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    광학활성 1,4-디데옥시-1,4-이미노-아라비니톨의 제조방법
    12.
    发明公开
    광학활성 1,4-디데옥시-1,4-이미노-아라비니톨의 제조방법 有权
    用于光活性的1,4-二脱氧-1,4-亚氨基阿拉伯糖的制备方法

    公开(公告)号：KR1020110087977A

    公开(公告)日：2011-08-03

    申请号：KR1020100007674

    申请日：2010-01-28

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  최환근 ,  하정미 ,  박동식 ,  함영진

    IPC: C07D207/46 ,  C07D207/00

    Abstract: PURPOSE: A method for preparing optically active 1,4-dideoxy-1,4-imino-arabinitol is provided to easily synthesize a target compound. CONSTITUTION: A method for preparing 1,4-dideoxy-1,4-imino-arabinitol comprises: a step of oxidizing N-protected aziridinylmethanole compound of chemical formula 2; a step of reacting the compound of chemical formula 2 with a phosphonoacetate compound to prepare an ester compound of chemical formula 3; a step of reacting dihydroxylation of the ester compound of chemical formula 3 to prepare a dihydroxy compound of chemical formula 4; a step of cyclizing the dihydroxy compound of chemical formula 4 under the presence of organic acid of R_3COOH to prepare a lactam compound of chemical formula 5; and a step of reducing the lactam compound of chemical formula 5 deprotecting.

    Abstract translation: 目的：提供光学活性1,4-二脱氧-1,4-亚氨基 - 阿拉伯糖醇的制备方法，以容易地合成目标化合物。 构成：制备1,4-二脱氧-1,4-亚氨基 - 阿拉伯糖醇的方法包括：氧化化学式2的N-保护的氮丙啶基甲烷化合物的步骤; 使化学式2的化合物与膦酰基乙酸酯化合物反应以制备化学式3的酯化合物的步骤; 使化学式3的酯化合物的二羟基化反应制备化学式4的二羟基化合物的步骤; 在R_3COOH的有机酸的存在下环化化学式4的二羟基化合物以制备化学式5的内酰胺化合物的步骤; 以及还原化学式5的内酰胺化合物去保护的步骤。

    광학활성 1,4-디데옥시-1,4-이미노-아라비니톨의 제조방법
    15.
    发明授权
    광학활성 1,4-디데옥시-1,4-이미노-아라비니톨의 제조방법 有权
    光学活性1,4-二脱氧-1,4-亚氨基 - 阿拉伯糖醇的制备方法

    公开(公告)号：KR101088827B1

    公开(公告)日：2011-12-06

    申请号：KR1020100007674

    申请日：2010-01-28

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  최환근 ,  하정미 ,  박동식 ,  함영진

    IPC: C07D207/46 ,  C07D207/00

    Abstract: 본 발명은 광학활성 1,4-디데옥시-1,4-이미노-아라비니톨의 제조방법에 관한 것으로, 더욱 상세하게는 상업적으로 쉽게 구입이 가능한
    N- 보호된 아지리딘일메탄올 화합물을 출발물질로 사용하고, 광학활성 락탐 화합물을 반응 중간체로 합성하는 새로운 경로를 통하여 광학활성 1,4-디데옥시-1,4-이미노-아라비니톨을 보다 용이하게 합성하는 신규 제조방법에 관한 것이다.

    신규 이미다졸 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종의 예방 및 치료용 약학적 조성물
    18.
    发明公开
    신규 이미다졸 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종의 예방 및 치료용 약학적 조성물 失效
    新的咪唑衍生物或其药学上可接受的盐，其制备方法和药物组合物，用于预防和治疗含有它们的活性成分的梅毒

    公开(公告)号：KR1020110044544A

    公开(公告)日：2011-04-29

    申请号：KR1020090101277

    申请日：2009-10-23

    Applicant: 한국과학기술연구원

    Inventor： 하정미 ,  유경호 ,  심태보 ,  오창현 ,  이정헌 ,  유하나 ,  김환

    IPC: C07D401/04 ,  C07D401/02 ,  A61K31/415 ,  A61P35/00

    CPC classification number: C07D403/14 ,  A61K31/415 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    Abstract: PURPOSE: A pharmaceutical composition containing a novel imidazole derivative or pharmaceutically acceptable salt thereof is provided to prevent and treat melanoma. CONSTITUTION: An imidazole derivative is denoted by chemical formula 1. A method for preparing the imidazole derivatives comprises: a step of reacting a compound of chemical formula 2 with a compound of chemical formula 3 to obtain a compound of chemical formula 4; a step of performing Buchwald amination of the compound of chemical formula 4 with a compound of chemical formula 5 to obtain a compound of chemical formula 6; a step of oxidizing the compound of chemical formula 6 to obtain a compound of chemical formula 7; a step of reacting the compound of chemical formula 7 with R^1NH_2 to obtain a compound of chemical formula 8; and a step of reducing the compound of chemical formula 8 to prepare a compound of chemical formula 1a. A pharmaceutical composition for preventing and treating melanoma contains the imidzaole derivative or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的：提供含有新型咪唑衍生物或其药学上可接受的盐的药物组合物以预防和治疗黑素瘤。 构成：咪唑衍生物由化学式1表示。咪唑衍生物的制备方法包括：使化学式2化合物与化学式3的化合物反应得到化学式4的化合物的步骤; 用化学式5的化合物进行化学式4的化合物的Buchwald胺化的步骤，得到化学式6的化合物; 氧化化学式6的化合物以获得化学式7的化合物的步骤; 使化学式7的化合物与R 1，1NH 2反应以获得化学式8的化合物的步骤; 还原化学式8的化合物以制备化学式1a的化合物的步骤。 用于预防和治疗黑素瘤的药物组合物含有亚胺唑衍生物或其药学上可接受的盐作为活性成分。

    단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
    19.
    发明公开
    단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 有权
    2,7-取代的噻吩并[3,2-D]吡啶化合物作为蛋白激酶抑制剂

    公开(公告)号：KR1020110044053A

    公开(公告)日：2011-04-28

    申请号：KR1020090100867

    申请日：2009-10-22

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  최환근 ,  하정미 ,  함영진 ,  전은진 ,  이정헌 ,  김환

    IPC: C07D495/04 ,  C07D495/02 ,  A61K31/505 ,  A61P35/00

    CPC classification number: C07D495/04 ,  C07D519/00

    Abstract: PURPOSE: A 2,7-substituted thieno[3,2-d]pyrimidine compound is provided to ensure excellent effect of suppressing various protein kinases and to prevent and treat abnormal cell growth diseases. CONSTITUTION: A 2,7-substituted thieno[3,2-d]pyrimidine compound is denoted by chemical formula 1. A pharmaceutical composition contains the compound of chemical formula 1 as an active ingredient. The pharmaceutical composition is used for preventing and treating abnormal cell growth diseases through ALK, Aurora A, EphA1, FAK, Flt3, Fms, Itk, KDR, Kit, Met, Ret, Src, Syk, Tie2, or TrkB protein kinase suppression mechanism. An agent for preventing and treating tumor contains the compound of chemical formula 1 as an active ingredient.

    Abstract translation: 目的：提供2,7-取代的噻吩并[3,2-d]嘧啶化合物，以确保抑制各种蛋白激酶和预防和治疗异常细胞生长疾病的优异效果。 构成：2,7-取代的噻吩并[3,2-d]嘧啶化合物由化学式1表示。药物组合物含有化学式1的化合物作为活性成分。 该药物组合物用于通过ALK，Aurora A，EphA1，FAK，Flt3，Fms，Itk，KDR，Kit，Met，Ret，Src，Syk，Tie2或TrkB蛋白激酶抑制机制预防和治疗异常细胞生长疾病。 用于预防和治疗肿瘤的药物含有化学式1的化合物作为活性成分。

    신규 피라졸로이미다졸계 화합물 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 비정상 세포 성장 질환의 예방 및 치료용 약학적 조성물
    20.
    发明公开
    신규 피라졸로이미다졸계 화합물 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 비정상 세포 성장 질환의 예방 및 치료용 약학적 조성물 有权
    新型的基于吡唑并咪唑的化合物或其药学上可接受的盐，其制备方法和药物组合物，用于预防和治疗含有作为活性成分的异常细胞生长疾病

    公开(公告)号：KR1020100137742A

    公开(公告)日：2010-12-31

    申请号：KR1020090055939

    申请日：2009-06-23

    Applicant: 한국과학기술연구원

    Inventor： 하정미 ,  유경호 ,  심태보 ,  오창현 ,  유하나 ,  김환 ,  정윤경 ,  이정헌

    IPC: C07D487/04 ,  C07D487/02 ,  A61K31/4188

    Abstract: PURPOSE: A novel pyrazoloimidazole compound is provided to suppress various protein kinase causing abnormal cell growth disorders. CONSTITUTION: A pyrazoloimidazole compound is denoted by chemical formula 1. A method for preparing the pyrazoloimidazole compound comprises: a step of performing cyclization and nitrosation of compounds of chemical formulas 2 and 3 to obtain a compound of chemical formula 4; a step of reducing the compound of chemical formula 4 to obtain a compound of chemical formula 5; a step of condensing the compound of chemical formula 5 with carboxylic acid compound of chemical formula 6 to obtain a compound of chemical formula 7; a step of reducing the compound of chemical formula 7 to obtain a compound of chemical formula 1a. A pharmaceutical composition for preventing and treating abnormal cell growth contains pyrazoloimidazole compounds of chemical formula 1 and pharmaceutically acceptable salt as an active ingredient.

    Abstract translation: 目的：提供一种新的吡唑并咪唑化合物，以抑制引起异常细胞生长障碍的各种蛋白激酶。 构成：吡唑并咪唑化合物由化学式1表示。吡唑并咪唑化合物的制备方法包括：使化学式2和化合物3化合物进行环化和亚硝化以获得化学式4化合物的步骤; 还原化学式4的化合物以获得化学式5的化合物的步骤; 将化学式5的化合物与化学式6的羧酸化合物缩合以获得化学式7的化合物的步骤; 还原化学式7的化合物以获得化学式1a的化合物的步骤。 用于预防和治疗异常细胞生长的药物组合物含有化学式1的吡唑并咪唑化合物和其药学上可接受的盐作为活性成分。

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