公开(公告)号：KR1020120115606A

公开(公告)日：2012-10-19

申请号：KR1020110016412

申请日：2011-02-24

Applicant: 한국화학연구원

Inventor： 가재원 ,  이미혜 ,  정혜인 ,  박정신 ,  김진수 ,  이계형

IPC: C07C237/20 ,  C07C233/88 ,  C09K19/32 ,  G02F1/1335

CPC classification number: C09K19/32 ,  C09K2019/328 ,  G02F1/13363 ,  G02F2001/133633

Abstract: PURPOSE: An acetylene-containing triphenylene-based reactive mesogen compound is provided to manufacture a thin film from a reinforcing film because of high double reflectivity. CONSTITUTION: An acetylene-containing triphenylene-based reactive mesogen compound is indicated in chemical formula 1. In chemical formula 1, X is selected from O, NH and S, L is selected from R, C(=O)R, C(=O)ArOR and -C(=O)ArNHR, Y is selected from CH2, Ar, ArO, ArS, ArNH, C(=O), C(=O)O, C(=O)NH, C(=O)Ar, C(=O)ArO, C(=O)ArS, C(=O)ArNH, ArC(=O), ArC(=O)O, ArC(=O)S and ArC(=O)NH, Z is selected from -OC(O)CH=CH2, -OC(O)C(CH3)=CH2, a functional group indicated in chemical formula a, a functional group indicated in chemical formula b, -NHC(O)CH=CH2, -NHC(O)C(CH3)=CH2, a functional group in chemical formula c, a functional group indicated in chemical formula d, A is selected from -R', C(=O)R', and -R'-Z, R is C1-20 alkylene, Ar is C6-30 arylene, and R' is C1-20 alkyl.

Abstract translation: 目的：提供含乙炔的三亚苯基反应性液晶元素化合物，由于双重反射率的高度，从加强膜制造薄膜。 化学式1中，X选自O，NH和S，L选自R，C（= O）R，C（= O）ArOR和-C（= O）ArNHR，Y选自CH 2，Ar，ArO，ArS，ArNH，C（= O），C（= O）O，C（= O）NH，C（= O ）Ar，C（= O）ArO，C（= O）ArS，C（= O）ArNH，ArC（= O），ArC（= O）O，ArC（= O） ，Z选自-OC（O）CH = CH 2，-OC（O）C（CH 3）= CH 2，化学式a表示的官能团，化学式b表示的官能团，-NHC（O）CH = CH 2，-NHC（O）C（CH 3）= CH 2，化学式c中的官能团，化学式d表示的官能团，A选自-R'，C（= O）R' R'-Z，R为C 1-20亚烷基，Ar为C 6-30亚芳基，R'为C 1-20烷基。

公开(公告)号：KR1020120063704A

公开(公告)日：2012-06-18

申请号：KR1020100124795

申请日：2010-12-08

Applicant: 한국화학연구원

Inventor： 김진수 ,  이미혜 ,  가재원 ,  박지민 ,  이계형

IPC: C09K19/32 ,  C09K19/34 ,  C08J5/18

Abstract: PURPOSE: A polymerizable liquid crystal compound is provided to enhance isotropic phase transition temperature, optical anisotropy, polymerization, and compatibility. CONSTITUTION: A polymerizable liquid crystal compound is represented by chemical formula 1. Here, X is independently selected from hydrogen and C1-12 straight-chain or side chain alkyl, L is -(C=O) -, - (C=O) -O-, - (C=O) -CH=CH-, - (C=O) -C≡C-, or - (C=O) -NR^1-, Ar is C6-12 monoaryl group, biaryl group, or C5-10 heteroaryl group, R is independently selected from hydrogen and C1-12 straight-chain or side chain alkyl, and P is -OCOCH=CH2, - OCOC (CH3) =CH2, - OCH 2, -OCOCH=CH-Ph, functional group of chemical formula 1a, -O-CH=CH2, -OCH2CH=CH2, functional group of chemical formula 1b, or functional group of chemical formula 1c.

Abstract translation: 目的：提供可聚合液晶化合物，以提高各向同性相转变温度，光学各向异性，聚合和相容性。 构成：可聚合的液晶化合物由化学式1表示。这里，X独立地选自氢和C 1-12直链或侧链烷基，L是 - （C = O） - ， - （C = O） -O - ， - （C = O）-CH = CH-， - （C = O）-C≡C-或 - （C = O）-NR 1 - ，Ar为C 6-12单芳基， 基团或C5-10杂芳基，R独立地选自氢和C1-12直链或侧链烷基，P是-OCOCH = CH 2，-OCOC（CH 3）= CH 2，-OCH 2，-OCOCH = CH-Ph，化学式1a的官能团，-O-CH = CH 2，-OCH 2 CH = CH 2，化学式1b的官能团或化学式1c的官能团。

公开(公告)号：KR100838692B1

公开(公告)日：2008-06-16

申请号：KR1020070069765

申请日：2007-07-11

Applicant: 한국화학연구원

Inventor： 전동주 ,  송종환 ,  이계형 ,  김익연

IPC: C07D487/04 ,  A61K31/52 ,  A61P29/00

Abstract: A novel 7-(3',4'-dialkoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine compound is provided to show excellent inhibitory activity and high enzyme selectivity on PDE-4 enzyme, thereby being used in order to prevent and treat inflammation related diseases, arthritis, atopic dermatitis, tumor, and brain diseases. A 7-(3',4'-dialkoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine compound is represented by a formula(1), wherein each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl, linear or branched saturated or unsaturated C1-7 alkyl including O, N or S, C3-7 cycloalkyl, C3-7 cycloalkyl including O, N or S, (C3-7)cycloalkyl(C1-7)alkyl, 3 to 7-membered saturated or unsaturated heterocycloalkyl including O, N or S in a hetero-ring, phenyl or benzyl, or R1 and R2 may be linked to each other by C1-3 alkylene or C1-3 alkylene including halogen; each R3 and R4 is independently H, formyl, halogen, linear or branched saturated or unsaturated C1-7 alkyl. C1-7 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, hydroxy(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, C1-7 alkyl carboxyl, carboxy(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, (C3-7)cycloalkylamino, morpholine, morpholine oxide, thio- morpholine, piperidine, piperazine, piperazine oxide, piperidine, piperidine oxide, pyrrolidine, cyano, nitro, carboxyl, guanidine, urea, phenoxy, benzyloxy or aryl represented by Ar; and R5 is H, linear or branched saturated or unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, mono or di(C1-7)alkylamino, carbonyl, cyano, C1-7 alkoxycarbonyl, aminocarbonyl, C1-7 alkylcarbonyl, (C6-10)ar(C1-7)alkylcarbonyl or C6-10 arylcarbonyl. A method for preparing the compound of the formula(1) comprises the steps of: (a) after reacting a 3-amino-5-substituted pyrazole compound represented by a formula(4) with a 3-(dimethylamino)-1-(3,4-dialkoxyphenyl)prophenone compound represented by a formula(5) or a 3-(3,4-dialkoxyphenyl)cinnamic aldehyde compound represented by a formula(6) in the presence of an acetic acid, reducing a reaction producing with NaBH4 to prepare a compound represented by the formula(1); and (b) subjecting the compound of a formula(10) to nucleophilic substitution. A pharmaceutical composition for treating or preventing asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof.

Abstract translation: 提供了一种新型的7-（3'，4'-二烷氧基苯基）-4,5,6,7-四氢吡唑并[1,5-a]嘧啶化合物，以显示优异的抑制活性和对PDE-4酶的高酶选择性 用于预防和治疗炎症相关疾病，关节炎，特应性皮炎，肿瘤和脑疾病。 7-（3'，4'-二烷氧基苯基）-4,5,6,7-四氢吡唑并[1,5-a]嘧啶化合物由式（1）表示，其中每个R 1和R 2独立地为H，线性 或支链饱和或不饱和C 1-7烷基，包括O，N或S，C 3-7环烷基的直链或支链饱和或不饱和C 1-7烷基，包括O，N或S的C 3-7环烷基，（C 3-7）环烷基（ C 1-7烷基，含有杂环中O，N或S的3至7元饱和或不饱和杂环烷基，苯基或苄基，或R 1和R 2可以通过C 1-3亚烷基或C 1-3 包括卤素的亚烷基; 每个R 3和R 4独立地是H，甲酰基，卤素，直链或支链饱和或不饱和的C 1-7烷基。 C 1-7烷氧基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，C 1-7烷基酮，羟基（C 1-7）烷基，（C 3-7）环烷基（C 1-7）烷基， （C 3-7）环烷基（C 1-7）烷氧基，C 1-7烷基羧基，羧基（C 1-10）烷基酯，羧基（C 1-10）烷基酰胺，氨基，单或二（C 1-7）烷基氨基，单或二 （C 1-7）烷基氨基羰基，（C 3-7）环烷基氨基，吗啉，吗啉氧化物，硫代吗啉，哌啶，哌嗪，哌嗪氧化物，哌啶，哌啶氧化物，吡咯烷，氰基，硝基，羧基，胍，脲，苯氧基， 或由Ar表示的芳基; 并且R 5为H，直链或支链饱和或不饱和的C 1-7烷基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，（C 3-7）环烷基（C 1-7） 7）环烷基（C 1-7）烷氧基，一或二（C 1-7）烷基氨基，羰基，氰基，C 1-7烷氧基羰基，氨基羰基，C 1-7烷基羰基，（C 6-10）芳（C 1-7）烷基羰基或C 6 -10芳基羰基。 制备式（1）化合物的方法包括以下步骤：（a）使由式（4）表示的3-氨基-5-取代的吡唑化合物与3-（二甲基氨基）-1-（ （5）表示的丙烯酮化合物或由式（6）表示的3-（3,4-二烷氧基苯基）肉桂醛化合物在乙酸存在下还原产生的反应 以制备由式（1）表示的化合物; 和（b）使式（10）的化合物进行亲核取代。 用于治疗或预防哮喘，慢性阻塞性肺病，关节炎，特应性皮炎，肿瘤和退行性脑疾病的药物组合物包含式（1）化合物或其药学上可接受的盐。

公开(公告)号：KR1020040003403A

公开(公告)日：2004-01-13

申请号：KR1020020038093

申请日：2002-07-03

Applicant: 한국화학연구원

Inventor： 이창진 ,  강영구 ,  김동욱 ,  김성림 ,  노재성 ,  이계형

IPC: C07D217/24

Abstract: PURPOSE: A π-conjugate compound for molecular electronic devices is provided. The compound can be self-assembled, has easy electron-delocalized structure by π -conjugate linkage of total molecules, and properties to easily trap electron by electric filed produced from the outside because cation is contained within the molecules. CONSTITUTION: A π-conjugate compound for molecular electronic devices is characterized by being represented by the formula(1) of R¬1-Z- £Redox|¬1-Z-R¬2, containing center £Redox| capable of oxidation/reduction, and being connected to aromatic compounds directly or via acetylene bond,, wherein R1 is selected from benzene, CH3COS-benzene, CH3SS-benzene and SiS-benzene; R2 is selected from S-COCH3-benzene and (S-benzene)2; Z is single bond or triple bond; £Redox|1 is selected from X-N+R3-benzene, N+R3-naphthalene, and N+CH3CH3R3-naphthalene; R3 is selected from hydrogen, C1-C4 alkyl and benzyl; X- is selected from I-, Cl-, Br-, CF3SO3, CH3-benzene-SO3-, C12H25-benzene-SO3-, BF4-, PF6- and SbF6-.

Abstract translation: 目的：提供分子电子器件的π-共轭化合物。 该化合物可以是自组装的，通过总共分子的π-共轭键具有容易的电子离域结构，以及由于阳离子包含在分子内而由外界产生的电场容易地捕获电子的性质。 构成：用于分子电子器件的π-共轭化合物的特征在于由式（1）表示：R 1-Z-£氧化还原|¬-Z-R-2，其含有中心£Redox | 能够进行氧化/还原，并直接或通过乙炔键与芳族化合物连接，其中R1选自苯，CH3COS-苯，CH3SS-苯和SiS-苯; R2选自S-COCH 3 - 苯和（S-苯）2; Z是单键或三键; £Redox | 1选自X-N + R3-苯，N + R3-萘和N + CH3CH3R3-萘; R3选自氢，C1-C4烷基和苄基; X-选自I-，Cl-，Br-，CF 3 SO 3，CH 3 - 苯-SSO 3 - ，C 12 H 25 - 苯-SSO 3 - ，BF 4 - ，PF 6 - 和SbF 6 - 。

公开(公告)号：KR1019920019755A

公开(公告)日：1992-11-19

申请号：KR1019910005392

申请日：1991-04-03

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  양희철 ,  연규환 ,  이계형 ,  이현규 ,  김성기 ,  이연수 ,  정영륜

IPC: C07D215/22

Abstract: 내용 없음

公开(公告)号：KR1020180106599A

公开(公告)日：2018-10-01

申请号：KR1020170035178

申请日：2017-03-21

Applicant: 한국화학연구원

Inventor： 고윤영 ,  김미현 ,  신진수 ,  구근본 ,  이계형 ,  임희종 ,  이상호

IPC: A61K31/136 ,  A61K31/09 ,  A23L33/10 ,  C07C217/80 ,  C07C213/08

CPC classification number: A23L33/10 ,  A61K31/09 ,  A61K31/136 ,  C07C213/08 ,  C07C217/80 ,  A23V2002/00 ,  A23V2200/30

Abstract: 본발명은코로나바이러스감염으로인한질환치료용화합물에관한것으로, 본발명에따른화합물은코로나바이러스에대해우수한억제활성을나타내므로코로나바이러스로인해유발되는메르스, 사스등 질환의예방또는치료용약학적조성물로유용하다.

公开(公告)号：KR101845931B1

公开(公告)日：2018-04-05

申请号：KR1020160067210

申请日：2016-05-31

Applicant: 한국화학연구원

Inventor： 이계형 ,  임희종 ,  조희영 ,  박우규 ,  김성환 ,  최정환

IPC: C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/506 ,  A23L1/30

CPC classification number: C07D487/04 ,  A61K9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D519/00

Abstract: 본발명은헤테로아릴유도체또는이의약학적으로허용가능한염, 이의제조방법및 이를유효성분으로포함하는 PI3 키나아제관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른헤테로아릴유도체는 PI3 키나아제에대하여선택적으로억제하는효과가우수하므로혈액암, 난소암, 자궁경부암, 유방암, 대장암, 간암, 위암, 췌장암, 결장암, 복막전이암, 피부암, 방광암, 전립선암, 폐암, 골육종, 섬유성종양, 뇌종양등과같은암, 류머티스성관절염, 전신홍반성루푸스, 다발성경화증, 제1형당뇨병, 갑상선기능항진증, 근무력증, 크론병, 강직성척추염, 건선, 자가면역성악성빈혈, 쇼그렌증후군등과같은자가면역질환, 만성폐쇄성폐질환(COPD), 비염, 천식, 만성기관지염, 만성폐 염증성질환, 규폐증, 폐형사르코이드증, 흉막염, 폐포염, 혈관염, 기종, 폐렴, 기관지확장증등과같은호흡기질환등의 PI3 키나아제관련질환을예방또는치료하는데유용하게사용할수 있다.

Abstract translation: 本发明涉及杂芳基衍生物或一个uiyakhak上可接受的盐，它们的制备和药物组合物包含其作为活性成分的PI3激酶相关的疾病的预防或治疗物质。 由于本发明的杂芳基衍生物是具有优异的效果，以选择性地抑制相对于PI3激酶血癌，卵巢癌，子宫颈癌，乳腺癌，结肠癌，肝癌，胃癌，胰腺癌，结肠直肠癌，腹膜转移，皮肤癌，膀胱癌， 癌症如前列腺癌，肺癌，骨肉瘤，纤维瘤，脑肿瘤，类风湿性关节炎，jeonsinhong红斑狼疮，多发性硬化症，1型糖尿病，甲状腺功能亢进症，重症肌无力，克罗恩病，强直性脊柱炎，牛皮癣，自身免疫性恶性贫血 自身免疫性疾病如斯耶格伦氏综合征，慢性阻塞性肺疾病（COPD），鼻炎，哮喘，慢性支气管炎，慢性肺部炎性疾病，矽肺，结节病pyehyeong，胸膜炎，肺泡炎，脉管炎，肺气肿，肺炎，支气管扩张，等等，和 一个PI3激酶相关的疾病，如呼吸道疾病可以是预防或治疗是有用的。

公开(公告)号：KR101810209B1

公开(公告)日：2017-12-19

申请号：KR1020160042938

申请日：2016-04-07

Applicant: 한국화학연구원 ,  김진홍

Inventor： 조희영 ,  박우규 ,  임희종 ,  이계형 ,  김현영 ,  정대영 ,  이나라 ,  이현준 ,  김진홍

IPC: A61K31/20 ,  A61K31/201 ,  A61K31/19 ,  A61K36/185 ,  A61K8/36 ,  A61K8/97 ,  A23L1/30 ,  A61Q19/00

Abstract: 본발명은아토피피부질환개선및 치료용조성물에관한것으로, 보다상세하게는히드노카핀산(hydnocarpic acid) 및고를산(gorlic acid)을포함하는아토피피부질환개선및 치료용조성물에관한것으로, 본발명을통해얻은아토피피부질환개선및 치료용조성물은종래의대풍자유추출물을이용한결과와비교하였을때 세포및 동물개체실험에서소량처리를통해서도현저한항아토피및 면역억제효과가있음을발견하였고, 이를통해향우아토피피부질환의완치를위해유용하게활용될수 있을것으로기대된다.

Abstract translation: 本发明涉及一种特应性皮肤病改善，而且用于治疗组合物，更具体地，羟丙基诺卡特应性皮炎改善和含有治疗性组合物中的酸（hydnocarpic酸）和挑酸（gorlic酸），本发明 特应性皮肤疾病，改善和通过获得治疗性组合物，发现当使用常规大丰游离提取物的细胞和动物个体实验少量通过显着的抗过敏性和免疫抑制处理相比，结果在效果，hyangwoo通过该 预计它可用于治疗特应性皮肤病。

公开(公告)号：KR1020150080249A

公开(公告)日：2015-07-09

申请号：KR1020130168603

申请日：2013-12-31

Applicant: 한국화학연구원 ,  가톨릭대학교 산학협력단

Inventor： 조희영 ,  박우규 ,  임희종 ,  이계형 ,  정대영 ,  김현영 ,  김완욱 ,  조철수 ,  박수정 ,  한은진 ,  김중호

IPC: A61K31/4375 ,  A61P19/02 ,  A61P29/00

CPC classification number: A61K31/4375 ,  C07D455/03 ,  C07D491/147 ,  Y10S514/825

Abstract: 본발명은프로토베르베린유도체또는이의약학적으로허용가능한염을유효성분으로함유하는 NFAT5의활성관련질환의예방또는치료용약학적조성물에관한것으로써, 본발명에따른옥소프로토베르베린유도체또는이의약학적으로허용가능한염은 NFAT5 활성을억제하므로, NFAT5 활성관련질환, 특히류마티스관절염또는염증질환등의예방또는치료용약학적조성물로유용하게사용될수 있다.

Abstract translation: 本发明涉及一种药物组合物，其包含作为预防或治疗与NFAT5的活化有关的疾病的活性成分的原青蒿素衍生物或其药学上可接受的盐。 根据本发明，氧八环柏因衍生物或药学上可接受的盐抑制NFAT5的活化，因此可以有效地用作预防或治疗与NFAT5的活化有关的疾病，特别是类风湿性关节炎或炎症性疾病等的药物组合物。

公开(公告)号：KR1020130122361A

公开(公告)日：2013-11-07

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: The present invention relates to 4-(benzimidazole-2-ylamino)pyrrolidine derivatives of chemical formula 1 or pharmaceutically acceptable salts thereof; a pharmaceutical composition containing the same as an active ingredient for preventing and treating neurodegenerative diseases; and an inhibitor composition of the activation of beta-secretase (BACE), containing the same as an active ingredient. The 4-(benzimidazole-2-ylamino)pyrrolidine derivatives according to the present invention suppresses the activation of BACE and generation of beta-amyloid proteins which cause damage to nerve cells, thereby effectively preventing or treating neurodegenerative diseases such as Alzheimer’s disease and Down syndrome.

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。