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公开(公告)号：KR1020090118879A
公开(公告)日：2009-11-18
申请号：KR1020090042035
申请日：2009-05-14
Applicant: 성균관대학교산학협력단
Abstract: PURPOSE: A PEG-human growth hormone complex is provided to minimize biological activation and last activation in a body. CONSTITUTION: A PEG-human growth hormone complex contains a human growth hormone and polyethyleneglycol(PEG) of 20 kDa-50 kDa. The PEG is methoxyPEG aldehyde(Mpeg-ALD). A pharmaceutical composition for treating dwarfism and growth hormone deficiency or diabetic ulcer contains PEG-human growth hormone complex.
Abstract translation: 目的：提供PEG-人生长激素复合物，以最小化身体中的生物活化和最终活化。 构成：PEG-人生长激素复合物含有20kDa-50kDa的人生长激素和聚乙二醇（PEG）。 PEG是甲氧基-PEG醛（Mpeg-ALD）。 用于治疗侏儒症和生长激素缺乏症或糖尿病性溃疡的药物组合物含有PEG-人生长激素复合物。
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公开(公告)号：KR101128108B1
公开(公告)日：2012-03-22
申请号：KR1020090118416
申请日：2009-12-02
Applicant: 성균관대학교산학협력단
IPC: A61K47/34 , A61K47/12 , A61K31/711 , A61K31/7105
Abstract: 본 발명은, 거대분자를 효율적으로 세포내로 전달할 수 있는, 폴리에틸렌이민 및 담즙산으로 구성된 회합체에 있어서, 상기 담즙산의 카르복시기와 폴리에틸렌이민의 아민기의 반응에 의하여 결합된 회합체에 관한 것이다.
폴리에틸렌이민, 담즙산, 세포내 전달 시스템-
3.发明授权
公开(公告)号：KR100918524B1
公开(公告)日：2009-09-21
申请号：KR1020070015586
申请日：2007-02-14
Applicant: 성균관대학교산학협력단
Abstract: 본 발명은 고분자 하이드로겔을 이용한 주사가능한 약물전달체 및 약물전달방법에 있어서, 음이온 전하를 가질 수 있는 약물제제와, 온도 민감성과 생분해성을 갖는 친수성 고분자와 소수성 고분자로 이루어진 공중합체와 상기 공중합체의 말단에 양이온 전하를 띄는 pH 민감성 성분이 결합된 고분자 하이드로겔을 포함하되, 상기 약물제제는 고분자 하이드로겔 내에 봉입되어, pH 7.2 내지 7.4, 온도 37℃ 조건에서 겔화되고 상기 pH 민감성 성분이 이온화되어 상기 음이온 전하를 갖는 약물제제와 이온성 복합체를 형성하는 온도 및 pH 민감성 블록공중합체 고분자 하이드로겔을 이용한 주사가능한(injectable) 약물전달체 및 약물전달방법을 제공한다.
온도 및 pH 민감성 블록공중합체, 고분자 하이드로겔, 약물전달체, 인슐린, 당뇨병 질환 치료-
公开(公告)号：KR100886783B1
公开(公告)日：2009-03-04
申请号：KR1020060052702
申请日：2006-06-12
Applicant: 성균관대학교산학협력단 , 주식회사 넥스엔텍
IPC: A61K47/48
CPC classification number: A61K47/48215 , A61K38/19 , A61K38/191 , A61K47/60 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96
Abstract: 본 발명은 N-말단이 수식된 PEG-TRAIL 결합체, 이의 제조방법 및 이의 용도에 관한 것으로서, 보다 구체적으로는 천연 TRAIL(
T umor Necrosis Factor
R elated
A poptosis
I nducing
L igand, TRAIL)과 동등 또는 유사한 약리활성을 나타내며 약물의 체내 반감기 및 안정성을 증가시킨 N-말단이 수식된 PEG-TRAIL 결합체에 관한 것이다. 본 발명의 N-말단이 수식된 PEG-TRAIL 결합체는 천연 TRAIL에 비하여 우수한 용해도 및 용액 안정성, 그리고 매우 향상된 약물 동력학적 거동을 보이며, 증식성 질환 및 자가면역 질환 등의 예방 및 치료에 유용하게 사용될 수 있다.
TRAIL, 폴리에틸렌 글리콜, 수용성고분자, 증식성 질환, 자가면역 질환-
5.发明公开
公开(公告)号：KR1020080076099A
公开(公告)日：2008-08-20
申请号：KR1020070015586
申请日：2007-02-14
Applicant: 성균관대학교산학협력단
CPC classification number: A61K47/59 , A61K9/0019 , A61K9/06 , A61K38/28
Abstract: An injectable and biodegradable drug delivery system is provided to control glucose concentration in blood by slowly releasing insulin, improve compliance of patient by reducing injection frequency, and minimize side effects of drug by using polymer hydrogel. An injectable and biodegradable drug delivery system contains a negatively charged drug included in polymer hydrogel having a copolymer consisting of temperature sensitive and biodegradable hydrophilic polymer and hydrophobic polymer, coupled with a pH sensitive component in the end, wherein the drug becomes gel under conditions of pH 7.2-7.4 and 37 deg. C, and the pH sensitive component is ionized positively and forms an ionic complex with the negatively charged drug. Further, the hydrophilic polymer is one or more selected from a group consisting of polyethylene glycol, poly(N-2-(hydroxypropyl)methacrylamide), poly(divinyl ether-co-maleic anhydride), poly(styrene-co-maleic anhydride), or a polymer synthesized from a group consisting of dextran, chitosan, glycol chitosan, poly-L-lysine, polyglutamic acid and polyaspartic acid.
Abstract translation: 提供可注射和可生物降解的药物递送系统，以通过缓慢释放胰岛素来控制血液中的葡萄糖浓度，通过降低注射频率提高患者的依从性，并通过使用聚合物水凝胶来最小化药物的副作用。 可注射和可生物降解的药物递送系统包含聚合物水凝胶中含有负电荷的药物，其具有由温度敏感性和可生物降解的亲水性聚合物和疏水性聚合物组成的共聚物，最终与pH敏感组分偶联，其中药物在pH条件下变成凝胶 7.2-7.4和37度 C，并且pH敏感组分被正电离并与带负电荷的药物形成离子络合物。 此外，亲水性聚合物是选自聚乙二醇，聚（N-2-（羟丙基）甲基丙烯酰胺），聚（二乙烯基醚 - 共 - 马来酸酐），聚（苯乙烯 - 共 - 马来酸酐） 或由由葡聚糖，壳聚糖，乙二醇壳聚糖，聚-L-赖氨酸，聚谷氨酸和聚天冬氨酸组成的组合成的聚合物。
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Patent Agency Ranking
公开(公告)号：KR1020070118492A
公开(公告)日：2007-12-17
申请号：KR1020060052702
申请日：2006-06-12
Applicant: 성균관대학교산학협력단 , 주식회사 넥스엔텍
IPC: A61K47/48
CPC classification number: A61K47/48215 , A61K38/19 , A61K38/191 , A61K47/60 , B01D15/361 , C07K14/52 , C07K14/525 , C07K14/70575 , C07K2319/73 , G01N30/96 , A61K47/50
Abstract: A N-terminal modified PEG(polyethylene glycol)-TRAIL(tumor necrosis factor related apoptosis inducing ligand) is provided to reduce liver toxicity, increase the in vivo retention time, and enhance solubility and stability in solution and pharmacokinetic profiles of TRAIL, so that it is useful for prevention and treatment of proliferative disease and autoimmune disease. A N-terminal modified PEG-TRAIL having non-toxicity to the liver is prepared by linking PEG or PEG derivatives specifically to the N-terminal of TRAIL, wherein PEG is selected from methoxy polyethylene glycol succinimidyl propionate, methoxy polyethylene glycol N-hydroxysuccinimide, methoxy polyethylene glycol aldehyde, methoxy polyethylene glycol maleimide and multi-branched type polyethylene glycol, and the TRAIL contains a zipper amino acid array inducing trimer formation or a terminal group for facilitating the separation and purification.
Abstract translation: 提供N-末端修饰的PEG（聚乙二醇）-TRAIL（肿瘤坏死因子相关的凋亡诱导配体），以减少肝毒性，增加体内保留时间，增强溶液中的溶解度和稳定性以及TRAIL的药代动力学特征，使得 它可用于预防和治疗增殖性疾病和自身免疫性疾病。 通过将PEG或PEG衍生物与TRAIL的N-末端特异性连接，制备具有对肝脏无毒性的N-末端修饰的PEG-TRAIL，其中PEG选自甲氧基聚乙二醇琥珀酰亚胺基丙酸酯，甲氧基聚乙二醇N-羟基琥珀酰亚胺， 甲氧基聚乙二醇醛，甲氧基聚乙二醇马来酰亚胺和多支链型聚乙二醇，TRAIL含有诱导三聚体形成的拉链氨基酸阵列或用于促进分离和纯化的末端基团。
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7.发明授权
公开(公告)号：KR100778633B1
公开(公告)日：2007-11-28
申请号：KR1020070036246
申请日：2007-04-13
Applicant: 성균관대학교산학협력단
IPC: C07D495/04 , A61K31/4188
Abstract: A biotin and biotin polyethylene glycol-linked GLP-1 derivative is provided to be usefully used for preventing or treating diseases caused by excessive secretion of insulin, lowering of glucose in plasma, inhibition of stomach or intestine motion, inhibition of an empty stomach or intestine, or inhibition of food intake, type 2 diabetes, obesity and irritable colon syndrome. A GLP-1 derivative in which biotin and biotin-polyethylene glycol are selectively linked to No. 26 lysine residue and No. 34 lysine residue is represented by the formula(2), wherein the biotin-polyethylene glycol is represented by the formula(1) having a molecular weight of 3,400. A method for preparing the GLP-1 derivative comprises the steps of: (a) adding biotin, biotin-polyethylene glycol and GLP to a buffer solution and an organic solvent to be subject to reaction; (b) storing the reaction mixture obtained from the step(a) under a certain temperature for a certain period of time; (c) removing non-reacted reaction products after the reaction completion of the step(b); and (d) isolating GLP-1 in which the biotin and biotin-polyethylene glycol are linked from the non-reacted products-removed products and purifying them. A pharmaceutical composition for preventing or treating diabetes or obesity comprises the biotin and biotin polyethylene glycol-linked GLP-1 derivative.
Abstract translation: 提供生物素和生物素聚乙二醇连接的GLP-1衍生物可用于预防或治疗由胰岛素过量分泌引起的疾病，血浆中葡萄糖降低，抑制胃或肠运动，抑制空腹或肠 ，或抑制食物摄入，2型糖尿病，肥胖症和肠易激综合征。 生物素和生物素 - 聚乙二醇与26号赖氨酸残基和34号赖氨酸残基选择性连接的GLP-1衍生物由式（2）表示，其中生物素 - 聚乙二醇由式（1 ），分子量为3400。 制备GLP-1衍生物的方法包括以下步骤：（a）将生物素，生物素 - 聚乙二醇和GLP加入缓冲溶液和有机溶剂进行反应; （b）将从步骤（a）获得的反应混合物在一定温度下储存一定时间; （c）在步骤（b）的反应完成后除去未反应的反应产物; 和（d）分离其中生物素和生物素 - 聚乙二醇与未反应的产物去除产物连接的GLP-1并纯化。 用于预防或治疗糖尿病或肥胖症的药物组合物包括生物素和生物素聚乙二醇连接的GLP-1衍生物。
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公开(公告)号：KR100746658B1
公开(公告)日：2007-08-06
申请号：KR1020070039445
申请日：2007-04-23
Applicant: 성균관대학교산학협력단
IPC: C07K14/46 , C07K14/47 , C07K14/575
Abstract: Provided are an exendin-4 derivative linked by hydrophobic bile acid which forms nanoparticles, improves albumin adsorption activity, and increases the in vivo half-life while it shows identical or similar biological activity to natural exendin-4, a method for the preparation thereof and a pharmaceutical composition comprising the same compound so as to be used for treating disease caused by excessive insulin secretion including diabetes, obesity and irritable colon syndrome. The exendin-4 derivative linked by hydrophobic bile acid in which 12th, 27th or 12th and 27th lysine residues are lined to the hydrophobic bile acid is provided. The method for preparing the exendin-4 derivative linked by hydrophobic bile acid comprises the steps of: (1) reacting bile acid with N-hydroxysuccinimide(NHS) to activate the carboxylic acid group of the bile acid; (2) reacting the activated bile acid-NHS with exendin-4; and (3) separating the exendin-4 derivative linked by hydrophobic bile acid from the reaction mixture.
Abstract translation: 提供了由疏水性胆汁酸连接的毒蜥外泌肽-4衍生物，其形成纳米颗粒，提高白蛋白吸附活性，并且增加体内半衰期，同时显示与天然毒蜥外泌肽-4相同或相似的生物活性，及其制备方法和 包含相同化合物的药物组合物，以用于治疗由过量的胰岛素分泌引起的疾病，包括糖尿病，肥胖症和肠易激综合征。 提供了由疏水性胆汁酸连接的毒蜥外泌肽-4衍生物，其中第12,27或12和27个赖氨酸残基排列在疏水胆汁酸上。 制备由疏水胆汁酸连接的毒蜥外泌肽-4衍生物的方法包括以下步骤：（1）使胆汁酸与N-羟基琥珀酰亚胺（NHS）反应以活化胆汁酸的羧酸基团; （2）使活化的胆汁酸-NHS与毒蜥外泌肽-4反应; 和（3）从反应混合物中分离疏水胆汁酸连接的毒蜥外泌肽-4衍生物。
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公开(公告)号：KR101104574B1
公开(公告)日：2012-01-11
申请号：KR1020090042035
申请日：2009-05-14
Applicant: 성균관대학교산학협력단
Abstract: 본 발명은 인간 성장 호르몬 및 20 kDa ~ 50 kDa의 분자량을 가지는 폴리에틸렌글리콜(polyethylene glycol, PEG)을 포함하는, PEG-인간 성장 호르몬 결합체에 관한 것이다. 이에 의하여, 아미노 말단에 PEG 한 분자를 선택적으로 결합시켜 생물학적 활성 저하를 최소화시키고, 인간 성장 호르몬의 안전성 및 체내 잔류 시간을 증가시킴으로써 생체 내 활성이 지속 가능하다.
폴리에틸렌 글리콜, PEG-인간 성장 호르몬 결합체, 왜소증, 당뇨성 궤양-
公开(公告)号：KR1020110061881A
公开(公告)日：2011-06-10
申请号：KR1020090118416
申请日：2009-12-02
Applicant: 성균관대학교산학협력단
IPC: A61K47/34 , A61K47/12 , A61K31/711 , A61K31/7105
CPC classification number: A61K47/34 , A61K31/7105 , A61K31/711 , A61K47/28
Abstract: PURPOSE: A conjugate containing polyethyleneimine and bile acid is provided to ensure high transport efficiency and to transport nucleic acid drugs. CONSTITUTION: A conjugate containing polyethyleneimine and bile acid is conjugated by reaction of carboxy group of bile acid and amine group of polyethyleneidmine. The bile acid is cholic acid, 5 beta-cholanic acid, chenodeoxycholic acid, glycoholic acid, taurocholic acid, deoxycholic acid, lithocholic acid, or 7-oxo-lithochoilc acid. The conjugated contain macromolecule or hydrophobic drugs. The macromolecule is plasmid DNA, siRNA, or antisense oligonucleotide. The hydrophobic drug is doxorubicin, adriamycin, cisplatin, paclitaxel, taxol, docetaxel, or daunomycin.
Abstract translation: 目的：提供含有聚乙烯亚胺和胆汁酸的缀合物，以确保高运输效率和运输核酸药物。 构成：含有聚乙烯亚胺和胆汁酸的共轭物通过胆汁酸羧基和聚乙烯胺胺基的反应而结合。 胆汁酸是胆酸，5β-胆酸，鹅脱氧胆酸，甘醇酸，牛磺胆酸，脱氧胆酸，石胆酸或7-氧代 - 苯基胆酸。 共轭含有大分子或疏水性药物。 大分子是质粒DNA，siRNA或反义寡核苷酸。 疏水性药物是多柔比星，阿霉素，顺铂，紫杉醇，紫杉醇，多西他赛或道诺霉素。
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