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1. 发明公开

KR1020060079122A 당뇨 및 비만 치료예방에 유효한 벤조티아졸 유도체 无效
标题翻译：用于治疗或预防糖尿病和肥胖的苯并噻唑衍生物
公开(公告)号：KR1020060079122A
公开(公告)日：2006-07-05
申请号：KR1020050134723
申请日：2005-12-30
申请人： 에스케이케미칼주식회사 , 한소 주식회사 , 경희대학교 산학협력단
发明人： 이남규 , 이준원 , 이석호 , 임광진 , 한혜영 , 김태곤 , 김용혁 , 곽의종 , 김상웅 , 하주헌 , 김언겸 , 이정규 , 유충열 , 이대연
IPC分类号： C07D277/74 , A61P3/04 , A61P3/10
CPC分类号： C07D239/91 , C07D239/93 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： 본 발명은 혈당 강하, 체중 감소를 나타내는 신규의 벤조티아졸 유도체와, 이 화합물을 유효성분으로 함유하는 당뇨 및 비만 치료예방제에 관한 것이다.
당뇨병 치료제, 비만 치료제, 벤조티아졸

2. 发明公开

KR1020060079121A 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체 无效
标题翻译：治疗或预防糖尿病和肥胖的喹唑啉衍生物
公开(公告)号：KR1020060079121A
公开(公告)日：2006-07-05
申请号：KR1020050134722
申请日：2005-12-30
申请人： 에스케이케미칼주식회사 , 한소 주식회사 , 경희대학교 산학협력단
发明人： 이남규 , 이준원 , 이석호 , 임광진 , 한혜영 , 김태곤 , 김용혁 , 곽의종 , 김상웅 , 하주헌 , 김언겸 , 이정규 , 유충열 , 이대연
IPC分类号： C07D239/74
CPC分类号： C07D413/12 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12
摘要： 본 발명은 혈당 강하, 체중 감소를 나타내는 신규의 퀴나졸린 유도체와, 이 화합물을 유효성분으로 함유하는 당뇨 및 비만 치료예방제에 관한 것이다.
당뇨병 치료제, 비만 치료제, 퀴나졸린

3. 发明公开

KR1020060093314A 퀴나졸린 유도체의 조합화학적 방법에 의한 분자다양성구축기술 无效
标题翻译：基于组合化学的喹啉酮图谱分子多样性技术
公开(公告)号：KR1020060093314A
公开(公告)日：2006-08-24
申请号：KR1020060068890
申请日：2006-07-24
申请人： 한소 주식회사
发明人： 김상웅 , 김언겸 , 유충열 , 이정규 , 이대연 , 이은주
IPC分类号： C07D239/72 , C07D239/74
摘要： 본 발명은 화학식 1과 같은 퀴나졸린(quinazoline) 유도체의 합성을 용액상(solution phase) 반응을 이용한 조합화학적 방법으로 분자다양성을 구축하는 기술로서 고전적인 합성법보다 더 용이하고 빠르게 순수한 목적 화합물을 고순도로 제조할 수 있는 방법에 관한 것이다.
[화학식 1]

(상기식에서 R1, R2, R3, 및 R4는 명세서에 정의한 바와 같다)
조합화학, 분자다양성, 퀴나졸린유도체, 신약개발

4. 发明公开

KR1020050020083A 피페리딘고리를 포함하는 5-아미노메틸옥사졸리딘-2-온화합물 및 이의 약제학적으로 허용되는 염과 이들의제조방법 无效
标题翻译：含氨基苯甲酸-2-羟基喹啉-2-酮的衍生物含有包含两种阳性细菌和抗菌细菌的抗菌活性的广谱光谱的哌啶环及其制备方法
公开(公告)号：KR1020050020083A
公开(公告)日：2005-03-04
申请号：KR1020030057740
申请日：2003-08-20
申请人： 한소 주식회사
发明人： 김상웅 , 이정규 , 이은주 , 김언겸 , 유충열 , 이대연 , 노경록 , 방남영
IPC分类号： C07D413/14
摘要： PURPOSE: Derivatives of 5-aminomethyloxazolidin-2-one containing a piperidine ring and preparation methods thereof are provided, which derivatives have a broad spectrum of antibacterial activity that includes both Gram-positive bacterium and Gram-negative bacterium. CONSTITUTION: The derivatives of 5-aminomethyloxazolidin-2-one containing a piperidine ring represented by formula (1), pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof are provided, wherein R3 is aryl group or heteroaryl group which is optionally mono-, di-, tri- or tetra-substituted with one substituent selected from lower alkyl, halogenized lower alkyl, nitro, halogen, amino, alkoxy and hydroxy; and R2 is lower alkyl, or aryl group or hetero group which is optionally mono- or di-substituted with one substituent selected from lower alkyl, halogen, amino, alkoxy and hydroxy.
摘要翻译：目的：提供含有哌啶环的5-氨基甲基恶唑烷-2-酮的衍生物及其制备方法，该衍生物具有广谱的抗菌活性，其包括革兰氏阳性细菌和革兰氏阴性细菌。构成：提供了含有由式（1）表示的哌啶环的5-氨基甲基恶唑烷-2-酮的衍生物，其药学上可接受的盐，其水合物或溶剂合物，其中R 3是芳基或杂芳基，被一个取代基选自低级烷基，卤代低级烷基，硝基，卤素，氨基，烷氧基和羟基的二取代，三取代或四取代; 和R 2是低级烷基或芳基或杂基，其任选地被一个选自低级烷基，卤素，氨基，烷氧基和羟基的取代基单取代或二取代。

5. 发明授权

KR100675552B1 항산화활성을 지닌 화합물, 그의 제조방법 및 그를함유하는 피부노화 억제용 조성물 失效
标题翻译： 항산화활성을지닌화합물，그의제조방법및그를함유하유피부노화억제용조성물
公开(公告)号：KR100675552B1
公开(公告)日：2007-01-30
申请号：KR1020060004336
申请日：2006-01-16
申请人： 한소 주식회사
发明人： 김상웅 , 이상한 , 이은주 , 유충열 , 이정규 , 이대연 , 김언겸
IPC分类号： C07C311/15 , C07C243/34 , C07C311/18
摘要： Provided are a compound having an antioxidant activity, which has a good antioxidant effect, exhibits neither irritation nor toxicity, and is effective in preventing skin aging, and a preparation thereof. The compound having an antioxidant activity has a structure of the following formula 1. In the formula 1, R1 is a C1-7 alkyl group, a benzyl group, an aromatic ring, or a polycyclic aromatic ring in which at least two aromatic rings are joined to each other, wherein the alkyl group is further substitutable by halogen or a hydroxyl group, the benzyl group is further substitutable by a halogen-substituted or unsubstituted C1-5 alkoxy group, the aromatic group is further substitutable by a halogen-substituted or unsubstituted C1-5 alkyl, nitro, halogen, a carboxy group, halogen-substituted or unsubstituted C1-5 alkoxy, or sulfonyl group, R2 is a C1-4 alkyl group or a benzyl group, wherein the alkyl group and benzyl group are substitutable by a hydroxyl group, and R3 is the formula (a) or (b), wherein R12 is a C1-3 alkyl group, an aromatic group, or an aromatic heterocyclic ring, wherein the aromatic group is further substitutable by mono- or di-C1-3 alkylamino, halogen-substituted or unsubstituted C1-5 alkyl, halogen, halogen-substituted or unsubstituted C1-5 alkoxy, C1-3 alkylcarbonyl, nitro, C1-5 sulfonyl, or cyano group, and the aromatic heterocyclic ring is further substitutable by halogen.
摘要翻译：本发明提供具有良好的抗氧化效果，既不刺激也不具有毒性，并且对防止皮肤老化有效的具有抗氧化活性的化合物及其制备方法。具有抗氧化活性的化合物具有下式1的结构。在式1中，R 1为其中至少两个芳环为C 1-7烷基，苄基，芳环或多环芳环其中所述烷基可被卤素或羟基进一步取代，所述苄基可被卤素取代或未取代的C 1-5烷氧基进一步取代，所述芳基可进一步被卤素取代的或未取代的C 1-5烷基，硝基，卤素，羧基，卤素取代或未取代的C 1-5烷氧基或磺酰基，R 2为C 1-4烷基或苄基，其中烷基和苄基可被取代（a）或（b），其中R12为C1-3烷基，芳族基团或芳族杂环，其中所述芳族基团可进一步被单 - 或二 - -C1-3烷基氨基，卤素取代或未取代取代的C 1-5烷基，卤素，卤素取代的或未取代的C 1-5烷氧基，C 1-3烷基羰基，硝基，C 1-5磺酰基或氰基，并且该芳族杂环可进一步被卤素取代。

6. 发明授权

KR100666118B1 피라졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술 失效
标题翻译：基于组合化学的吡唑基分子多样性技术
公开(公告)号：KR100666118B1
公开(公告)日：2007-01-09
申请号：KR1020060088625
申请日：2006-09-13
申请人： 한소 주식회사
发明人： 김상웅 , 김언겸 , 유충렬 , 이정규 , 이대연 , 이은주 , 김도훈
IPC分类号： C40B99/00 , C07D231/12 , C07D231/00
CPC分类号： C40B40/04 , C07D231/40 , G06F19/701
摘要： A molecular diversity technology of pyrazole derivatives based on combinatorial chemistry is provided to enable a user to easily test biological activity with respect to disease target and manufacture a high purity of target compound with high yield more easily and rapidly than a classical synthetic method. The molecular diversity technology of pyrazole derivatives based on combinatorial chemistry manufactures pyrazole derivatives having a structure of the formula(1) by composing pyrazole derivative compound by performing cyclization by reacting R1COCH2CN compound with R2NHNH2ÀHCl compound firstly and using solution state reaction of R3C6H5NCO compound with the composed compound. In formula(1), X and Z are NH, Y is O and S, and R1, R2, R3 are H, alkyl group of C1-C8 or cyclo alkyl group of C3-C6, phenyl alkyl group of C1-C8, hydroxy alkyl group of C1-C8, and aromatic compound alkyl group of C3-C8.
摘要翻译：提供了基于组合化学的吡唑衍生物的分子多样性技术，使得用户能够容易地测试与疾病靶标相关的生物活性，并且比传统的合成方法更容易和快速地以高产率制造高纯度的目标化合物。基于组合化学的吡唑衍生物的分子多样性技术通过首先通过使R1COCH2CN化合物与R2NHNH2-HCl化合物反应进行环化反应，并通过使R3C6H5NCO化合物与组成的化合物的溶液状态反应，通过组成吡唑衍生物化合物制备具有式（1）结构的吡唑衍生物复合。在式（1）中，X和Z是NH，Y是O和S，R1，R2，R3是H，C1-C8的烷基或C3-C6的环烷基，C1-C8的苯基烷基， C1-C8的羟基烷基和C3-C8的芳族化合物烷基。

7. 发明授权

KR100670974B1 티아졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술 失效
标题翻译： 티아졸유도체의조합화학적방법에의한분자다양성구축기티
公开(公告)号：KR100670974B1
公开(公告)日：2007-02-28
申请号：KR1020060090205
申请日：2006-09-18
申请人： 한소 주식회사
发明人： 김상웅 , 유충렬 , 김언겸 , 이대연 , 이은주 , 김도훈
IPC分类号： C40B99/00 , C07D277/02 , C07D277/22
摘要： Molecular diversity technology using a combinatorial chemical method of a thiazole derivate is provided to easily test biological activation of a disease target by quickly producing a target compound with high purity by using a solution phase reaction. In a method for producing a thiazole derivate represented by formula(1) generated by combinatorially and chemically reacting compounds of a formula(A) or a formula(B) with compounds of a formula(C), R^a in the formula(1) is selected from a group comprising alkyl, cycloalkyl, heterocyclic which is not substituted or substituted for phenyl substituted as alkyl, alkenyl, alkynyl, alkoxy, and halogen of C1-C10. R^b is aliphatic and aromatic hydrocarbon derivate compounds of C5-C10 which are not substituted or substituted for C1 and alkoxy and includes straight or side chain alkyl, phenoxymethyl, substituted phenoxymethyl, aniline, C6H4NHCOR2(Anilide), and pyridine of C1-C8. R^c consists of hydrogen atom, CN(Cyano Group), C1, COOH(Carboxyl Group), methoxy, ethoxy, and CONHR3N(Amide). X contains sulfur atom, SO2(Sulfur Dioxide), NH, piperazine, and single-bond morpholine. R2 is phenyl or phenylmethyl substituted for alkyl or alkoxy. R3 is aliphatic and aromatic hydrocarbon derivate compounds of C5-C10 which are substituted or not substituted.
摘要翻译：提供使用噻唑衍生物的组合化学方法的分子多样性技术，以通过使用溶液相反应通过快速生产高纯度的目标化合物来容易地测试疾病目标的生物活化。在由式（A）或式（B）化合物与式（C）化合物组合和化学反应产生由式（1）表示的噻唑衍生物的方法中，式）选自烷基，环烷基，未取代或取代苯基的杂环，所述苯基被取代为C1-C10的烷基，烯基，炔基，烷氧基和卤素。 R 1b是未被取代或取代C 1和烷氧基并且包括直链或侧链烷基，苯氧基甲基，取代的苯氧基甲基，苯胺，C 6 H 4 NHCOR 2（N-酰苯胺）和C 1 -C 8的吡啶的C 5 -C 10的脂族和芳族烃衍生化合物。 R c由氢原子，CN（氰基），C 1，COOH（羧基），甲氧基，乙氧基和CONHR 3 N（酰胺）组成。 X含有硫原子，SO2（二氧化硫），NH，哌嗪和单键吗啉。 R2是苯基或被烷基或烷氧基取代的苯基甲基。 R3是被取代或未被取代的C5-C10的脂族和芳族烃衍生化合物。

8. 发明授权

KR100666108B1 벤조티아졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술 失效
标题翻译：基于组合化学的苯并噻唑图谱的分子多样性技术
公开(公告)号：KR100666108B1
公开(公告)日：2007-01-09
申请号：KR1020060077458
申请日：2006-08-17
申请人： 한소 주식회사
发明人： 김상웅 , 김언겸 , 유충렬 , 이정규 , 이대연 , 이은주 , 김도훈
IPC分类号： C40B99/00 , C07D277/20 , C40B60/00
CPC分类号： C40B40/04 , C07D277/20 , G06F19/701
摘要： A molecular diversity technology of benzothiazole derivatives based on combinatorial chemistry is provided to enable a user to easily test biological activity with respect to disease target and reduce time and cost for developing new medicine. The manufacturing method of a product represented by the formula(I) is capable of securing molecular diversity by performing solution state reaction by varying R2, X, Y, z based on combinational chemistry after replacing with a benzothiazole-2-thiol as a starting material. In the formula(I), X is SO2, Y is O, CH2 or NH, z is S, O or CH2, R1 is H, alkyl group of C1-C8 or cyclo alkyl group of C3-C6, and R2 is alkyl group of C1-C18, cyclo alkyl group of C3-C6, alkenyl group of C2-C8, alkoxy alkyl group of C1-C8, hydroxy alkyl group of C1-C8, phenyl alkyl group of C1-C8, phenyl alkenyl group of C1-C8, piperidine alkyl group of C1-C8, naphthalene alkyl group of C1-C8, morpholine alkyl group of C1-C8, pyridine alkyl group of C1-C8, pyrrolidine alkyl group of C1-C8, thiophene alkyl group of C1-C8, or alkyl group replaced by hydroxy amide of C1-C8.
摘要翻译：提供了基于组合化学的苯并噻唑衍生物的分子多样性技术，使用户能够容易地测试关于疾病靶标的生物活性，并减少开发新药的时间和成本。由式（I）表示的产物的制造方法能够通过在用苯并噻唑-2-硫醇替代后作为起始原料，通过基于组合化学改变R2，X，Y，z进行溶液状态反应来确保分子多样性。在式（I）中，X是SO 2，Y是O，CH 2或NH，z是S，O或CH 2，R 1是H，C 1 -C 8烷基或C 3 -C 6环烷基， C1-C18，C1-C8的环烷基，C2-C8的烯基，C1-C8的烷氧基烷基，C1-C8的羟基烷基，C1-C8的苯基烷基，C1的苯基烯基 -C8，C1-C8的哌啶烷基，C1-C8的萘烷基，C1-C8的吗啉烷基，C1-C8的吡啶烷基，C1-C8的吡咯烷基，C1-C8的噻吩烷基，或被C1-C8的羟基酰胺取代的烷基。

9. 发明公开

KR1020020043512A 니트로 알켄 유도체의 합성법 无效
标题翻译：合成NITROKENE衍生物的方法
公开(公告)号：KR1020020043512A
公开(公告)日：2002-06-10
申请号：KR1020020025969
申请日：2002-05-10
申请人： 한소 주식회사
发明人： 김상웅 , 강민석 , 이은주 , 김언겸 , 이정규 , 유충열 , 이대연 , 이용인 , 방남영
IPC分类号： C07C309/74
摘要： PURPOSE: Provided is a method for more economically and effectively producing nitroalkene derivatives through one process. CONSTITUTION: The nitroalkene derivatives are represented by formula 1, 2, 3, and 4. In the formulae, R represents at least one substituents selected from hydrogen, hydroxyl group, branched alkyl group, linear alkyl group, halogen, methoxy, phenoxy, benzyloxy, ethoxy, propoxy, sulfonyl group, and ester group. The nitroalkene derivatives are produced by using a methanol as solvent, a reaction temperature of 0 deg.C, and sodium hydroxide and hydrochloric acid as reaction reagent. The solvent is dichloromethane, and the reaction reagent is dimethylaminopyridine and acetic anhydride.
摘要翻译：目的：提供一种通过一种方法更经济有效地生产硝基烯烃衍生物的方法。构成：硝基烯烃衍生物由式1,2,3和4表示。在该式中，R代表至少一个选自氢，羟基，支链烷基，直链烷基，卤素，甲氧基，苯氧基，苄氧基，乙氧基，丙氧基，磺酰基和酯基。通过使用甲醇作为溶剂，反应温度为0℃，氢氧化钠和盐酸作为反应试剂制备硝基烯烃衍生物。溶剂为二氯甲烷，反应试剂为二甲基氨基吡啶和乙酸酐。

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