公开(公告)号：KR1020050039573A

公开(公告)日：2005-04-29

申请号：KR1020040083363

申请日：2004-10-19

Applicant: (주)아모레퍼시픽

Inventor： 김재현 ,  모주현 ,  박영호 ,  김정주 ,  심영철 ,  배준호

IPC: C07C335/12

CPC classification number: C07C335/12 ,  A61K31/17 ,  A61K31/255

Abstract: 본 발명은, 바닐로이드 수용체(Vanilloid Receptor1, VR1)에 대한 뛰어난 길항작용을 가지고 있으나 물에 난용성인 티오우레아 유도체 또는 약제학적으로 허용가능한 그의 염, 시클로덱스트린 또는 그의 유도체, 그리고, 임의적으로, 약제학적으로 허용되는 첨가제를 포함하는 약제학적 조성물에 관한 것이다.
본 발명의 약제학적 조성물은 티오우레아 유도체의 용해도 및 용출율이 크게 개선되어 매우 우수한 생체내이용률을 나타내었다. 따라서 바닐로이드 수용체에 대한 뛰어난 길항작용을 가지고 있는 티오우레아 유도체의 다양하고 효과적인 투여용 제제화가 가능하게 되었으며 이에 상기 화합물의 인체에 대한 적용이 더욱 현실적으로 실현가능하게 되어 그 유용성이 크게 기대된다.

公开(公告)号：KR1020040067969A

公开(公告)日：2004-07-30

申请号：KR1020040003871

申请日：2004-01-19

Applicant: (주)아모레퍼시픽

Inventor： 박진우 ,  배준호 ,  김정주

IPC: A61K9/16

CPC classification number: A61K9/2077 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/2846 ,  A61K9/2866 ,  A61K31/00 ,  A61K31/485

Abstract: PURPOSE: Provided is a controlled release preparation which minimizes the addition of a hydrophobic material, and prevents the surface adhesion of granules. The controlled release preparation continuously releases the drug content for 12 hours while maintaining the effective drug concentration in blood. CONSTITUTION: The controlled release preparation comprises 0.5-80wt.% of drug, 10-65wt.% of a hydrophobic release control additive, and 1-35wt.% of a hydrophobic wet granulating material. The drug is first melt-granulated using the hydrophobic release control additive, and the resulting granules are second wet-granulated using the hydrophobic wet granulating material.

Abstract translation: 目的：提供一种控制释放制剂，其最小化添加疏水性材料，并防止颗粒的表面粘附。 控释制剂连续释放药物含量12小时，同时保持血液中有效的药物浓度。 构成：控释制剂包含0.5-80重量％的药物，10-65重量％的疏水释放控制添加剂和1-35重量％的疏水湿法制粒材料。 首先使用疏水性释放控制添加剂对药物进行熔融造粒，并使用疏水性湿法制粒材料将得到的颗粒进行第二次湿法造粒。

公开(公告)号：KR1020030041433A

公开(公告)日：2003-05-27

申请号：KR1020010072226

申请日：2001-11-20

Applicant: (주)아모레퍼시픽

Inventor： 이영대 ,  김정주 ,  김중수 ,  이옥섭

IPC: A61K31/198

Abstract: PURPOSE: A composition for transdermal administration comprising L-arginine which has excellent therapeutic effect and presents no adverse effects even when administered in excess as a main drug is provided. The composition is an external application which overcomes the defects of conventional injections or oral therapeutic agents and effective in treatment of erectile dysfunction and frigidity. CONSTITUTION: A preparation for transdermal administration contains 1 to 20% by weight of L-arginine, 1 to 30% by weight of a skin permeation enhancer, a pharmaceutically acceptable carrier and additionally 1 to 80% by weight of one or more additives selected from a solubilizing aid, a softening agent, a surfactant, a thickening agent and a pH controller. The preparation is applied to the peripheral surface of the penis and the clitoris in a single dose of about 0.1 to 2g.

Abstract translation: 目的：用于透皮给药的组合物，其包含L-精氨酸，其具有优异的治疗效果，并且即使以过量作为主要药物也不会产生不良反应。 该组合物是克服常规注射或口服治疗剂的缺陷并有效治疗勃起功能障碍和寒冷的外部应用。 构成：用于透皮给药的制剂含有1至20重量％的L-精氨酸，1至30重量％的皮肤渗透促进剂，药学上可接受的载体，另外1至80重量％的一种或多种添加剂选自 增溶助剂，软化剂，​​表面活性剂，增稠剂和pH控制剂。 该制剂以约0.1至2g的单次剂量施用于阴茎和阴蒂的外周表面。

公开(公告)号：KR101349200B1

公开(公告)日：2014-01-09

申请号：KR1020060121432

申请日：2006-12-04

Applicant: (주)아모레퍼시픽

Inventor： 조선아 ,  이창훈 ,  김광미 ,  김대권 ,  김형준 ,  성기사 ,  김혁 ,  김정주 ,  김수열

IPC: A61K31/351 ,  A61P41/00

Abstract: 본 발명은 활성성분으로서 하기 화학식 1의 헥소사민 화합물 및 이의 약학적으로 허용가능한 염을 포함하는, 수술 후 유착증 (Post-operative adhesion)의 예방 또는 치료용 약학 조성물에 관한 것으로, 본 발명의 조성물에 포함된 헥소사민 화합물 또는 이의 약학적으로 허용 가능한 염은 복강에서 섬유소성 장 유착을 유발시킨 쥐 (rat) 모델에서 우수한 장 유착 저해활성을 나타내므로, 각종 외과적 수술 후 유발되는 부작용 중 하나인 섬유소성 장 유착 병증을 예방 또는 치료하는 데 유용하게 사용될 수 있다.

公开(公告)号：KR101349188B1

公开(公告)日：2014-01-08

申请号：KR1020060100703

申请日：2006-10-17

Applicant: (주)아모레퍼시픽

Inventor： 성기사 ,  김형준 ,  김혁 ,  김대권 ,  조선아 ,  김광미 ,  이창훈 ,  김정주

IPC: A61K31/047 ,  A61K31/13

CPC classification number: A61K31/047

Abstract: 본 발명은 스핑고실포스포릴콜린 (sphingosylphosphorylcholine; SPC)의 조절제 (modulator)를 이용하여 CCL27/CTACK (Cutaneous T-cell-attracting chemokine)의 발현을 억제시키는 방법 및 CCL27/CTACK 발현의 억제정도를 측정하여 SPC의 조절제 후보 물질을 스크리닝하는 방법에 관한 것으로, SPC가 아토피 피부염, 건선 및 염증성 피부 질환 환자들에서 발현 증가 양상을 보이고 있는 CCL27/CTACK의 발현을 증가시키므로, 본 발명에 따라 SPC 조절제를 투여하여 CCL27/CTACK의 발현을 억제시킴으로써 CCL27/CTACK 발현 증가 관련 질환의 치료 및 예방 효과를 얻을 수 있으며, CCL27/CTACK 유전자 또는 이들 단백질의 발현 억제 정도를 분석하여 SPC 조절제를 효율적으로 검색 (screening)할 수 있다.

公开(公告)号：KR1020090056632A

公开(公告)日：2009-06-03

申请号：KR1020070123865

申请日：2007-11-30

Applicant: (주)아모레퍼시픽

Inventor： 김상훈 ,  조시영 ,  박필준 ,  송민정 ,  이형호 ,  이태룡 ,  김정주 ,  김남수

IPC: C12N15/10 ,  C12N15/09 ,  C12Q1/68

CPC classification number: C12Q1/6876 ,  C12Q2600/158

Abstract: A kit and a method for screening a candidate material which promotes the lipolysis is provided to increase the melanocortin 2 receptor accessory protein(Mrap) gene expression, promote the lipolysis by ACTH(adrenocorticotropic hormone) and prevent and treat the obesity relating disease. A kit for screening a candidate material which promotes the lipolysis comprises a vector containing a promoter and reporter gene. The promoter comprises 842th to 853th bases of the sequence number 1(SEQ ID NO:1) or additional 1569th to 1581th bases thereon. The reporter gene is a luciferase gene, enhanced green fluorescent protein(EGFP) gene, or beta galactosidase(lacZ) gene. A method for screening the candidate material which promotes the lipolysis comprises: a step of transfecting a test cell which is designated to express a PPAR-gamma(peroxisome proliferator-activated receptor-gamma) with the vector; a step of treating with the candidate material in the transfected test cell; and a step of measuring the expression degree of the reporter gene in the test cell and selecting the candidate material.

Abstract translation: 提供用于筛选促进脂肪分解的候选物质的试剂盒和方法以增加黑皮质素2受体辅助蛋白（Mrap）基因表达，促进ACTH（促肾上腺皮质激素）的脂解，并预防和治疗肥胖症相关疾病。 用于筛选促进脂肪分解的候选物质的试剂盒包含含有启动子和报告基因的载体。 启动子包含序列号1（SEQ ID NO：1）的第842位至第853位碱基或其上第1569至1581位碱基。 报告基因是荧光素酶基因，增强型绿色荧光蛋白（EGFP）基因或β半乳糖苷酶（lacZ）基因。 用于筛选促进脂肪分解的候选物质的方法包括：转染被称为用载体表达PPAR-γ（过氧化物酶体增殖物激活受体-γ）的测试细胞的步骤; 在转染的测试细胞中用候选物质处理的步骤; 以及测定测定单元中的报道基因的表达程度并选择候选材料的步骤。

公开(公告)号：KR1020090032372A

公开(公告)日：2009-04-01

申请号：KR1020070097553

申请日：2007-09-27

Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

Inventor： 공영대 ,  조희영 ,  전문국 ,  이태호 ,  최길돈 ,  공재양 ,  정대영 ,  황순희 ,  김정주 ,  이창훈 ,  고재영 ,  노민수 ,  한은실 ,  김형준 ,  김혁 ,  윤준원 ,  모주현 ,  김도훈

IPC: C07D277/44 ,  C07D417/04 ,  C07D417/12 ,  A61K31/426

CPC classification number: C07D277/46 ,  C07D417/04 ,  C07D417/12

Abstract: Provided is 2,4,5-trisubstituted-1,3-thiazole derivatives having excellent inhibiting activity about SPC(sphingosylphosphorylcholine) receptor to treat inflammatory diseases caused by activity of the SPC acceptor. A therapeutic agent for treating inflammatory diseases caused by activity of SPC acceptor comprises a 2,4,5-trisubstituted-1,3-thiazole derivative represented by the formula 1 and pharmaceutically allowable salts thereof. A method for preparing the 2,4,5-trisubstituted-1,3-thiazole derivative consists of the following steps of: reacting methyl cyanocarbonimidodithionate represented by the formula 2 to 2-haloacetophenone in order to synthesize 4-amino-1,3-thiazol represented by the formula 3; and polymerizing chloridation carboxylic acid to 4-amino group of the 4-amino-1,3-thiazol to synthesize 4-N-acyl-1,3-thiazole represented by the formula 4.

Abstract translation: 提供对SPC（鞘氨基磷酰胆碱）受体具有优异抑制活性的2,4,5-三取代-1,3-噻唑衍生物，用于治疗由SPC受体的活性引起的炎性疾病。 用于治疗由SPC受体的活性引起的炎性疾病的治疗剂包括由式1表示的2,4,5-三取代-1,3-噻唑衍生物及其药学上允许的盐。 制备2,4,5-三取代-1,3-噻唑衍生物的方法包括以下步骤：使由式2表示的氰基羰基亚氨基二硫代乙酸甲酯与2-卤代苯乙酮反应，以合成4-氨基-1,3- 由式3表示的噻唑; 并将氯化羧酸聚合成4-氨基-1,3-噻唑-4-氨基，合成由式4表示的4-N-酰基-1,3-噻唑。

公开(公告)号：KR1020090027734A

公开(公告)日：2009-03-17

申请号：KR1020097001187

申请日：2007-07-26

Applicant: (주)아모레퍼시픽

Inventor： 배준호 ,  이종휘 ,  이혁 ,  김정주

IPC: A61K9/14 ,  A61K9/10

CPC classification number: A61K9/5123 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/145 ,  A61K9/146 ,  A61K9/5161 ,  A61K9/5192

Abstract: A manufacturing method of powder including nano particles of insoluble drug is provided to maintain stability in case that insoluble drug is re-dispersed at aqueous solution, to be no side effect by impurity and to improve bio-availability. A manufacturing method of powder including nano particles of insoluble drug comprises steps of: adding particles of insoluble drug which is active component, a surface passivating agent and additional dispersion secondary particle in aqueous solution including dispersion secondary particle to aturation concentration; mixing, shattering and homogenizing the obtained dispersed solution; and centrifuging or filtering the homogenized dispersed solution and drying it and obtaining the powder from the dispersed solution.

Abstract translation: 提供包含不溶性药物的纳米颗粒的粉末的制造方法，以在不溶性药物在水溶液中再分散的情况下保持稳定性，不会由杂质产生副作用并提高生物利用度。 包含不溶性药物纳米颗粒的粉末的制造方法包括以下步骤：在包含分散二次颗粒的水溶液中加入作为活性成分的不溶性药物颗粒，表面钝化剂和附加的分散二次颗粒以使其成为浓度; 混合，粉碎和均化所得分散溶液; 离心或过滤均匀分散的溶液并干燥并从分散溶液中获得粉末。

公开(公告)号：KR1020090016595A

公开(公告)日：2009-02-16

申请号：KR1020087030865

申请日：2006-12-08

Applicant: (주)아모레퍼시픽

Inventor： 김형준 ,  김혁 ,  성기사 ,  김대권 ,  성대석 ,  박종희 ,  조선아 ,  김광미 ,  이창훈 ,  김정주

IPC: A61K31/661 ,  C07K14/47 ,  C12Q1/68 ,  A61P17/00

CPC classification number: C12Q1/18 ,  G01N33/92 ,  G01N2405/08 ,  G01N2800/202 ,  A61K31/661 ,  C07K14/47

Abstract: A sphingosylphosphorylcholine(SPC) antagonist is provided to prevent and treat diseases related to the expression decrease of anti-bacterial peptide such as atopic dermatitis, and screen the SPC antagonist by analyzing the expression recover of gene or protein of the anti-bacterial peptide. The sphingosylphosphorylcholine(SPC) antagonist manufactures the medicine for restoring the expression of anti-bacterial peptide back to the normal level in mammal requiring the expression restoration of anti-bacterial peptide. The screening method of the sphingosylphosphorylcholine(SPC) antagonist comprises the steps of: treating the object with sphingosylphosphorylcholine or its derivative to inhibit expression of anti-bacterial peptide; and treating the object with the SPC antagonist candidate material, and analyzing the expression restoration level of the anti-bacterial peptide in the object.

Abstract translation: 提供鞘糖基磷酰胆碱（SPC）拮抗剂以预防和治疗与抗细菌肽如特应性皮炎的表达降低相关的疾病，并通过分析抗细菌肽的基因或蛋白质的表达恢复来筛选SPC拮抗剂。 鞘氨醇磷酰胆碱（SPC）拮抗剂在需要抗菌肽表达恢复的哺乳动物中制备了将抗菌肽的表达恢复至正常水平的药物。 鞘氨醇磷酰胆碱（SPC）拮抗剂的筛选方法包括以下步骤：用鞘糖基磷酰胆碱或其衍生物处理物体以抑制抗菌肽的表达; 并用SPC拮抗剂候选物质处理对象，分析对象中抗菌肽的表达恢复水平。

公开(公告)号：KR1020080050760A

公开(公告)日：2008-06-10

申请号：KR1020060121432

申请日：2006-12-04

Applicant: (주)아모레퍼시픽

Inventor： 조선아 ,  이창훈 ,  김광미 ,  김대권 ,  김형준 ,  성기사 ,  김혁 ,  김정주 ,  김수열

IPC: A61K31/351 ,  A61P41/00

CPC classification number: A61K31/7008 ,  A61K9/06 ,  A61K9/10 ,  A61K9/20 ,  A61K9/48

Abstract: A hexosamine derivative is provided to show excellent intra-abdominal fibrinous adhesion inhibitory activity, thereby being usefully used for preventing or treating post-operative adhesion. A pharmaceutical composition for preventing or treating post-operative adhesion such as intra-abdominal fibrinous adhesion comprises a hexosamine compound represented by a formula(1) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein the active ingredient is selected from the group consisting of galactosamine, D-(+)-glucosamine hydrochloride, and D-(+)-galactosamine hydrochloride.

Abstract translation: 提供了一种己糖胺衍生物以显示优异的腹内纤维粘附抑制活性，从而有效地用于预防或治疗术后粘连。 用于预防或治疗术后粘连（例如腹内纤维粘连）的药物组合物包含由式（1）表示的己糖胺化合物或其药学上可接受的盐作为活性成分，其中活性成分选自 的半乳糖胺，D - （+） - 葡糖胺盐酸盐和D - （+） - 半乳糖胺盐酸盐。