公开(公告)号：KR1020090056584A

公开(公告)日：2009-06-03

申请号：KR1020070123798

申请日：2007-11-30

Applicant: (주)아모레퍼시픽 ,  재단법인서울대학교산학협력재단

Inventor： 고재영 ,  한은실 ,  김혁 ,  김정주 ,  노민수 ,  김상희 ,  임채민

IPC: A61K31/16 ,  A61K31/13 ,  A61P31/00

CPC classification number: A61K31/16

Abstract: A pharmaceutical composition regulating the activity of sphingosylphosphorylcholine(SPC) is provided to regulate cell proliferation, inflammation and pruritus and treat inflammmatin or pruritus of dermatitis such as atopic dermatitis. A pharmaceutical composition which regulates the activity of sphingosylphosphorylcholine(SPC) comprises a compound of the chemical formula 1 or its pharmaceutically allowable salt. In the chemical formula 1, X is O or S, Y is CH2 or carbonyl. R1 is hydrogen or C1-10 alkyl, R2 is hydrogen or methyl, but when X is O, either R1 or R2 cannot be hydrogen, R3 is C1-4 alkyl. A method for manufacturing a compound of the chemical formula 1a comprises: a step of reacting a compound of the chemical formula 2 and a compound of the chemical formula 3 under the presence of base to obtain a compound of the chemical formula 4; a step of stirring the compound of the chemical formula 4 under the presence of base to obtain a compound of the chemical formula 5; and a step of performing the peptide bond between the compound of the chemical formula 5 and a compound of the chemical formula 6 to obtain the compound of the chemical formula 1a.

Abstract translation: 提供调节肌动蛋白磷酰胆碱（SPC）活性的药物组合物，用于调节细胞增殖，炎症和瘙痒，并治疗诸如特应性皮炎等炎性炎症或皮炎瘙痒症。 调节鞘糖基磷酰胆碱（SPC）活性的药物组合物包含化学式1的化合物或其药学上可允许的盐。 在化学式1中，X为O或S，Y为CH 2或羰基。 R1是氢或C1-10烷基，R2是氢或甲基，但当X是O时，R1或R2不能是氢，R3是C1-4烷基。 制备化学式1a化合物的方法包括：使化学式2的化合物与化学式3化合物在碱存在下反应得到化学式4的化合物的步骤; 在碱的存在下搅拌化学式4的化合物以获得化学式5的化合物的步骤; 在化学式5的化合物与化学式6的化合物之间进行肽键的步骤，得到化学式1a的化合物。

公开(公告)号：KR101232993B1

公开(公告)日：2013-02-13

申请号：KR1020060068578

申请日：2006-07-21

Applicant: 한국생명공학연구원 ,  (주)아모레퍼시픽

Inventor： 오원근 ,  안종석 ,  김보연 ,  나민균 ,  이상준 ,  김정주 ,  김유

IPC: C07C49/703 ,  C07C49/603 ,  C07C49/403

Abstract: 본 발명은 관중 유래의 지방산 생합성 효소 (fatty acid synthase, FAS) 저해용 플로르글루시놀계 화합물 및 이를 유효성분으로 포함하는 암 및 비만 예방과 치료용 조성물에 관한 것으로, 관중을 에탄올 추출한 후 크로마토그래피를 이용하여 순수 분리 정제하여 얻은 FAS 저해 화합물과 이를 유효성분으로 함유하는 암 및 비만의 예방과 치료 용도에 관한 것이다.
관중, 지방산 생합성 효소 (FAS), 암, 비만, 플로르글루시놀계 화합물, 에탄올 추출

公开(公告)号：KR101018819B1

公开(公告)日：2011-03-04

申请号：KR1020087019182

申请日：2007-02-14

Applicant: (주)아모레퍼시픽

Inventor： 김대권 ,  김광미 ,  성대석 ,  박종희 ,  김형준 ,  윤준원 ,  박영호 ,  임경민 ,  최진규 ,  고현주 ,  정연수 ,  이창훈 ,  김정주

IPC: A61K31/17 ,  A61K31/765 ,  A61P17/00

CPC classification number: A61K9/0014 ,  A61K31/17 ,  A61K47/10 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26 ,  A61K47/32

Abstract: 본 발명은 바닐로이드 수용체 길항제로서 티오우레아 유도체와 약제학적으로 허용가능한 담체를 함유하는 외용제 조성물 및 이의 약제학적 용도에 관한 것이다.
본 발명의 외용제 조성물은 피부투과와 안정성에서 우수하며 소양성 또는 자극성 피부질환에 유용하다.

公开(公告)号：KR100903974B1

公开(公告)日：2009-06-25

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: 본 발명은 하기 화학식 1로 표시되는 2,4,5-삼중치환-1,3-티아졸 유도체 및 약제학적으로 허용 가능한 그의 염, 그의 제조방법 및 그를 유효성분으로 함유하는 SPC 수용체 활성으로 유발되는 염증관련 질환에 유용한 그의 용도에 관한 것이다.
본 발명의 2,4,5-삼중치환-1,3-티아졸 유도체는 사람으로부터 유래된 진피세포 및 마우스를 이용한 동물실험을 통하여 항염증 효과를 검색한 결과, SPC 수용체에 대한 우수한 억제활성을 규명함으로써, 상기 2,4,5-삼중치환-1,3-티아졸 유도체 및 약제학적으로 허용 가능한 그의 염을 유효성분으로 함유하여 SPC 수용체 활성으로 유발되는 아토피성 피부염, 기타 질환에서 나타나는 염증, 소양증 또는 피부 감염증에 유효한 염증관련 질환 치료제로서 유용하게 활용될 수 있다.


(상기 식에서, R
1 , R
2 , 및 R
3 는 명세서에서 정의한 바와 같다.)
1,3-티아졸, 스핀고실포스포릴콜린, 아토피 피부염, 염증치료제

公开(公告)号：KR1020090032373A

公开(公告)日：2009-04-01

申请号：KR1020070097554

申请日：2007-09-27

Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

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

IPC: C07D401/12 ,  A61K31/498 ,  A61P29/00

CPC classification number: C07D401/12

Abstract: Provided is a 3-chloro-5-substituted-quinoxaline-2-amine derivative and a therapeutic agent using the 3-chloro-5-substituted-quinoxaline-2-amine derivative so as to treat diseases associated with inflammation. A 3-chloro-5-substituted-quinoxaline-2-amine derivative is represented by the formula 1. In the formula 1, R∧1 indicates hydrogen, linear or branched C1-C10 alkyl group, C1-C10 alkoxy group or halogen; R∧2 shows linear or branched C1-C10 alkyl group, C1-C10 alkoxy group, hydroxyl group, halogen group, amine group or substituted amine group, amide group, carbamate group or urea group. In the formula 1, the substituted group indicates a substituted phenyl group wherein one or four groups selected from the group consisting of a linear or branched C1-C10 alkyl group, halogen, nitro group, C1-C10 alkyl group, C1-C10 alkoxy group and C1-C10 haloalkyl group are substituted.

Abstract translation: 本发明提供3-氯-5-取代喹喔啉-2-胺衍生物和使用3-氯-5-取代喹喔啉-2-胺衍生物的治疗剂，以治疗与炎症相关的疾病。 3-氯-5-取代喹喔啉-2-胺衍生物由式1表示。在式1中，R 1表示氢，直链或支链C 1 -C 10烷基，C 1 -C 10烷氧基或卤素; R 2表示直链或支链C 1 -C 10烷基，C 1 -C 10烷氧基，羟基，卤素基，胺基或取代胺基，酰胺基，氨基甲酸酯基或脲基。 在式1中，取代基表示取代的苯基，其中选自直链或支链C 1 -C 10烷基，卤素，硝基，C 1 -C 10烷基，C 1 -C 10烷氧基中的一个或四个基团 和C 1 -C 10卤代烷基被取代。

公开(公告)号：KR1020090030497A

公开(公告)日：2009-03-25

申请号：KR1020070095848

申请日：2007-09-20

Applicant: (주)아모레퍼시픽

Inventor： 조시영 ,  박필준 ,  이정오 ,  이태룡 ,  김정주

IPC: C12N15/64 ,  C12N15/09 ,  C12N15/10

Abstract: A signal peptide targeting to nucleus is provided to move signal peptide to nucleus through the fusion of the signal peptide and to perform function of heterologous protein in nucleus. An expression vector comprises a gene coding the signal peptide of SEQ ID NO:1 and a gene coding heterologous protein. The heterologous protein is an orphan receptor or steroid receptor response element binding protein 1(SREBP1). The orphan receptor is retinoic acid receptor(RAR), peroxisome proliferator-activated receptor(PPAR) or Liver X receptor(LXR).

Abstract translation: 提供靶向细胞核的信号肽，以通过信号肽的融合将信号肽移动到细胞核，并在细胞核中进行异源蛋白质的功能。 表达载体包含编码SEQ ID NO：1的信号肽的基因和编码异源蛋白质的基因。 异源蛋白是孤儿受体或类固醇受体反应元件结合蛋白1（SREBP1）。 孤儿受体是视黄酸受体（RAR），过氧化物酶体增殖物激活受体（PPAR）或肝X受体（LXR）。

公开(公告)号：KR1020090030070A

公开(公告)日：2009-03-24

申请号：KR1020070095389

申请日：2007-09-19

Applicant: (주)아모레퍼시픽

Inventor： 조시영 ,  박필준 ,  이정오 ,  이태룡 ,  김정주

IPC: C12N15/64 ,  C12N15/12 ,  C12N15/09

Abstract: A signal peptide targeting to lipid droplet for targeting a heterologous protein to lipid droplet is provided to cure and prevent lipid droplet-related diseases containing obesity, diabetes and arteriosclerosis. An expression vector comprises a gene coding signal peptide of SEQ ID NO:1 and a gene coding heterologous protein. The heterologous protein is the lipase or protein kinase A(PKA). The composition for targeting a heterologous protein to lipid droplet comprises the expression vector.

Abstract translation: 提供靶向脂滴以将异源蛋白质靶向脂质液滴的信号肽，以治愈和预防含有肥胖，糖尿病和动脉硬化的脂滴相关疾病。 表达载体包含SEQ ID NO：1的基因编码信号肽和编码异源蛋白质的基因。 异源蛋白是脂肪酶或蛋白激酶A（PKA）。 将异源蛋白质靶向脂滴的组合物包含表达载体。

公开(公告)号：KR1020080051201A

公开(公告)日：2008-06-11

申请号：KR1020060121861

申请日：2006-12-05

Applicant: (주)아모레퍼시픽

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

IPC: A61K31/685 ,  A61K31/661

CPC classification number: A61K31/688 ,  Y10S514/863 ,  Y10S514/886

Abstract: A pharmaceutical composition comprising sphingosylphosphorylcholine or derivatives thereof is provided to inhibit proliferation and promote differentiation of keratinocyte, inhibit proliferation of splenocyte and T cell, induce reduction of leucocyte, and reduce mouse ear swelling induced by TPA(tetradecanoyl phorbol acetate), so that the composition is useful for treating psoriasis. A pharmaceutical composition for treating psoriasis comprises sphingosylphosphorylcholine(SPC) represented by the formula(1) or derivatives thereof and is formulated as tablet, pill, powder, sachet, elixir, suspension, emulsion, solution, syrup, aerosol, soft or hard gelatin capsule, sterile injection or sterile powder, wherein the daily dosage is 1-100 mg/kg, preferably 5-70 mg/kg.

Abstract translation: 提供包含鞘氨醇磷酰胆碱或其衍生物的药物组合物，以抑制角质形成细胞的增殖和促进分化，抑制脾细胞和T细胞的增殖，诱导白细胞的减少，并减少TPA（十四酰基佛波醇乙酸酯）诱导的小鼠耳肿胀，使组合物 可用于治疗牛皮癣。 用于治疗牛皮癣的药物组合物包含由式（1）表示的鞘糖基磷酰胆碱（SPC）或其衍生物，并配制成片剂，丸剂，粉末，小药囊，酏剂，悬浮液，乳剂，溶液，糖浆，气雾剂，软或硬明胶胶囊 无菌注射或无菌粉末，其中日剂量为1-100mg / kg，优选5-70mg / kg。

公开(公告)号：KR1020080006961A

公开(公告)日：2008-01-17

申请号：KR1020060066357

申请日：2006-07-14

Applicant: (주)아모레퍼시픽 ,  주식회사 에스트라

Inventor： 기한뫼 ,  최양규 ,  아영창 ,  김정주

IPC: A61K9/70

CPC classification number: A61K9/7038 ,  A61K31/192 ,  A61K31/196

Abstract: A transdermal preparation is provided to promote the drug absorption by the skin hydration through a hydrophobic adhesive layer, show continuous and high effect of a drug by maintaining the thermodynamic activity of the hydrophobic drug in an adhesive caused by moisture discharged from skin and be able to reduce the cost and the time due to a very simple preparing process. A transdermal preparation for a hydrophobic drug comprises a supportive layer(1) which is the uppermost portion of a layered structure and has the elasticity; a hydrophobic adhesive layer(2) which is layered under the supportive layer and prevents the loss of moisture absorbed from skin and the reverse conversion of the drug; and a drug containing adhesive layer(3) which is layered under the hydrophobic adhesive layer, includes a drug and attaches the transdermal preparation to the skin and is characterized in that the drug adhesive layer includes a hydrophobic drug such as a non-steroidal antiphlogistics and an absorption promoting agent, where a hydrophobic adhesive of the hydrophobic adhesive layer is selected from the group consisting of polyisobutylene adhesive, styrene-isoprene-styrene adhesive, and styrene-butadiene-styrene adhesive, the drug containing adhesive layer is an acrylate polymer made from acrylate, hydroxypropyl acrylate, acrylamide, acrylamide vinyl acetate, vinyl derivative, methacrylate, hydroxypropyl methacrylate and methacrylamide. The preparation further comprises a release layer(4) which is layered under the drug adhesive layer and protects the drug adhesive layer before use.

Abstract translation: 提供透皮制剂以通过疏水粘合剂层通过皮肤水合促进药物吸收，通过将疏水药物的热力学活性保持在由皮肤排出的水分引起的粘合剂中，显示出药物的连续和高效果，并且能够 由于非常简单的准备过程，降低了成本和时间。 用于疏水性药物的透皮制剂包括支撑层（1），其是层状结构的最上部并具有弹性; 疏水性粘合剂层（2），其被层叠在支撑层下方并防止皮肤吸收的水分的损失和药物的逆转换; 和层叠在疏水性粘合剂层下面的药物含有粘合剂层（3）的药物包含药物，并将透皮制剂附着于皮肤，其特征在于，所述药物粘合剂层包括疏水性药物，例如非甾体消炎药， 吸水促进剂，其中疏水性粘合剂层的疏水性粘合剂选自聚异丁烯粘合剂，苯乙烯 - 异戊二烯 - 苯乙烯粘合剂和苯乙烯 - 丁二烯 - 苯乙烯粘合剂，所述药物粘合剂层是由 丙烯酸酯，丙烯酸羟丙酯，丙烯酰胺，丙烯酰胺乙酸乙烯酯，乙烯基衍生物，甲基丙烯酸酯，甲基丙烯酸羟丙酯和甲基丙烯酰胺。 该制剂还包括层叠在药物粘合剂层下面的释放层（4），并在使用前保护药物粘合剂层。

公开(公告)号：KR1020080006960A

公开(公告)日：2008-01-17

申请号：KR1020060066353

申请日：2006-07-14

Applicant: (주)아모레퍼시픽 ,  주식회사 에스트라

Inventor： 최양규 ,  기한뫼 ,  아영창 ,  김정주

IPC: A61K9/70

CPC classification number: A61K9/7061 ,  A61K47/32

Abstract: A transdermal preparation is provided to continuously allow a highly concentrated hydrophobic drug to be absorbed into skin until a patch is detached from the skin with minimized skin side effects and provide the enough adhesive capability during the time of exhibiting the medical efficacy by being attached to the skin. A transdermal preparation for a hydrophobic drug comprises a supportive layer(1) which is the uppermost portion of a layered structure and has the elasticity; a hydrophobic adhesive layer(2) which is layered under the supportive layer and prevents the loss of moisture absorbed from skin and the reverse conversion of the drug; and a drug adhesive layer(3) which is layered under the hydrophobic adhesive layer, includes a drug and attaches the transdermal preparation to the skin and is characterized in that the drug adhesive layer includes a hydrophobic drug such as a non-steroidal antiphlogistics and an acryl adhesive agent and the acryl adhesive agent includes a hydrophilic monomer promoting the skin absorption from the skin and is selected from the group consisting of acrylic acid, methyl methacrylate, ethyl acrylate, hydroxyethyl acrylate, butyl acrylate, octyl acrylate, 2-ethylhexyl acrylate, and hexyl acrylate. The preparation further comprises a release layer(4) which is layered under the drug adhesive layer and protects the drug adhesive layer before use.

Abstract translation: 提供透皮制剂以连续地允许高度浓缩的疏水性药物被吸收到皮肤中，直到贴片从皮肤上分离出来，使皮肤的副作用最小化，并且在展示医疗功效的时间期间提供足够的粘合能力， 皮肤。 用于疏水性药物的透皮制剂包括支撑层（1），其是层状结构的最上部并具有弹性; 疏水性粘合剂层（2），其被层叠在支撑层下方并防止皮肤吸收的水分的损失和药物的逆转换; 以及层叠在疏水性粘合剂层下方的药物粘合剂层（3），包括药物，并且将透皮制剂附着于皮肤，其特征在于，所述药物粘合剂层包括疏水性药物，例如非甾体消炎药和 丙烯酸粘合剂和丙烯酸粘合剂包括促进皮肤吸收皮肤的亲水单体，并且选自丙烯酸，甲基丙烯酸甲酯，丙烯酸乙酯，丙烯酸羟乙酯，丙烯酸丁酯，丙烯酸辛酯，丙烯酸2-乙基己酯， 和丙烯酸己酯。 该制剂还包括层叠在药物粘合剂层下面的释放层（4），并在使用前保护药物粘合剂层。