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Phthalazinone derivatives for ibhibiting the activity of the enzyme poly (ADP-ribose)polymerase-1 (PARP-1)

机译:抑制塑料多(ADP-核糖)聚合酶-1(PARP-1)酶活性的酞嗪酮衍生物

摘要

A phthalazinone derivative compound of the formula (I) is disclosed, wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; Rc is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocydyl and C5-20 aryl, which groups are optionally substituted. These compounds are useful in the preparation of a medicament for inhibiting the activity of PARP for the treatment of : vascular disease; septic shock; ischaemic injury; neurotoxicity; haemorraghic shock; viral infection; or for use as an adjunct in cancer therapy or for potentiating tumour cells for treatment with ionizing radiation or chemotherapeutic agents.
机译:公开了式(I)的酞嗪酮衍生物化合物,其中:A和B一起代表任选取代的稠合芳环; X和Y分别选自CH和CH,CF和CH,CH和CF以及N和CH; R c选自H,C 1-4烷基; R 1选自C 1-7烷基,C 3-20杂环基和C 5-20芳基,这些基团是任选取代的。这些化合物可用于制备抑制PARP活性的药物,该药物可用于治疗以下疾病:血管疾病;败血性休克;缺血性损伤神经毒性血流性休克;病毒感染;或用作癌症治疗的辅助剂或增强肿瘤细胞的电离辐射或化学治疗剂的治疗能力。

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