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    다이하이드로 벤조퓨란구조를 골격으로 하는 카이네이즈저해 화합물
    13.
    发明公开
    다이하이드로 벤조퓨란구조를 골격으로 하는 카이네이즈저해 화합물 失效
    用DIHYDROBENZOFURAN SCAFFOLD进行激酶抑制化合物

    公开(公告)号：KR1020030067161A

    公开(公告)日：2003-08-14

    申请号：KR1020020007039

    申请日：2002-02-07

    Applicant: 한국과학기술연구원

    Inventor： 양범석 ,  박호군 ,  서선희 ,  이승표 ,  심선미

    IPC: C07D307/83

    Abstract: PURPOSE: Provided are kinase inhibitory compounds with dihydrobenzofuran scaffold, which has therapeutic effect on hepatocirrhosis, rheumatism, cancer, sclerosis of the arteries, and the like. CONSTITUTION: Kinase inhibitory compound is characterized by comprising dihydrobenzofuran scaffold, and a functional group attached to the dihydrobenzofuran scaffold and providing hydrogen bond. The kinase inhibitory compound is characteristically represented by the formula(1).

    Abstract translation: 目的：提供具有二氢苯并呋喃支架的激酶抑制化合物，其具有对肝硬化，风湿病，癌症，动脉硬化等的治疗作用。 构成：激酶抑制化合物的特征在于包含二氢苯并呋喃支架和连接于二氢苯并呋喃支架并提供氢键的官能团。 激酶抑制化合物由式（1）表征。

    DDR2 단백질의 티로신 키나아제 활성 저해 화합물
    15.
    发明公开
    DDR2 단백질의 티로신 키나아제 활성 저해 화합물 失效
    用于抑制DDR2蛋白的酪氨酸激酶活性的化合物

    公开(公告)号：KR1020070012648A

    公开(公告)日：2007-01-26

    申请号：KR1020067018588

    申请日：2005-01-05

    Applicant: 한국과학기술연구원

    Inventor： 양범석 ,  양경미 ,  김해종 ,  박인성 ,  박성대 ,  이장혁 ,  권혁만 ,  우병영

    IPC: C07D491/048 ,  A61K31/5025

    CPC classification number: C07D491/04

    Abstract: A novel furopyrimidine compound is provided to show the DDR2 tyrosine kinase inhibition activity, thereby being usefully used for treating a disease caused by tyrosine kinase activity of DDR2 protein such as a tissue fibrosis, rheumatism and cancer. The furopyrimidine compound is represented by one of the formulae(1), (2), (3), (4), (XI) and (XII), where Z is O, S or NH, Y is C or N, X is O, S or NH, n is an integer between 0 and 4, n' is an integer between 0 and 4, each R1, R3 and R3' is single-substituted or independently double-substituted by H, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-4 alkyl, C1-4 halo alkyl, C1-7 alkoxy, C1-4 alkyl amino, C1-4 alkylthio, C1-4 alkyl amide, C1-4 acyl amino, C1-4 acyl oxy, C1-4 alkyl sulfone amide, C1-4 alkyl sulfonate, imidic acid C1-4 alkyl ester, thioimidic acid C1-4 alkyl ester, hydroxy or amino, morpholine, acetate, acetamide, methanesulfoneamide group-substituted methyl, C1-4 halo alkyl, C1-4 alkoxy, or a halogen-substituted benzyl oxy, R" is H, C1-4 alkyl, C1-4 halo alkyl, C1-7 alkoxy, C1-4 alkyl amino, C1-4 alkyl thio, C1-4 alkyl amide, C1-4 acyl amino, C1-4 acyl oxy, imidic acid C1-4 alkyl ester, thiol-imidic acid C1-4 alkyl ester, hydroxy or amino, morpholine, acetate, acetamide, methanesulfoneamide group-substituted methyl, C1-4 halo alkyl, C1-4 alkoxy, or a halogen-substituted phenyl, A ring is benzene, pyrrole, furan, thiophene, imidazole, oxazol, thiazole, triazole, pyrazol, pyrazine, pyridazine, pyrimidine, cyclo hexyl, piperidine or morpholine, R2 is H, halogen, cyano, nitro, hydroxy, amino, C02H, CONH2, CSNH2, C1-5 alkyl, C1-5 haloalkyl, alkylester, phenyl, halogen-substituted phenyl, C1-4 alkoxy group-substituted phenyl or C1-4 haloalkoxy group-substituted phenyl, and R is single-substituted or independently double-substituted by H, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-4 alkyl, C1-4 haloalkyl, C1-7 alkoxy, C1-4 alkylamino, C1-4 alkylthio, C1-4 alkylamide, C1-4 acylamino, C1-4 acyloxy, or C1-4 alkylsufonamide.

    Abstract translation: 提供了一种新的呋喃嘧啶化合物以显示DDR2酪氨酸激酶抑制活性，从而有效地用于治疗由DDR2蛋白的酪氨酸激酶活性引起的疾病，例如组织纤维化，风湿病和癌症。 呋喃并嘧啶化合物由式（1），（2），（3），（4），（XI）和（XII）之一表示，其中Z为O，S或NH，Y为C或N，X 是O，S或NH，n是0和4之间的整数，n'是0和4之间的整数，每个R 1，R 3和R 3'被H，卤素，氰基，硝基的单取代或独立地被双取代 ，羟基，氨基，CO 2 H，CONH 2，CSNH 2，脒，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1-4烷硫基，C 1-4烷基酰胺，C 1-4酰基 氨基，C 1-4酰氧基，C 1-4烷基砜酰胺，C 1-4烷基磺酸酯，酰亚胺酸C 1-4烷基酯，硫代亚氨酸C 1-4烷基酯，羟基或氨基，吗啉，乙酸酯，乙酰胺，甲磺酰胺基 - 取代的甲基，C 1-4卤代烷基，C 1-4烷氧基或卤素取代的苄氧基，R“是H，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1 -4-烷基硫代，C 1-4烷基酰胺，C 1-4酰基氨基，C 1-4酰氧基，酰亚胺酸C 1-4烷基酯，硫醇 - 酰亚胺酸C 1-4烷基酯，羟基或氨基， 乙酰胺，甲磺酰胺基取代的甲基，C 1-4卤代烷基，C 1-4烷氧基或卤素取代的苯基，A环为苯，吡咯，呋喃，噻吩，咪唑，恶唑，噻唑，三唑，吡唑 吡嗪，哒嗪，嘧啶，环己基，哌啶或吗啉，R2是H，卤素，氰基，硝基，羟基，氨基，CO2H，CONH2，CSNH2，C1-5烷基，C1-5卤代烷基，烷基酯，苯基， 取代的苯基，C 1-4烷氧基取代的苯基或C 1-4卤代烷氧基取代的苯基，R是被H，卤素，氰基，硝基，羟基，氨基，CO 2 H，CONH 2，CSNH 2单取代或独立地双取代的 ，脒，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1-4烷硫基，C 1-4烷基酰胺，C 1-4酰氨基，C 1-4酰氧基或C 1-4烷基磺酰胺。

    4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법
    16.
    发明公开
    4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법 失效
    4-（苯基氨基） - （1,4）二氧杂环己烷（2,3-Q）喹唑啉衍生物及其制备方法

    公开(公告)号：KR1020030001992A

    公开(公告)日：2003-01-08

    申请号：KR1020010037867

    申请日：2001-06-28

    Applicant: 한국과학기술연구원

    Inventor： 이용섭 ,  박호군 ,  이재열 ,  양범석 ,  서선희

    IPC: C07D491/08

    CPC classification number: C07D491/04

    Abstract: PURPOSE: Provided are 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline inhibiting the activity of tyrosine kinase which is a receptor of the epidermic growth factor and used for prevention and treatment of cancers, its pharmaceutically acceptable salts, hydrates, solvates and a preparation method thereof. The compounds. CONSTITUTION: 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline is represented by the formula (I) and its preparation method comprises mixing one equivalent of quinazoline derivative of the formula(II) with two equivalent of substituted aniline of the formula(III); and adding HCl then allowing them to react at 20-80 deg.C. In the above formulae, R1 is hydrogen, halogen, hydroxy, C1-6 alkyl, alkoxy, thioalkoxy, and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoromethyl, trifluroro- methoxy, alkenyl, alkynyl, aryl or heterocycle group; R2 and R3 are the same or different and represent -(CH2)m-R4 wherein m is 0 or 1; R4 is hydrogen, halogen, C1-6 hydroxy, C1-6 alkyl, alkoxy, thioalkoxy,and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoro-methyl, trifluroro methoxy, alkenyl, alkynyl, aryl or heterocycle, carboxy, alkoxycarbonyl, amido, N-monoalkyl (C1-6) amido, N,N-dialkyl(C1-6)amido, thioamido, N,N-dialkyl(C1-6)thioamido, guanidino, ureido, C1-6sulfaido, C1-6alkylsulfonyl, morphorino, 4-C1-6alkylpiperidino, mono(hydroxy(C1-6)alkyl)amino, mono(pyrrolidine (C1-6)alkyl)amino, di(pyrrolidine (C1-6) alkyl)amino or -N(R5)(CHR6R7), wherein R5 is hydrogen or C1-6 alkyl; R6 is (CH2)nOH, wherein n is an integer 1-4; R7 is hydrogen, C1-5 alkyl, hydroxyalkyl, thiohydroxyalkyl, phenyl C1-5 alkyl, 4-hydroxyphenyl (C1-5) alkyl or heteroaryl alkyl group; and n is 1,2 or 3.

    Abstract translation: 目的：提供4-（苯基氨基） - （1,4）二氧杂环丁烷（2,3-Q）喹唑啉，其抑制作为表皮生长因子受体的酪氨酸激酶的活性，并用于预防和治疗癌症 可接受的盐，水合物，溶剂合物及其制备方法。 化合物。 构成：4-（苯基氨基） - （1,4）二氧杂环丁烷（2,3-Q）喹唑啉由式（I）表示，其制备方法包括将一当量的式（II）喹唑啉衍生物与两当量 的式（III）的取代苯胺; 并加入HCl，然后使其在20-80℃反应。 在上式中，R 1是氢，卤素，羟基，C 1-6烷基，烷氧基，硫代烷氧基和烷氧基氨基，C 3-6环烷基，环烷氧基和硫代烷氧基，（芳基或杂芳基）氧基，硫代（芳基或杂芳基） ，氨基，N-单（C 1-6）烷基氨基，N，N-二（C 1-6）烷基氨基，甲酰氨基，碘，乙酰氧基，羟基氨基，肼基，三氟甲基，三氟甲氧基，烯基，炔基，芳基或杂环基团; R2和R3相同或不同，表示 - （CH2）m -R4，其中m为0或1; R4是氢，卤素，C1-6羟基，C1-6烷基，烷氧基，硫代烷氧基和烷氧基氨基，C3-6环烷基，环烷氧基和硫代烷氧基，（芳基或杂芳基）氧基，硫代（芳基或杂芳基） ，N-单（C 1-6）烷基氨基，N，N-二（C 1-6）烷基氨基，甲酰氨基，碘，乙酰氧基，羟基氨基，肼基，三氟甲基，三氟甲氧基，烯基，炔基，芳基或杂环， 烷氧基羰基，酰氨基，N-单烷基（C 1-6）酰胺基，N，N-二烷基（C 1-6）酰氨基，硫代酰氨基，N，N-二烷基（C 1-6）硫代酰氨基，胍基，脲基，C 1-6亚硫酰基， 氨基，单（吡咯烷（C 1-6）烷基）氨基，二（吡咯烷（C 1-6）烷基）氨基或-N（R 5（C 1-6）烷基）氨基， ）（CHR 6 R 7），其中R 5是氢或C 1-6烷基; R6是（CH2）nOH，其中n是整数1-4; R 7是氢，C 1-5烷基，羟烷基，硫代羟烷基，苯基C 1-5烷基，4-羟基苯基（C 1-5）烷基或杂芳基烷基; n为1,2或3。

    당뇨병 치료 효과를 가지는 누에 기주 동충하초의 재배 방법
    17.
    发明公开
    당뇨병 치료 효과를 가지는 누에 기주 동충하초의 재배 방법 失效
    使用日粮作为主体使用丝朊和对糖尿病进行治疗效果的方法及其培养方法

    公开(公告)号：KR1020020087570A

    公开(公告)日：2002-11-23

    申请号：KR1020010026194

    申请日：2001-05-14

    Applicant: 한국과학기술연구원 ,  주식회사 엔에스케이텍

    Inventor： 조정혁 ,  오창현 ,  양범석 ,  이기수

    IPC: A61K36/068 ,  A61P3/10

    Abstract: PURPOSE: A method for cultivation of Paecilomyces Japonica using a silkworm without a pupa as a host and a freeze drying method is provided. Therefore, a product having an excellent therapeutic effect on diabetic is produced with high productivity without causing the depletion of nutrients. CONSTITUTION: In the process for artificial cultivation of Paecilomyces Japonica, a 5 day old silkworm as a host is subjected to sterilization using chlorine dioxide water with a concentration of 1 to 5ppm without using heat treatment, a compound selected from the group consisting of silk amino acid, sugar and a mixture thereof is added to a medium for cultivation thereof, and then the silkworm is freeze dried and killed through an electric shock method.

    Abstract translation: 目的：提供使用没有蛹作为宿主的蚕培养拟青藓的方法和冷冻干燥方法。 因此，以高生产率生产对糖尿病具有优异治疗效果的产品，而不会导致营养物质的消耗。 构成：在人造培养拟青藓的过程中，将5日龄的蚕作为宿主，使用浓度为1〜5ppm的二氧化氯水进行灭菌，不用热处理，选自丝氨基 酸，糖及其混合物加入到培养基中，然后通过电击法将蚕冷冻干燥灭活。

    티로신 키나아제 저해 화합물, 이의 이성질체 또는 이의 약학적으로 허용가능한 염 및 이를 포함하는 약학적 조성물
    19.
    发明公开
    티로신 키나아제 저해 화합물, 이의 이성질체 또는 이의 약학적으로 허용가능한 염 및 이를 포함하는 약학적 조성물 有权
    酪氨酸激酶抑制化合物，其异构体或其药物可接受的盐，以及包含其的药物组合物

    公开(公告)号：KR1020100060300A

    公开(公告)日：2010-06-07

    申请号：KR1020080118850

    申请日：2008-11-27

    Applicant: 한국과학기술연구원 ,  주식회사 레고켐 바이오사이언스

    Inventor： 양범석 ,  김선영 ,  조종운 ,  이향숙 ,  우성호 ,  박태교 ,  김용주 ,  김승태 ,  이홍범

    IPC: C07D513/04 ,  C07D513/02

    CPC classification number: C07D513/04

    Abstract: PURPOSE: A tyrosine kinase compound is provided to suppress the tyrosine kinase activation of DDR1 and DDR2 and to prevent or treat cancer, arteriosclerosis, rheumatoid arthritis, and osteoarthritis. CONSTITUTION: A tyrosine kinase suppression compound is denoted by chemical formula 1. A pharmaceutical composition for anti-cancer contains a compound of chemical formula 1, isomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutically acceptable salt is hydrochloride or trifluoroacetic acid salt. A pharmaceutical composition for preventing or treating rheumatism or osteoarthritis contains the compound of chemical formula 1, the isomer, and the salt as active ingredients.

    Abstract translation: 目的：提供酪氨酸激酶化合物以抑制DDR1和DDR2的酪氨酸激酶活化，并预防或治疗癌症，动脉硬化，类风湿性关节炎和骨关节炎。 构成：酪氨酸激酶抑制化合物由化学式1表示。用于抗癌的药物组合物含有化学式1，异构体或其药学上可接受的盐作为活性成分的化合物。 药学上可接受的盐是盐酸盐或三氟乙酸盐。 用于预防或治疗风湿病或骨关节炎的药物组合物含有化学式1，异构体和盐作为活性成分的化合物。

    ＤＤＲ과 콜라겐 결합 저해물질을 검색하는 방법
    20.
    发明授权
    ＤＤＲ과 콜라겐 결합 저해물질을 검색하는 방법 失效
    筛选抑制剂对DDR蛋白与胶原结合的方法

    公开(公告)号：KR100945018B1

    公开(公告)日：2010-03-05

    申请号：KR1020070108127

    申请日：2007-10-26

    Applicant: 한국과학기술연구원

    Inventor： 양범석 ,  조승주

    IPC: G01N33/68 ,  G01N33/53

    Abstract: 본 발명은 디스코이딘 도메인 리셉터(Discoidin Domain Receptor, DDR)와 콜라겐 결합 저해물질을 검색하는 방법에 관한 것으로, 보다 구체적으로는 DDR의 세포외 도메인과 세포막 통과 도메인을 포함하는 단백질을 곤충세포에서 발현시 세포막에 올바른 방향성으로 존재하며 DDR의 세포외 부위와 배양 접시 표면에 코팅된 콜라겐 단백질이 결합하는 특성을 이용하여 이들 결합을 저해하는 물질을 세포차원에서 검색하는 방법에 관한 것이다. 본 발명의 검색법은 간편하여 짧은 시간 내에 많은 물질을 탐색할 수 있고 DDR 단백질의 과잉 활성에 의해 유발되는 질환의 예방 및 치료제 개발에 유용하게 사용될 수 있다.
    DDR, 곤충세포, 티로신 키나아제, 콜라겐

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