公开(公告)号：KR101260235B1

公开(公告)日：2013-05-03

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: 본발명은액정표시장치의보상필름용액정화합물로, 보다상세하게는아세틸렌을포함하는트리페닐렌계반응성메조겐화합물에관한것이다. 본발명에서제조한아세틸렌함유트리페닐렌계반응성메조겐화합물은복굴절율이높아보상필름을박막으로제조할수 있으며이 보상필름을채용한액정장치는대화면의광시야각을구현할수 있는장점이있다.

公开(公告)号：KR1020090112167A

公开(公告)日：2009-10-28

申请号：KR1020080037896

申请日：2008-04-23

Applicant: 한국화학연구원

Inventor： 이미혜 ,  가재원 ,  안택 ,  김진수 ,  이계형

IPC: C09K19/12

CPC classification number: C09K19/32 ,  C09K2019/0429 ,  C09K2019/328

Abstract: PURPOSE: Photoinitiator-free reactive mesogens based on triphenylene are provided to form a wide-viewing angle compensation film. CONSTITUTION: Photoinitiator-free reactive mesogens based on triphenylene are represented by formula 1. The triphenylene-based mesogen compounds comprise various long branched chains for adjusting a temperature range in liquid crystal. The branched chains are alkyl, poly ethylene glycol, phenyl alkyl ester, and phenyl polyethylene glycol esther. The triphenylene-based mesogen compounds have phenyl acryloyl(cinnamoyl), naphthyl acryloyl, and biphenyl acryloyl groups on the end of the branched chains.

Abstract translation: 目的：提供基于三亚苯的无光引发剂的反应性介晶，形成宽视角补偿膜。 构成：基于三亚苯的无光引发剂的反应性介晶由式1表示。三亚苯基介晶化合物包含用于调节液晶温度范围的各种长支链。 支链是烷基，聚乙二醇，苯基烷基酯和苯基聚乙二醇酯。 三亚苯基介晶化合物在支链末端具有苯基丙烯酰基（肉桂酰基），丙烯酰基萘基和联苯基丙烯酰基。

公开(公告)号：KR1020080065722A

公开(公告)日：2008-07-15

申请号：KR1020070002715

申请日：2007-01-10

Applicant: 한국화학연구원

Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  박창민 ,  소원영 ,  이지선 ,  김은주 ,  강남숙 ,  천혜경 ,  조영식 ,  송진숙 ,  배명애 ,  김지현 ,  조중명 ,  노성구 ,  현영란 ,  이철순 ,  이재일 ,  유성은

IPC: C07D231/12 ,  C07D401/04 ,  C07D403/10 ,  C07D413/04

Abstract: A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.

Abstract translation: 提供了一种新型化合物，以显示对PDE-4酶的优异活性和对其他PDE酶的高选择性，从而被用作炎症相关疾病，关节炎，特应性皮炎，白血病，各种癌症和退行性脑病的治疗剂 效果。 1-（1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑化合物由式（1）表示，通过式（2）表示的卤代苄基化合物与吡唑化合物 由公式（3）表示。 在式（1）中，每个R 1和R 2独立地为H，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，C 3-7环烷基，（C 3-7）环烷基（C 1-7） 烷基，芳基或杂芳基，芳（C 1-5）烷基或芳（C 1-5）烷氧基，或者R 1和R 2可以被C 1-3亚烷基相互连接; 每个R 3，R 4和R 5独立地为H，苯基，吡啶基，N-氧代吡啶基，直链或支链饱和和不饱和C 1-7烷基，C 3-7环烷基，（C 3-10）环烷基（C 1-7）烷基，卤素，氰基 ，硝基，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，C3-7环烷基氨基，3至7元饱和或不饱和杂环，包括O，N或S，胍基 （C 1-7）烷基，羟基（C 1-7）烷基，羧基或（C 1-7）烷氧基羰基;（C 1-7）烷氧基， R6是直链或支链饱和和不饱和的C1-7烷基，C3-7环烷基，（C3-10）环烷基（C1-7）烷基，苯基，苯氧基，苄基，苄氧基，C1-7烷氧基或（C1-7） 烷氧基（C 1-7）烷基。 用于治疗或预防与气道炎症，关节炎，特应性皮炎，白血病，癌症或退行性脑疾病相关的疾病的药物组合物包括1- [1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑衍生物作为有效的 成分。

公开(公告)号：KR100753017B1

公开(公告)日：2007-08-30

申请号：KR1020060046860

申请日：2006-05-25

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  박창민 ,  소원영 ,  강남숙 ,  홍석주 ,  천혜경 ,  조영식 ,  김기영 ,  배명애 ,  송진숙 ,  노성구 ,  현영란 ,  이운영 ,  김용은 ,  강봉균 ,  이혜련 ,  유성은

IPC: A61K31/437 ,  A61P35/00

Abstract: A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.

Abstract translation: 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病，其包括7-（3,4-二烷氧基） - 吡唑并提供[1,5-a]嘧啶化合物抑制PDE-4的活性（phosphodiesterase-的药物组合物 4）并通过减少HARBS（高亲和力咯利普兰结合位点）亲和力来减少副作用，例如呕吐。 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病的药物组合物包含7-（3,4-二烷氧基） - 吡唑并[1,5-a]嘧啶化合物由式（1）表示，其中R1和R2 （C 1 -C 7）烷基，含有卤素原子的直链或支链饱和或不饱和（C 1 -C 7）烷基，（C 3 -C 7）环烷基，含有3至7元杂环烷基的3元至7元杂环烷基 （C4-C10）环烷基（C1-C7）烷基，在杂环中含有氧，氮或硫的3元至7元杂环烷基（C1-C7）烷基，苯基 ，苄基或烯丙基; （C 1 -C 7）烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，（C 1 -C 7）烷氧基， （C 1 -C 7）烷基，羧酸，羧基（C 1 -C 7）烷基酯，羧基（C 1 -C 7）烷基酰胺，氨基或单或二（C 1 -C 7）烷基氨基羰基; （C 1 -C 7）烷基，（C 3 -C 7）环烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，羟基（C 1 -C 7）烷基， C1-C7）烷基酮，（C1-C10）烷基羧酸，羧基（C1-C10）烷基酯，羧基（C1-C10）烷基酰胺，氨基，单或二（C1-C7）烷基氨基，单或二（C1-C7 ）烷基氨基羰基，（C3-C7）环烷基胺，吗啉，氧化吗啉，哌啶，哌嗪，哌嗪氧化物或芳基。

公开(公告)号：KR100689961B1

公开(公告)日：2007-03-08

申请号：KR1020050018325

申请日：2005-03-04

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  정준원 ,  박창민 ,  정순민 ,  김지영 ,  강남숙 ,  홍석주 ,  천혜경 ,  남지연 ,  장범수 ,  곽현정 ,  송진숙 ,  허준영 ,  양승돈 ,  전영호 ,  노성구 ,  이태규 ,  현영란 ,  조중명 ,  허용석 ,  윤정민 ,  유성은

IPC: C07D277/42 ,  A61P11/06 ,  A61P25/28

Abstract: 본 발명은 하기의 화학식 1로 표시되는 신규한 4-(3,4-디알콕시페닐)-2-아미노티아졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 알쯔하이머를 포함한 중추신경계통 질환의 치료, 예방을 위한 약제학적 조성물에 관한 것이다.
[화학식 1]

4-(3,4-디알콕시페닐)-2-아미노티아졸, PDE-4, 천식, 만성폐쇄성 폐질환, 염증관련 질환, 중추신경계 질환, 알쯔하이머.

公开(公告)号：KR1020030005787A

公开(公告)日：2003-01-23

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：提供能够有效地用作有效的抗氧化剂和抗癌剂的含有对人类癌细胞具有优异抗癌活性的粘液素-A的药物组合物，以及优异的抗氧化活性为主要成分。 构成：药物组合物含有通过与粘液细菌分离或化学合成或半合成获得的式1的粘液素-A。 通过以下步骤纯化粘液素-A：通过在吸收树脂存在下培养球状球形细菌菌株作为粘液细菌分离生物质和吸收树脂并离心培养液; 加入有机溶剂，优选丙酮和甲醇的混合溶剂; 提取和过滤除去生物质和吸收树脂; 通过减压浓缩滤液并在有机溶剂中萃取粗提取物制备活性级分; 并依次进行硅胶液相色谱和再循环制备型HPLC。

公开(公告)号：KR1019930009820B1

公开(公告)日：1993-10-11

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: 2-Quinolinone derivs. of formula (I) are prepd. by reacting 4- alkylsulfoxy-2- quinolinone derivs. and an amine cpds. in an inert solvent. In the formula (I), R1,R2,R3 and R4 are each H, aryl, heterocycle, aryloxy, C1-10 aralkyl or alkyl, C1-10 alkoxy, C1-6 haloalkyl, halogen, nitro, cyano or heterocycle; R5 is C1-6 alkyl, aryl or heteroaryl; X=NHR6, NHZAr; R6 is C1-16 opt. substd. saturated or unsaturated alkyl, C3-10 opt. substd. cycloalkyl, piperidine, piperazine, aryl or heteroaryl; Z is C1-6 alkyl; Ar is heteroaryl, pyrrolidine or aryl. The cpds. (I) are useful as an insect-fungicide.

Abstract translation: 2-喹啉酮衍生物。 式（I）的化合物是制备的。 通过4-烷基亚磺酰基-2-喹啉酮衍生物反应。 和胺cpds。 在惰性溶剂中。 在式（I）中，R 1，R 2，R 3和R 4各自为H，芳基，杂环，芳氧基，C 1-10芳烷基或烷基，C 1-10烷氧基，C 1-6卤代烷基，卤素，硝基，氰基或杂环; R5是C1-6烷基，芳基或杂芳基; X = NHR 6，NHZAr; R6是C1-16选择。 substd。 饱和或不饱和的烷基，C3-10选择。 substd。 环烷基，哌啶，哌嗪，芳基或杂芳基; Z是C 1-6烷基; Ar是杂芳基，吡咯烷基或芳基。 cpds。 （I）可用作昆虫杀真菌剂。

公开(公告)号：KR1019930009819B1

公开(公告)日：1993-10-11

申请号：KR1019910005391

申请日：1991-04-03

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  양희철 ,  연규환 ,  이계형 ,  이현규 ,  김성기 ,  이연수 ,  이광우 ,  김흥태

IPC: C07D215/22

Abstract: 2-Quinolinone derivs. of formula (I) are prepd. by a cyclization of ketene dithio acetal -anilide cpds. at 140-250 deg.C. In the formula (I), R1,R2,R3 and R4 are each H, halogen, alkyl, alkoxy, thioalkoxy, halogenated lower alkyl, nitro, cyano, aryl, aryloxy, arylsulfone, alkoxycarbonyl, carboxylic or heterocyclic; R5 is alkyl or aryl; R6 is R7 or R8; R7 is alkyl or H, alkyl or haloalkyl substd. benzyl; R8 is aryl or H, halogen, alkyl or haloalkyl substd. benzyl; n = 0 or 1. The cpds. (I) have antibacterial activities.

Abstract translation: 2-喹啉酮衍生物。 式（I）的化合物是制备的。 通过烯酮二硫代乙酰苯胺的环化。 在140-250℃。 在式（I）中，R 1，R 2，R 3和R 4各自为H，卤素，烷基，烷氧基，硫代烷氧基，卤代低级烷基，硝基，氰基，芳基，芳氧基，芳基砜，烷氧基羰基，羧基或杂环; R5是烷基或芳基; R6是R7或R8; R7是烷基或H，烷基或卤代烷基。 苄基; R8是芳基或H，卤素，烷基或卤代烷基。 苄基; n = 0或1. cpds。 （一）具有抗菌活性。

公开(公告)号：KR1020170074381A

公开(公告)日：2017-06-30

申请号：KR1020150183563

申请日：2015-12-22

Applicant: 한국화학연구원

Inventor： 이계형 ,  임희종 ,  조희영 ,  박우규 ,  정대영

IPC: C07D487/04 ,  C07D498/04 ,  C07D401/12 ,  C07D403/14 ,  A61K31/519 ,  A61K31/47 ,  A61K31/53 ,  A23L1/30

Abstract: 본발명은피리미도옥사진유도체또는이의약학적으로허용가능한염, 이의제조방법및 이를유효성분으로포함하는 PI3 키나아제관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른피리미도옥사진유도체는 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: 本发明涉及嘧啶并 - 恶嗪衍生物或其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。 由于根据本发明的嘧啶并 - 恶嗪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，前列腺癌，肺癌，骨肉瘤，纤维瘤，癌症，如脑肿瘤，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 所述呼吸系统疾病的PI3激酶相关的疾病，如如支气管扩张可以是用于预防或治疗是有用的。

公开(公告)号：KR1020160150006A

公开(公告)日：2016-12-28

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 ,  A61K31/506 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00 ,  Y02P20/55 ,  C07D403/12 ,  A23L33/10 ,  A23V2200/308 ,  A23V2200/314

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.