18 ,21-Didesoxymacbecin Derivatives for the Treatment of Cancer
    3.
    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

    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。

    NOVEL COMPOUNDS
    6.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    新型化合物

    公开(公告)号:US20090312316A1

    公开(公告)日:2009-12-17

    申请号:US12296482

    申请日:2007-05-17

    CPC分类号: C07D405/12

    摘要: The present invention relates to derivatives of borrelidin that are useful in medicine, e.g. in the treatment of cancer or B-cell malignancies, or other diseases in which angiogenesis contributes to the pathology including ophthalmic disorders such as diabetic retinopathy as well as age related macular degeneration (AMD), corneal neovascularisation and retinopathy or prematurity. 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 and other diseases in which angiogenesis is implicated in the pathogenic process.

    摘要翻译: 本发明涉及可用于医药的例如硼砂灵兰衍生物。 在治疗癌症或B细胞恶性肿瘤或其它血管发生有助于包括眼部疾病如糖尿病性视网膜病变以及年龄相关性黄斑变性(AMD),角膜新生血管形成和视网膜病变或早产的病理学的疾病中。 本发明还提供了这些化合物的制备方法及其在药物中的用途,特别是在治疗和/或预防癌细胞或B细胞恶性肿瘤以及血管生成涉及致病过程的其它疾病中的用途。

    C21-Deoxy Ansamycin Derivatives as Antitumor Agents
    7.
    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

    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。

    PRODUCTION OF POLYKETIDES AND OTHER NATURAL PRODUCTS
    8.
    发明申请
    PRODUCTION OF POLYKETIDES AND OTHER NATURAL PRODUCTS 有权
    生产多晶硅及其他天然产品

    公开(公告)号:US20080021211A1

    公开(公告)日:2008-01-24

    申请号:US11778264

    申请日:2007-07-16

    IPC分类号: C07D273/00

    摘要: The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).

    摘要翻译: 本发明涉及聚酮化合物和其它天然产物的生产以及化合物和单个新化合物的文库。 一个重要的领域是产生这些化合物的新型FKBP-配体类似物和宿主细胞的分离和潜在的使用。 本发明特别涉及有效转化产生FKBP类似物的菌株和重组细胞的方法,其中克隆的基因或基因盒被表达以产生新的化合物,例如聚酮化合物(特别是雷帕霉素)FKBP-配体类似物, 制备和其中使用的手段(例如核酸,载体,基因盒和遗传修饰的菌株)。

    Production of polyketides and other natural products
    9.
    发明授权
    Production of polyketides and other natural products 有权
    生产聚酮化合物等天然产物

    公开(公告)号:US07300942B2

    公开(公告)日:2007-11-27

    申请号:US10497135

    申请日:2003-07-16

    IPC分类号: C07D498/18 A61P31/00

    摘要: The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their,preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).

    摘要翻译: 本发明涉及聚酮化合物和其它天然产物的生产以及化合物和单个新化合物的文库。 一个重要的领域是产生这些化合物的新型FKBP-配体类似物和宿主细胞的分离和潜在的使用。 本发明特别涉及有效转化产生FKBP类似物的菌株和重组细胞的方法,其中克隆的基因或基因盒被表达以产生新的化合物,例如聚酮化合物(特别是雷帕霉素)FKBP-配体类似物, ,制备和其中使用的手段(例如核酸,载体,基因盒和遗传修饰的菌株)。