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    2-피페라지노-4,5-이중치환-1,3-티아졸 유도체, 그의 제조방법 및 그를 유효성분으로 함유하는 ＳＰＣ 수용체 활성으로 유발되는 염증관련질환 치료제
    11.
    发明公开
    2-피페라지노-4,5-이중치환-1,3-티아졸 유도체, 그의 제조방법 및 그를 유효성분으로 함유하는 ＳＰＣ 수용체 활성으로 유발되는 염증관련질환 치료제 失效
    2-哌嗪基-4,5-取代-1,3-噻唑衍生物，其制备方法，用于由含有SPC活性诱导的抗炎性疾病的治疗剂

    公开(公告)号：KR1020100064952A

    公开(公告)日：2010-06-15

    申请号：KR1020080123618

    申请日：2008-12-05

    Applicant: 한국화학연구원

    Inventor： 공영대 ,  이태호 ,  전문국 ,  황순희

    IPC: C07D417/02 ,  A61K31/445

    CPC classification number: C07D417/04 ,  C07D417/14

    Abstract: PURPOSE: A 2-piperazino-4,5-double substitution-1,3-thiazole derivative is provided to treat atopic dermatitis caused by sphingosylphosphorylcholine(SPC). CONSTITUTION: A 2-piperazino-4,5-double substitution-1,3-thiazole derivative is denoted by chemical formula 1. A method for manufacturing the 2-piperazino-4,5-double substitution-1,3-thiazole derivative comprises: a step of reacting 2-haloacetophenone derivative with thio aminocarbonate which is linked by sulfanyl linker of chemical formula 2 to obtain a compound of chemical formula 3; a step of polymerizing chloridation carboxylic acid with 4-amino group of the compound of chemical formula 3 to obtain a compound of chemical formula 4; and a step of synthesizing a sulfanyl resin part of the compound of chemical formula 4 to obtain a compound of chemical formula 5.

    Abstract translation: 目的：提供2-哌嗪基-4,5-双取代-1,3-噻唑衍生物，用于治疗由鞘氨醇磷酰胆碱（SPC）引起的特应性皮炎。 构成：2-哌嗪基-4,5-双取代-1,3-噻唑衍生物由化学式1表示。制备2-哌嗪基-4,5-双取代-1,3-噻唑衍生物的方法包括 ：使2-卤代苯乙酮衍生物与硫代氨基碳酸酯反应的步骤，其通过化学式2的硫烷基连接体连接，得到化学式3的化合物; 将化学式3的化合物的4-氨基的氯化羧酸聚合以获得化学式4的化合物的步骤; 以及合成化学式4化合物的硫烷基树脂部分以获得化学式5的化合物的步骤。

    항암활성을 갖는1'-알킬피페리딘-4'-스피로-2-6-(아미도)-2Ｈ-벤조피란유도체
    13.
    发明公开
    항암활성을 갖는1'-알킬피페리딘-4'-스피로-2-6-(아미도)-2Ｈ-벤조피란유도체 失效
    具有抗病毒活性的1'-烷基哌啶-4'-SPIRO-2-6-（氨基）-2H-苯并噻吩衍生物

    公开(公告)号：KR1020090022936A

    公开(公告)日：2009-03-04

    申请号：KR1020070088641

    申请日：2007-08-31

    Applicant: 한국화학연구원 ,  제이더블유중외제약 주식회사

    Inventor： 공영대 ,  전문국 ,  이태호 ,  황순희 ,  이태임 ,  이지민 ,  정경윤 ,  정재욱

    IPC: C07D491/107 ,  A61K31/4433 ,  A61P35/00

    CPC classification number: C07D491/107 ,  C07D491/10

    Abstract: A 1'-alkylpiperidine-4'-spiro-2-6-(amido)-2h-benzopyran derivative is provided to suppress expression of a NF-kappaB target gene and proliferation of cancer cells. A 1'-alkylpiperidine-4'-spiro-2-6-(amido)-2h-benzopyran derivative is represented by the formula 1. In the formula 1, A indicates a hydrogen atom, halogen atom, C1-C6 alkyl group, or a C1-C6 alkoxy group; B shows a hydrogen atom or a C1-C6 alkyl group; R1 is a C1-C6 alkyl group; and R2 is aryl or heteroaryl. The aryl or heteroaryl is substituted with one or three substituents selected from the group consisting of a halogen atom, hydroxyl group, C1-C6 alkyl group, C1-C6 halo alkyl group, and a C1-C6 alkoxy group.

    Abstract translation: 提供1'-烷基哌啶-4'-螺-2-6-（酰氨基）-2H-苯并吡喃衍生物以抑制NF-κB靶基因的表达和癌细胞的增殖。 1'-烷基哌啶-4'-螺-2-2-（酰胺基）-2H-苯并吡喃衍生物由式1表示。在式1中，A表示氢原子，卤素原子，C1-C6烷基， 或C 1 -C 6烷氧基; B表示氢原子或C1-C6烷基; R1是C1-C6烷基; 并且R 2是芳基或杂芳基。 芳基或杂芳基被一个或三个选自卤素原子，羟基，C 1 -C 6烷基，C 1 -C 6卤代烷基和C 1 -C 6烷氧基的取代基取代。

    염증억제 활성을 가지는Ｎ-[1'-치환술폰아미드-스파이로(2Ｈ-1-벤조피란-2,4-피페리딘)-6-일]치환아민 유도체, 그의 약학적으로허용가능한 염, 그의 제조방법 및 그의 용도
    14.
    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。

    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체를 유효성분으로 함유하는 PGE2 활성에 관련된 염증질환 치료제
    15.
    发明授权
    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체를 유효성분으로 함유하는 PGE2 활성에 관련된 염증질환 치료제 失效
    由含有作为有效成分的2,2-二甲基-3-异恶唑-4-基烷氧基苯甲酰基衍生物的PGE2活性诱导的抗炎性疾病治疗剂

    公开(公告)号：KR100687522B1

    公开(公告)日：2007-02-27

    申请号：KR1020050045293

    申请日：2005-05-28

    Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

    Inventor： 공영대 ,  전문국 ,  서진수 ,  이창훈 ,  양혜진

    IPC: A61K31/351

    Abstract: 본 발명은 하기 화학식 1로 표시되는 2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체에 대한 프로스타그란딘 E2(prostagrandine E2 ; PGE2)의 생성에 관한 억제활성 및 그로 인한 용도에 관한 것이다.
    본 발명은 2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체가 PGE2 의 생성에 대하여 우수한 억제활성을 나타냄을 세포 수준 및 동물실험을 통하여 규명함으로써, 상기 2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체를 유효성분으로 함유하여 PGE2 활성으로 유발되는 염증관련 질환 치료제 개발에 유용하다.

    (상기 식에서, R
    1 , R
    2 및 R
    3 는 명세서에서 정의한 바와 같다.)
    아미노벤조피란, 프로스타그란딘, 산화적스트레스, 라디칼, 염증치료제

    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체를 유효성분으로 함유하는 PGE2 활성에 관련된 염증질환 치료제
    16.
    发明公开
    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노벤조피란 유도체를 유효성분으로 함유하는 PGE2 활성에 관련된 염증질환 치료제 失效
    含有2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯甲酰基衍生物的PGE2生产抑制剂作为有效成分

    公开(公告)号：KR1020060122999A

    公开(公告)日：2006-12-01

    申请号：KR1020050045293

    申请日：2005-05-28

    Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

    Inventor： 공영대 ,  전문국 ,  서진수 ,  이창훈 ,  양혜진

    IPC: A61K31/351

    Abstract: PGE2(prostagrandine E2) production inhibitors containing 2,2-dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyrane derivatives as an effective ingredient are provided to inhibit inflammation caused by the activity of PGE2, so that diseases associated with inflammation are treated. The PGE2 production inhibitors contain 2,2-dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyrane derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof as an effective ingredient, wherein R^1 and R^2 are identical or different, and are each independently C1-C10 alkyl group, optionally substituted benzyl group or penethyl group; and R^3 is C1-C10 alkyl group, C2-C10 alkenyl group, C2-C10 alkynyl group, optionally substituted benzyl group, naphthylmethyl group or 5- to 7-membered heteroring containing hetero atom selected from oxygen and sulfur atom.

    Abstract translation: 提供含有2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃衍生物作为有效成分的PGE2（前列腺素E2）产生抑制剂，以抑制由PGE2的活性引起的炎症，从而与炎症相关的疾病 被处理。 PGE 2生产抑制剂含有式（1）表示的2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃衍生物或其药学上可接受的盐作为有效成分，其中R 1和R 2 各自独立地为C1-C10烷基，任选取代的苄基或penethyl基; R 3是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，任选取代的苄基，萘甲基或含有选自氧和硫原子的杂原子的5-至7-元杂环。

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