Ming Zhang

    发明人： Steven Moss ,  Christine Martin ,  Ming Zhang

    IPC分类号： A61K31/675 ,  C07D225/06 ,  A61K31/33 ,  A61P35/00 ,  A61P31/00 ,  A61P25/00 ,  A61P37/06 ,  A61P9/00

    CPC分类号： C07D225/06

    摘要： According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.

    摘要翻译： 根据本发明，提供了一种C21-脱氧安莎霉素或其盐的衍生物，其含有在位置3具有氨基羧基取代基的1-羟基苯基部分，其中位置5和位置3上的氨基羧基取代基通过脂族链连接 变化的长度，其特征在于苯环的1-羟基位置被氨基亚烷基氨基羰基衍生，该亚烷基（其可以任选被烷基取代）具有2或3个碳原子的链长，磷酸或 磷酸酯（例如烷基酯）或其盐，并且该衍生基增加了母体分子的水溶性和/或生物利用度。 这样的化合物可用于治疗，例如治疗癌症和B细胞恶性肿瘤。