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PHARMACEUTICAL PREPARATIONS FOR INCREASING BRAIN GLUCOSE UTILIZATION

机译:增强脑葡萄糖利用率的药物制剂

摘要

Brain glucose utilization can be increased by administering an agent that improves central nervous system insulin sensivity. By improving the central nervous system insulin sensivity and increasing brain glucose utilization, age-related memory loss and dementia can be prevented and/or reduced. The improvement in brain glucose utilization is independent of treatment for Type II diabetes. Among the central nervous system insulin sensitizers that can be administered to increase brain glucose utilization are thiazolidinediones, including troglitazone, rosiglotazone and pioglitazone. Other useful compounds include oxyzolidinediones, including JPP501, and non-chiral acyclic agents, including GL 262370, and substituted 4-hydroxy-phenylalcanoic acid derivatives which are PPAR gamma receptor activators. All of these agents act on the nuclear receptor PPAR gamma. In a preferred embodiment, the agents are administered in the form of prodrugs which are designed to cross the blood brain barrier.
机译:可以通过服用改善中枢神经系统胰岛素敏感性的药物来提高脑部葡萄糖的利用率。通过改善中枢神经系统的胰岛素敏感性和增加脑葡萄糖利用,可以预防和/或减少与年龄有关的记忆丧失和痴呆。脑葡萄糖利用的改善与II型糖尿病的治疗无关。可以给药以增加脑葡萄糖利用的中枢神经系统胰岛素敏化剂是噻唑烷二酮,包括曲格列酮,罗格列酮和吡格列酮。其他有用的化合物包括:包括JPP501的羟唑烷二酮和包括GL 262370的非手性无环试剂,以及作为PPARγ受体活化剂的取代的4-羟基-苯基烷酸衍生物。所有这些试剂都作用于核受体PPARγ。在一个优选的实施方案中,所述试剂以被设计为穿过血脑屏障的前药形式给药。

著录项

  • 公开/公告号IL143768A

    专利类型

  • 公开/公告日2008-04-13

    原文格式PDF

  • 申请/专利权人 MINDSET BIOPHARMACEUTICALS (USA) INC.;

    申请/专利号IL20010143768

  • 发明设计人

    申请日2001-06-14

  • 分类号C07D263/44;A61K9/50;A61K31/00;A61K31/192;A61K31/205;A61K31/221;A61K31/421;A61K31/427;A61K45/00;A61K45/06;A61K47/36;A61K47/42;A61K47/48;C07D417/06;C07D417/12;F42C15/26;

  • 国家 IL

  • 入库时间 2022-08-21 20:08:04

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