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公开(公告)号：EP1694363A2
公开(公告)日：2006-08-30
申请号：EP04814802.7
申请日：2004-12-16
CPC分类号： C08G65/337 , A61K47/60 , C08G65/332 , C08G65/33317 , C08G65/33396 , C08L2203/02
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
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公开(公告)号：EP2010539A2
公开(公告)日：2009-01-07
申请号：EP07755867.4
申请日：2007-04-19
发明人： CHENG, Lin , BENTLEY, Michael D.
IPC分类号： C07D489/02
CPC分类号： C07D489/02 , Y02P20/55
摘要： A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.
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公开(公告)号：EP1436012A2
公开(公告)日：2004-07-14
申请号：EP02795531.9
申请日：2002-10-18
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： The invention provides polymer conjugates of opioid antagonists comprising at least one polymer backbone, such as poly(ethylene glycol), covalently attached to a residue of an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treatment of one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.
摘要翻译： 本发明提供了阿片样物质拮抗剂的聚合物缀合物，其包含共价连接到阿片样物质拮抗剂的残基的至少一种聚合物主链，例如聚（乙二醇）。 聚合物和阿片样物质拮抗剂之间的连接优选是水解稳定的。 本发明还包括通过施用本发明的聚合物缀合物来治疗与使用阿片类止痛剂如便秘，恶心或瘙痒相关的一种或多种副作用的方法。
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