항비만 효과를 나타내는 히드록삼산 유도체 및 이의제조방법
    51.
    发明授权
    항비만 효과를 나타내는 히드록삼산 유도체 및 이의제조방법 有权
    具有抗生素活性的羟基酸衍生物及其制备方法

    公开(公告)号:KR100845511B1

    公开(公告)日:2008-07-10

    申请号:KR1020070029253

    申请日:2007-03-26

    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。

    항노화 효과를 나타내는 레티노익산 유도체 및 이의제조방법
    52.
    发明授权
    항노화 효과를 나타내는 레티노익산 유도체 및 이의제조방법 有权
    具有抗老化活性的视黄酸衍生物及其制备方法

    公开(公告)号:KR100837186B1

    公开(公告)日:2008-06-13

    申请号:KR1020060095279

    申请日:2006-09-29

    Abstract: 본 발명은 하기 화학식 1로 표시되는 항노화 효과를 나타내는 레티노익산(Retinoic acid) 유도체 및 이의 제조방법에 관한 것이다:
    [화학식 1]

    [상기 화학식 1에서, R
    1 은 수소, 직쇄 또는 분쇄의 (C
    1 -C
    7 )알킬 또는 (C
    3 -C
    7 )시클로알킬이고; R
    2 는 히드록시, 1~4개의 히드록시기가 치환된 직쇄 또는 분쇄의 (C
    1 -C
    7 )알킬 또는 히드록시피라논이 치환된 직쇄 또는 분쇄의 (C
    1 -C
    5 )알킬이다.]
    또한 본 발명은 상기 화학식 1의 레티노익산 유도체를 유효성분으로 함유하는 피부노화 방지용 피부 외용제 조성물에 관한 것이다.
    레티노익산 * 레티노익산 수용체 * 항노화 * 콜라겐 * 콜라게나아제 발현억제 * 주름 개선 * 피부 외용제

    카텝신 G 저해제를 함유하는 피부노화 방지용 피부외용제조성물 및 항노화용 물질을 스크리닝하는 방법
    53.
    发明公开
    카텝신 G 저해제를 함유하는 피부노화 방지용 피부외용제조성물 및 항노화용 물질을 스크리닝하는 방법 有权
    用于外用于含皮肤抑制剂G抑制剂以防止皮肤老化的筛选组合物和用于开发抗病材料的筛选方法

    公开(公告)号:KR1020080040612A

    公开(公告)日:2008-05-08

    申请号:KR1020070111803

    申请日:2007-11-02

    CPC classification number: A61K8/42 A61K2800/522 A61Q19/08

    Abstract: A skin external composition comprising a cathepsin G inhibitor is provided to prevent an adhesion protein from being degraded by intrinsic aging and photo-aging, reduce the production of metalloproteinase and inhibit the activity of metalloproteinase, thereby being more potent anti-aging substance than existing anti-aging substances. A method for screening anti-aging materials is provided to develop the anti-aging materials which effectively inhibit the quantitative and qualitative increase of metalloproteinase, resulting from the degradation of an adhesion protein by cathepsin G in skin cells without direct UV irradiation. A skin external composition for preventing skin aging comprises 0.01-10 wt% a cathepsin G inhibitor as an effective ingredient, wherein the cathepsin G inhibitor is at least one selected from the group consisting of compounds represented by formulae(1) to (4). The composition is formulated into skin lotion, astringent lotion, milk lotion, nourishing cream, essence, massage cream, eye cream, pack, body lotion, body cream, body oil or body essence. A method for screening an anti-aging material comprises the steps of: (a) adding an anti-aging candidate material to a substrate in the presence of cathepsin G enzyme; and (b) measuring the inhibition of activity of the cathepsin G enzyme. Further, the measure of the inhibition of activity of the cathepsin G enzyme is performed by measuring a concentration of a produced metalloprotease.

    Abstract translation: 提供包含组织蛋白酶G抑制剂的皮肤外用组合物,以防止粘附蛋白由于内在老化和光老化而降解,减少金属蛋白酶的产生并抑制金属蛋白酶的活性,从而比现有的抗老化物质更有效的抗衰老物质 化学物质。 提供了一种筛选抗衰老材料的方法,以开发有效抑制金属蛋白酶定量和定性增加的抗衰老材料,这是由皮肤细胞中组织蛋白酶G在组织蛋白酶G中的降解引起的,而不需要直接的紫外线照射。 用于防止皮肤老化的皮肤外用组合物包含0.01-10重量%的组织蛋白酶G抑制剂作为有效成分,其中组织蛋白酶G抑制剂是选自由式(1)至(4)表示的化合物中的至少一种。 该组合物配制成皮肤洗剂,收敛剂,乳液,滋养霜,精华液,按摩霜,眼霜,包装,身体乳液,身体霜,身体油或身体精华。 用于筛选抗衰老材料的方法包括以下步骤:(a)在组织蛋白酶G酶存在下将抗老化候选材料加入到底物中; 和(b)测量组织蛋白酶G酶的活性的抑制。 此外,组织蛋白酶G酶的活性的抑制的测量是通过测量产生的金属蛋白酶的浓度进行的。

    엘라스테아제 저해 효과를 갖는 3,5-디히드록시벤조산유도체 화합물과 그 제조방법 및 이를 함유하는 항노화화장료 조성물
    54.
    发明授权

    公开(公告)号:KR100726280B1

    公开(公告)日:2007-06-11

    申请号:KR1020060035603

    申请日:2006-04-20

    Abstract: Provided is a 3,5-dihydroxybenzoic acid derivative, which shows an elastase inhibitory effect and an excellent effect of scavenging free radicals generated by UV irradiation, has an excellent anti-aging effect, and is useful for an anti-aging cosmetic composition. The 3,5-dihydroxybenzoic acid derivative is a compound represented by a formula 1, substituted with hydroxyl groups at 3,5-position thereof and the amide group being substituted with a bulky substituent. The 3,5-dihydroxybenzoic acid derivative is obtained by the method comprising the steps of: (A) reacting 3,5-dihydroxybenzoic acid with acetic anhydride to form 3,5-diacetyloxybenzoic acid; (B) forming an amide compound from the 3,5-diacetyloxybenzoic acid by using ethyl chloroformate and an oleophilic group; and (C) hydrolyzing the acetyl group of the amide compound to provide a 3,5-dihydroxybenzoic acid derivative.

    Abstract translation: 本发明提供一种3,5-二羟基苯甲酸衍生物,其显示出弹性蛋白酶抑制作用,并且通过UV照射产生的清除自由基的优异效果,具有优异的抗老化作用,并且可用于抗老化化妆品组合物。 3,5-二羟基苯甲酸衍生物是由式3表示的化合物,其3,5-位被羟基取代且酰胺基被大体积取代基取代。 3,5-二羟基苯甲酸衍生物通过包括以下步骤的方法获得:(A)使3,5-二羟基苯甲酸与乙酸酐反应形成3,5-二乙酰氧基苯甲酸; (B)通过使用氯甲酸乙酯和亲油基团由3,5-二乙酰氧基苯甲酸形成酰胺化合物; 和(C)水解酰胺化合物的乙酰基得到3,5-二羟基苯甲酸衍生物。

    세사몰 유도체 및 그의 제조방법
    56.
    发明公开
    세사몰 유도체 및 그의 제조방법 有权
    SESAMOL衍生物及其制备方法

    公开(公告)号:KR1020070013482A

    公开(公告)日:2007-01-31

    申请号:KR1020050067815

    申请日:2005-07-26

    Abstract: Sesamol derivatives and a process for preparing the same compounds are provided to improve anti-oxidizing activity and stability of sesamol, recover the skin damaged by reactive oxygen species, prevent aging of biological membranes, and inhibit production of peroxides of unsaturated fatty acid and its derivatives. The sesamol derivatives represented by the formula(1) are provided, wherein the sesamol derivatives are prepared by reacting sesamol with adamantanol in an equivalence ratio of 1:1.0~1.3 under acid condition, and recrystallizing the resulting product in polar solvent; the acid is hydrochloric acid, nitric acid, sulfuric acid, p-toluenesulfonic acid, benzene sulfonic acid, acetic acid, trichloroacetic acid or trifluoroacetic acid; the solvent used in the reaction is dichloromethane, tetrahydrofuran, ethyl acetate, acetonitrile, chloroform, ethyl ether, trichloro ethylene, benzene or toluene; and the polar solvent is methanol, ethanol, isopropanol, acetone, acetonitrile or water.

    Abstract translation: 提供了芝麻酚衍生物和制备相同化合物的方法,以提高芝麻素的抗氧化活性和稳定性,回收活性氧损伤的皮肤,防止生物膜老化,抑制不饱和脂肪酸及其衍生物过氧化物的产生 。 提供由式(1)表示的芝麻酚衍生物,其中芝麻酚衍生物通过在酸性条件下使芝麻酚与当量比为1:1.0〜1.3的金刚烷醇反应制备,并将所得产物在极性溶剂中重结晶; 酸是盐酸,硝酸,硫酸,对甲苯磺酸,苯磺酸,乙酸,三氯乙酸或三氟乙酸; 反应中使用的溶剂是二氯甲烷,四氢呋喃,乙酸乙酯,乙腈,氯仿,乙醚,三氯乙烯,苯或甲苯; 极性溶剂为甲醇,乙醇,异丙醇,丙酮,乙腈或水。

    락토바실러스 플란타룸을 포함하는 항진균용 조성물
    57.
    发明公开
    락토바실러스 플란타룸을 포함하는 항진균용 조성물 审中-实审
    包含植物乳杆菌的抗真菌剂组合物

    公开(公告)号:KR1020170090997A

    公开(公告)日:2017-08-08

    申请号:KR1020160182201

    申请日:2016-12-29

    Abstract: 본명세서에는, 락토바실러스플란타룸균주, 그파쇄물, 그배양액또는그 추출물을유효성분으로포함하는항진균용조성물이개시된다. 상기조성물은, 말라세지아속진균에대한항진균력이있으므로, 지루성두피염또는비듬을예방, 개선또는치료하는데사용할수 있다.

    Abstract translation: 在本说明书中,公开了包含植物乳杆菌菌株,其裂解物,其培养物或其提取物作为活性成分的抗真菌剂组合物。 该组合物具有抗马拉色菌真菌的抗真菌活性,因此可用于预防,改善或治疗脂溢性皮炎或头皮屑。

    신규 히드록시 피라논 화합물, 이의 제조방법 및 이를 포함하는 화장료 조성물
    58.
    发明公开
    신규 히드록시 피라논 화합물, 이의 제조방법 및 이를 포함하는 화장료 조성물 审中-实审
    新颖的羟基糠酮化合物,其制备方法和含有它们的化妆品组合物

    公开(公告)号:KR1020170064198A

    公开(公告)日:2017-06-09

    申请号:KR1020150169638

    申请日:2015-12-01

    CPC classification number: A61K8/49 A61Q19/00 C07D309/34

    Abstract: 본발명은신규한히드록시피라논화합물, 이의제조방법및 이를포함하는화장료조성물에관한것이다. 본발명에따른히드록시피라논화합물은기존의지방세포분화촉진물질대비현저히개선된효과를나타내므로, 피부볼륨또는탄력증진을위한화장료조성물의유효성분으로바람직하게함유된다.

    Abstract translation: 本发明涉及一种新颖的羟基蒽酮酮化合物,其制备方法和含有该化合物的化妆品组合物。 根据本发明的羟基非吡唑化合物显示出常规的脂肪细胞分化促进材料相比显著改善效果,被包含,优选地,如化妆品组合物用于改善皮肤弹性或体积的活性成分。

    표면 개질된 양친매성 이방성 분체 및 이를 함유하는 유화 조성물과 이의 제조방법
    59.
    发明公开
    표면 개질된 양친매성 이방성 분체 및 이를 함유하는 유화 조성물과 이의 제조방법 审中-实审
    表面改性的人造血液颗粒和包含其的乳液组合物及其制造方法

    公开(公告)号:KR1020160081823A

    公开(公告)日:2016-07-08

    申请号:KR1020150187736

    申请日:2015-12-28

    Abstract: 본명세서에는표면개질된양친매성이방성분체및 이를함유하는유화조성물과이의제조방법이개시된다. 상기양친매성이방성분체는표면개질되어친수성이증대되고양친매성을조절하여유화특성조절이가능하다. 또한, 상기유화조성물은표면개질된양친매성이방성분체를함유함으로써, 극성오일과의유화안정성, 점증제와같은음이온성물질과의상용성또는점증제사용량을최소화할수 있는유화입자의분산성이개선되는효과가있다.

    Abstract translation: 公开了表面改性的两亲性各向异性粉末,含有它们的乳液组合物及其制备方法。 根据本发明,两亲性各向异性粉末由于表面改性而表现出增加的亲水性,并且通过调节两亲性来确保乳化性能的可调性。 此外,乳液组合物含有表面改性的两亲性各向异性粉末,因此显示出极性油提高乳液稳定性的效果,与粘度增加剂等阴离子物质的相容性,以及分散乳液粒子以使粘度最小化的能力 增加代理

    과립형 화장료 제형 및 그 제조방법
    60.
    发明授权
    과립형 화장료 제형 및 그 제조방법 有权
    颗粒型化妆品配方及其制备方法

    公开(公告)号:KR101543017B1

    公开(公告)日:2015-08-12

    申请号:KR1020080097602

    申请日:2008-10-06

    Abstract: 무수제형의과립형화장료제형및 그제조방법이개시된다. 상기과립형화장료제형은, 불안정한수용성활성성분의안정화를도모할수 있으며, 점증현상에의해서시각적으로소비자에게과립입자에함유되어있는수용성활성성분의용해시점을알려줄뿐만아니라, 시각적차별화가가능한제품으로활용이가능하다.

Patent Agency Ranking