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    클로로이미다졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증 또는 비만의 예방 또는 치료용 약학적 조성물
    33.
    发明公开
    클로로이미다졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증 또는 비만의 예방 또는 치료용 약학적 조성물 失效
    用于预防或治疗包含氯霉素衍生物的药物或药物的药物组合物或其作为活性成分的药物可接受的盐

    公开(公告)号：KR1020100130015A

    公开(公告)日：2010-12-10

    申请号：KR1020090048661

    申请日：2009-06-02

    Applicant: 한국화학연구원

    Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  황은숙 ,  홍정호

    IPC: C07D487/04 ,  C07D487/02 ,  A61K31/415 ,  A61P19/10

    Abstract: PURPOSE: A pharmaceutical composition containing chloroimidazole derivative for preventing or treating osteoporosis, obesity, diabetes or hyperlipidemia is provided to control TAZ(transcriptional coactivator with PDZbinding motif) protein. CONSTITUTION: A pharmaceutical composition for preventing or treating osteoporosis contains a compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for obesity, diabetes or hyperlipidemia contains the compound or pharmaceutically acceptable salt as an active ingredient. The compound is chloroimidazole derivatives.

    Abstract translation: 目的：提供含有用于预防或治疗骨质疏松症，肥胖，糖尿病或高脂血症的氯咪唑衍生物的药物组合物以控制TAZ（具有PDZ结合基序的转录共激活物）蛋白质。 构成：用于预防或治疗骨质疏松症的药物组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。 用于肥胖，糖尿病或高脂血症的药物组合物含有化合物或药学上可接受的盐作为活性成分。 该化合物是氯咪唑衍生物。

    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물
    36.
    发明授权
    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물 失效
    用于治疗或预防包含1,2,4-噻二唑-3,5-二酮化合物的药物的药物组合物

    公开(公告)号：KR100837785B1

    公开(公告)日：2008-06-13

    申请号：KR1020070005148

    申请日：2007-01-17

    Applicant: 한국화학연구원

    Inventor： 이계형 ,  원종화 ,  김익연 ,  노재성 ,  김지영 ,  원혜경 ,  정은주 ,  허민규 ,  김성주 ,  김영림 ,  전동주 ,  송종환 ,  강남숙 ,  유성은

    IPC: A61K31/4152 ,  A61P29/00

    CPC classification number: A61K31/433 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/5377 ,  Y10S514/825 ,  Y10S514/886

    Abstract: A novel 1,2,4-thiadiazolidine-3,5-dione compound is provided to show excellent activity and enzyme selectivity on Lck SH2, thereby being usefully used for treating and preventing inflammation related diseases such as rheumatoid arthritis with high selectivity without side effects. A pharmaceutical composition for treating and preventing a disease induced by inflammation comprises a 1,2,4-thiadiazolidine-3,5-dione compound represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient. In the formula(1), A is linear or branched saturated or unsaturated C1-7 alkyl, indenyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, benzyl or C2H5(C=O)HR2R3(wherein A may be substituted by halogen, carboxyl, C1-7 alkoxycarbonyl, C1-7 alkoxy, nitro or hydroxy when A is alkyl, phenyl or benzyl); R1 is H, linear or branched saturated or unsaturated C1-7 alkyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, phenyl(C1-5)alkyl or phenylcarbonylmethyl; and each R2 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl or phenyl, or R2 and R3 may form a ring together with C1-5 alkylene. A pharmaceutical composition for treating and preventing rheumatoid arthritis comprises the 1,2,4-thiadiazolidine-3,5-dione compound of the formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient.

    Abstract translation: 提供了一种新的1,2,4-噻二唑烷-3,5-二酮化合物，以显示对Lck SH2的极好的活性和酶选择性，从而有效地用于治疗和预防炎症相关疾病如类风湿性关节炎，具有高选择性，无副作用 。 用于治疗和预防炎性疾病的药物组合物包含由式（1）表示的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。 在式（1）中，A是直链或支链饱和或不饱和的C1-7烷基，茚基，（C1-7）烷氧基羰基（C1-7）烷基，苯基，苄基或C2H5（C = O）HR2R3（其中A可以 苯基或苄基）被卤素，羧基，C 1-7烷氧基羰基，C 1-7烷氧基，硝基或羟基取代。 R1是H，直链或支链饱和或不饱和的C1-7烷基，（C1-7）烷氧基羰基（C1-7）烷基，苯基，苯基（C1-5）烷基或苯基羰基甲基; 并且每个R 2和R 2独立地为H，直链或支链饱和或不饱和的C 1-7烷基或苯基，或者R 2和R 3可与C 1-5亚烷基一起形成环。 用于治疗和预防类风湿性关节炎的药物组合物包含式（1）的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。

    인간 ＦＡＦ1 단백질 억제제를 유효성분으로 함유하는허혈성 질환 치료용 조성물
    38.
    发明授权
    인간 ＦＡＦ1 단백질 억제제를 유효성분으로 함유하는허혈성 질환 치료용 조성물 有权
    用于治疗包含人FAF1蛋白抑制剂作为活性成分的疾病的组合物

    公开(公告)号：KR100818752B1

    公开(公告)日：2008-04-01

    申请号：KR1020060095742

    申请日：2006-09-29

    Applicant: 한국화학연구원

    Inventor： 김은희 ,  이윤숙 ,  정용삼 ,  유성은 ,  서지희 ,  채순기 ,  이공주

    IPC: A61K38/16 ,  A61P9/10

    CPC classification number: A61K38/1761 ,  C07K14/4747

    Abstract: A human FAF1 protein inhibitor is provided to inhibit expression or function of an FAF1 protein effectively and inhibit ischemic cell death effectively by acting on a caspase non-dependent cell death passage during the ischemic cell death, and generation of reactive oxygen species, activation of PARP-1, and a nucleus movement passage of AIF, thereby being used as a pharmaceutical composition for treating or preventing ischemic diseases. A composition for treating or preventing ischemic diseases comprises a human FAF1(Fas-associated factor 1) inhibitor as an effective ingredient, which is selected from the group consisting of a double stranded siRNA consisting of a forward single stranded siRNA having a sequence of SEQ ID : NO. 3 and a reverse single stranded siRNA having a sequence of SEQ ID : NO. 4, a double stranded siRNA consisting of a forward single stranded siRNA having a sequence of SEQ ID : NO. 5 and a reverse single stranded siRNA having a sequence of SEQ ID : NO. 6, and a protein having an amino acid sequence of SEQ ID : NO. 7, wherein the ischemic diseases is cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, heart failure, myocardial hypertrophy, retinal ischemia, ischemic colitis, and ischemic acute renal failure mediated by ischemic cell death.

    Abstract translation: 提供人FAF1蛋白抑制剂以有效抑制FAF1蛋白的表达或功能，并通过在缺血性细胞死亡期间作用于胱天蛋白酶非依赖性细胞死亡通道并产生活性氧，有效激活PARP，有效抑制缺血性细胞死亡 -1和AIF的核运动通道，因此用作治疗或预防缺血性疾病的药物组合物。 用于治疗或预防缺血性疾病的组合物包含作为有效成分的人FAF1（Fas相关因子1）抑制剂，其选自由具有SEQ ID NO：1的序列的正向单链siRNA组成的组 ：否 3和具有SEQ ID NO：3的序列的反向单链siRNA。 4，由具有SEQ ID NO：1的序列的正向单链siRNA组成的双链siRNA。 5和具有SEQ ID NO：5的序列的反向单链siRNA。 6，以及具有SEQ ID NO：6的氨基酸序列的蛋白质。 7，其中缺血性疾病是脑缺血，心脏缺血，糖尿病心血管疾病，心力衰竭，心肌肥大，视网膜缺血，缺血性结肠炎和由缺血性细胞死亡介导的缺血性急性肾衰竭。

    싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물
    39.
    发明公开
    싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물 失效
    噻唑衍生物，其制备方法及包括其的药物组合物

    公开(公告)号：KR1020080016249A

    公开(公告)日：2008-02-21

    申请号：KR1020060078095

    申请日：2006-08-18

    Applicant: 한국화학연구원

    Inventor： 천혜경 ,  유성은 ,  조영식 ,  송진숙 ,  김희연 ,  정원훈 ,  배명애 ,  서지희 ,  이규양 ,  김낙정 ,  황순희 ,  송종환

    IPC: C07D277/42 ,  C07D277/36 ,  C07D277/34 ,  A61P29/00

    Abstract: A novel thiazole derivative is provided to inhibit effectively the enzymatic activity of 5-lipoxygenase(5-LO) acting when an arachidonic acid is converted into a leukotriene metabolite, thereby being used as a prophylactic and therapeutic agent of various inflammatory diseases and cancers. A thiazole derivative is represented by the formula(1), wherein each R1 and R2 is independently H, OR7, NO2, halogen or C1-4 linear, branched, or cyclic alkyl; each R3, R4, R5 and R6 is independently H, CF3, OR7, CO2R7, NR7R8, NO2, NHCOR7, C(=O)R7, SR7, halogen, C1-4 linear, branched or cyclic alkyl(in which each R7 and R8 is independently H, unsubstituted or F-substituted C1-6 linear, branched, or cyclic alkyl, or aryl); X is NH, O, S or SO2; Y is C or N. A method for preparing a thiazole derivative represented by the formula(1a) comprises a step of reacting an acetophenone derivative represented by the formula(2) with an aniline derivative represented by the formula(2) and a thiocyanate salt, wherein the R1 to R6, and Y are same as defined above. A pharmaceutical composition for preventing or treating asthma, chronic obstructive lung disease, arthritis, psoriasis, atopic dermatitis, allergy, enteritis, and cancer comprises the thiazole derivative, or a pharmaceutically acceptable salt thereof, a hydrate, solvate or isomer thereof as an effective ingredient.

    Abstract translation: 提供了一种新的噻唑衍生物，用于有效地抑制花生四烯酸转化为白三烯代谢物时作用的5-脂氧合酶（5-LO）的酶活性，从而用作各种炎性疾病和癌症的预防和治疗剂。 噻唑衍生物由式（1）表示，其中每个R 1和R 2独立地为H，OR 7，NO 2，卤素或C 1-4直链，支链或环状烷基; 每个R 3，R 4，R 5和R 6独立地是H，CF 3，OR 7，CO 2 R 7，NR 7 R 8，NO 2，NHCOR 7，C（= O）R 7，SR 7，卤素，C 1-4直链，支链或环状烷基（其中每个R 7和 R8独立地是H，未取代的或F-取代的C 1-6直链，支链或环状烷基或芳基）; X是NH，O，S或SO 2; Y为C或N.由式（1a）表示的噻唑衍生物的制备方法包括使式（2）表示的苯乙酮衍生物与式（2）表示的苯胺衍生物和硫氰酸盐 ，其中R1至R6和Y与上述定义相同。 用于预防或治疗哮喘，慢性阻塞性肺病，关节炎，牛皮癣，特应性皮炎，过敏，肠炎和癌症的药物组合物包含噻唑衍生物或其药学上可接受的盐，其水合物，溶剂化物或异构体作为有效成分 。

    염증억제 활성을 가지는Ｎ-[1'-치환술폰아미드-스파이로(2Ｈ-1-벤조피란-2,4-피페리딘)-6-일]치환아민 유도체, 그의 약학적으로허용가능한 염, 그의 제조방법 및 그의 용도
    40.
    发明授权
    염증억제 활성을 가지는Ｎ-[1'-치환술폰아미드-스파이로(2Ｈ-1-벤조피란-2,4-피페리딘)-6-일]치환아민 유도체, 그의 약학적으로허용가능한 염, 그의 제조방법 및 그의 용도 失效
    염증억제활성을가지는N- [1'-치환술폰아미드 - 스파이로（2H-1-벤조피란-2,4-피페리딘）-6-일]치환아민유도체，그의약학적으로허용가능한염， 그의제조방법및그의용도

    公开(公告)号：KR100746939B1

    公开(公告)日：2007-08-07

    申请号：KR1020060073546

    申请日：2006-08-04

    Applicant: 한국화학연구원

    Inventor： 공영대 ,  천혜경 ,  전문국 ,  조영식 ,  서진수 ,  유성은

    IPC: C07D491/107 ,  A61K31/407 ,  A61P29/00

    Abstract: N-[1'-substituted sulfonamide-spiro(2H-1-benzopyrane-2,4-piperidin)-6-yl]substituted amine derivatives, a process for preparation of the same compounds and use thereof are provided to inhibit 5-lipoxygenase and improve simplicity and yield of preparation, so that the compounds are useful for prevention and treatment of diseases caused by activation of leukotriens. The N-[1'-substituted sulfonamide-spiro(2H-1-benzopyrane-2,4-piperidin)-6-yl]substituted amine derivatives represented by the formula(1) and pharmaceutically acceptable salts thereof are provided, wherein R^1 is C1-C10 alkyl group, benzyl or substituted benzyl group, 2-pyrimidylmethyl group, thiophene group, 2-methylthiophenemethyl group, 5-methyl-2-thiophenemethyl group, indolylmethyl group, benzo dioxolanylmethyl group, naphthalenylmethyl group or furanylmethyl group; and R^2 is C1-C10 alkyl group, phenyl or substituted phenyl group, or hetero atom-containing 5- to 7-membered hetero ring and corresponding sulfonyl group.

    Abstract translation: 提供了N- [1'-取代的磺酰胺 - 螺（2H-1-苯并吡喃-2,4-哌啶）-6-基]取代的胺衍生物，制备相同化合物的方法及其用途，以抑制5-脂氧合酶 并且提高制剂的简单性和收率，因此该化合物可用于预防和治疗由白三烯激活引起的疾病。 提供由式（1）表示的N- [1'-取代的磺酰胺 - 螺（2H-1-苯并吡喃-2,4-哌啶）-6-基]取代的胺衍生物及其药学上可接受的盐， 图1是C1-C10烷基，苄基或取代苄基，2-嘧啶甲基氧基，噻吩基，2- methylthiophenemethyl基，5-甲基-2- thiophenemethyl基，吲哚基，苯并二氧戊环基，萘基甲基氧基或呋喃基甲基; 和R ^ 2为C1-C10烷基，苯基或取代的苯基，或含杂原子的5至7元杂环和相应的磺酰基。

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