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    Anthracycline Derivatives For Treating Tumor Diseases
    1.
    发明申请
    Anthracycline Derivatives For Treating Tumor Diseases 审中-公开
    蒽环类衍生物治疗肿瘤疾病

    公开(公告)号：US20150252069A1

    公开(公告)日：2015-09-10

    申请号：US14435907

    申请日：2013-10-15

    申请人： Produkem Molekulares Design GmbH

    发明人： Christian R. Noe ,  Michael Sonntagbauer ,  Sébastien Queva ,  Ernst Urban

    IPC分类号： C07H15/244 ,  C07D317/34 ,  C07C45/59 ,  C07D317/26 ,  C07D307/20 ,  C07D317/32 ,  C07F7/18

    CPC分类号： C07H15/244 ,  C07C15/28 ,  C07C45/59 ,  C07C2603/24 ,  C07C2603/44 ,  C07D307/20 ,  C07D317/26 ,  C07D317/32 ,  C07D317/34 ,  C07F7/1804 ,  C07H15/08 ,  C07H15/252

    摘要： The invention relates to compounds of the general formula (I) in which R1 is a hydrogen atom, a hydroxy or methoxy group, a halogen atom, or an NO2 group; R2 is a hydrogen atom, a hydroxy or methoxy group, or an acyl or aroyl group; R3 is hydrogen, trifluoroacetyl (C(═O)CF3), or p-nitrobenzoyl (C(═O)PhNO2), and in each case the wavy line represents both possible configurations of —OR3 relative to the skeleton; Y is [C(═O)], [C(═N)—OH], [CH—OH], or [CH—NR5R6] in the two possible stereoisomer arrangements, wherein R5 and R6 either each represent a hydrogen atom or a hydrogen atom and a trifluoroacetyl group (TFA); X=O, S, or NR, in which R=hydrogen or a C1 to C4 alkyl group; and R4 is an unbranched or branched alkyl or heteroalkyl chain with a chain length of 1 to 19 elements, maximally 6 heteroatoms (O, N, S) being separated from one another in any combination by at least two carbon atoms. The invention further relates to, among others, methods for producing the compounds according to formula (I), to pharmaceutical compositions, to a pharmaceutical kit, and to the use thereof as a medicament for treating proliferative diseases or conditions, preferably cancer.

    摘要翻译： 本发明涉及其中R 1为氢原子，羟基或甲氧基，卤素原子或NO 2基团的通式（I）的化合物; R2是氢原子，羟基或甲氧基，或酰基或芳酰基; R3是氢，三氟乙酰基（C（= O）CF 3）或对硝基苯甲酰基（C（= O）PhNO 2），并且在每种情况下，波浪线表示-OR3相对于骨架的可能构型; 两种可能的立体异构体排列中Y是[C（= O）]，[C（= N）-OH]，[CH-OH]或[CH-NR5R6]，其中R5和R6各自表示氢原子或 氢原子和三氟乙酰基（TFA）; X = O，S或NR，其中R =氢或C1至C4烷基; 并且R4是链长为1至19个元素的非支链或支链烷基或杂烷基链，最多6个杂原子（O，N，S）以任何组合彼此分开至少两个碳原子。 本发明还涉及用于制备式（I）化合物，药物组合物，药物试剂盒及其用作治疗增殖性疾病或病症（优选癌症）的药物的用途的方法。