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    • 8. 发明申请
    • NEW USES OF DINUCLEOTIDE POLYPHOSPHATE DERIVATIVES
    • 新型磷酸二氢钙衍生物的应用
    • WO2006082397A1
    • 2006-08-10
    • PCT/GB2006/000343
    • 2006-02-01
    • IC VEC LIMITEDMILLER, Andrew, DavidWRIGHT, MichaelTANNER, Julian, AlexanderLOZOVAYA, Natalya
    • MILLER, Andrew, DavidWRIGHT, MichaelTANNER, Julian, AlexanderLOZOVAYA, Natalya
    • A61K31/7084C07H21/00C07H21/02C07H21/04
    • A61K31/7084C07H21/00C07H21/02C07H21/04
    • The present invention provides the use of analogues and derivatives of dinucleoside polyphosphates with formula (I) or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in one or more of: the treatment of ischemia, inducing ischemic tolerance, modulating cerebral ischemia, to delay the onset of a hypoxic depolarisation stage when ischemic events are initiated; as a neurological protection agent; as a tissue protection agent; the treatment of pain; and the treatment of inflammation, wherein X, is selected from wherein X 1 and X 2 are independently selected from H, Cl, Br and F; each Y is independently selected from S and O; each Z is independently selected from -CX 3 X 4 -,-NH-,-O- ; wherein X 3 and X 4 are selected from H, CI, Br and F; B1 and B2 are independently selected from adenine, guanine, xanthine, thymine, uracil, cytosine and inosine; S 1 and S 2 are independently selected from ribose, open chain ribose, 2'-deoxyribose, 3'deoxyribose and arabinofuranoside. V is selected from 0, 1 , 2, 3, 4 and 5; W is selected from 0, 1 , 2, 3, 4 and 5; and V plus W is an integer from 2 to 6.
    • 本发明提供了式(I)的二核苷多磷酸类似物和衍生物或其药学上可接受的盐在制备用于以下一种或多种中的一种或多种药物中的用途:治疗缺血,诱导缺血耐受,调节脑 缺血,当缺血事件发生时延迟缺氧去极化阶段的发作; 作为神经保护剂; 作为组织保护剂; 治疗疼痛; 和炎症的治疗,其中X选自其中X 1和X 2独立地选自H,Cl,Br和F; 每个Y独立地选自S和O; 每个Z独立地选自-CX 3 - , - NH - , - O - ; - 其中X 3和X 4选自H,Cl,Br和F; B1和B2独立地选自腺嘌呤,鸟嘌呤,黄嘌呤,胸腺嘧啶,尿嘧啶,胞嘧啶和肌苷; S 1和S 2独立地选自核糖,开链核糖,2'-脱氧核糖,3'-脱氧核糖和阿拉伯呋喃糖苷。 V选自0,1,2,3,4和5; W选自0,1,2,3,4和5; V加W是2〜6的整数。