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    • 1. 发明授权
    • 티아졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술
    • 티아졸유도체의조합화학적방법에의한분자다양성구축기티
    • KR100670974B1
    • 2007-02-28
    • KR1020060090205
    • 2006-09-18
    • 한소 주식회사
    • 김상웅유충렬김언겸이대연이은주김도훈
    • C40B99/00C07D277/02C07D277/22
    • 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.
    • 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。
    • 2. 发明授权
    • 벤조티아졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술
    • 基于组合化学的苯并噻唑图谱的分子多样性技术
    • KR100666108B1
    • 2007-01-09
    • KR1020060077458
    • 2006-08-17
    • 한소 주식회사
    • 김상웅김언겸유충렬이정규이대연이은주김도훈
    • C40B99/00C07D277/20C40B60/00
    • C40B40/04C07D277/20G06F19/701
    • 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.
    • 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。
    • 3. 发明授权
    • 피라졸 유도체의 조합화학적 방법에 의한 분자다양성구축기술
    • 基于组合化学的吡唑基分子多样性技术
    • KR100666118B1
    • 2007-01-09
    • KR1020060088625
    • 2006-09-13
    • 한소 주식회사
    • 김상웅김언겸유충렬이정규이대연이은주김도훈
    • C40B99/00C07D231/12C07D231/00
    • C40B40/04C07D231/40G06F19/701
    • 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.
    • 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。