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    피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물
    46.
    发明公开
    피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 有权
    对于含有其作为活性成分的抗癌剂，吡嗪-2,4-二胺衍生物和药物组合物

    公开(公告)号：KR1020150102252A

    公开(公告)日：2015-09-07

    申请号：KR1020140023897

    申请日：2014-02-28

    Applicant: 한국화학연구원

    Inventor： 정희정 ,  김형래 ,  김필호 ,  박지훈 ,  안선주 ,  윤창수 ,  이광호 ,  이정옥 ,  조성윤 ,  채종학 ,  하재두 ,  황종연

    IPC: C07D401/12 ,  A61K31/506 ,  A61P35/00

    CPC classification number: A61K31/506 ,  C07D401/12

    Abstract: 본 발명은 피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 의한 화합물은 역형성 림프종 키나아제(ALK) 활성을 억제하는 효과가 우수하므로 이에 따른 EML4-ALK, NPM-ALK 등의 역형성 림프종 키나아제(ALK) 융합 단백질을 가진 암세포에 대한 치료효과가 향상될 수 있으며, 암의 재발을 막는데 효과적일 것으로 예상되므로 암의 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.

    Abstract translation: 本发明涉及嘧啶-2,4-二胺衍生物或其药学上可接受的盐，以及用于预防或治疗含有其作为活性成分的癌症的药物组合物。 根据本发明的化合物显示出抑制间变性淋巴瘤激酶（ALK）的优异效果，结果可以提高对具有间变性淋巴瘤激酶（ALK）融合蛋白（例如EML4-ALK）的癌细胞的治疗效果，以及 NPM-ALK。 此外，化合物可用于预防或治疗癌症的药物组合物，因为预期有效地预防癌症复发。

    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노 벤조피란유도체와 고체상 평형합성법에 의한 이의 합성방법
    47.
    发明公开
    2,2-디메틸-3-에스테르-4-알콕시-6-알킬 아미노 벤조피란유도체와 고체상 평형합성법에 의한 이의 합성방법 失效
    2,2-二甲基-3-异恶唑-4-烷氧基-6-烷基氨基苯并噻吩衍生物和衍生物在固相上的平行合成

    公开(公告)号：KR1020040022382A

    公开(公告)日：2004-03-12

    申请号：KR1020030037592

    申请日：2003-06-11

    Applicant: 한국화학연구원

    Inventor： 공영대 ,  전용석 ,  황종연 ,  유성은

    IPC: C07D311/74

    Abstract: PURPOSE: 2,2-Dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyran derivatives and a parallel synthesis of the derivatives on solid-phase are provided. The compounds have improved lipid peroxidation inhibiting activity, and are thus useful for the prevention and treatment of disease caused by stimulation of lipid peroxidation or accumulation of oxidizing materials. CONSTITUTION: 2,2-dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyran derivatives are represented by the formula(5a), wherein R1 is C1-C10 saturated, unsaturated or cyclic alkyl, benzyl or substituted benzyl; R2 is C1-C10 saturated, unsaturated or cyclic alkyl, benzyl, substituted benzyl, or penethyl; and R3a is C2-C10 unsaturated or cyclic alkyl, phenyl, substituted phenyl, or 5- to 7-membered hetero ring containing a hetero atom selected from oxygen and sulfur in which the substituted benzyl or substituted phenyl is benzyl or phenyl substituted by 1 to 4 substituents selected from halogen atom, nitro, C1-C10 alkyl, C1-C10 alkoxy and C1-C10 haloalkyl. A parallel synthesis of the 2,2-dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyran derivatives of the formula(5) on solid-phase comprises the steps of: selectively introducing R1 substituent to nitrogen of benzopyran of a compound of the formula(1) to prepare N-alkyl substituted carbamate resin of the formula(2); adding meta-chlorobenzoic acid and alcohol into the compound of the formula(2) and reacting them to prepare 2,2-dimethyl-3-hydroxy-6-alkyl amino benzopyran resin of the formula(3); reacting 3-hydroxy of the compound of the formula(3) with electrophile selected from carbonyl halide compounds containing R3 to prepare 2,2-dimethyl-3-ester-4-alkoxy-6-alkyl amino benzopyran resin of the formula(4); and treating the compound of the formula(4) with trifluoroacetic acid(TFA) containing a dichloromethane solution or organic acid containing an organic solvent, wherein (P) is a polymer type solid support selected from polystyrene-divinylbenzene, methacrylic acid-dimethylacrylamide and hydroxy methacrylic acid.

    Abstract translation: 目的：提供2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃衍生物和固相衍生物的平行合成。 所述化合物具有改善的脂质过氧化抑制活性，因此可用于预防和治疗由脂质过氧化或氧化物质的积累引起的疾病。 构成：2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃衍生物由式（5a）表示，其中R1是C1-C10饱和，不饱和或环状烷基，苄基或取代的苄基; R2是C1-C10饱和，不饱和或环状烷基，苄基，取代的苄基或penethyl; R3a是C2-C10不饱和或环状烷基，苯基，取代的苯基或含有选自氧和硫的杂原子的5至7元杂环，其中取代的苄基或取代的苯基是苄基或被1至 4个选自卤素原子，硝基，C 1 -C 10烷基，C 1 -C 10烷氧基和C 1 -C 10卤代烷基的取代基。 在固相上平行合成式（5）的2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃衍生物包括以下步骤：选择性地将R 1取代基引入到苯并吡喃的氮 式（1）的化合物，制备式（2）的N-烷基取代的氨基甲酸酯树脂; 向式（2）的化合物中加入间氯苯甲酸和醇，并使其反应制备式（3）的2,2-二甲基-3-羟基-6-烷基氨基苯并吡喃树脂; 使式（3）化合物的3-羟基与选自含有R 3的羰基卤化合物的亲电试剂反应制备式（4）的2,2-二甲基-3-酯-4-烷氧基-6-烷基氨基苯并吡喃树脂， ; 并用含有二氯甲烷溶液或含有机溶剂的有机酸的三氟乙酸（TFA）处理式（4）化合物，其中（P）是选自聚苯乙烯 - 二乙烯基苯，甲基丙烯酸 - 二甲基丙烯酰胺和羟基的聚合物型固体载体 甲基丙烯酸。

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