Abstract:
본 발명은 티아졸 유도체가 치환된 신규한 벤즈아미딘 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학 조성물에 관한 것이다. 본 발명의 티아졸 유도체가 치환된 벤즈아미딘 유도체는 매우 낮은 농도에서 파골세포에 대한 분화를 효과적으로 억제하며, 조골세포에 대한 활성이 우수하여 골다공증의 예방 및 치료에 유용하게 사용될 수 있다. 또한, 본 발명의 티아졸 유도체가 치환된 벤즈아미딘 유도체는 골절시 형성된 가골의 소실 및 가골의 골화를 촉진시켜 골절 치료제로 유용하게 사용될 수 있으며, 천식시 유발되는 만성염증을 감소시킴으로, 천식을 포함한 알러지성 염증성 질환의 예방 및 치료에 유용하게 사용할 수 있다. 벤즈아미딘 유도체
Abstract:
PURPOSE: Provided are a three-dimensional structure of TRAIL-sDR5 complex of a human derived apoptotic factor and a receptor thereof by X-ray crystallography and TRAIL(TNF Related Apoptosis Inducing Ligand) deletion mutant protein. CONSTITUTION: TRAIL-sDR5 complex is prepared by mixing TRAIL protein of SEQ ID NO:1 and sDR5 protein of SEQ ID NO:2. It can be crystallization method comprises the steps of: injecting a solution consisting of 16% of polyethyleneglycol 3000, 0.05M of sodium acetate(pH 4.5), 0.22 M of sodium acetate and 0.6M of sodium chloride into a well; mixing the precipitation solution and protein solution in a mixing ratio of 1:1 on the surface of a cover slip; and covering the well with the cover slip to crystallize the protein.
Abstract translation:目的:提供通过X射线晶体学和TRAIL(TNF相关凋亡诱导配体)缺失突变蛋白的人源性凋亡因子及其受体的TRAIL-sDR5复合物的三维结构。 构成:通过混合SEQ ID NO:1的TRAIL蛋白和SEQ ID NO:2的sDR5蛋白来制备TRAIL-sDR5复合物。 结晶方法包括以下步骤:将由16%聚乙二醇3000,0.05M乙酸钠(pH4.5),0.22M乙酸钠和0.6M氯化钠组成的溶液注入孔中; 将沉淀溶液和蛋白质溶液以1:1的混合比混合在盖板的表面上; 并用盖子覆盖井,使蛋白质结晶。
Abstract:
PURPOSE: A 2,6-site-substituted 3-nitropyridine derivative compound is provided to suppress formation of osteroclast and to use in preventing and treating osteroporosis. CONSTITUTION: A novel 2,6-substituted 3-nitro derivative compound is denoted by chemical formula 1. A method for manufacturing the 2,6-substituted 3-nitro derivative compound comprises: a step of reating 2,6-dichloro-3-nitropyridine and 5-aminoindazole under the presence of base to prepare 2(1H-indazole-5-yl)amino-6-chloro-3-nitropyridine; and a step of reacting an amine compound of 2-methyl-2-imidazoline, 2-methyl imidazole, 2-isopropylimidazol, or 5-methyl imidazole with 2(1H-indazole-5-yl)amion-6-chloro-3-nitropyridine. A composition for preventing or treating osteoporosis contains the 3-nitropyridine derivative compound or salt thereof.
Abstract:
PURPOSE: A 3-nitropyridine derivative compound which is substituted at 2,6-site is provided to suppress differentiation of osteoclast and to prevent and treat osteoporosis. CONSTITUTION: A 3-nitropyridine derivative compound which is substituted at 2,6-site is denoted by chemical formula 1. A method for preparing the 3-nitropyridine derivative compound comprises: a step of reacting aniline compound of chemical formula 3 with 2,6-dichloro-3-nitropyridine under the presence of base to obtain a 6-chloro-3-nitropyridine derivative compound of chemical formula 4; and a step of reacting amine compound of chemical formula 5 with a compound of chemical formula 4 to obtain the 3-nitropyridine derivative compound. A pharmaceutical composition for preventing or treating osteoporosis contains the 3-nitropyridine derivative or pharmaceutically acceptable salt as an active ingredient.
Abstract:
PURPOSE: A composition for preventing and treating osteoporosis is provided to suppress osteoclast and bone absorption by using two kinds of compounds. CONSTITUTION: A composition for preventing or treating osteoporosis contains N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thizole-4-yl)phenoxy]pentoxy}benzamidine of chemical formula 1, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazole-4-yl)phenoxy]pentoxy}benzamidine compound of chemical formula 2, alendronic acid of chemical formula 3 or its salt as an active ingredient.
Abstract:
PURPOSE: Provided is N,N-diisopropyl-4-(7-(4-aminophenoxy)heptoxy)-3-methoxybenzamide(DW1259) which has leukotriene-B4 receptor antagonistic action and has excellent effects on inhibition of bone absorption by effectively inhibiting the function of osteoclast cells. CONSTITUTION: The agent for prophylaxis and treatment of osteoporosis contains an effective amount of N,N-diisopropyl-4-(7-(4-aminophenoxy)heptoxy)-3-methoxybenzamide of formula(1). The compound has an excellent inhibition effect on a differentiation, formation, fusion process and bone absorption function of osteoclast cells, is excellent in an inhibition function of osteoclast cells as compared to any compound such as DW1231, DW1234, DW1166, DW1235 having structural similarity as well as HS-1141 and CGS-25019C and has increased efficacy in increasing the activity of osteoblast cells.
Abstract:
PURPOSE: Provided are a detecting method of hepatitis C virus(HCV) using recombinant mixed antigens derived from HCV and a diagnostic kit thereof, particularly by immuno chromatography using recombinant mixed antigens including core, NS3 and NS5A proteins of HCV gene as main components. CONSTITUTION: A recombinant Baculovirus(KCCM 10218) is manufactured by cotransfection of Baculovirus transfer vector including HCV derived core protein gene. HCV derived core protein is expressed from the recombinant Baculovirus(KCCM 10218) and has amino acid sequence of SEQ ID NO: 8. A recombinant Baculovirus(KCCM 10219) is manufactured by cotransfection of Baculovirus transfer vector including HCV derived NS3 protein gene. HCV derived NS3 proteins expressed from the recombinant Baculovirus(KCCM 10219) and has amino acid sequence of SEQ ID NO:9. An E.coli transformant(KCCM 10217) is transformed with a recombinant expression vector including HCV derived NS5A protein gene. HCV derived NS5A protein is expressed from the transformant and has amino acid sequence of SEQ ID NO: 10. The HCV diagnostic kit contains a mixed antigen consisting of core, NS3 and NS5A proteins derived from HCV.
Abstract translation:目的:提供使用HCV衍生的重组混合抗原的丙型肝炎病毒(HCV)的检测方法及其诊断试剂盒,特别是使用包含HCV基因的核心,NS3和NS5A蛋白的重组混合抗原的免疫色谱作为主要成分。 构成:通过共转染包括HCV衍生的核心蛋白基因的杆状病毒转移载体来制备重组杆状病毒(KCCM 10218)。 HCV衍生的核心蛋白由重组杆状病毒(KCCM 10218)表达并具有SEQ ID NO:8的氨基酸序列。通过共转染包含HCV衍生的NS3蛋白基因的杆状病毒转移载体来制备重组杆状病毒(KCCM 10219)。 由重组杆状病毒(KCCM 10219)表达的HCV衍生的NS3蛋白,具有SEQ ID NO:9的氨基酸序列。 用包含HCV衍生的NS5A蛋白基因的重组表达载体转化大肠杆菌转化体(KCCM 10217)。 HCV衍生的NS5A蛋白由转化体表达,并具有SEQ ID NO:10的氨基酸序列。HCV诊断试剂盒含有由核心,NS3和源自HCV的NS5A蛋白组成的混合抗原。
Abstract:
PURPOSE: A 3-nitropyridine derivative compound in which 2,6-site is substituted is provided to suppress osteoclast formation and to prevent and treat osteoporosis. CONSTITUTION: A 3-nitropyridine derivative compound in which 2,6-site is substituted is denoted by chemical formula 1. A method for preparing the 3-nitropyridine derivative comprises: and a step of reacting 2,6dichloro-3-nitropyridine and 5-amino triazole under the presence of base to obtain 2-(1H-benzotriazole-5-yl)amino-6-chloro-3-nitropyridine with HNR_2(CH_2)nR1 amine compound to obtain 3-nitropyridine derivative in which 1,6 site of chemical formula 1. A pharmaceutical composition for preventing or treating osteoporosis contains 3-nitropyridine derivative compound or pharmaceutically acceptable salt as an active ingredient.
Abstract translation:目的:提供2,6-取代的3-硝基吡啶衍生物,以抑制破骨细胞形成和预防和治疗骨质疏松症。 构成:其中2,6-位被取代的3-硝基吡啶衍生物化合物由化学式1表示。制备3-硝基吡啶衍生物的方法包括:使2,6-二氯-3-硝基吡啶与5- 氨基三唑在碱存在下反应,得到2-(1H-苯并三唑-5-基)氨基-6-氯-3-硝基吡啶与HNR 2(CH 2)n R 1胺化合物,得到3-硝基吡啶衍生物,其中, 化学式1.用于预防或治疗骨质疏松症的药物组合物含有3-硝基吡啶衍生物化合物或药学上可接受的盐作为活性成分。
Abstract:
The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.