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21.发明授权ＴＡＬＬＹＨＯ／ＪｎｇＪ 마우스를 이용한 골다공증 및골대사 이상 질환 예방 또는 치료용 조성물의 스크리닝방법 有权使用TALLYHO / JngJ小鼠预防或治疗骨质疏松症和代谢性骨病的组合物筛选方法
公开(公告)号：KR101322390B1
公开(公告)日：2013-10-29
申请号：KR1020070098323
申请日：2007-09-28
Applicant: 한국화학연구원
IPC: C12N15/12
CPC classification number: A01K67/027 , A01K2227/105 , A01K2267/03
Abstract: 본 발명은 TALLYHO/JngJ 마우스를 이용한 골다공증 및 골대사 이상 질환 예방 또는 치료용 조성물의 스크리닝 방법에 관한 것으로, 보다 구체적으로 골다공증 신약 개발 시 동물에서의 약효를 평가할 때 통상적으로 사용되는 난소적출 동물 대신에 TALLYHO/JngJ 마우스을 이용함으로서 조골세포 분화 촉진, 파골세포 분화 억제, 혈청 내의 사이토카인 변화 등의 골 재생 활성 평가를 통해 골다공증을 포함한 골대사 이상으로 파생되는 질환군에 대한 치료 및 예방 효과를 지니는 화합물을 스크리닝하는 방법에 관한 것이다. 본 발명의 TALLYHO/JngJ 마우스를 이용한 스크리닝 방법은 종래 난소적출 동물을 이용한 방법에 비하여 실험과정이 용이하고 안정적일 뿐만 아니라 골다공증 이외에도 골대사 이상 질환에 대한 간접적인 약효를 예측하는데 유용하게 이용될 수 있다.
TALLYHO/JngJ 마우스, 골다공증 질환동물 모델-
22.发明公开티에노피리미딘 유도체, 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨 관련 질환의 예방 또는 치료용 약학적 조성물 有权噻吩并嘧啶衍生物，其药学上可接受的盐的制备方法和用于预防或治疗含有其作为活性成分的糖尿病相关疾病的药物组合物
公开(公告)号：KR1020120127309A
公开(公告)日：2012-11-21
申请号：KR1020120050290
申请日：2012-05-11
Applicant: 한국화학연구원
IPC: C07D495/04 , A61K31/519 , A61P3/00 , A61P9/00
CPC classification number: C07D401/12 , C07D495/04
Abstract: PURPOSE: A pharmaceutical composition containing novel thienopyrimidine derivative for preventing or treating various diabetic diseases is provided to enhance saccharide-dependent insulin secretion and to improve saccharide and lipid metabolism. CONSTITUTION: A thienopyrimidine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating diabetic diseases contains the thienopyrimidine derivative of chemical formula 1, a pharmaceutically acceptable salt thereof, or solvate thereof as an active ingredient. The pharmaceutical composition is used by oral or parenteral administration. The daily dose of the pharmaceutical composition is 0.01-100 mg/kg.
Abstract translation: 目的：提供含有新型噻吩并嘧啶衍生物用于预防或治疗各种糖尿病疾病的药物组合物，以增强糖依赖性胰岛素分泌和改善糖和脂质代谢。 构成：噻吩并嘧啶衍生物由化学式1表示。用于预防或治疗糖尿病的药物组合物含有化学式1的噻吩并嘧啶衍生物，其药学上可接受的盐或其溶剂化物作为活性成分。 药物组合物通过口服或肠胃外给药使用。 药物组合物的日剂量为0.01-100mg / kg。
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公开(公告)号：KR1020120111347A
公开(公告)日：2012-10-10
申请号：KR1020110029772
申请日：2011-03-31
Applicant: 한국화학연구원
IPC: C07C311/43 , C07C311/41 , A61K31/18 , A61P3/10
Abstract: PURPOSE: An arylsulfoneamide derivative comprising a cyclopropyl group is provided to have excellent 11B-HSD1 restraining activity and to treat or prevent diseases like hardening of the arteries, osteoporosis, damaged glucose resistance, etc which are carried by 11B-HSD1. CONSTITUTION: An arylsulfoneamide derivative comprising a cyclopropyl group or a pharmaceutically acceptable salt thereof is represented by chemical formula 1. In chemical formula 1, if R^1 and R^2 is cyclopropyl then R^3 is methyl, if R^3 is cyclopropyl then R^1 and R^2 is respectively hydrogen, Ar is a functional group in chemical formula 1-a, a functional group in chemical formula 1-b, a functional group in chemical formula 1-c or naphthyl, R^a is respectively and independently methyl, isopropyl, t-butyl, C1-6 alkyl, methoxy, OCF3, halogen or CF3, and R^b and R^c is respectively and independently hydrogen, methyl, halogen or CF3.
Abstract translation: 目的：提供包含环丙基的芳基砜酰胺衍生物，以具有优异的11B-HSD1抑制活性，并治疗或预防由11B-HSD1携带的动脉硬化，骨质疏松症，损伤的葡萄糖耐药性等疾病。 构成：包含环丙基的芳基磺酰胺衍生物或其药学上可接受的盐由化学式1表示。在化学式1中，如果R 1和R 2是环丙基，则R 3是甲基，如果R 3是环丙基 那么R 1和R 2分别是氢，Ar是化学式1-a中的官能团，化学式1-b中的官能团，化学式1-c中的官能团或萘基，R 1 a 分别独立地为甲基，异丙基，叔丁基，C 1-6烷基，甲氧基，OCF 3，卤素或CF 3，R 1b和R cc分别独立地为氢，甲基，卤素或CF 3。
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24.发明公开ＴＡＬＬＹＨＯ／ＪｎｇＪ 마우스를 이용한 골다공증 및골대사 이상 질환 예방 또는 치료용 조성물의 스크리닝방법 有权使用TALLYHO / JNGJ小鼠预防或治疗骨质疏松和代谢性骨髓疾病的组合物的筛选方法
公开(公告)号：KR1020090032809A
公开(公告)日：2009-04-01
申请号：KR1020070098323
申请日：2007-09-28
Applicant: 한국화학연구원
IPC: C12N15/12
CPC classification number: A01K67/027 , A01K2227/105 , A01K2267/03
Abstract: A method for screening medicine for treatment and prevention of osteoporosis and metabolic bone disease using TALLYHO/JngJ mouse is provided to facilitate an examination process. A method for screening medicine for treatment and prevention of osteoporosis and metabolic bone disease comprises the following steps of: injecting medicine candidates for treating osteoporosis and metabolic bone disease to a TALLYHO/JngJ male mouse; measuring an index value correlated to osteoporosis and metabolic bone disease from the medicine candidate-injected mouse; and selecting medicine candidates which change the index values of the medicine candidate-injected mouse by comparing to a control group to which the medicine candidate is not injected.
Abstract translation: 提供了使用TALLYHO / JngJ小鼠筛选药物治疗和预防骨质疏松症和代谢性骨病的方法，以便于检查过程。 一种用于治疗和预防骨质疏松症和代谢性骨病的药物的方法，包括以下步骤：向TALLYHO / JngJ雄性小鼠注射用于治疗骨质疏松症和代谢性骨病的候选药物; 从候选药物注射的小鼠中测量与骨质疏松症和代谢性骨病相关的指标值; 并且通过与不注射药物候选者的对照组进行比较来选择改变注射了候选药物的小鼠的指标值的候选药物。
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25.发明公开1,3,5-트리아진-2,4,6-트리아민 화합물 또는 그의 약학적으로 허용 가능한 염, 및 이를 포함하는 약학적 조성물 失效1,3,5-三氮杂-2,4,6-三胺化合物或其药学上可接受的盐，以及包含其的药物组合物
公开(公告)号：KR1020090023245A
公开(公告)日：2009-03-04
申请号：KR1020080084723
申请日：2008-08-28
Applicant: 한올바이오파마주식회사 , 한국화학연구원
IPC: C07D251/56 , A61K31/53 , A61P3/10
CPC classification number: C07D251/70 , A61K31/53 , C07D251/54 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
Abstract: A pharmaceutical composition containing a 1,3,5-triazine-2,4,6-triamine compound or pharmaceutically allowable salts thereof is provided to prevent and treat metabolic syndrome, diabetes, or p53-deficient cancer. A pharmaceutical composition comprises a 1,3,5-triazine-2,4,6-triamine compound represented by the formula 1. In the formula 1, R1 and R2 independently show hydrogen or a C1-C5 alkyl group; and R3 and R4 independently indicate hydrogen, C1-C7 alkyl, C3-C7 cycloalkyl, phenyl, phenyl (C1-C3)alkyl, naphthyl, naphthyl (C1-C3)alkyl, (C3-C7)heterocycloalkyl (C1-C6)alkyl, heteroaryl, or a heteroaryl (C1-C6)alkyl group or form a (C3-C8)heterocycloalkyl group with nitrogen which is bonded with R3 and R4.
Abstract translation: 提供含有1,3,5-三嗪-2,4,6-三胺化合物或其药学上允许的盐的药物组合物以预防和治疗代谢综合征，糖尿病或p53缺陷型癌症。 药物组合物包含由式1表示的1,3,5-三嗪-2,4,6-三胺化合物。在式1中，R 1和R 2独立地表示氢或C 1 -C 5烷基; 并且R 3和R 4独立地表示氢，C 1 -C 7烷基，C 3 -C 7环烷基，苯基，苯基（C 1 -C 3）烷基，萘基，萘基（C 1 -C 3）烷基，（C 3 -C 7）杂环烷基（C 1 -C 6） ，杂芳基或杂芳基（C1-C6）烷基或与R3和R4键合的氮形成（C 3 -C 8）杂环烷基。
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Patent Agency Ranking
公开(公告)号：KR1020080012621A
公开(公告)日：2008-02-12
申请号：KR1020060073717
申请日：2006-08-04
Applicant: 한국화학연구원 , 한올바이오파마주식회사
IPC: C07D307/68 , A61K31/341 , A61P3/10 , A61P3/06
CPC classification number: C07D307/68
Abstract: Furan-2-carboxylic acid derivatives are provided to inhibit formation of sugars or lipids and promote absorption of sugars by activating AMPK(AMP(adenosine monophosphate)-activated protein kinase), so that the furan-2-carboxylic acid derivatives are useful for prevention and treatment of metabolic syndrome including diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver and steatohepatitis. Furan-2-carboxylic acid derivatives represented by the formula(1), wherein X is hydrogen or halogen, n is 1, 2 or 3, m is 0, 1 or 2 and R is hydrogen or C1-4 alkyl, are prepared by reacting compounds represented by the formula(2) with compounds represented by the formula(3) in organic solvent in the presence of base in which Y is triphenylphosphonium bromide salt, triphenylphosphonium iodide salt or benzothiazol-2-sulfonyl. A composition for prevention or treating metabolic syndrome comprises the furan-2-carboxylic acid derivatives represented by the formula(1).
Abstract translation: 提供呋喃-2-羧酸衍生物以抑制糖或脂质的形成，并通过活化AMPK（AMP（腺苷一磷酸）活化的蛋白激酶）促进糖的吸收，使得呋喃-2-羧酸衍生物可用于预防 和代谢综合症的治疗，包括糖尿病，肥胖症，高脂血症，高胆固醇血症，脂肪肝和脂肪性肝炎。 由式（1）表示的呋喃-2-羧酸衍生物，其中X是氢或卤素，n是1,2或3，m是0,1或2，R是氢或C 1-4烷基，是由 将式（2）表示的化合物与式（3）表示的化合物在有机溶剂中，在Y是三苯基溴化鏻盐，三苯基碘化鏻盐或苯并噻唑-2-磺酰基的碱存在下反应。 用于预防或治疗代谢综合征的组合物包括由式（1）表示的呋喃-2-羧酸衍生物。
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27.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：KR100547193B1
公开(公告)日：2006-01-31
申请号：KR1020030035444
申请日：2003-06-02
Applicant: 한국화학연구원 , 씨제이 주식회사 , 제일파마홀딩스 주식회사
IPC: C07D403/06
Abstract: 본 발명은 하기 화학식 1의 신규한 시아노-피라졸린 유도체와 이의 약학적으로 허용가능한 염 및 이의 제조 방법에 관한 것이다. 본 발명의 시아노-피라졸린 유도체는 디펩티딜 펩티다제-IV(DPP-IV)의 활성을 억제하므로 이를 포함하는 약학 조성물은 DPP-IV에 의해서 매개되는 인슐린 의존성, 비인슐린 의존성 당뇨병, 관절염, 비만, 골다공증 및 손상된 글루코스 내성과 같은 질환의 치료제로서 매우 유용하다:
상기 식에서, A는 또는 이고,
상기 식에서, R
1 은 서로 같거나 다른 하나 또는 두 개의 C
1 -C
4 알킬, C
1 -C
4 알콕시, 할로겐, 트리플루오르메틸, 시아노 또는 니트로로 치환된 피리디닐, 피리미디닐 또는 페닐 잔기이고;
R
2 는 서로 같거나 다른 하나 또는 두 개의 C
1 -C
4 알킬, C
1 -C
4 알콕시, 할로겐, 트리플 루오르메틸, 시아노 또는 니트로로 치환된 피리디닐, 피리미디닐, 페닐 또는 치환되지 않거나 서로 같거나 다른 하나 또는 두 개의 할로겐, 트리플루오르메틸, 시아노 또는 니트로로 치환된 벤조일 잔기이고;
R
3 은 치환된 아다만틸이고;
R
4 는 서로 같거나 다른 하나 또는 두 개의 수소, 하이드록시, C
1 -C
4 알킬, C
1 -C
4 알콕시, 또는 할로겐이다.Abstract translation: 本发明涉及式（I）的新型氰基 - 吡唑啉衍生物，其药学上可接受的盐及其制备。 本发明吡唑啉衍生物的氰基的二肽基肽-IV包括相同的，所以抑制（DPP-IV）的活性的药物组合物是胰岛素依赖由DPP-IV介导的，非胰岛素依赖型糖尿病，关节炎， 肥胖，骨质疏松和葡萄糖耐量降低。
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公开(公告)号：KR100524699B1
公开(公告)日：2005-11-01
申请号：KR1020030024557
申请日：2003-04-18
Applicant: 한국화학연구원
IPC: C07D265/02
Abstract: 본 발명은 사이클로펜타[
d ][1,2]-옥사진 유도체에 관한 것으로서, 더욱 상세하게는 신규 구조를 가지는 사이클로펜타[
d ][1,2]-옥사진 유도체와, 상기한 신규 화합물이 PTP1B(protein tyrosine phosphatase 1B), Prl-3, CD45, LAR(Leukocyte Antigen-Related), Cdc25A, Cdc25B, Cdc25C, Yop, PP1, VHR(vaccina human-related)과 같은 단백질 포스파타제(protein phosphatase, PPase)에 대한 약리학적 억제활성이 우수하므로 신규 화합물 또는 이들의 약제학적으로 허용 가능한 염을 자가면역 질병, 급성 및 만성 염증, 제1형 및 제2형 당뇨병, 손상된 글루코스 내성, 인슐린 저항성, 비만, 암 및 악성질병 등과 관련된 질병의 치료 및 예방제로 사용하는 용도에 관한 것이다.-
公开(公告)号：KR1020040104054A
公开(公告)日：2004-12-10
申请号：KR1020030035443
申请日：2003-06-02
Applicant: 한국화학연구원 , 씨제이 주식회사 , 제일파마홀딩스 주식회사
IPC: C07D231/04 , A61P3/10 , C07D213/81 , C07D213/83
Abstract: PURPOSE: Pyrazolidine derivatives comprising acyl group and pharmaceutical acceptable salts thereof, and a method for the preparation thereof are provided, which derivatives have improved DPP-IV(dipeptidyl peptidase-IV) inhibiting activity, so that they are useful for treatment of disease associated with DPP-IV, such as insulin or non-insulin dependent diabetes, arthritis, obeseness, osteoporosis and damaged glucose resistance. CONSTITUTION: The pyrazolidine derivatives comprising acyl group represented by formula (1) or pharmaceutical acceptable salts thereof are provided, wherein R1 is the same or different, and hydrogen, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-C4 alkyl, C1-C4 haloalkyl, C1-C7 alkoxy, C1-C4 alkylamino, C1-C4 alkylthio, C1-C4 alkylamide, C1-C4 acylamide, C1-C4 acyloxy, C1-C4 alkylsulfoneamide, C1-C4 alkylsulfonate, imidic acid C1-C4 alkylester, thioimidic acid C1-C4 alkylester, methyl substituted with hydroxy, amino, cyano, morpholine, acetate, acetamide or methanesulfonamide, phenyl substituted with C1-C4 haloalkyl, C1-C4 alkoxy or halogen, or benzyloxy substituted with C1-C4 haloalkyl, C1-C4 alkoxy or halogen; m is 1 or 2; n is 0 or 1; X is O, S or N-CN; ACO is a group of formula (2) or formula (3); R2 is a substituent present in alanine, arginine, aspartic acid, cysteine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, hydroxyproline, serine, threonine, tryptophane, tyrosine, valine, cyclohexylglycine, threonine, isoleucine-isoleucine, isoleucine-valine, valine-isoleucine, proline-isoleucine or isoleucine-proline; and R3 is C1-C6 alkyl, hydrogen or benzoylamide substituted C5-C8 cycloalkyl, hydrogen or hydroxy substituted adamantyl, morpholine or C1-C4 alkyl substituted piperazine, hydroxy or C1-C4 alkyl substituted piperazine, or ethylamino pyridine substituted with cyano, halogen, nitro or C1-C4 haloalkyl.
Abstract translation: 目的：提供包含酰基的吡唑烷衍生物及其药学上可接受的盐及其制备方法，该衍生物具有改善的DPP-IV（二肽基肽酶-IV）抑制活性，因此它们可用于治疗与 DPP-IV，例如胰岛素或非胰岛素依赖性糖尿病，关节炎，肥胖，骨质疏松症和损伤的葡萄糖耐药性。 提供了包含式（1）表示的酰基的吡唑烷衍生物或其药学上可接受的盐，其中R 1相同或不同，氢，卤素，氰基，硝基，羟基，氨基，CO 2 H，CONH 2，CSNH 2，脒 ，C1-C4烷基，C1-C4卤代烷基，C1-C7烷氧基，C1-C4烷基氨基，C1-C4烷硫基，C1-C4烷基酰胺，C1-C4酰基酰胺，C1-C4酰氧基，C1-C4烷基磺酰胺，C1-C4烷基磺酸酯 ，亚氨酸C 1 -C 4烷基酯，硫代亚氨酸C 1 -C 4烷基酯，被羟基，氨基，氰基，吗啉，乙酸酯，乙酰胺或甲磺酰胺取代的甲基，被C 1 -C 4卤代烷基，C 1 -C 4烷氧基或卤素取代的苯基或苄氧基取代 与C 1 -C 4卤代烷基，C 1 -C 4烷氧基或卤素; m为1或2; n为0或1; X是O，S或N-CN; ACO是式（2）或式（3）的一组; R2是存在于丙氨酸，精氨酸，天冬氨酸，半胱氨酸，谷氨酸，甘氨酸，组氨酸，异亮氨酸，亮氨酸，赖氨酸，甲硫氨酸，苯丙氨酸，脯氨酸，羟脯氨酸，丝氨酸，苏氨酸，色氨酸，酪氨酸，缬氨酸，环己基甘氨酸，苏氨酸， 异亮氨酸 - 异亮氨酸，异亮氨酸 - 缬氨酸，缬氨酸 - 异亮氨酸，脯氨酸 - 异亮氨酸或异亮氨酸 - 脯氨酸; 氢或羟基取代的金刚烷基，吗啉或C 1 -C 4烷基取代的哌嗪，羟基或C 1 -C 4烷基取代的哌嗪或被氰基，卤素取代的乙基氨基吡啶， 硝基或C 1 -C 4卤代烷基。
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