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    • 2. 发明申请
    • C21-DE0XY ANSAMYCIN DERIVATIVES AS ANTITUMOR AGENTS
    • C21-DE0XY ANSAMYCIN衍生物作为抗菌剂
    • WO2008104812A3
    • 2008-10-30
    • PCT/GB2008050150
    • 2008-03-03
    • BIOTICA TECH LTDMOSS STEVENMARTIN CHRISTINEZHANG MING
    • MOSS STEVENMARTIN CHRISTINEZHANG MING
    • C07D225/06A61K31/395A61P35/00
    • C07D225/06
    • 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.
    • 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。
    • 4. 发明申请
    • 17-OXYMACBECIN DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND/OR B-CELL MALIGNANCIES
    • 17-OXYMACBECIN衍生物及其在治疗癌症和/或B细胞恶性肿瘤中的应用
    • WO2007128827A8
    • 2008-01-03
    • PCT/EP2007054473
    • 2007-05-09
    • BIOTICA TECH LTDMARTIN CHRISTINEZHANG MINGGAISSER SABINECOATES NIGEL
    • MARTIN CHRISTINEZHANG MINGGAISSER SABINECOATES NIGEL
    • C07D225/06A61K31/395
    • C07D225/06
    • The present invention relates to 17-oxymacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt thereof, wherein: R 1 represents H, OH or OCH 3 ; R 2 represents H or CH 3 R 3 represents H or CONH 2 R 4 and R 5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R 6 represents H or OH; and R 7 represents H or CH 3 . 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.
    • 本发明涉及根据下式(IA)或(IB)的17-氧基锍类似物或其药学上可接受的盐,其中:R 1表示H,OH或OCH 3 ; R 2表示H或CH 3 R 3 R 3表示H或CONH 2 R 4 S / >和R 5都表示H或一起表示键(即C4至C5是双键); R 6表示H或OH; 且R 7表示H或CH 3。 这是有用的,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。