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公开(公告)号：KR100845511B1
公开(公告)日：2008-07-10
申请号：KR1020070029253
申请日：2007-03-26
Applicant: (주)아모레퍼시픽
IPC: C07D317/68 , A61K31/357
Abstract: A hydroxamic acid derivative is provided to induce the activity increase of each promoter of IDH3alpha and CPT1 involving with energy consumption metabolism, thereby being usefully used for preventing or treating diseases related to dyslipidemia such as obesity, hyperlipidemia and diabetes. A hydroxamic acid is represented by a formula(1), wherein R1 is CONH, NHCO, CONR4 or NR4CO(where R4 is H or C1-10 alkyl); R2 is -(CH2)n-(where n is 0 or 1); and R3 is H or C1-10 alkyl. A method for preparing the hydroxamic acid comprises the steps of: (a) reacting an anhydrous compound synthesized by reacting ethyl chloroformate with piperonic acid using pyridine or N-methyl morpholine as a solvent with methyl 4-amino benzoate or 4-amino phenyl acetic acid ethyl ester at a temperature of 10-20 deg.C using pyridine or N-methyl morpholine as a solvent to prepare a benzamide compound; (b) reacting the benzamide with an alkyl halide selected from the group consisting of bromomethane, bromoethane, bromopropane, bromo isopropane, bromo butane, and bromo tert-butane to substitute an amide bond of the benzamide with an alkyl group; (c) hydrolyzing methyl ester in the benzamide obtained from the step(a) or the benzamide compound obtained from the step(b) to prepare an acid and reacting the acid with ethyl chloroformate using pyridine or N-methyl morpholine as a solvent to covert the acid into an anhydrous compound; and (d) reacting the anhydrous compound with hydroxyl amine chloride or N-methyl hydroxyl amine chloride at a temperature of 0-10 deg.C using pyridine or N-methyl morpholine as a solvent to obtain the product of the formula(1). An agent for anti-obese, treating diabetes or hyperlipidemia comprises the hydroxamic acid.
Abstract translation: 提供异羟肟酸衍生物以诱导与能量代谢相关的IDH3α和CPT1的每种启动子的活性增加，从而有效地用于预防或治疗与脂肪血症如肥胖症，高脂血症和糖尿病有关的疾病。 异羟肟酸由式（1）表示，其中R1是CONH，NHCO，CONR4或NR4CO（其中R4是H或C1-10烷基）; R2是 - （CH2）n-（其中n是0或1）; 并且R 3是H或C 1-10烷基。 制备异羟肟酸的方法包括以下步骤：（a）使吡啶或N-甲基吗啉作为溶剂与4-氨基苯甲酸甲酯或4-氨基苯基乙酸反应，使氯甲酸乙酯与胡椒酸反应合成的无水化合物 乙酯，使用吡啶或N-甲基吗啉作为溶剂，在10-20℃的温度下制备苯甲酰胺化合物; （b）使苯甲酰胺与选自溴甲烷，溴乙烷，溴丙烷，溴异丙烷，溴丁烷和溴叔丁烷的烷基卤反应，以苯甲酰胺与烷基取代; （c）水解由步骤（a）获得的苯甲酰胺中的甲酯或由步骤（b）获得的苯甲酰胺化合物制备酸，并使用吡啶或N-甲基吗啉作为溶剂使酸与氯甲酸乙酯反应，从而使 将酸变成无水化合物; 和（d）使用吡啶或N-甲基吗啉作为溶剂，在0-10℃的温度下使无水化合物与羟胺或N-甲基羟胺氯化物反应，得到式（1）的产物。 用于抗肥胖，治疗糖尿病或高脂血症的药物包括异羟肟酸。
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22.发明授权ＩＤＨ３Ａ 프로모터 및 루시퍼라제 함유 벡터로형질전환된 세포주, 및 그를 이용한 비만억제 후보물질검색방법 失效与含有IDH3 ALPHA促进剂和促生长素的载体转染的细胞系以及使用其的肥料控制材料的搜索方法
公开(公告)号：KR100821457B1
公开(公告)日：2008-04-11
申请号：KR1020060117066
申请日：2006-11-24
Applicant: (주)아모레퍼시픽
Abstract: A transformed cell line is provided to identify a chemical material controlling expression of an IDH3A gene at a transcription step and also find out an anti-obese material such as genistein. An expression vector pIDH3A comprises: a kanamycin resistant gene(Kana+) and a neomycin resistant gene(Neo+); a luciferase gene(LUC+); and an IDH3A promoter of SEQ ID : NO. 1 and has a structure depicted in Fig. 2. A cell line PRDC IDH3A transformed by the expression vector is deposited as a deposition no. KCTC 10981BP. A method for searching an obesity controlling material comprises the steps of: (a) treating the cell line with an obesity controlling candidate material; and (b) detecting the fluorescence emitting reaction, wherein the obesity controlling candidate material is treated with at least two concentrations.
Abstract translation: 提供转化细胞系以鉴定在转录步骤中控制IDH3A基因表达的化学物质，并且还可以找到抗肥胖材料如染料木素。 表达载体pIDH3A包含：卡那霉素抗性基因（Kana +）和新霉素抗性基因（Neo +）; 荧光素酶基因（LUC +）; 和SEQ ID NO：1的IDH3A启动子。 具有图1所示的结构。 由表达载体转化的细胞系PRDC IDH3A沉积为沉积物。 KCTC 10981BP。 用于搜索肥胖控制材料的方法包括以下步骤：（a）用肥胖控制候选物质处理细胞系; 和（b）检测荧光发射反应，其中以至少两种浓度处理肥胖控制候选物质。
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公开(公告)号：KR101327028B1
公开(公告)日：2013-11-13
申请号：KR1020070005217
申请日：2007-01-17
Applicant: (주)아모레퍼시픽
Abstract: 본 발명은 TCA회로에서 ATP 생성에 관여하는 아이소사이트레이트 탈수소효소 3 알파(IDH3A)를 과발현하는 형질전환 생쥐(transgenic mouse) 및 그 제조방법에 관한 것으로 상세하게는 CMV 프로모터, IDH3A 유전자 및 폴리아데닐화 서열을 포함하는 발현벡터로 형질전환된 생쥐 및 이러한 생쥐의 제조방법에 관한 것이다. 이러한 형질전환 생쥐는 IDH3A를 과발현하는 결과 비만 억제 형질을 나타내므로 비만 치료 및 연구를 위한 모델 동물로 이용할 수 있다.
IDH3A, TCA회로, 형질전환 생쥐, 비만-
公开(公告)号：KR1020110011233A
公开(公告)日：2011-02-08
申请号：KR1020090068784
申请日：2009-07-28
Applicant: (주)아모레퍼시픽
IPC: A61K31/722 , A61P3/02 , A23L1/30
CPC classification number: A61K31/722 , A23L33/28 , A23V2002/00 , A23V2250/511 , A23V2200/33
Abstract: PURPOSE: An anti-fatigue composition containing chitooligosaccharide is provided to be variously used in health foods or the medicinal field. CONSTITUTION: An anti-fatigue composition contains chitooligosaccharide lactate as an active ingredient. The molecular weight of chitooligosaccharide is 700-90,000. The composition is a health food composition or pharmaceutical composition. The content of chitooligosaccharide is 10-90 weight%. A method for preparing chitooligosaccharide comprises: a step of pulverizing crab and shrimp shells and desalinating; a step of removing protein and impurities to obtain chitin; a step of performing deacetylation to obtain chitosan; and a step of performing chemical or enzyme decomposition of chitosan.
Abstract translation: 目的：提供含有壳低聚糖的抗疲劳组合物，用于保健食品或药用领域。 构成：抗疲劳组合物含有壳寡糖乳酸盐作为活性成分。 壳低聚糖的分子量为700-90,000。 组合物是保健食品组合物或药物组合物。 壳低聚糖的含量为10-90重量％。 一种制备壳寡糖的方法，其特征在于，包括：对蟹壳和虾壳进行粉碎和脱盐的步骤; 去除蛋白质和杂质以获得甲壳素的步骤; 进行脱乙酰化以获得壳聚糖的步骤; 以及进行壳聚糖的化学或酶分解的步骤。
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公开(公告)号：KR1020100028616A
公开(公告)日：2010-03-12
申请号：KR1020100015699
申请日：2010-02-22
Applicant: (주)아모레퍼시픽
Abstract: PURPOSE: An oral composition for preventing and treating obesity is provided to promote fat lysis and combustion using soybean extract, carnitine, caffeine and arginine. CONSTITUTION: An oral composition for preventing and treating obesity contains 0.0001-10 weight% of isoflavone, 0.001-40 weight% of L-carnitine, 0.0001-10 weight% of caffeine, and 0.001-40 weight% of arginine as an active ingredient. The isoflavone is a soybean extract containing the isoflavone. An inhibitor of abdomenal obesity contains the oral composition.
Abstract translation: 目的：提供一种用于预防和治疗肥胖症的口服组合物，以促进使用大豆提取物，肉碱，咖啡因和精氨酸的脂肪裂解和燃烧。 构成：用于预防和治疗肥胖症的口服组合物含有0.0001-10重量％的异黄酮，0.001-40重量％的L-肉毒碱，0.0001-10重量％的咖啡因和0.001-40重量％的精氨酸作为活性成分。 异黄酮是含有异黄酮的大豆提取物。 腹部肥胖的抑制剂含有口服组合物。
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Patent Agency Ranking
公开(公告)号：KR1020080087273A
公开(公告)日：2008-10-01
申请号：KR1020070029255
申请日：2007-03-26
Applicant: (주)아모레퍼시픽
IPC: C07C233/07 , C07C233/10
Abstract: A 3,5-dihydroxybenzoic acid derivative compound having anti-obesity activity is provided to obtain a pharmaceutical agent for preventing and treating diseases caused by abnormal fat metabolism, including obesity, hyperlipidemia, diabetes by inducing activation of IDH3-alpha and CPT1 promoters. A 3,5-dihydroxybenzoic acid derivative compound having anti-obesity activity is represented by the following formula 1, wherein R is adamantyl, cyclohexyl or hexyl. The 3,5-dihydroxybenzoic acid derivative compound includes N-adamantyl-3,5-dihydroxybenzamide, N-cyclohexyl-3,5-dihydroxybenzamide or N-hexyl-3,5-dihydroxybenzamide.
Abstract translation: 提供具有抗肥胖活性的3,5-二羟基苯甲酸衍生物化合物，以获得通过诱导IDH3-α和CPT1启动子的激活来预防和治疗由异常脂肪代谢引起的疾病，包括肥胖症，高脂血症，糖尿病的药剂。 具有抗肥胖活性的3,5-二羟基苯甲酸衍生化合物由下式1表示，其中R是金刚烷基，环己基或己基。 3,5-二羟基苯甲酸衍生物包括N-金刚烷基-3,5-二羟基苯甲酰胺，N-环己基-3,5-二羟基苯甲酰胺或N-己基-3,5-二羟基苯甲酰胺。
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公开(公告)号：KR1020080049175A
公开(公告)日：2008-06-04
申请号：KR1020060119449
申请日：2006-11-30
Applicant: (주)아모레퍼시픽
IPC: A61K31/722 , C08B37/00
CPC classification number: A61K31/722
Abstract: A composition comprising chito-oligosaccharide is provided to promote energy metabolism of liver cells by influencing on the AMPK(AMP-activated protein kinase) activity and lipid metabolism related enzymes. A composition for improving fatigue comprises 10-90 wt.% of chito-oligosaccharide having a molecular weight of 700-9,000 as an effective ingredient and is characterized in that it inhibits the ACC activity and promotes fatty acid oxidation. Further, a molecular weight of the chito-oligosaccharide is 700 to 9000.
Abstract translation: 提供包含低聚半乳糖的组合物，以通过影响AMPK（AMP活化蛋白激酶）活性和脂质代谢相关酶来促进肝细胞的能量代谢。 用于改善疲劳的组合物包含10-90重量％的分子量为700-9,000的低聚半乳糖作为有效成分，其特征在于其抑制ACC活性并促进脂肪酸氧化。 而且，低聚半乳糖的分子量为700〜9000。
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公开(公告)号：KR100829691B1
公开(公告)日：2008-05-16
申请号：KR1020060119575
申请日：2006-11-30
Applicant: (주)아모레퍼시픽
IPC: A61K36/904 , A61K36/70 , A61P3/04
Abstract: 본 발명에 의한 지질 분해 촉진용 조성물은 사간 추출물, 갈퀴덩굴 추출물, 여뀌 추출물, 울릉국화 추출물 및 파드득나물 추출물로 구성된 군으로부터 선택된 하나 이상의 추출물을 유효성분으로 함유함으로써, IDH3α 유전자 프로모터의 활성을 유도하여 TCA 회로를 활성화시키고 이를 통해 지질의 산화 분해를 촉진시키는 기능을 하며, 더 나아가 비만의 치료 또는 예방, 고지혈증의 치료 또는 예방에 이용될 수 있다.
비만, IDH3α, TCA 회로, 갈퀴덩굴, 여뀌, 울릉국화, 파드득나물, 생약, 사간, 지질 분해-
公开(公告)号：KR1020080042349A
公开(公告)日：2008-05-15
申请号：KR1020060110640
申请日：2006-11-09
Applicant: (주)아모레퍼시픽
IPC: A61K31/352 , A61P3/04
Abstract: A composition comprising genistein is provided to inhibit activation of SREBP-1(sterol regulatory element binding protein-1) related to the expression of genes associated with neutral fat synthesis, and expression of fatty acid synthase(FAS) by inhibiting site-1-protease(S1P), so that the composition is useful for development of anticancer agents and anti-obesity agents. A composition for inhibiting site-1-protease(S1P) comprises 0.001-0.1 wt.% of genistein(5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) which is isolated from plants including soybean, arrowroot, clover and apple, and is formulated as powder, granule, tablet, capsule, suspension, emulsion, syrup, aerosol, ointment, cream, suppository or sterile injection, wherein the daily dosage of genistein is 0.001-100 mg/kg. Further, the virus is Bombyx mori Nuclear Polyhedrosis Virus or Autographa californica Nuclear Polyhedrosis Virus.
Abstract translation: 提供了包含染料木素的组合物以抑制与中性脂肪合成相关基因表达相关的SREBP-1（固醇调节元件结合蛋白-1）的活化，以及通过抑制位点-1蛋白酶表达脂肪酸合酶（FAS） （S1P），使得该组合物可用于抗癌剂和抗肥胖剂的开发。 用于抑制位点-1-蛋白酶（S1P）的组合物包含0.001-0.1重量％的染料木黄酮（5,7-二羟基-3-（4-羟基苯基）-4H-1-苯并吡喃-4-酮），其从 植物包括大豆，竹芋，三叶草和苹果，并配制成粉末，颗粒，片剂，胶囊，悬浮液，乳剂，糖浆，气雾剂，软膏，霜剂，栓剂或无菌注射剂，其中染料木素的日剂量为0.001-100mg /公斤。 此外，病毒是家蚕核多角体病毒或苜蓿银纹夜蛾核多角体病毒。
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公开(公告)号：KR100701269B1
公开(公告)日：2007-03-29
申请号：KR1020060129745
申请日：2006-12-19
Applicant: (주)아모레퍼시픽
CPC classification number: A23L33/11 , A23V2002/00 , A23V2200/332 , A23V2250/20
Abstract: A food composition for improving and preventing obesity is provided to promote a beta oxidation of fatty acids effectively, and prevent and reduce an accumulation of excessive fat. The food composition for improving and preventing obesity contains coumestrol, a coumesterol-containing natural materials or an extract thereof as an active component. The active component promotes expression of Carnitine Palmitoyl Transferase 1A gene to increase a beta oxidation of fatty acids. The food composition for improving and preventing obesity is formulated into drink, diet bar, chocolate, caramel, or confectionery. The coumestrol is contained in an amount of 0.02-10wt% based on the total composition.
Abstract translation: 提供用于改善和预防肥胖症的食物组合物，用于有效促进脂肪酸的β氧化，并防止和减少过量脂肪的积累。 用于改善和预防肥胖症的食物组合物含有作为活性成分的香豆素，含有壳聚糖的天然材料或其提取物。 活性成分促进肉碱棕榈酰转移酶1A基因的表达，增加脂肪酸的β氧化。 用于改善和预防肥胖症的食物组合物被配制成饮料，饮食酒吧，巧克力，焦糖或糖果。 基于总组合物，孕菊酯的含量为0.02-10重量％。
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