公开(公告)号：KR100994687B1

公开(公告)日：2010-11-17

申请号：KR1020080106962

申请日：2008-10-30

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  유경호 ,  심태보 ,  이소하 ,  하정미 ,  김희진 ,  정명호

IPC: C07D487/04

Abstract: 본 발명은 신규 피롤로[3,2-ｂ]피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종 예방 또는 치료용 약학적 조성물에 관한 것으로, 더욱 상세하게는 하기 화학식 1로 표시되는 신규 피롤로[3,2-ｂ]피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명에 따른 피롤로[3,2-b]피리딘 유도체는 흑색종 세포에 대하여 뛰어난 흑색종 항증식 활성을 나타내며, 종래 흑색종 치료제로 사용되는 소라페닙에 비하여 10배 이상의 흑색종 항증식 활성을 나타내기 때문에 흑색종 예방 또는 치료에 유용하게 사용될 수 있다.
[화학식 1]

(상기 화학식 1에서 R
1 및 R
2 는 본 명세서에서 정의한 바와 같다)
피롤로[3,2-b]피리딘 유도체, DTIC, 흑색종, 항증식효과

公开(公告)号：KR1020100112672A

公开(公告)日：2010-10-20

申请号：KR1020090031068

申请日：2009-04-10

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  유병용 ,  김정훈 ,  유승원 ,  구대호

IPC: C07D501/22 ,  C07D501/20 ,  C07D501/06 ,  C07D501/32

CPC classification number: Y02P20/55 ,  C07D501/22 ,  A61K31/545

Abstract: PURPOSE: A 7-amino-3-vinyl-cephalosphorinic acid salt hydrate with a novel crystal and a method for preparing the same are provided to industrially synthesize novel crystalline 7-AVCA hydrate of high yield and high purity. CONSTITUTION: A 7-amino-3-vinyl-cephalosphorinic acid salt hydrate of chemical formula 1 with a novel crystal has characteristic peak at 8.98±0.3, 18.06±0.3, 28.95±0.3, 32.32±0.3, 33.76±0.3 and 34.40±0.3. A method for preparing the crystalline 7-amino-3-vinyl-cephalosphorinic acid salt hydrate comprises: a step of adding cresol or phenol to p-methoxybenzyl-7-phenylaceteamido3-vinyl-3-cefem-4-carboxylate and stirring to deprotect a protection group of carboxylic group; a step of adjusting pH with alkali and adding cinta CELC-PA enzyme to deprotect a protection group of amino group; a step of crystallizing the deprotected 7-AVCA by adjusting pH with inorganic acid; and a step of adding methanol solution and base to 7-AVCA and adding acid.

Abstract translation: 目的：提供具有新晶体的7-氨基-3-乙烯基头孢菌素酸盐水合物及其制备方法，以工业合成高产率和高纯度的新型结晶7-AVCA水合物。 构成：具有新颖结晶的化学式1的7-氨基-3-乙烯基头孢菌素酸盐水合物在8.98±0.3,18.06±0.3,28.95±0.3,32.32±0.3,33.76±0.3和34.40±0.3的特征峰 。 制备结晶7-氨基-3-乙烯基头孢菌素酸盐水合物的方法包括：向对甲氧基苄基-7-苯基乙酰氨基-3-乙烯基-3-头孢呋喃-4-羧酸甲酯中加入甲酚或苯酚并搅拌以脱保护 羧基保护基; 用碱调节pH值，加入cinta CELC-PA酶去保护氨基保护基; 通过用无机酸调节pH使得脱保护的7-AVCA结晶的步骤; 并向7-AVCA中加入甲醇溶液和碱并加入酸的步骤。

公开(公告)号：KR100980681B1

公开(公告)日：2010-09-07

申请号：KR1020080090659

申请日：2008-09-16

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  조정혁

IPC: C07D413/10 ,  C07D413/02

CPC classification number: C07D413/10

Abstract: 본 발명은 하기 화학식 1로 표시되는 디플루오로페닐 유도체를 갖는 신규한 옥사졸리디논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 항생제 조성물에 관한 것으로, 본 발명에 따른 조성물에 유효성분으로 함유되는 옥사졸리디논 유도체 및 이의 약학적으로 허용가능함 염은 헤모필루스 인플루엔자(Haemophilus influenza), 비병원성 포도상구균(Coagulase negative staphylococi) 등을 포함하는 그람양성균 및 반코마이신 내성 장내구균(VRE) 등을 포함하는 내성 균주들에 대하여 유의한 항균 활성을 나타내므로, 항생제로서 유용하게 사용될 수 있다.
[화학식 1]
.
(상기 화학식 1에서, R은 본 명세서에서 정의한 바와 같다.)
옥사졸리디논, 리네졸리드, 스피로[2,4]헵탄, MRSA, 반코마이신내성균

公开(公告)号：KR1020090073659A

公开(公告)日：2009-07-03

申请号：KR1020070141668

申请日：2007-12-31

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  조정혁 ,  조남현 ,  안광일 ,  천기정 ,  이교철 ,  문병석 ,  최태현 ,  구대호

IPC: C07D405/04 ,  C07H15/22

Abstract: A manufacturing method for manufacturing a 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is provided to produce a compound having high intake rate by specifically activating in a cell line which HSV-TK gene is specifically expressed. A 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is denoted by the chemical formula 1. A method for manufacturing the 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound comprises: a step of reacting anhydrous trifluoro methanesulfonyl in a compound of the chemical formula 2 under the presence of organic solvent to produce the tribenzoyl triflate saccharide compound of the chemical formula 3; a step of introducing fluorine-18 to produce a compound of the chemical formula 4; a step of reacting the compound of the chemical formula 4 with anhydrous acetic acid under the presence of organic solvent to produce a compound of the chemical formula 5; a step of reacting the compound of the chemical formula 5 with silylated thymine to produce a compound of the chemical formula 7; and a step of hydrolyzing the compound of the chemical formula 7 to produce the compound of the chemical formula 1.

Abstract translation: 提供了制备2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物的制备方法，通过在细胞系中特异性活化以产生高摄入率的化合物，其中HSV-TK 基因被特异表达。 2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物由化学式1表示。制备2-脱氧-2- [18 F]氟-5- 甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物包括：在有机溶剂的存在下，使化学式2的化合物中的无水三氟甲烷磺酰化反应生成化学式3的三苯甲酰基三氟甲磺酸酯化合物的步骤; 引入氟-18以制备化学式4的化合物的步骤; 在有机溶剂的存在下使化学式4的化合物与无水乙酸反应以产生化学式5的化合物的步骤; 使化学式5的化合物与甲硅烷基化的胸腺嘧啶反应以产生化学式7的化合物的步骤; 以及水解化学式7的化合物以制备化学式1的化合物的步骤。

公开(公告)号：KR1020050021835A

公开(公告)日：2005-03-07

申请号：KR1020030059624

申请日：2003-08-27

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현

IPC: A01G31/02

CPC classification number: Y02P60/216

Abstract: PURPOSE: A method of growing bean sprouts with a bean sprout growing apparatus for sterilizing or disinfecting collected cultivation water with a disinfectant, coagulating pollutants or impurities contained in the cultivation water with a coagulant and an coagulant aid and purifying cultivation water with a bottom-up sand filter layer is provided. The bean growing method can recycle the purified cultivation water, thereby reducing production cost and preventing environmental pollution. CONSTITUTION: The bean sprouts growing method consists of: collecting cultivation water containing pollutants or impurities discharged from a bean sprouts cultivation part; sterilizing or disinfecting cultivation water by adding a disinfectant to the collected cultivation water; coagulating the pollutant or impurities by inputting a coagulant and an coagulant aid to the sterilized cultivation water; purifying cultivation water containing coagulated sludge by passing through a sand filter layer(5,6) from the lower part to the upper part; and resupplying the purified cultivation water to the bean sprouts cultivation part. The disinfectant is 0.5 to 5ppm chlorine dioxide. The coagulant is at least one selected from polyaluminum chloride or polyacrylamide and the coagulant aid is at least one selected from clay, loess, kaolin, vermiculite, active carbon, carbonized rice hull, carbonized rice hull ash, quicklime, K2CO3 and KOH.

Abstract translation: 目的：一种用豆芽生长装置种植豆芽的方法，用消毒剂消毒或消毒收集的培养水，用絮凝剂和助凝剂将培养水中含有的污染物或杂质凝结，并用自下而上的方式净化培养水 提供砂滤层。 豆类生长方法可以回收纯化的培养水，从而降低生产成本，防止环境污染。 规定：豆芽生长方法包括：收集含有从豆芽种植部分排出的污染物或杂质的培养水; 通过向收集的培养水中加入消毒剂来消毒或消毒培养水; 通过向灭菌的栽培水输入凝结剂和助凝剂来使污染物或杂质凝结; 通过从下部到上部通过砂过滤层（5,6）来净化含有凝结污泥的培养水; 并将纯化的培养水补给豆芽培养部分。 消毒剂为0.5〜5ppm二氧化氯。 絮凝剂是选自聚氯化铝或聚丙烯酰胺中的至少一种，絮凝剂是选自粘土，黄土，高岭土，蛭石，活性炭，碳化米壳，碳化稻壳灰，生石灰，K 2 CO 3和KOH中的至少一种。

公开(公告)号：KR100441406B1

公开(公告)日：2004-07-23

申请号：KR1020010054467

申请日：2001-09-05

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  조한원

IPC: C07D487/02

Abstract: PURPOSE: Antibacterial carbapenem derivatives which are active against resistant strains are provided. They are pyrrolidine thiol carbapenems represented by formula(1), wherein R1 is hydrogen, substituted or unsubstituted lower alkly, heterocycles containing N or S, sulfonyl substituted with lower alkyl, carbonyl substituted with heterocycles containing N or S, benzyl, amide or hydroxy group; R2 is hydrogen, hydroxy alkyl, amide or ester group. CONSTITUTION: The method of preparation comprises: reacting phosphate compound with thiol derivatives represented by formula(2) under base and obtaining protected carbapenem derivatives; de-protecting them using hydrogen and palladium as a catalyst; and purifying with porous resin and freeze drying. In formula (2), R1 and R2 are same as in formula(1) and PNZ is p-nitrobenzyloxycarbonyl group.

Abstract translation: 目的：提供对抗性菌株有活性的抗菌碳青霉烯衍生物。 它们是由式（1）表示的吡咯烷硫醇碳青霉烯类，其中R1是氢，取代或未取代的低级烷基，含有N或S的杂环，被低级烷基取代的磺酰基，被含有N或S的杂环取代的羰基，苄基，酰胺基或羟基 ; R2是氢，羟基烷基，酰胺或酯基。 构成：制备方法包括：使磷酸酯化合物与式（2）所示的硫醇衍生物在碱的作用下反应，得到被保护的碳青霉烯衍生物; 用氢和钯作为催化剂对其进行脱保护; 并用多孔树脂纯化并冷冻干燥。 式（2）中，R 1和R 2与式（1）相同，PNZ是对硝基苄氧基羰基。

公开(公告)号：KR1020020059043A

公开(公告)日：2002-07-12

申请号：KR1020000087303

申请日：2000-12-30

Applicant: 한국과학기술연구원

Inventor： 오창석 ,  조정혁 ,  오창현 ,  이인우 ,  이기수

IPC: C07C247/08

Abstract: PURPOSE: Provided is a vinyl carbamoyl azide derivative, which is more stable than a conventional carbamoyl azide derivative and has an effective sterilizing power against mold harmful to the crops. CONSTITUTION: The vinyl carbamoyl azide derivative represented by the formula 1 is produced by reacting an isocyanate compound(R1NCO) and hydrazoic acid(NH3) or sodium azide(NaN3). In the formula, R1 is at least one C1-C6 alkyl, or furyl or phenyl capable of being substituted by at least one substituent selected from the group consisting of halogen, C1-C6 alkoxy, and nitro.

Abstract translation: 目的：提供一种乙烯基氨基甲酰基叠氮化物衍生物，其比常规的氨基甲酰基叠氮化物衍生物更稳定，并且对于对作物有害的霉菌具有有效的杀菌力。 构成：由式1表示的乙烯基氨基甲酰基叠氮化物衍生物是通过使异氰酸酯化合物（R 1 NCO）和叠氮酸（NH 3）或叠氮化钠（NaN 3）反应而制备的。 在该式中，R 1是至少一个C 1 -C 6烷基，或可被至少一个选自卤素，C 1 -C 6烷氧基和硝基的取代基取代的呋喃基或苯基。

公开(公告)号：KR1020020055460A

公开(公告)日：2002-07-09

申请号：KR1020000083443

申请日：2000-12-28

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창석 ,  오창현 ,  이기수

IPC: A01G31/00

Abstract: PURPOSE: Provided is a method of growing beans and vegetables such as bean sprouts using the fungicide which is safe to men. The fungicide residues do not remain in the bean sprouts, while the fungicide enhances the yield and quality of the bean sprouts. CONSTITUTION: The growing method comprises: a step of germinating the bean sprouts by soaking beans in the water in which 0.1-100ppm of chlorine dioxide based fungicide is dissolved; and a step of growing the germinated bean sprouts in the dark with the supply of the water in which 0.01-10ppm of the chlorine dioxide based fungicide is dissolved.

Abstract translation: 目的：提供使用杀虫剂生长豆类和蔬菜如豆芽的方法，该杀菌剂对男性是安全的。 杀菌剂残留物不保留在豆芽中，而杀真菌剂提高了豆芽的产量和质量。 构成：生长方法包括：将豆子浸泡在其中溶解有0.1-100ppm二氧化氯的杀真菌剂的水中发芽豆芽的步骤; 以及在二氧化氯类杀真菌剂溶解有0.01-10ppm的水的供给下，在黑暗中生长发芽的豆芽的步骤。

公开(公告)号：KR100325375B1

公开(公告)日：2002-03-06

申请号：KR1020000004630

申请日：2000-01-31

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  이기수 ,  이창식 ,  이인규 ,  이숙자

IPC: C07D477/20

Abstract: 본 발명은 다음 화학식 1을 갖는 신규한 카바페넴 유도체 및 그의 제조 방법을 제공한다:
화학식 1

식 중, R은 수소이거나, 하이드록시기, 아민기, 설포닐기 및 아미노설포닐기로 이루어진 군 중에서 선택된 한 가지 이상의 치환기로 치환될 수 있는 C
1∼6 의 저급 알킬기, 알릴기 또는 벤질기이다.

公开(公告)号：KR1020020008445A

公开(公告)日：2002-01-31

申请号：KR1020000041597

申请日：2000-07-20

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  이기수

IPC: A01G31/00

Abstract: PURPOSE: A method and an apparatus for cultivation of bean sprouts capable of preventing putrefaction of bean sprouts during cultivation by recycling spend water after treatment are provided, which prevent environmental pollution, improve productivity and reduce water consumption. CONSTITUTION: A coagulant is introduced into spent water containing pollutant or impurities discharged from the cultivating part of bean sprouts(1) in a dissolved air flotation(DAF) tank(3) to coagulate the pollutant or impurities, sludge is removed from the sludge-containing spent water by DAF treatment of the spent water and treated water is resupplied to the cultivating part of bean sprouts after sterilization of spent water with an antiseptic and pouring of inorganic nutrients thereto. The concentration of the coagulant and the antiseptic are 1 to 20ppm and 0.1 to 10ppm respectively.

Abstract translation: 目的：提供一种能够通过回收处理后的花水来防止豆芽腐败的豆芽的种植方法和装置，其防止环境污染，提高生产率，降低耗水量。 构成：在溶解空气浮选（DAF）罐（3）中将絮凝剂引入含有从豆芽（1）的栽培部分排出的污染物或杂质的废水中，使污染物或杂质凝结，污泥从污泥中除去， 通过DAF处理废水和处理水的废水通过消毒剂和无机营养物质的无水营养物质的废水灭菌后补充到豆芽的培养部分。 絮凝剂和防腐剂的浓度分别为1〜20ppm和0.1〜10ppm。