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公开(公告)号：US20150057219A1
公开(公告)日：2015-02-26
申请号：US14468672
申请日：2014-08-26
Applicant: Yeda Research and Development Co., Ltd.
Inventor： Yoram SHECHTER , Matityahu Fridkin , Haim Tsubery
CPC classification number: A61K47/60 , A61K31/7036 , A61K38/1709 , A61K38/212 , A61K38/22 , A61K38/2242 , A61K38/2278 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/54 , A61K47/545 , C07D207/404 , C07D207/416 , C07D207/452 , C07D403/12
Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.
Abstract translation: 可逆的聚乙二醇化药物通过衍生自选自氨基，羟基，巯基，磷酸酯和/或羧基的药物的游离官能团与对温和碱性条件敏感的基团如9-芴基甲氧基羰基（Fmoc）或2-磺基-9-芴基甲氧基羰基 （FMS），连接有PEG部分的基团。 在这些聚乙二醇化药物中，PEG部分和药物残留物不直接相互连接，而是两个残基都连接到对碱基高度敏感并在生理条件下可去除的支架Fmoc或FMS结构的不同位置。 药物优选是含有氨基的药物，最优选低分子量或中等分子量的肽和蛋白质。 提供了类似的分子，其中蛋白质载体或另一种聚合物载体取代了PEG部分。
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公开(公告)号：US20160324975A1
公开(公告)日：2016-11-10
申请号：US15216870
申请日：2016-07-22
Applicant: Yeda Research and Development Co., Ltd.
Inventor： Yoram SHECHTER , Matityahu FRIDKIN , Haim TSUBERY
CPC classification number: A61K47/60 , A61K31/7036 , A61K38/1709 , A61K38/212 , A61K38/22 , A61K38/2242 , A61K38/2278 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/54 , A61K47/545 , C07D207/404 , C07D207/416 , C07D207/452 , C07D403/12
Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.
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公开(公告)号：US20160000927A1
公开(公告)日：2016-01-07
申请号：US14795974
申请日：2015-07-10
Applicant: Yeda Research and Development Co., Ltd.
Inventor： Yoram SHECHTER , Matityahu FRIDKIN , Haim TSUBERY
CPC classification number: A61K47/60 , A61K31/7036 , A61K38/1709 , A61K38/212 , A61K38/22 , A61K38/2242 , A61K38/2278 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/54 , A61K47/545 , C07D207/404 , C07D207/416 , C07D207/452 , C07D403/12
Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.
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