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    Tumor selective and biodegradable polyphosphazene-platinum(II) conjugate antitumor agent, and preparation method thereof
    2.
    发明授权
    Tumor selective and biodegradable polyphosphazene-platinum(II) conjugate antitumor agent, and preparation method thereof 失效
    肿瘤选择性和生物降解性聚磷腈 - 铂（II）缀合物抗肿瘤剂及其制备方法

    公开(公告)号：US06951953B2

    公开(公告)日：2005-10-04

    申请号：US10752042

    申请日：2004-01-07

    申请人： Youn Soo Sohn ,  Yong Joo Jun ,  Joo Ik Kim

    发明人： Youn Soo Sohn ,  Yong Joo Jun ,  Joo Ik Kim

    IPC分类号： C07F19/00 ,  A61K31/80 ,  C07F15/00 ,  A61K31/28 ,  C08L85/02

    CPC分类号： A61K31/80

    摘要： Disclosed are a new class of a polyphosphazene-platinum(II) conjugate antitumor agent having high tumor tissue selectivity due to its enhanced permeability and retention effect to tumor tissues, and a preparation method thereof: wherein x represents the number of the ethylene oxide repeating unit and is 7, 12 or 16; y is 0, 1 or 2; z represents molar content of polyethylene glycol in the range of 0.5-1.5; n represents degree of polymerization of polyphosphazene in the range of 30-100; and A-A represents a diamine.

    摘要翻译： 公开了由于其增加的对肿瘤组织的渗透性和保留作用而具有高肿瘤组织选择性的新一类聚磷腈 - 铂（II）缀合物抗肿瘤剂及其制备方法：其中x表示环氧乙烷重复单元 是7,12或16; y为0,1或2; z表示在0.5-1.5范围内的聚乙二醇的摩尔含量; n表示聚磷腈的聚合度在30-100范围内; A-A表示二胺。

    Dendritic oligopeptide-grafteded cyclotriphosphazene, a process for the preparation thereof and a drug delivery system containing the same
    3.
    发明授权
    Dendritic oligopeptide-grafteded cyclotriphosphazene, a process for the preparation thereof and a drug delivery system containing the same 有权
    树突状寡肽接枝的环三磷腈，其制备方法和含有它们的药物递送系统

    公开(公告)号：US08344173B2

    公开(公告)日：2013-01-01

    申请号：US12990089

    申请日：2009-04-28

    申请人： Youn Soo Sohn ,  Yong Joo Jun ,  Sung Mo Choi

    发明人： Youn Soo Sohn ,  Yong Joo Jun ,  Sung Mo Choi

    IPC分类号： C07C271/12 ,  C07K5/00

    CPC分类号： A61K47/24 ,  A61K9/0024 ,  C07F9/65815

    摘要： A cyclotriphosphazene represented by Formula 1 prepared by introducing a dendritic tetrapeptide and a hydrophilic polyethylene glycol into a cyclotriphosphazene ring, a method of preparing the same, and a drug carrier including the cyclotriphosphazene of Formula 1.The compound according to the present invention may form a strong molecular hydrogel in a very low concentration of 2 w/w % or less. Furthermore, the hydrogel prepared using the compound of Formula 1 exhibits biodegradability, thermosensitivity at around body temperature, biocompatibility with protein drugs, and an easy way to prepare along with a sustained release property without any burst effect in the early stage of release. Therefore, the present cyclotriphosphazene molecular hydrogel may be efficiently used as a drug carrier for a sustained release of a drug, particularly, a protein drug.

    摘要翻译： 通过将环状三磷腈环中引入树枝状四肽和亲水性聚乙二醇制备的式1所示的环三磷腈，其制备方法和包含式1的环三磷腈的药物载体。根据本发明的化合物可以形成 强分子水凝胶的浓度为2w / w％以下。 此外，使用式1化合物制备的水凝胶显示生物降解性，体温周围的热敏感性，与蛋白质药物的生物相容性，以及在释放的早期阶段，缓释性能良好而不发生突发作用的简便方法。 因此，本发明的环三磷腈分子水凝胶可以有效地用作药物载体，用于药物，特别是蛋白质药物的持续释放。

    DENDRITIC OLIGOPEPTIDE-GRAFTEDED CYCLOTRIPHOSPHAZENE, A PROCESS FOR THE PREPARATION THEREOF AND A DRUG DELIVERY SYSTEM CONTAINING THE SAME
    4.
    发明申请
    DENDRITIC OLIGOPEPTIDE-GRAFTEDED CYCLOTRIPHOSPHAZENE, A PROCESS FOR THE PREPARATION THEREOF AND A DRUG DELIVERY SYSTEM CONTAINING THE SAME 有权
    致密性低聚赖氨酸环孢菌素，其制备方法和含有其的药物递送系统

    公开(公告)号：US20110046347A1

    公开(公告)日：2011-02-24

    申请号：US12990089

    申请日：2009-04-28

    申请人： Youn Soo Sohn ,  Yong Joo Jun ,  Sung Mo Choi

    发明人： Youn Soo Sohn ,  Yong Joo Jun ,  Sung Mo Choi

    IPC分类号： C07K5/113 ,  C07K1/00

    CPC分类号： A61K47/24 ,  A61K9/0024 ,  C07F9/65815

    摘要： A cyclotriphosphazene represented by Formula 1 prepared by introducing a dendritic tetrapeptide and a hydrophilic polyethylene glycol into a cyclotriphosphazene ring, a method of preparing the same, and a drug carrier including the cyclotriphosphazene of Formula 1.The compound according to the present invention may form a strong molecular hydrogel in a very low concentration of 2 w/w % or less. Furthermore, the hydrogel prepared using the compound of Formula 1 exhibits biodegradability, thermosensitivity at around body temperature, biocompatibility with protein drugs, and an easy way to prepare along with a sustained release property without any burst effect in the early stage of release. Therefore, the present cyclotriphosphazene molecular hydrogel may be efficiently used as a drug carrier for a sustained release of a drug, particularly, a protein drug.

    摘要翻译： 通过将环状三磷腈环中引入树枝状四肽和亲水性聚乙二醇制备的式1所示的环三磷腈，其制备方法和包含式1的环三磷腈的药物载体。根据本发明的化合物可以形成 强分子水凝胶的浓度为2w / w％以下。 此外，使用式1化合物制备的水凝胶显示生物降解性，体温周围的热敏感性，与蛋白质药物的生物相容性，以及在释放的早期阶段，缓释性能良好而不发生突发作用的简便方法。 因此，本发明的环三磷腈分子水凝胶可以有效地用作药物载体，用于药物，特别是蛋白质药物的持续释放。

    Thermosensitive and biocompatible amphiphilic poly(organophosphazenes) and preparation method thereof
    5.
    发明授权
    Thermosensitive and biocompatible amphiphilic poly(organophosphazenes) and preparation method thereof 失效
    热敏和生物相容性两亲性聚（有机膦腈）及其制备方法

    公开(公告)号：US07598318B2

    公开(公告)日：2009-10-06

    申请号：US11229525

    申请日：2005-09-20

    申请人： Youn Soo Sohn ,  Ji Yeon Seong ,  Yong Joo Jun ,  Joo Ik Kim

    发明人： Youn Soo Sohn ,  Ji Yeon Seong ,  Yong Joo Jun ,  Joo Ik Kim

    IPC分类号： C07F15/00 ,  C08L85/02 ,  A61K31/28 ,  C08G79/00 ,  C08G79/02

    CPC分类号： C08G69/42

    摘要： The present invention relates to a thermosensitive and biocompatible poly(organophosphazenes) represented by Formula 1, and a preparation method thereof: wherein R is a methyl or ethyl group; R′ is selected from the group consisting of COOR, CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R″ is selected from the group consisting of CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R′″ is a group selected from the group consisting of CH2COOR, CH2CH2COOR and H, wherein R is the same as defined above; n is a number between from 30 to 100; x is a number selected from the integers of 3, 4, 7, 12 and 16; y is a number between from 0.5 to 1.5; a equals to 1; and b and c equal to 0 or 1.

    摘要翻译： 本发明涉及由式1表示的热敏和生物相容性聚（有机膦腈）及其制备方法：其中R是甲基或乙基; R'选自COOR，CH 2 COOR，CH 2 CH 2 COOR，CH 2 CH（CH 3）2，CH 2 C 6 H 5，CH（CH 3）CH 2 CH 3和CH 3; R“选自CH 2 COOR，CH 2 CH 2 COOR，CH 2 CH（CH 3）2，CH 2 C 6 H 5，CH（CH 3）CH 2 CH 3和CH 3; R“是选自CH 2 COOR，CH 2 CH 2 COOR和H的基团，其中R与上述定义相同; n是从30到100之间的数字; x是从3，4，7，12和16的整数中选出的数字; y是从0.5到1.5之间的数字; a等于1; b和c等于0或1。

    Platinum(II) complexes of N-substituted amino dicarboxylates and the preparation method thereof
    6.
    发明授权
    Platinum(II) complexes of N-substituted amino dicarboxylates and the preparation method thereof 失效
    N-取代氨基二羧酸铂（II）络合物及其制备方法

    公开(公告)号：US06867316B2

    公开(公告)日：2005-03-15

    申请号：US10752566

    申请日：2004-01-08

    申请人： Youn Soo Sohn ,  Yeong-Sang Kim ,  Rita Song

    发明人： Youn Soo Sohn ,  Yeong-Sang Kim ,  Rita Song

    IPC分类号： A61K31/28 ,  C07F15/00

    CPC分类号： C07F15/0093 ,  A61K31/28

    摘要： Disclosed are a platinum (II) complex of N-substituted amino dicarboxylate showing antitumor activity represented by the following formula (1) and a preparation method thereof: wherein n is 1 or 2; A—A is a diamine selected from the group consisting of trans-(±)-1,2-diaminocyclohexane, ethylenediamine and 2,2-dimethyl-1,3-propanediamine; and R1 is hydrogen and R2 is RCO or RSO2, wherein R is an alkyl selected from the group consisting of methyl, ethyl, n-propyl, n-butyl and t-butyl or an aryl selected from the group consisting of phenyl and substituted phenyl group, or R1R2 is phthaloyl.

    摘要翻译： 公开了显示由下式（1）表示的抗肿瘤活性的N-取代氨基二羧酸的铂（II）络合物及其制备方法：其中n为1或2; A-A是选自反式（±） - 1,2-二氨基环己烷，乙二胺和2,2-二甲基-1,3-丙二胺的二胺; 并且R 1为氢，R 2为RCO或RSO 2，其中R为选自甲基，乙基，正丙基，正丁基和叔丁基的烷基或选自苯基和取代苯基 基团，或R1R2是邻苯二甲酰基。

    Thermosensitive cyclotriphosphazene derivatives and a preparation method thereof
    7.
    发明授权
    Thermosensitive cyclotriphosphazene derivatives and a preparation method thereof 失效
    热敏环三磷腈衍生物及其制备方法

    公开(公告)号：US06417383B1

    公开(公告)日：2002-07-09

    申请号：US09869761

    申请日：2001-07-05

    申请人： Youn Soo Sohn ,  Soo-Chang Song ,  Sang Beom Lee

    发明人： Youn Soo Sohn ,  Soo-Chang Song ,  Sang Beom Lee

    IPC分类号： C07F902

    CPC分类号： C07F9/65815

    摘要： The present invention relates to novel cyclotriphosphazene derivatives represented by Formula (1) and a preparation method thereof wherein HNA is an amino acid group selected from glycine group(—NHCH2COO−), aminomalonic acid group(—NHCH(COO−)2), aspartic acid group (—NHCH(CH2COO−)COO−) and glutamic acid group (—NHCH(CH2CH2COO−)COO−), m is a repeating unit of poly(alkoxyethyleneglycol) selected from 2, 7, 12 and 16, and n is an integer representing number of alkyl carbons and selected from 0, 1, and 3.

    摘要翻译： 本发明涉及由式（1）表示的新型环三磷腈衍生物及其制备方法，其中HNA是选自甘氨酸基（-NHCH 2 COO-），氨基马来酸（-NHCH（COO-）2）），天冬氨酸 酸基（-NHCH（CH2COO-）COO-）和谷氨酸基（-NHCH（CH2CH2COO-）COO-）），m是选自2,7,12和16的聚（烷氧基乙二醇）的重复单元，n是 代表烷基碳数并且选自0,1和3的整数。