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1. 发明授权

US08344173B2 Dendritic oligopeptide-grafteded cyclotriphosphazene, a process for the preparation thereof and a drug delivery system containing the same 有权
标题翻译：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。

2. 发明申请

US20110046347A1 DENDRITIC OLIGOPEPTIDE-GRAFTEDED CYCLOTRIPHOSPHAZENE, A PROCESS FOR THE PREPARATION THEREOF AND A DRUG DELIVERY SYSTEM CONTAINING THE SAME 有权
标题翻译：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。

3. 发明申请

US20130266661A1 AMPHIPHILIC CYCLIC PHOSPHAZENE TRIMER, PHARMACEUTICAL FORMULATION OF HYDROPHOBIC DRUGS BY MICELLE-ENCAPSULATION USING THE AMPHIPHILIC CYCLIC PHOSPHAZENE TRIMER, AND PREPARATION METHODS THEREOF 审中-公开
标题翻译： AMPHIPHILIC循环磷酸三酯，通过使用AMPHIPHILIC循环磷酸二酯的MICELLE-ENCAPSULATION制备疏水性药物及其制备方法
公开(公告)号：US20130266661A1
公开(公告)日：2013-10-10
申请号：US13995557
申请日：2011-12-16
申请人： Youn Soo Sohn , Yong Joo Jun
发明人： Youn Soo Sohn , Yong Joo Jun
IPC分类号： A61K47/42 , A61K9/48
CPC分类号： A61K47/42 , A61K9/0019 , A61K9/107 , A61K9/4833 , A61K31/337 , A61K47/24 , C07F9/65815
摘要： The present invention relates to an amphiphilic cyclic phosphazene trimer which is biocompatible and a method for preparing the same. The present invention also relates to pharmaceutical formulations of hydrophobic drugs that are micelle-encapsulated by the amphiphilic cyclic phosphazene trimer and a method for preparing the same.
摘要翻译：本发明涉及生物相容性的两亲性环状磷腈三聚体及其制备方法。本发明还涉及由两亲性环磷腈三聚体胶束包封的疏水药物的药物制剂及其制备方法。

4. 发明授权

US06951953B2 Tumor selective and biodegradable polyphosphazene-platinum(II) conjugate antitumor agent, and preparation method thereof 失效
标题翻译：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。

5. 发明授权

US07598318B2 Thermosensitive and biocompatible amphiphilic poly(organophosphazenes) and preparation method thereof 失效
标题翻译：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。

6. 发明授权

US06867316B2 Platinum(II) complexes of N-substituted amino dicarboxylates and the preparation method thereof 失效
标题翻译： 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。

7. 发明授权

US06417383B1 Thermosensitive cyclotriphosphazene derivatives and a preparation method thereof 失效
标题翻译：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。

8. 发明授权

US06319984B1 Biodegradable and thermosensitive polyphosphazenes and their preparation method 有权
标题翻译：生物降解和热敏聚磷腈及其制备方法
公开(公告)号：US06319984B1
公开(公告)日：2001-11-20
申请号：US09546566
申请日：2000-04-11
申请人： Soo-Chang Song , Youn Soo Sohn , Bae Hoon Lee , Sang Beom Lee
发明人： Soo-Chang Song , Youn Soo Sohn , Bae Hoon Lee , Sang Beom Lee
IPC分类号： C08G7902
CPC分类号： C08G79/025
摘要： The present invention relates to novel biodegradable polyphosphazenes represented by Formula 1 and a preparation method thereof. Polyphosphazenes of the present invention not only have thermosensitivity and biodegradability simultaneously, but also their phase transition temperature and degradation rate can be controlled.
摘要翻译：本发明涉及由式1表示的新型生物可降解聚磷腈及其制备方法。本发明的聚磷酰胺不仅具有热敏性和生物降解性，而且可以控制它们的相变温度和降解速率。

9. 发明授权

US5998648A Anticancer (IV) complexes for oral administration and a method of making the same 失效
标题翻译：用于口服给药的抗癌（IV）复合物及其制备方法
公开(公告)号：US5998648A
公开(公告)日：1999-12-07
申请号：US134697
申请日：1998-08-14
申请人： Youn Soo Sohn , Sung Sil Lee , Young-A Lee , Kwan Mook Kim , Chong Ock Lee
发明人： Youn Soo Sohn , Sung Sil Lee , Young-A Lee , Kwan Mook Kim , Chong Ock Lee
IPC分类号： A61K31/28 , A61P35/00 , C07C53/122 , C07C53/124 , C07C53/126 , C07C209/00 , C07C211/09 , C07C211/10 , C07C211/11 , C07C211/18 , C07C211/36 , C07D309/04 , C07F13/00 , C07F15/00
CPC分类号： C07C53/122 , C07C211/10 , C07C211/11 , C07C211/18 , C07C211/36 , C07C53/124 , C07D309/04 , C07F15/0093
摘要： Platinum (IV) complexes for oral administration represented by the structural formula ##STR1## where A--A is a symmetrical diamine that can chelate to platinum and is selected from the group consisting of ethylene diamine, t(.+-.)-1,2-diaminocyclohexane, 2,2-dimethyl-1,3-propanediamine, cyclohexane-1,1-dimethaneamine and tetrahydro-4H-pyran-4,4-dimethaneamine; and R is propionyl, butyryl or valeryl. These complexes are useful in the treatment of cancer.
摘要翻译：用于口服给药的铂（IV）络合物，其结构式为AA，其为螯合铂的对称二胺，并且选自乙二胺，t（+/-） - 1,2-二氨基环己烷， 2-二甲基-1,3-丙二胺，环己烷-1,1-二甲胺和四氢-4H-吡喃-4,4-二甲胺; R是丙酰基，丁酰基或戊酰基。这些复合物可用于治疗癌症。

10. 发明授权

US10336867B2 Cationic polyphosphazene compound, polyphosphazenes-drug conjugate compound and method for preparing same 有权
公开(公告)号：US10336867B2
公开(公告)日：2019-07-02
申请号：US15125543
申请日：2015-03-13
申请人： Youn Soo Sohn , CNPHARM CO., LTD
发明人： Youn Soo Sohn , Yong Joo Jun , Prakash Gouda Avaji
IPC分类号： C08G79/025 , A61K31/337 , A61K31/4745 , A61K31/555 , C08G81/00 , A61K47/60 , A61K47/58
摘要： The present invention relates to a new class of cationic linear polyphosphazenes bearing as side groups a hydrophilic poly(ethylene glycol) and a spacer group selected from the group consisting of lysine, oligopeptides containing lysine, amino-ethanol, amino-propanol, amino-butanol, amino-pentanol and amino-hexanol, and the polyphosphazene-drug conjugates comprising hydrophobic anticancer drugs by covalent bonding and the preparation methods thereof. The present polyphosphazene-drug conjugates exhibit outstanding tumor selectivity and low toxicity.

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