公开(公告)号：KR101051077B1

公开(公告)日：2011-07-21

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: 본 발명은 하기 화학식 1로 표시되는 2-피페라지노-4,5-이중치환-1,3-티아졸 유도체, 그의 제조방법 및 그를 유효성분으로 함유하는 SPC 수용체 활성으로 유발되는 염증관련 질환에 유용한 그의 용도에 관한 것이다.
본 발명의 2-피페라지노-4,5-이중치환-1,3-티아졸 유도체는 사람으로부터 유래된 진피세포 및 마우스를 이용한 동물실험을 통하여 항염증 효과를 검색한 결과, 종래 SPC 수용체에 유용한 공지된 티아졸 유도체보다 더욱 우수한 억제활성을 규명함으로써, 상기 2-피페라지노-4,5-이중치환-1,3-티아졸 유도체 또는 그로부터 분리된 광학이성질체를 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 , R
3 , X 및 Y는 명세서에서 정의한 바와 같다.)
2-피페라지노-1,3-티아졸, 조합화학합성, 스핀고실포스포릴콜린, 아토피, 염증치료

Abstract translation: 本发明2-哌嗪基-4,5-双取代-1,3-噻唑衍生物，含有它们作为由下述通式表示的活性成分所造成的SPC受体活性产生和炎症相关的疾病的方法（1） 对其使用有用。

公开(公告)号：KR100967590B1

公开(公告)日：2010-07-05

申请号：KR1020080016257

申请日：2008-02-22

Applicant: 한국화학연구원

Inventor： 공영대 ,  전문국 ,  이태호 ,  황순희 ,  유성은

IPC: C07D241/44 ,  A61K31/498

Abstract: 본 발명은 우수한 멜라닌-집중형 호르몬 수용체(melanin-concentrating hormone 1 receptor, 이하 "MCH1R"이라 한다) 억제 활성을 가지는 하기 화학식 1로 표시되는 퀴녹살린 유도체 및 약제학적으로 허용 가능한 그의 염, 그 제조방법 및 그를 유효성분으로 함유하는 비만치료제의 용도에 관한 것이다.

(상기에서, R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , NR
7 R
8
및 X는 명세서에서 정의한 바와 같다.)
퀴녹살린, MCH1R, 비만치료제

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。

公开(公告)号：KR100954611B1

公开(公告)日：2010-04-26

申请号：KR1020070109233

申请日：2007-10-29

Applicant: 한국화학연구원 ,  제이더블유중외제약 주식회사

Inventor： 공영대 ,  전문국 ,  이태호 ,  정경윤 ,  정재욱

IPC: C07D311/04 ,  C07D405/12 ,  C07D417/12

Abstract: 본 발명은 우수한 NF-κB 표적유전자 발현 억제 활성 및 암세포 증식 억제 활성을 가지는 신규 2-메틸-2-(옥시메틸)-6-(우레이도)-2
H -벤조피란 유도체와 약제학적으로 허용 가능한 이의 염, 이 화합물의 제조방법, 그리고 이 화합물의 항암제로서의 용도에 관한 것이다.
벤조피란, NF-κB, 항암제, 암세포 증식 억제 활성

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。

公开(公告)号：KR1020090022398A

公开(公告)日：2009-03-04

申请号：KR1020070087718

申请日：2007-08-30

Applicant: 한국화학연구원

Inventor： 공영대 ,  황순희 ,  이상한 ,  허진철

IPC: A61K31/353 ,  A61P27/14

Abstract: A 2-methyl-2-hydroxymethyl-6-amido benzopyran derivative and its salt are promote Th1 differentiation with high activity in a T-bet promotor assay, thereby effectively curing bronchial asthma, atopic dermatitis, and allergic rhinitis. A 2-methyl-2-hydroxymethyl-6-amido benzopyran derivative is represented by the formula 1. In the formula 1, R1 indicates a C1-C5 alkyl group, benzyl or substituted benzyl group, phenethyl group, 2- pyrimidyl methyl group, thiophene group, 2-methyl thiophene methyl group, 5-methyl-2-thiophene methyl group, 3-thiophene methyl group, indolyl methyl group, naphthalene ylmethyl group, or a furanylmethyl group.

Abstract translation: 2-甲基-2-羟甲基-6-氨基苯并吡喃衍生物及其盐在T-bet启动子测定中促进Th1分化的高活性，从而有效地治愈了支气管哮喘，特应性皮炎和过敏性鼻炎。 2-甲基-2-羟甲基-6-氨基苯并吡喃衍生物由式1表示。在式1中，R1表示C1-C5烷基，苄基或取代苄基，苯乙基，2-嘧啶基甲基， 噻吩基，2-甲基噻吩甲基，5-甲基-2-噻吩甲基，3-噻吩甲基，吲哚基甲基，萘基甲基或呋喃基甲基。

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。

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

公开(公告)号：KR1020060123000A

公开(公告)日：2006-12-01

申请号：KR1020050045294

申请日：2005-05-28

Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

Inventor： 공영대 ,  이일영 ,  이종철 ,  조희영 ,  황종연 ,  최형섭 ,  전현숙 ,  유성은 ,  이창훈 ,  성대석 ,  김광미 ,  김대권 ,  양혜진 ,  김형준 ,  박종희 ,  심영철

IPC: C07D311/22 ,  C07D311/24

CPC classification number: C07D311/22

Abstract: 2,2-Dimethyl-3-alkylether-4-alkoxy-6-alkyl amino benzopyrane derivatives and PGE2(prostagrandine E2) production inhibitors containing the same compounds as an effective ingredient are provided to treat diseases associated with the activity of PGE2 by suppressing inflammation caused by PGE2. The 2,2-dimethyl-3-alkylether-4-alkoxy-6-alkyl amino benzopyrane derivatives represented by the formula(1) or their pharmaceutically acceptable salts are provided, wherein R^1 and R^2 are identical or different, and are each independently C1-C10 linear, branched or cyclic alkyl group, optionally substituted benzyl group or penethyl group; and R^3 is hydrogen, C1-C10 alkyl group, C2-C10 alkenyl group, C2-C10 alkynyl group, optionally substituted benzyl group or naphthylmethyl group. The PGE2 production inhibitors contain 2,2-dimethyl-3-alkylether-4-alkoxy-6-alkyl amino benzopyrane derivatives represented by the formula(1) or their pharmaceutically acceptable salts as effective ingredient.

Abstract translation: 提供含有相同化合物作为有效成分的2,2-二甲基-3-烷基醚-4-烷氧基-6-烷基氨基苯并吡喃衍生物和PGE2（前列腺素E2）产生抑制剂，用于通过抑制炎症来治疗与PGE2的活性相关的疾病 由PGE2引起。 提供由式（1）表示的2,2-二甲基-3-烷基醚-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，其中R 1和R 2相同或不同，和 各自独立地为C 1 -C 10直链，支链或环状烷基，任选取代的苄基或苯乙基; R 3为氢，C 1 -C 10烷基，C 2〜C 10烯基，C 2〜C 10炔基，任意取代的苄基或萘甲基。 PGE 2生成抑制剂含有式（1）表示的2,2-二甲基-3-烷基醚-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。

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。