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    베타-세크리테아제 활성을 억제하는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물
    12.
    发明授权
    베타-세크리테아제 활성을 억제하는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물 有权
    抑制β-分泌酶活性的4-（苯并咪唑-2-基氨基）吡咯烷衍生物和含有其作为活性成分的药物组合物

    公开(公告)号：KR101383239B1

    公开(公告)日：2014-04-10

    申请号：KR1020120045621

    申请日：2012-04-30

    Applicant: 한국화학연구원

    Inventor： 임희종 ,  이계형 ,  박우규 ,  조희영

    IPC: C07D403/12 ,  C07D235/14 ,  A61K31/4178 ,  A61P25/00

    Abstract: 본 발명은 하기 화학식 1로 표시되는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 또는 이의 약제학적으로 허용 가능한 염, 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 및 치료용 약제학적 조성물 및 이를 유효성분으로 함유하는 베타-세크리테아제(BACE)의 활성 억제제 조성물에 관한 것이다.
    [화학식 1]

    본 발명에 따른 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체는 베타-세크리테아제(BACE)의 활성을 억제하여 신경세포를 손상시키는 베타-아밀로이드 단백질의 생성을 억제함으로써 알츠하이머, 다운증후군 등의 신경퇴행성 질환을 치료하거나 예방하는데 효과적으로 사용될 수 있다.

    Abstract translation: 本发明涉及化学式1的4-（苯并咪唑-2-基氨基）吡咯烷衍生物或其药学上可接受的盐; 含有与用于预防和治疗神经变性疾病的活性成分相同的药物组合物; 以及含有与活性成分相同的β-分泌酶（BACE）活化的抑制剂组合物。 根据本发明的4-（苯并咪唑-2-基氨基）吡咯烷衍生物抑制BACE的活化和产生引起神经细胞损伤的β-淀粉样蛋白，从而有效地预防或治疗神经变性疾病如阿尔茨海默氏病和 唐氏综合症。

    할로겐을 함유하는 트리페닐렌계 반응성 메조겐 화합물의 합성
    13.
    发明公开
    할로겐을 함유하는 트리페닐렌계 반응성 메조겐 화합물의 합성 有权
    含有基于三聚氰胺核的反应体系的卤化物

    公开(公告)号：KR1020120065657A

    公开(公告)日：2012-06-21

    申请号：KR1020100126907

    申请日：2010-12-13

    Applicant: 한국화학연구원

    Inventor： 가재원 ,  이미혜 ,  정혜인 ,  김진수 ,  이계형

    IPC: C07C43/225 ,  C07C69/76 ,  C09K19/32 ,  G02F1/13

    Abstract: PURPOSE: A triphenylene-based reactive mesogen compound is provided to have high double refraction ratio, thereby capable of manufacturing a compensation film to thin film, and providing a liquid crystal display device capable of obtaining wide viewing angle. CONSTITUTION: A triphenylene-based reactive mesogen compound is in chemical formula 1. In chemical formula 1, X is one selected from a bromo group, a chloro group and iodo group, Y is one selected from O, NH and S, L is selected from -R-, -C(=O)-R-, -C(=O)-Ar-O-R- and C(=O)-Ar-NH-R-, R is linear or branched C1-20 alkylene group, Ar is C6-30 arylene group, Z is selected from -OCOCHCH2, -OCOC(CH3)CH2, -OCOCHCH-Ph, -OCOCHCH-furanyl, -NHCOCHCH2, -HNCOC(CH3)CH2, -HNCOCHCH-Ph, and -NHCOCHCH-furanyl.

    Abstract translation: 目的：提供一种具有高双折射率的三亚苯基反应性液晶组合物，从而能够制造薄膜补偿膜，并提供能够获得宽视角的液晶显示装置。 构成：以亚苯基为基的反应性介晶化合物为化学式1.在化学式1中，X为选自溴基，氯基和碘基的一个，Y为选自O，NH和S的一个，选择L为 由-C（= O）-R - ， - C（= O）-Ar-OR-和C（= O）-Ar-NH-R-，R是直链或支链C 1-20亚烷基 ，Ar为C6-30亚芳基，Z选自-OCOCHCH2，-OCOC（CH3）CH2，-OCOCHCH-Ph，-OCOCHCH-呋喃基，-NHCOCHCH2，-HNCOC（CH3）CH2，-HNCOCHCH-Ph，和 - NHCOCHCH呋喃基。

    신규한 1-[1-(3,4-디알콕시벤질)-1Ｈ-피롤 화합물, 이의제조방법 및 이를 포함하는 천식 및 만성폐쇄성 폐질환을포함한 염증관련 질환, 관절염, 아토피 피부염, 암 및뇌질환의 치료 및 예방을 위한 약제학적 조성물
    15.
    发明公开
    신규한 1-[1-(3,4-디알콕시벤질)-1Ｈ-피롤 화합물, 이의제조방법 및 이를 포함하는 천식 및 만성폐쇄성 폐질환을포함한 염증관련 질환, 관절염, 아토피 피부염, 암 및뇌질환의 치료 및 예방을 위한 약제학적 조성물 失效
    1- [1-（3,4-二甲氧基苄基）-1H-吡咯烷酮化合物，其制备方法和药物组合物，用于治疗或预防哮喘，慢性阻塞性肺动脉疾病，ARTHRITIS，原发性恶性肿瘤，包括其的肿瘤和变应性脑疾病

    公开(公告)号：KR1020090058752A

    公开(公告)日：2009-06-10

    申请号：KR1020070125491

    申请日：2007-12-05

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  송종환 ,  이계형 ,  김익연

    IPC: C07D207/325 ,  A61K31/40 ,  A61P35/00 ,  A61P29/00

    Abstract: A 1-[1-(3,4-dialkoxybenzyl)-1H-pyrrole compound is provided to obtain excellent inhibition activity to PDE-4 enzyme and high enzyme selectivity. A 1-[1-(3,4-dialkoxybenzyl)-1H-pyrrole compound is denoted by the chemical formula 1. In the chemical formula 1, R1 and R2 are different or same. The R1 and R2 are individually hydrogen, saturated or unsaturated alkyl(C1-C7) of straight chain and branch chain, saturated or unsaturated alkyl(C1-C7) of straight chain and branch chain containing oxygen, nitrogen or sulfur, cycloalkyl of C3-C7, and cycloalkyl of C3-C7 containing oxygen, nitrogen, or sulfur. R1 and R2 is connected with (C1 - C3) alkylene or (C1 - C3) alkylene containing halogen.

    Abstract translation: 提供1- [1-（3,4-二烷氧基苄基）-1H-吡咯化合物以获得对PDE-4酶的优异抑制活性和高酶选择性。 化学式1表示1- [1-（3,4-二烷氧基苄基）-1H-吡咯化合物。在化学式1中，R 1和R 2不同或相同。 R1和R2分别是氢，饱和或不饱和的直链和支链烷基（C1-C7），含有氧，氮或硫的直链和支链的饱和或不饱和烷基（C1-C7），C3- C7和含有氧，氮或硫的C3-C7的环烷基。 R1和R2与（C1-C3）亚烷基或（C1-C3）亚烷基的卤素连接。

    1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1Ｈ-피라졸 화합물의제조방법
    18.
    发明授权
    1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1Ｈ-피라졸 화합물의제조방법 失效
    制备1- [1-（3,4-二氮代烷基） - 吡咯烷基] -1H-吡唑化合物的方法

    公开(公告)号：KR100838702B1

    公开(公告)日：2008-06-16

    申请号：KR1020070013408

    申请日：2007-02-08

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  송종환 ,  이계형 ,  김익연 ,  소원영

    IPC: C07D401/06

    Abstract: A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound is provided to produce a desired product with high purity economically and industrially compared with a method for separating the desired product using a chiral column. A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound represented by a formula(1) comprises the steps of: (a) subjecting an aryl aldehyde compound represented by a formula(2) and 2-methyl-2-propanesulfinamide to condensation in the presence of titanium ethoxide(Ti(OEt)4) to prepare a compound represented by a formula(4); (b) reacting the compound of the formula(4) with a compound represented by a formula(5) to prepare a compound represented by a formula(6); (c) removing a sulfinyl group of the compound of the formula(6) under acidic condition to prepare an amine compound represented by a formula(7); (d) reacting the compound of the formula(7) with a compound represented by a formula(8) to prepare a cis-type compound represented by a formula(9); and (e) after N-aminating the cis-type compound of the formula(9) by dropping amino 4-nitrobenzoate represented by a formula(10) therein in the existence of a strong base, cyclizing the N-aminated compound to prepare the compound of the formula(1). In the formulae, A is CH; R1 is linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen; R2 is C3-7 cycloalkyl or (C3-10)cycloalkyl(C1-7)alkyl; and R3 is phenyl which may be substituted by at least one substituent selected from the group consisting of C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, (C1-7)alkylsiloxy(C1-7)alkyl, C1-5 alkoxycarbonyl, benzyloxy, halogen, nitro, cyano, C1-7 alkylsiloxy, carboxyl and formyl.

    Abstract translation: 提供了一种制备1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物的方法，与使用手性的分离所需产物的方法相比，在经济和工业上产生具有高纯度的所需产物 柱。 制备由式（1）表示的1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物的方法包括以下步骤：（a）使由式 2）和2-甲基-2-丙磺酰胺在乙醇钛（Ti（OEt）4）存在下缩合以制备由式（4）表示的化合物; （b）使式（4）的化合物与式（5）表示的化合物反应，制备由式（6）表示的化合物; （c）在酸性条件下除去式（6）化合物的亚磺酰基以制备由式（7）表示的胺化合物; （d）使式（7）的化合物与式（8）表示的化合物反应，制备由式（9）表示的顺式化合物; 和（e）通过在存在强碱的情况下滴加由式（10）表示的式（10）表示的氨基-4-硝基苯甲酸将式（9）的顺式式化合物N-胺化后，使N-胺化化合物环化以制备 式（1）的化合物。 在式中，A为CH; R1是可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基; R2是C3-7环烷基或（C3-10）环烷基（C1-7）烷基; 并且R 3是可以被至少一个选自C 1-7烷基，C 3-7环烷基，（C 3-10）环烷基（C 1-7）烷基，C 1-7烷氧基， 7）烷氧基（C 1-7）烷基，（C 1-7）烷基甲硅烷氧基（C 1-7）烷基，C 1-5烷氧基羰基，苄氧基，卤素，硝基，氰基，C 1-7烷基甲硅烷氧基，羧基和甲酰基。

    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물
    19.
    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。

    믹소첼린-에이를 유효성분으로 하는 항산화 및 항암용약학 조성물
    20.
    发明授权
    믹소첼린-에이를 유효성분으로 하는 항산화 및 항암용약학 조성물 失效
    믹소첼린 - 에이를유효성분으로하는항산화및항암용약학조성물

    公开(公告)号：KR100424392B1

    公开(公告)日：2004-03-24

    申请号：KR1020010041239

    申请日：2001-07-10

    Applicant: 한국화학연구원

    Inventor： 안종웅 ,  이호현 ,  노재성 ,  이계형 ,  이정옥 ,  최상운 ,  권중호

    IPC: A61K31/165

    Abstract: PURPOSE: A pharmaceutical composition containing myxochelin-A which exhibits excellent anticancer activity against human cancer cells, together with excellent antioxidant activity as a main component is provided which can be effectively used as an effective antioxidant and anticancer agent. CONSTITUTION: The pharmaceutical composition contains myxochelin-A of formula 1 obtained by being separated from myxobacteria or being chemically synthesized or semisynthesized. The myxochelin-A is purely separated by the steps of: separating a biomass and absorption resin by culturing Angiococcus disciformis strains as myxobacteria in the presence of absorption resin and centrifuging a culture solution; adding an organic solvent, preferably a mixed solvent of acetone and methanol; extracting and filtering to remove the biomass and absorption resin; preparing an active fraction by concentrating the filtrate under reduced pressure and extracting a crude extract in an organic solvent; and successively performing silica gel liquid chromatography and recycling preparative HPLC.

    Abstract translation: 目的：提供一种药物组合物，其含有对人癌细胞具有优异的抗癌活性以及优异的抗氧化活性作为主要组分的粘液溶血素A，其可以有效地用作有效的抗氧化剂和抗癌剂。 组成：药物组合物含有通过从粘细菌分离或化学合成或半合成获得的式1的粘多糖蛋白-A。 通过在吸附树脂存在下离心培养溶液培养作为粘细菌的粘细菌属细菌菌株来分离生物质和吸附树脂，纯粹分离粘液粘连素-A; 加入有机溶剂，优选丙酮和甲醇的混合溶剂; 提取并过滤去除生物质和吸收树脂; 通过在减压下浓缩滤液并在有机溶剂中萃取粗提取物来制备活性部分; 并连续进行硅胶液相色谱和再循环制备型HPLC。

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