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    2-설파닐-벤즈이미다졸-4-카르복스아미드 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 폴리(ＡＤＰ-리보스)폴리머라제-1(ＰＡＲＰ-1)의 과활성에 의해 유발되는 질환의 예방 또는 치료용 약학적 조성물
    59.
    发明公开
    2-설파닐-벤즈이미다졸-4-카르복스아미드 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 폴리(ＡＤＰ-리보스)폴리머라제-1(ＰＡＲＰ-1)의 과활성에 의해 유발되는 질환의 예방 또는 치료용 약학적 조성물 有权
    2-磺基苯并咪唑-4-羧酰胺衍生物或其药学上可接受的盐，其制备方法和含有该成分的药物组合物作为活性成分用于预防和治疗由多聚（ADP-糖基）聚合酶引起的疾病引起的疾病， 1

    公开(公告)号：KR1020100022618A

    公开(公告)日：2010-03-03

    申请号：KR1020080081209

    申请日：2008-08-20

    Applicant: 한국화학연구원

    Inventor： 이규양 ,  이선경 ,  김낙정 ,  서지희 ,  임채조 ,  이병호 ,  오광석 ,  서호원 ,  유성은 ,  이경희 ,  김유선

    IPC: C07D235/28 ,  A61K31/137 ,  A61K9/20

    Abstract: PURPOSE: A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is provided to repair damaged DNA and suppress poly(ADP-ribose)polymerase-1(PARP-1) which is an enzyme causing cell damage and apoptosis. CONSTITUTION: A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is denoted by chemical formula 1. A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is prepared by performing alkylation of a compound of chemical formula 2 and a compound of chemical formula 3. A basic catalyst is used in the preparation. The basic catalyst is carbonate including sodium carbonate, potassium carbonate, or cesium carbonate; hydroxide including potassium hydroxide or sodium hydroxide; hydride including sodium hydride; alkoxide including sodium methoxide and sodium t-butoxide; triethylamine; or pyridine. A pharmaceutical composition for preventing or treating diseases caused by over-activation contains the 2-sulfanyl-benzimidazole-4-carboximidazole derivative or its pharmaceutically acceptable salt as an active ingredient.

    Abstract translation: 目的：提供2-硫基 - 苯并咪唑-4-甲胺唑衍生物修复损伤的DNA，并抑制作为引起细胞损伤和细胞凋亡的酶的聚（ADP-核糖）聚合酶-1（PARP-1）。 构成：2-硫基 - 苯并咪唑-4-甲胺唑衍生物由化学式1表示。2-硫基 - 苯并咪唑-4-甲胺咪唑衍生物是通过化学式2的化合物和化学式3的化合物的烷基化制备的 在制备中使用碱性催化剂。 碱性催化剂是碳酸钠，碳酸钾或碳酸铯; 氢氧化物包括氢氧化钾或氢氧化钠; 氢化物包括氢化钠; 包括甲醇钠和叔丁醇钠的醇盐; 三乙胺; 或吡啶。 用于预防或治疗由过度活化引起的疾病的药物组合物含有2-硫基 - 苯并咪唑-4-甲胺唑衍生物或其药学上可接受的盐作为活性成分。

    ＭＣＨ1Ｒ 억제 활성을 가지는 퀴녹살린 유도체 및약제학적으로 허용 가능한 그의 염, 그 제조방법 및비만치료용 그의 용도
    60.
    发明公开
    ＭＣＨ1Ｒ 억제 활성을 가지는 퀴녹살린 유도체 및약제학적으로 허용 가능한 그의 염, 그 제조방법 및비만치료용 그의 용도 失效
    喹啉衍生物和具有MCH1R抑制活性的药物接受盐，其制备方法及其用于治疗肥胖症的方法

    公开(公告)号：KR1020090090792A

    公开(公告)日：2009-08-26

    申请号：KR1020080016257

    申请日：2008-02-22

    Applicant: 한국화학연구원

    Inventor： 공영대 ,  전문국 ,  이태호 ,  황순희 ,  유성은

    IPC: C07D241/44 ,  A61K31/498

    Abstract: A quinoxaline derivatives having activity of suppressing melanin-concentrating hormone 1 receptor (MCH1R) is provided to treat diseases related to obesity caused by the activation of MCH1R. A quinoxaline derivative of the chemical formula 1 has the activation of suppressing a melanin-concentrating hormone receptor (MCH1R). A method for manufacturing the quinoxaline derivative of the chemical formula 1 comprises: a first step of condensing a compound of the chemical formula 3 with 2-chloro-6-nitroquinoxaline compound of the chemical formula 2 to produce a 6-nitroquinoxaline derivative of the chemical formula 4; a second step of reducing the 6-nitroquinoxaline derivative of the chemical formula 4 to produce a 6-aminoquinoxaline derivative of the chemical formula 5; and a third step of condensing biphenyl-4-carboxylic acid compound of the chemical formula 6 with the aminoquinoxaline derivative of the chemical formula 5 to a quinoxaline derivative which 6-(biphenyl-4-carboxamido) group is substituted.

    Abstract translation: 提供具有抑制黑色素浓缩激素1受体（MCH1R）活性的喹喔啉衍生物，用于治疗由MCH1R的激活引起的与肥胖相关的疾病。 化学式1的喹喔啉衍生物具有抑制黑色素浓缩激素受体（MCH1R）的活化。 制备化学式1的喹喔啉衍生物的方法包括：将化学式3的化合物与化学式2的2-氯-6-硝基喹喔啉化合物缩合以产生化学式的6-硝基喹喔啉衍生物的第一步骤 公式4; 还原化学式4的6-硝基喹喔啉衍生物以产生化学式5的6-氨基喹喔啉衍生物的第二步; 和将化学式6的联苯-4-羧酸化合物与化学式5的氨基喹喔啉衍生物缩合成6-（联苯-4-甲酰胺基）基取代的喹喔啉衍生物的第三步骤。

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