티아(옥사)졸로피리딘 화합물 및 이의 제조 방법
    31.
    发明公开
    티아(옥사)졸로피리딘 화합물 및 이의 제조 방법 失效
    THIA(OXA)ZOLOPYRIDINE化合物及其制备方法

    公开(公告)号:KR1020100035063A

    公开(公告)日:2010-04-02

    申请号:KR1020080094366

    申请日:2008-09-25

    CPC classification number: C07D513/04 C07D498/04

    Abstract: PURPOSE: A thia(oxa)zolopyridine compound and a method for preparing the same are provided to suppress beta-amyloid fibril formation and use as an agent for preventing and treating neurodegenerative diseases. CONSTITUTION: A thia(oxa)zolopyridine compound is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by cyclizing a compound of chemical formula 2. An agent for suppressing formation of beta-amyloid fibril contains the thia(oxa)zolopyridine compound of chemical formula 1 or pharmaceutically acceptable salt as an active ingredient. A pharmaceutical composition for treating neurodegenerative diseases contains the thia(oxa)zolopyridine compound or pharmaceutically acceptable salt as an active ingredient.

    Abstract translation: 目的:提供硫代(oxa)唑吡啶化合物及其制备方法以抑制β-淀粉样蛋白原纤维形成和用作预防和治疗神经变性疾病的药剂。 构成:化学式1表示噻吩(oxa)唑吡啶化合物。化学式1的化合物是通过使化学式2的化合物环化而制备的。用于抑制β-淀粉样蛋白原纤维形成的试剂含有硫代(oxa)唑吡啶 化学式1的化合物或其药学上可接受的盐作为活性成分。 用于治疗神经变性疾病的药物组合物含有硫代(oxa)唑吡啶化合物或其药学上可接受的盐作为活性成分。

    발광 특성을 갖는 디페닐아민 유도체
    32.
    发明公开
    발광 특성을 갖는 디페닐아민 유도체 失效
    具有发光性能的二苯胺衍生物

    公开(公告)号:KR1020100028992A

    公开(公告)日:2010-03-15

    申请号:KR1020080109444

    申请日:2008-11-05

    Abstract: PURPOSE: A diphenylamine derivative having light emitting property is provided to ensure light emitting property by UV RAY or visible ray and use in organic electro luminescence device or electronic element for display. CONSTITUTION: A diphenylamine is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are dependently hydrogen stom, C1-C8 alkyl group, substituted or non-substituted paenylgroup, biphenyl group. An organic electroluminescent (EL) device or display contains the pigment. A method for preparing palladium(Pd) diphenylamine derivative comprises: a first step of synthesizing ethanone compound of chemical formula 4 under the presence of catalyst and nitrogen; a second step of reacting ethanone compound of chemical formula 4 with N,N-dimethylformamide dimethylacetal to synthesize prophenone compound of chemical formula 5; a third step of reacting the prophenone compound with sodium ethoxide and guanidine hydrochloride to obtain amine compound of chemical formula 1a; and a step of reacting the amine compound with halide compound of R1-X or R2-X.

    Abstract translation: 目的:提供具有发光性的二苯胺衍生物,以通过UV RAY或可见光确保发光特性,并用于有机电致发光元件或显示用电子元件。 构成:二苯胺由化学式1表示。在化学式1中,R 1和R 2是氢气,C 1 -C 8烷基,取代或未取代的苯基,联苯基。 有机电致发光(EL)装置或显示器含有颜料。 制备钯(Pd)二苯胺衍生物的方法包括:在催化剂和氮气存在下合成化学式4的乙酮化合物的第一步; 使化学式4的乙酮化合物与N,N-二甲基甲酰胺二甲缩醛反应合成化学式5的丙酮化合物的第二步; 使丙酮化合物与乙醇钠和盐酸胍反应的第三步骤,得到化学式1a的胺化合物; 以及使胺化合物与R1-X或R2-X的卤化物反应的步骤。

    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물
    33.
    发明授权
    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물 失效
    신규피라졸로피리미딘계유도체,그의제조방법및이를유효성분으로하는약학적조성물

    公开(公告)号:KR100468352B1

    公开(公告)日:2005-01-27

    申请号:KR1020020057933

    申请日:2002-09-24

    Abstract: PURPOSE: A pyrazolopyrimidine derivative as a cyclin-dependent kinase inhibitor and a process for preparing the same are provided. The compound inhibits cyclin-dependent kinase(CDK) regulating cell division cycle and has low toxicity. Therefore, it can be useful for prevention and treatment of liver cancer, breast cancer, stomach cancer, colon cancer or rectal cancer caused by activation of CDK. CONSTITUTION: A pyrazolopyrimidine derivative is represented by the formula(1), wherein R1 comprises ortho, meta, or para substituent, and is bromo, chloro, fluoro, methoxy, hydrogen, nitro or amino; R2 is hydrogen or C3 or less of lower alkyl; R3 is hydrogen or C3 or less of lower alkyl, or hydroxyethyl; and n is an integer of 0 or 1. A method for preparing the pyrazolopyrimidine derivative represented by the formula(1) comprises the steps of: reacting 6-methylmercaptopyrazolopyrimidine of the formula(IV) with meta-chloroperbenzoic acid in the presence of an organic solvent such as chloroform or dichloromethane at -10 to 10 deg. C for 2 to 5 hours and at room temperature for 3 to 12 hours to prepare 6-methylsulfonylpyrazolopyrimidine of the formula(II); and nucleophilic substitution reaction of 6-methylsulfonylpyrazolopyrimidine of the formula(II) with hydroxyethylamine in the presence of a mixed organic solvent of isopropanol or n-butanol and dimethylsulfoxide or dimethylformamide at 70 to 100 deg. C for 1 to 6 hours.

    Abstract translation: 目的:提供了作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶衍生物及其制备方法。 该化合物抑制细胞周期蛋白依赖性激酶(CDK)调节细胞分裂周期并具有低毒性。 因此,它可用于预防和治疗由CDK活化引起的肝癌,乳腺癌,胃癌,结肠癌或直肠癌。 结构式:吡唑并嘧啶衍生物由式(1)表示,其中R 1包含邻位,间位或对位取代基,并且是溴,氯,氟,甲氧基,氢,硝基或氨基; R2是氢或C3或更少的低级烷基; R3是氢或C3或更少的低级烷基或羟乙基; 制备式(1)代表的吡唑并嘧啶衍生物的方法包括下列步骤:使式(IV)的6-甲基巯基吡唑并嘧啶与间氯过苯甲酸在有机 溶剂如氯仿或二氯甲烷在-10至10℃下进行。 (II)的6-甲基磺酰基吡唑并嘧啶;将式(II)的6-甲基磺酰基吡唑并嘧啶在室温下搅拌2至5小时,并在室温下反应3至12小时。 (II)的6-甲基磺酰基吡唑并嘧啶与羟基乙胺在异丙醇或正丁醇和二甲基亚砜或二甲基甲酰胺的混合有机溶剂存在下在70-100℃下进行亲核取代反应。 C 1至6小时。

    아지리디닐퀴놀린디온 유도체와 그의 제조방법
    34.
    发明授权
    아지리디닐퀴놀린디온 유도체와 그의 제조방법 失效
    아지리디닐퀴놀린디온유도체와그의제조방법

    公开(公告)号:KR100390767B1

    公开(公告)日:2003-07-10

    申请号:KR1020000062695

    申请日:2000-10-24

    CPC classification number: C07D401/04

    Abstract: The present invention relates to aziridinylquinolinedione derivatives having an anti-tumor effect of formula (1), a process for their preparation and their use as an anti-cancer agent, wherein R is a hydrogen atom or C1-C4 alkyl; one of R and R is an aziridinyl or 2-methylaziridinyl and the other one is a halogen atom, C1-C4 alkoxy, azido, or amino.

    Abstract translation: 本发明涉及具有式(1)的抗肿瘤作用的氮丙啶基喹啉二酮衍生物,它们的制备方法以及它们作为抗癌剂的用途,其中R 1是氢。 是氢原子或C 1 -C 4烷基; R 2中的一个是R 2。 并且R 3是氢。 是吖丙啶基或2-甲基氮丙啶基,另一个是卤素原子,C 1 -C 4烷氧基,叠氮基或氨基。

    5'-헤테로아릴티오메틸피롤리딘-3'-일티오기를 갖는 신규 1-베타메틸카바페넴 유도체 및 그의 제조방법
    35.
    发明授权
    5'-헤테로아릴티오메틸피롤리딘-3'-일티오기를 갖는 신규 1-베타메틸카바페넴 유도체 및 그의 제조방법 失效
    5'-헤테로아릴티메틸피롤리딘-3'-일티오기를갖는신규1-베타메틸카바페넴유도체및그의제조방5

    公开(公告)号:KR100385093B1

    公开(公告)日:2003-05-22

    申请号:KR1020000049675

    申请日:2000-08-25

    Abstract: PURPOSE: Provided are a novel 1-β-methylcarbapenem derivative useful as antibiotics, its pharmaceutically acceptable salt, its manufacturing method and a pharmaceutical composition. containing it. CONSTITUTION: 1-β-methylcarbapenem derivative is represented by the formula(1), wherein R is represented by formulae; X is trifluormethyl or C1-C3 alkyl; Y is C1-C3 linear or branched aliphatic alkyl, C1-C3 sulfonamido alkyl in which one or two C1-C3 alkyl groups are substituted, C1-C3 alkyl substituted or unsubstituted C1-C3 carbo amidoalkyl group, C1-C3 hydroxyalkyl group, and C1-C3 alkyl substituted C1-C3 aminoalkyl or aryl; and Z is C1-C3 alkyl group.

    Abstract translation: 目的:提供一种可用作抗生素的新型1-&β-甲基碳代青霉烯衍生物,其药学上可接受的盐,其制备方法和药物组合物。 包含它。 构成:1-β-甲基碳代青霉烯衍生物由式(1)表示,其中R由式表示; X是三氟甲基或C 1 -C 3烷基; Y是C1-C3直链或支链脂族烷基,其中一个或两个C1-C3烷基被取代的C1-C3亚磺酰氨基烷基,C1-C3烷基取代或未取代的C1-C3碳酰氨基烷基,C1-C3羟烷基和 C 1 -C 3烷基取代的C 1 -C 3氨基烷基或芳基; Z是C1-C3烷基。

    새로운 알파형 퀴나크리돈계 유도체 및 그 제조방법
    36.
    发明授权
    새로운 알파형 퀴나크리돈계 유도체 및 그 제조방법 失效
    新的α-型喹吖啶酮衍生物及其制备方法

    公开(公告)号:KR1019930010503B1

    公开(公告)日:1993-10-25

    申请号:KR1019900015291

    申请日:1990-09-26

    CPC classification number: C09B67/0027 C09B48/00

    Abstract: Quinacridone derivatives of formula (I) are prepd. by (a) reacting diethyl 1,4-dicyclohexadione-2,5-dicarboxylate with aromatic amine derivatives such as 5-aminoindane, 3,4-(methylenedioxy) aniline, 2-aminofluorene, 3- amino-9-ethylcarbazole in the presence of trifluoroacetic acid to obtain diethyl 2,5-dianilino-3,6-dihydroterephthalate (II), (b) reacting (II) in a mixed solvent of biphenyl and diphenylether at 250-270 deg.C for 1 hr to obtain 6,13-dihydroquinacridone (II), and (c) oxidn. of (III) with m-nitrobenzene sulfonic acid sodium salt in ethanol, water and NaOH solution. In formula (I), A= cyclopentyl, methylenedioxy, indanyl or N-ethyl indolyl.

    Abstract translation: 式(I)的喹吖啶酮衍生物是制备的。 通过(a)使1,4-二环己酮-2,5-二羧酸二乙酯与芳族胺衍生物如5-氨基茚满,3,4-(亚甲二氧基)苯胺,2-氨基芴,3-氨基-9-乙基咔唑的存在 的三氟乙酸,得到2,5-二苯胺基-3,6-二氢对苯二甲酸二乙酯(II),(b)在联苯和二苯基醚的混合溶剂中于250-270℃反应1小时,得到6, (II)和(c)氧化物。 的(III)与间硝基苯磺酸钠盐在乙醇,水和NaOH溶液中。 在式(I)中,A =环戊基,亚甲二氧基,茚满基或N-乙基吲哚基。

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