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公开(公告)号：US20110237614A1
公开(公告)日：2011-09-29
申请号：US13063919
申请日：2009-09-16
IPC分类号： A61K31/485 , A61P25/36 , A61P25/04 , C07D489/02
CPC分类号： A61K31/485 , A61K47/60
摘要： The invention provides opioid agonists covalently bound to a water-soluble oligomer having reduced potential for substance abuse and uses thereof. The compounds of the invention possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
摘要翻译： 本发明提供了与具有降低的药物滥用潜力的水溶性低聚物共价结合的阿片样物质激动剂及其应用。 本发明的化合物相对于单独的阿片样物质激动剂具有改变的药代动力学特征，但不具有物理篡改的风险，其允许与某些替代递送制剂相关的阿片样物质激动剂的恢复和滥用。
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2.发明申请公开(公告)号：US20130023553A1
公开(公告)日：2013-01-24
申请号：US13521556
申请日：2011-01-12
IPC分类号： C07D489/02 , A61P25/36 , A61P25/00 , A61K31/485
CPC分类号： A61K31/075 , A61K31/485
摘要： Provided are methods for reducing the addiction potential and/or reducing one or more CNS-side effects related to the administration of an opioid analgesic drug by administering the opioid analgesic drug in the form of an oligomeric polyethylene glycol conjugate compound. The compounds provided demonstrate notably reduced potential for substance abuse, and possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
摘要翻译： 提供了通过以寡聚聚乙二醇缀合化合物的形式施用阿片样物质止痛药，降低成瘾潜能和/或降低与阿片类止痛药的给药有关的一种或多种CNS副作用的方法。 所提供的化合物显示出显着降低药物滥用的潜力，并且相对于单独的阿片样物质激动剂具有改变的药代动力学特征，但不具有物理篡改的风险，其允许与某些替代递送制剂相关的阿片样物质激动剂的恢复和滥用 。
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