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DEOXY- CYTIDINE OR URIDINE DERIVATIVES FOR USE IN CANCER THERAPIES

机译:用于癌症疗法的脱氧 - 胞苷或尿苷衍生物

摘要

Formula (I) Compounds of formula (I), and stereoisomers, solvates, tautomers and pharmaceutically acceptable salts of formula (I), wherein W1, W2, X, Y, Z are as defined herein, for use in therapy. Also claimed is the use of compounds of formula (I) for use in the treatment of cancer, e.g. brain cancer, preferably glioma. Most preferably, R1 is a hydroxy group or a triphosphate. Most preferably, R2 is hydroxyl. Most preferably, R3 is H. Most preferably, X is either an aldehyde or CH2OH. Preferably, the compound of formula (I) is 5-hydroxymethyl-2’deoxycytidine or 5-formyl-2’deoxycytidine. The tumour to be treated may overexpress CDA, or may express CDA at a level of less than, or equal to, 140 TPM (transcripts per million). Compounds of formula (I) may be used against cancers resistant to gemcitabine, cytarabine, temozolomide, of 5-fluorouracil. Compounds of formula (I) may be used in conjunction with other anticancer agents (e.g. 5-FU). Also disclosed is a method of treating or preventing cancer.
机译:式(I)式(I)化合物,和立体异构体,溶剂化物,互变异构体和式(I)的药学上可接受的盐,其中W1,W2,X,Y,Z如本文所定义,用于治疗。还要求保护用于式(I)化合物用于治疗癌症,例如癌症。脑癌,优选胶质瘤。最优选地,R1是羟基或三磷酸。最优选地,R 2是羟基。最优选地,R 3是H.最优选地,X是醛或CH 2 OH。优选地,式(I)化合物是5-羟甲基-2'Deoxycyidine或5-甲酰基-2'deoxycyidinine。待治疗的肿瘤可能过表达CDA,或者可以以少于或等于140ppm(每百万转录物)的水平表达CDA。式(I)化合物可以针对抗噬菌胺,巨蛋白,替代5-氟尿嘧啶的癌症的癌症。式(I)化合物可以与其他抗癌剂(例如5-FU)结合使用。还公开了一种治疗或预​​防癌症的方法。

著录项

  • 公开/公告号EP3917538A1

    专利类型

  • 公开/公告日2021-12-08

    原文格式PDF

  • 申请/专利权人 HEMISPHERIAN AS;

    申请/专利号EP20200703447

  • 发明设计人 ROBERTSON ADAM BRIAN;PRIKRYLOVA TEREZIA;

    申请日2020-02-03

  • 分类号A61K31/7068;A61K31/7072;A61K45/06;A61P35;

  • 国家 EP

  • 入库时间 2022-08-24 22:41:39

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