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公开(公告)号：KR100979462B1
公开(公告)日：2010-09-02
申请号：KR1020070077934
申请日：2007-08-03
Applicant: 한국화학연구원
Abstract: 본 발명은 안트라사이클라인계 항암약물 봉입용 리포솜 및 이의 제조방법에 관한 것으로, 더욱 상세하게는 양전하를 갖는 지질과 인지질을 함유하는 리포솜에 폴리에틸렌글리콜(PEG) 유도체를 도입하여 이온성 리포솜을 제조함으로써 암세포 내로 효과적으로 이입되어 항암약물의 투여가 용이한 세포이입성이 증진된 안트라사이클라인계 항암약물 봉입용 리포솜 및 이의 제조방법에 관한 것이다.
안트라사이클라인계 항암약물, 리포솜, 폴리에틸렌글리콜 유도체, 세포이입성-
公开(公告)号：KR1020090013848A
公开(公告)日：2009-02-06
申请号：KR1020070077934
申请日：2007-08-03
Applicant: 한국화학연구원
CPC classification number: A61K9/1273 , A61K47/34
Abstract: A liposome for encapsulating anthracycline anticancer drug is provided to improve absorption efficiency of liposome delivered to the tumor tissue into the cancer cell by introducing PEG(polyethylene glycol) to the phospholipid having positive charge or the surface of liposome containing this. The ionic liposome for encapsulating anthracycline anticancer drug is prepared by introducing PEG derivative into the phospholipid having positive charge which is 1,2-disteroyl-3-trimethylammonium-propane(DOTAP), dimethyldioctadecylammonium(DDAB), 1,2-diacyl-3-dimethyl ammonium propane(DAP) or L-a-dioleylphosphatidylethanolamine(DOPE), or the surface of liposome containing this.
Abstract translation: 提供用于包封蒽环类抗癌药物的脂质体，以通过将PEG（聚乙二醇）引入具有正电荷的磷脂或含有这种脂质体的表面来提高向肿瘤组织递送至肿瘤组织的脂质体的吸收效率。 通过将PEG衍生物引入具有1,2-二甲酰基-3-三甲基铵 - 丙烷（DOTAP），二甲基二十八烷基铵（DDAB），1,2-二酰基-3-甲基丙烷的正电荷的磷脂中制备用于封装蒽环类抗癌药物的离子脂质体， 二甲基铵丙烷（DAP）或者La-二油基磷脂酰乙醇胺（DOPE），或含有此的脂质体的表面。
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3.发明公开
公开(公告)号：KR1020070087953A
公开(公告)日：2007-08-29
申请号：KR1020060017372
申请日：2006-02-22
IPC: C07D231/04 , C07D237/04
CPC classification number: Y02P20/55 , C07D231/04 , C07D237/04 , C07D243/02 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D417/12
Abstract: A cyclic hydrazide derivative having a beta-amino group is provided to inhibit the activity of DPP-IV, thereby being useful for treating various diseases mediated by the DPP-IV. The cyclic hydrazide derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(a) or (b), R2 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, or a group represented by the structural formula(a), (b), (c), (d), (e), (f), (g), or (h)[wherein R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCH2O, OCF3, phenoxy, halogen, CN, NO2, CF3, COOR^b or NR^bR^c(wherein each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl), R^d is a group represented by the structural formula(a), (b), (i), (j), (k), (l), or (m), R^e is C1-6 alkyl, C3-6 cycloalkyl, or a group represented by the structural formula(a) or (b), R^f is halogen, NR^b, R^c, a group represented by the structural formula(n) or (o), -S-heteroayl, tetrahydroisoquinoline, thiazolidine, proline, piperidine-4-carboxylic acid or tetrahydropyrimidine(where X is O or S)], and n is an integer from 1 to 3. The method comprises the steps of: (a) performing a condensation reaction of an amino acid represented by the formula(2) and a cyclic hydrazine represented by the formula(3) to obtain a compound represented by the formula(4); (b) reacting the compound of the formula(4) with chloroacetyl chloride to obtain a compound represented by the formula(6); (c) reacting the compound of the formula(6) with an R2 substituted nucleophilic compound to obtain a compound represented by the formula(5); and (d) deprotecting the compound of the formula(5). In the reaction formula(2), BOC is a protecting group, and each R1, R2, and n is the same as defined above.
Abstract translation: 提供具有β-氨基的环状酰肼衍生物以抑制DPP-IV的活性，从而可用于治疗由DPP-IV介导的各种疾病。 具有β-氨基的环状酰肼衍生物由式（1）表示，其中R 1是由结构式（a）或（b）表示的基团，R 2是H，C 1-6烷基，C 3-6环烷基 或者由结构式（a），（b），（c），（d），（e），（f），（g）或（h） a独立地是H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCH 2 O，OCF 3，苯氧基，卤素，CN，NO 2，CF 3，COOR b或NR b R c c（其中每个R b和 （a），（b），（i），（j），（k），（j），（k） 1）或（m）R e是C 1-6烷基，C 3-6环烷基或由结构式（a）或（b）表示的基团，R f是卤素，NR b， c，由结构式（n）或（o）表示的基团，-S-杂芳基，四氢异喹啉，噻唑烷，脯氨酸，哌啶-4-甲酸或四氢嘧啶（其中X为O或S）]，n为 从1到3的整数。该方法包括以下步骤：（a）pe （2）表示的氨基酸与式（3）表示的环状肼的缩合反应，得到式（4）表示的化合物。 （b）使式（4）的化合物与氯乙酰氯反应，得到式（6）表示的化合物; （c）使式（6）化合物与R2取代的亲核化合物反应得到式（5）表示的化合物; 和（d）使式（5）的化合物脱保护。 在反应式（2）中，BOC为保护基，R1，R2和n各自与上述相同。
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公开(公告)号：KR100154279B1
公开(公告)日：1998-11-16
申请号：KR1019950016623
申请日：1995-06-21
Applicant: 한국화학연구원
IPC: C07D495/04
Abstract: 본 발명은 포유동물의 위산분비 억제능력을 보유하고 있어 항궤양제의 유효성분으로서 매우 유용한 다음 구조식(I)로 표시되는 알킬아미드를 함유한 티에노피리미돈 유도체에 관한 것이다.
상기식에서, R
1 및R
2 는 각각 같거나 다른 것으로서 수소원자 또는 탄소원자수 1 내지 4의 알킬기이고, R
3 은 할로겐원자이고, R
4 는 수소원자 또는 탄소원자수 1 내지 4 의 알킬기이고, R
5 는 수소원자, 탄소원자수 1 내지 4 의 알콕시기, 페닐아미노, 페닐 또는 치환된 페닐기로서, 이때 치환기로는 할로겐원자 또는 탄소원자수 1 내지 4의 알킬기이고, n은 0또는 1이다.-
公开(公告)号：KR100996975B1
公开(公告)日：2010-11-29
申请号：KR1020080019750
申请日：2008-03-03
Applicant: 한국화학연구원
Abstract: 본 발명은 혈류 내 순환시간을 증가시킨 단백질로 수식된 리포솜 및 이의 제조방법에 관한 것으로서, 더욱 상세하게는 생체적합성 단백질을 양이온성 리포솜 표면에 정전기적 상호인력으로 이온 결합시키고, 리포솜 표면에 결합된 단백질을 변성시켜 리포솜과의 결합력이 강화시킴으로써 리포솜이 혈류 내에서 순환할 때 혈장 내 단백질의 흡착을 방지하여 혈류 내에서 리포솜의 안정성을 강화하는 한편, 체내 순환시간을 증가시키는 리포솜 및 이의 제조방법에 관한 것이다.
단백질, 수식, 리포솜, 이온 결합, 체내 순환시간-
Patent Agency Ranking
公开(公告)号：KR1020100094337A
公开(公告)日：2010-08-26
申请号：KR1020097017134
申请日：2008-01-16
Applicant: (주) 카이노스메드 , 한국화학연구원 , 영진약품 주식회사
IPC: C07D277/22 , C07D417/12 , A61K31/427 , A61P19/10
CPC classification number: C07D277/06 , C07D417/12 , Y02P20/55
Abstract: PURPOSE: A dipeptidyl peptidase(DPP-IV) inhibitor is provided to use in treating DPP-IV-mediated disease. CONSTITUTION: A 2-carbonyl-3-acyl-1,3-thiazolidine of salt or prodrug form has a beta-amino group on acyl chain. A method for preparing the 2-carbonyl-3-acyl-1,3-thiazolidine derivative comprises: a step of condensing an amino acid of chemical formula Q-2 with a 2-cabonyl-1,3-thiazolidine compounds of chemical formula Q-3 to form a compound of chemical formula Q-4; and a step of deprotecting the compound of chemical formula Q-4 to obtain 2-carbonyl-3-acyl-1,3-thiazolidine derivative of chemical formula Q-1a. A pharmaceutical composition contains the 2-carbonyl-3-acyl-1,3-thiazolidine, pharmaceutically acceptable diluents, or carrier. The pharmaceutical composition is used for preventing or treating dipeptidyl peptidase IV(DPP-IV)-mediated disease.
Abstract translation: 目的：提供二肽基肽酶（DPP-IV）抑制剂用于治疗DPP-IV介导的疾病。 构成：盐或前药形式的2-羰基-3-酰基-1,3-噻唑烷在酰基链上具有β-氨基。 制备2-羰基-3-酰基-1,3-噻唑烷衍生物的方法包括：将化学式Q-2的氨基酸与化学式Q的2-缩水甘油基-1,3-噻唑烷化合物缩合的步骤 -3以形成化学式Q-4的化合物; 以及使化学式Q-4的化合物脱保护，得到化学式Q-1a的2-羰基-3-酰基-1,3-噻唑烷衍生物的工序。 药物组合物含有2-羰基-3-酰基-1,3-噻唑烷，药学上可接受的稀释剂或载体。 该药物组合物用于预防或治疗二肽基肽酶IV（DPP-IV）介导的疾病。
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公开(公告)号：KR1020100031320A
公开(公告)日：2010-03-22
申请号：KR1020080090356
申请日：2008-09-12
Applicant: 한국화학연구원
CPC classification number: A61K47/42 , A61K9/1271 , A61K9/1277 , A61K31/663 , A61K38/12
Abstract: PURPOSE: A liposome with increases circulation time in blood is provided to suppress adsorption of a protein in blood by strengthening binding force of the protein and liposome. CONSTITUTION: A liposome having increased circulation time in blood is produced by binding a protein on the surface of liposome containing negative ionic lipid and denaturing the protein. The protein is selected from albumin, globulin, glutenin, prolamine, albunoid, nuclear protein, glycoprotein, phosphoprotein, lipoprotein, chromoprotein, and gelatin.
Abstract translation: 目的：提高血液循环时间增加的脂质体，通过加强蛋白质和脂质体的结合力来抑制血液中蛋白质的吸附。 构成：通过在含有负离子脂质的脂质体的表面上结合蛋白质并使蛋白质变性来产生具有增加血液循环时间的脂质体。 蛋白质选自白蛋白，球蛋白，谷蛋白，谷醇溶蛋白，类白蛋白，核蛋白，糖蛋白，磷蛋白，脂蛋白，色蛋白和明胶。
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公开(公告)号：KR100848491B1
公开(公告)日：2008-07-28
申请号：KR1020070004577
申请日：2007-01-16
IPC: C07D277/06 , C07D417/06 , A61P3/08 , A61P3/04
CPC classification number: C07D277/06 , C07D417/12 , Y02P20/55
Abstract: 2-Thiazolidine derivatives having beta-amino group are provided to inhibit activity of DPP-IV(dipeptidyl peptidase-IV) associated with activity regulation of various hormones, so that the compounds are useful for treating diseases mediated by DPP-IV including type 2 diabetes mellitus. The 2-thiazolidine derivatives having beta-amino group represented by the formula(1) are prepared by reacting an amino acid represented by the formula(2) with 2-thiazolidine compounds represented by the formula(3) to prepare compounds represented by the formula(4), and deprotecting the compounds represented by the formula(4), wherein BOC is a protecting group; A is -NR^e(CH2)nR2 or -OR^b; R^a is hydrogen, C1-6 alkyl, C1-6 alkoxy, -OCF3, halogen, -CN or -CF3; R^b is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, isopropyl, t-butyl, -CH2CH2OH, -CH2CH2NH2, -CH2CH2N(CH2CH2)2O, -CH2CH2N(CH2CH3)2 or -CH2CH2NHCOCH3; R^c is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, benzyl, isopropyl or t-butyl; R^d and R^e are each independently hydrogen, C1-6 alkyl or C3-6 cycloalkyl; Y is carbon, oxygen, sulfur or nitrogen; Z is hydrogen, C1-6 alkyl, C3-6 cycloalkyl or -CO2R^b; and n is an integer of 0, 1 or 2.
Abstract translation: 提供具有β-氨基的2-噻唑烷衍生物以抑制与各种激素的活性调节相关的DPP-IV（二肽基肽酶-IV）的活性，使得该化合物可用于治疗包括2型糖尿病的DPP-IV介导的疾病 糖尿病。 由式（1）表示的具有β-氨基的2-噻唑烷衍生物通过使由式（2）表示的氨基酸与由式（3）表示的2-噻唑烷化合物反应来制备由式 （4）表示的化合物，并使由式（4）表示的化合物脱保护，其中BOC为保护基; A是-NR e（CH 2）n R 2或-OR b; R a a是氢，C 1-6烷基，C 1-6烷氧基，-OCF 3，卤素，-CN或-CF 3; 异丙基，叔丁基，-CH 2 CH 2 OH，-CH 2 CH 2 NH 2，-CH 2 CH 2 N（CH 2 CH 2）2 O，-CH 2 CH 2 N（CH 2 CH 3）2或-CH 2 CH 2 NHCOCH 3; R c是氢，C 1-6烷基，C 3-6环烷基，苄基，异丙基或叔丁基; R d和R e e各自独立地为氢，C 1-6烷基或C 3-6环烷基; Y是碳，氧，硫或氮; Z是氢，C 1-6烷基，C 3-6环烷基或-CO 2 R b; 且n为0,1或2的整数。
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9.发明公开베타아미노기를 갖는 1,2,5-트리아제판 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법 有权具有β型-AMINO ACYL组的1,2,5-三唑衍生物及其药物可接受的盐及其制备方法
公开(公告)号：KR1020080007764A
公开(公告)日：2008-01-23
申请号：KR1020060066812
申请日：2006-07-18
IPC: C07D255/02 , A61P3/00
Abstract: A 1,2,5-triazepane derivative showing excellent DPP-IV inhibitory activity is provided to be effectively used for preventing or treating diseases mediated by DPP-IV such as insulin-dependent, insulin non-dependent diabetes, arthritis, obesity, osteoporosis, and damaged glucose resistance. A 1,2,5-triazepane derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(1-1) or (1-2); R2 is H, C1-6 alkyl, or a group represented by the structural formula(1-3); R3 is H, C1-6 alkyl, C3-6 cycloalkyl, CH2CO2R^b, COCO2R^b, pyrazine, and a group represented by the structural formula(1-4), (1-5) or (1-6); R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCF3, halogen, CN, CF3, COOR^b or NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl; R^d is C1-6 alkyl, trifluoromethyl, and a group represented by the structural formula(1-1), (1-7), (1-8), or (1-9); R^e is C1-6 alkyl, C3-6 cycloalkyl, and a group represented by the structural formula(1) or (2); R^f is H, halogen, NR^bR^c, tetrazole, proline, and a group represented by the structural formula(1-10), (1-11), (1-12), or (1-13); A is CH, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl or CO2R^d; X is O or S; and n is 0 or 1. A method for preparing the 1,2,5-triazepane derivative comprises the steps of: (a) subjecting an amino acid represented by the formula(2) and 1,2,5-triazepane to a condensation reaction to prepare a compound represented by the formula(4); (b) reacting the compound of the formula(4) with an electrophilic compound substituted with R2 to prepare a compound represented by the formula(5); and (c) deprotecting the compound of the formula(5). A pharmaceutical composition for preventing or treating diseases mediated by DPP-IV comprises an effective amount of the 1,2,5-triazepane derivative or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.
Abstract translation: 提供了显示优异的DPP-IV抑制活性的1,2,5-三氮丙平衍生物，其有效用于预防或治疗由DPP-IV介导的疾病，例如胰岛素依赖性，胰岛素非依赖型糖尿病，关节炎，肥胖症，骨质疏松症， 并损害葡萄糖耐量。 具有β-氨基的1,2,5-三氮杂环庚烷衍生物由式（1）表示，其中R1是由结构式（1-1）或（1-2）表示的基团。 R2是H，C1-6烷基或由结构式（1-3）表示的基团; R 3是H，C 1-6烷基，C 3-6环烷基，CH 2 CO 2 R b，COCO 2 R b，吡嗪和由结构式（1-4），（1-5）或（1-6）表示的基团。 R a a独立地为H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCF 3，卤素，CN，CF 3，COOR b或NR b R c; 每个R b和R c独立地是H，C 1-6烷基或C 3-6环烷基; R 1-6是C1-6烷基，三氟甲基和由结构式（1-1），（1-7），（1-8）或（1-9）表示的基团。 R 1-6是C 1-6烷基，C 3-6环烷基和由结构式（1）或（2）表示的基团。 （1-10），（1-11），（1-12）或（1-13）表示的基团，其中R为氢，卤素，NR 4 b R c，四唑，脯氨酸和由结构式 ; A是CH，N，O或S; B是H，C 1-6烷基，C 3-6环烷基，苄基或CO 2 R d; X是O或S; 并且n为0或1.制备1,2,5-三氮杂环庚烷衍生物的方法包括以下步骤：（a）使由式（2）表示的氨基酸和1,2,5-三氮杂环庚烷进行缩合 反应制备式（4）表示的化合物; （b）使式（4）的化合物与被R 2取代的亲电子化合物反应，制备由式（5）表示的化合物。 和（c）使式（5）的化合物脱保护。 用于预防或治疗由DPP-IV介导的疾病的药物组合物包含有效量的1,2,5-三氮丙烯衍生物或其药学上可接受的盐和药学上可接受的载体。
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公开(公告)号：KR100792275B1
公开(公告)日：2008-01-08
申请号：KR1020060017372
申请日：2006-02-22
IPC: C07D231/04 , C07D237/04
CPC classification number: Y02P20/55
Abstract: 하기 화학식 1로 표시되는, 베타아미노기를 갖는 고리화된 히드라자이드 유도체 또는 이의 약학적으로 허용 가능한 염이 제공된다. 이 고리화된 히드라자이드 유도체는 DPP-IV의 활성을 억제하여, DPP-IV에 의해 매개되는 각종 질환을 치료하는데 유용하다.
[화학식 1]
상기 식에서, R
1 , R
2 및 n은 명세서에 정의되는 바와 같다.
고리화된 히드라자이드 유도체, DPP-IV, 제조 방법, 약학 조성물
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