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公开(公告)号：KR101465234B1
公开(公告)日：2014-12-01
申请号：KR1020110029772
申请日：2011-03-31
Applicant: 한국화학연구원
IPC: C07C311/43 , C07C311/41 , A61K31/18 , A61P3/10
Abstract: 본발명은하기화학식 1 표시되는, 사이클로프로필기를갖는아릴설폰아마이드유도체또는이의약학적으로허용가능한염이제공된다. 이아릴설폰아마이드유도체는 11베타하이드록시스테로이드디하이드로게나이제유형1의 (11-hydroxystreroid dehydrogenase type1, 11-HSD1) 활성을억제하여, 11-HSD1에의해매개되는각종질환을치료하는데유용하다. 화학식 1
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公开(公告)号：KR101343668B1
公开(公告)日：2013-12-20
申请号：KR1020110086553
申请日：2011-08-29
Applicant: 한국화학연구원
IPC: A61K31/404 , C07D209/04 , G01N33/15 , A61P3/00
Abstract: 본발명은지질만을특이적으로염색하는화합물을포함하는대사증후군치료약물의스크리닝키트및 이를이용하는대사증후군치료약물의스크리닝방법을제공한다. 본발명의화학식 1 또는 2로표시된 3-인돌리논유도체또는그의염은지방조직만을특이적으로높은민감도로염색하는특성이있어, 이를통해발생하는형광강도를측정하여광학적방법으로지방조직의양을확인할수 있다. 이방법은수술이나조직의추출없이도가능하므로, 실험용동물의불필요한희생을막을수 있으며, 생체내에서지방조직의이동및 생성, 소멸을장기간동안관찰할수 있다. 따라서본 발명의화학식 1 또는 2로표시된 3-인돌리논유도체또는그의염을포함하는스크리닝키트는대사증후군치료약물의개발에유용하게사용될수 있다.
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公开(公告)号：KR1020130023635A
公开(公告)日：2013-03-08
申请号：KR1020110086553
申请日：2011-08-29
Applicant: 한국화학연구원
IPC: A61K31/404 , C07D209/04 , G01N33/15 , A61P3/00
Abstract: PURPOSE: A method for screening a therapeutic drug for metabolic syndrome using 3- indolinone derivatives is provided to specifically and sensitively stain only fat tissues, and to confirm the amount of fat tissues. CONSTITUTION: A method for screening a therapeutic drug for metabolic syndrome using 3-indolinone derivatives comprises: a step of administering an indolinone derivative and a candidate drug to an animal model; and a step of analyzing a fluorescence image of the animal model. A kit for screening a therapeutic drug for metabolic syndrome contains the indolinone derivative or a salt thereof.
Abstract translation: 目的：提供使用3-二氢吲哚酮衍生物筛选代谢综合征治疗药物的方法，以特异性地敏感地仅染色脂肪组织，并确认脂肪组织的量。 构成：使用3-二氢吲哚酮衍生物筛选代谢综合征治疗药物的方法包括：向动物模型施用吲哚啉酮衍生物和候选药物的步骤; 以及分析动物模型的荧光图像的步骤。 用于筛选代谢综合征治疗药物的试剂盒含有二氢吲哚酮衍生物或其盐。
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公开(公告)号：KR101051057B1
公开(公告)日：2011-07-21
申请号：KR1020080111603
申请日：2008-11-11
Applicant: 한국화학연구원
IPC: A61K31/165 , A61P21/00
Abstract: 본 발명은 하이드록시아마이드 유도체를 이용한 신경전구세포(neural precursor cell) 또는 줄기세포(stem cell)의 신경세포로의 분화 유도용 조성물 및 이를 이용하여 신경전구세포 또는 줄기세포를 신경세포로 분화시키는 방법에 관한 것으로, 본 발명에 따라 하이드록시아마이드 유도체를 이용하여 분화된 신경세포는 신경 손상 질환의 치료에 효과적으로 사용될 수 있다.
하이드록시아마이드 유도체, 신경전구세포, 줄기세포, 신경세포Abstract translation: 如何实现本发明，以区分具有神经祖细胞中的羟基酰胺衍生物（神经前体细胞）或干细胞的神经祖细胞或分化诱导组合物干细胞和（干细胞）使用它们的神经元细胞为神经元 根据本发明，使用羟基酰胺衍生物分化的神经元细胞可以有效地用于治疗神经损伤疾病。
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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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Patent Agency Ranking
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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17.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-
公开(公告)号：KR1020030032592A
公开(公告)日：2003-04-26
申请号：KR1020010064474
申请日：2001-10-18
IPC: C07F1/06
CPC classification number: C07C235/84 , A61K31/166
Abstract: PURPOSE: Provided are a preparation method of 1,2-naphthoquinone derivatives of formula(1) and their pharmaceutically acceptable salt which inhibit the activity of protein phosphatase. The compounds are widely used in treatment of type 1 and 2 diabetes, autoimmune diseases, acute and chronic infection and various cancers. CONSTITUTION: The method of preparation of 1,2-naphthoquinone derivatives represented by the formula(1) as defined in the specification and their pharmaceutically acceptable salt comprises the steps of: oxidizing a naphthol compound of formula(2) with selenium oxides and obtaining a compound of formula(3); and substituting B at 4 position of the compound(3) using mixtures selected from (Pb(OAc)2),CeCl3 7H2O and NaIO3 mixture and RMgX and CuCN mixture.
Abstract translation: 目的：提供抑制蛋白磷酸酶活性的式（1）的1,2-萘醌衍生物及其药学上可接受的盐的制备方法。 该化合物广泛用于治疗1型和2型糖尿病，自身免疫性疾病，急性和慢性感染和各种癌症。 构成：由说明书中定义的式（1）表示的1,2-萘醌衍生物及其药学上可接受的盐的制备方法包括以下步骤：用氧化硒氧化式（2）的萘酚化合物，得到 式（3）化合物; 并且使用选自（Pb（OAc）2），CeCl 3·7H 2 O和NaIO 3混合物的混合物和RMgX和CuCN混合物在化合物（3）的4位置取代B。
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公开(公告)号：KR101791501B1
公开(公告)日：2017-10-30
申请号：KR1020150191020
申请日：2015-12-31
Inventor： 김기영 , 이상달 , 김희연 , 정원훈 , 안진희 , 강승규 , 서지희 , 배명애 , 신대섭 , 유욱준 , 이진수 , 김원태 , 정지성 , 김영훈 , 배현주 , 이주희 , 양은영 , 오세환 , 김영하
IPC: C07D277/04 , C07D417/06 , C07D413/06 , C07D409/06 , C07D279/12 , C07D265/30
Abstract: 본발명은 11β-하이드록시스테로이드디하이드로게나제타입 1(11-hydroxystreroid dehydrogenase type1,11-HSD1)의활성을억제하는하기화학식 1로표시되는아다만틸기를갖는헤테로고리카복스아미드유도체, 그의프로드럭, 그의용매화물, 그의입체이성질체또는약제학적으로허용가능한그의염, 이의제조방법및 이를유효성분으로함유하는약제학적조성물에관한것이다. [화학식 1]상기화학식 1에서, W, X, R, R, L, a 및 b은발명의상세한설명에서정의한바와같다.
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