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    단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
    2.
    发明授权
    단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 有权
    2,4,7-取代的噻吩并[3,2-d]嘧啶化合物作为蛋白激酶抑制剂

    公开(公告)号：KR101094446B1

    公开(公告)日：2011-12-15

    申请号：KR1020090112132

    申请日：2009-11-19

    Applicant: 한국과학기술연구원

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

    IPC: C07D495/04 ,  C07D495/02 ,  A61K31/4365 ,  A61P35/00

    CPC classification number: C07D495/04

    Abstract: 본 발명은 단백질 키나아제 저해활성을 갖는 2,4,7-치환된 티에노[3,2
    -d ]피리미딘 화합물, 이의 약학적으로 허용 가능한 염, 그리고 이 화합물을 유효성분으로 함유하는 비정상 세포 성장으로 유발되는 질환의 예방 및 치료용 약학적 조성물에 관한 것이다.
    본 발명의 신규 2,4,7-치환된 티에노[3,2
    -d ]피리미딘 화합물은 성장 인자 신호 전달에 관여하는 다양한 단백질 키나아제에 대하여 우수한 억제 효과를 나타내므로, 이들 단백질 키나아제에 의해 유발되는 비정상 세포 성장 질환의 예방 및 치료제로서 유용하다.
    2,4,7-치환된 티에노[3,2-d]피리미딘, 단백질, 키나아제, 억제제, 비정상 세포 성장 질환

    단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
    3.
    发明公开
    단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 有权
    作为蛋白激酶抑制剂的2,4,7-取代的三[3,2-D]吡啶化合物

    公开(公告)号：KR1020110055202A

    公开(公告)日：2011-05-25

    申请号：KR1020090112132

    申请日：2009-11-19

    Applicant: 한국과학기술연구원

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

    IPC: C07D495/04 ,  C07D495/02 ,  A61K31/4365 ,  A61P35/00

    CPC classification number: C07D495/04

    Abstract: PURPOSE: A 2,4,7-substituted thieno[3,2-d]pyrimidine compound is provided to inhibit protein kinase activity and to prevent abnormal cell proliferation-induced diseases. CONSTITUTION: A 2,4,7-substituted thieno[3,2-d]pyrimidine compound with an activity of suppressing protein kinase, isomer, pharmaceutically acceptable salt, hydrate, or solvate thereof is denoted by chemical formula 1. In chemical formula 1, A is hydroxy C1-C6 alkyl group, phenyl group, or hetero aryl group containing 1-3 nitrogen atoms; and Ra is hydrogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, or heterocycloalkyl group containing 1-3 hetero atoms selected from oxygen and nitrogen.

    Abstract translation: 目的：提供2,4,7-取代的噻吩并[3,2-d]嘧啶化合物以抑制蛋白激酶活性并防止异常细胞增殖诱导的疾病。 构成：具有抑制蛋白激酶，异构体，药学上可接受的盐，水合物或溶剂合物的活性的2,4,7-取代的噻吩并[3,2-d]嘧啶化合物由化学式1表示。在化学式1中 A是羟基C1-C6烷基，苯基或含1-3个氮原子的杂芳基; 并且R a是氢原子，C 1 -C 6烷基，C 1 -C 6烷氧基或含1-3个选自氧和氮的杂原子的杂环烷基。

    단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물
    4.
    发明公开
    단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물 有权
    新颖的1,6-二取代吲哚化合物作为蛋白激酶抑制剂

    公开(公告)号：KR1020110045688A

    公开(公告)日：2011-05-04

    申请号：KR1020090102359

    申请日：2009-10-27

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  함영진 ,  유경호 ,  오창현 ,  하정미 ,  최환근 ,  김환 ,  전은진

    IPC: C07D403/04 ,  C07D209/04 ,  A61K31/40 ,  A61P35/00

    CPC classification number: C07D403/04 ,  A61K31/404 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

    Abstract: PURPOSE: A 1,6-substituted indole compound with an activity of suppressing protein kinase is provided to prevent and treat tumor caused by protein kinase. CONSTITUTION: A 1,6-substituted indole compound is denoted by chemical formula 1. A pharmaceutical composition contains the 1,6-subsituted indole compound as an active ingredient. The pharmaceutical composition is used for preventing and treating tumor disease caused by mechanism of protein kinase of Raf, KDR, Fms, Tie2, SAPK2a, Ret, Abl, Abl(T315I), ALK, Aurora A, Bmx, Src, EphA1, FGFR, Flt3, Itk, JAK2, Met, PDGFR, Plk, Ret, Syk, or Trk.

    Abstract translation: 目的：提供具有抑制蛋白激酶活性的1,6-取代吲哚化合物，以预防和治疗由蛋白激酶引起的肿瘤。 构成：1,6-取代的吲哚化合物由化学式1表示。药物组合物含有1,6-取代的吲哚化合物作为活性成分。 该药物组合物用于预防和治疗由Raf，KDR，Fms，Tie2，SAPK2a，Ret，Abl，Abl（T315I），ALK，Aurora A，Bmx，Src，EphA1，FGFR等蛋白激酶的机制引起的肿瘤疾病， Flt3，Itk，JAK2，Met，PDGFR，Plk，Ret，Syk或Trk。

    아미노퀴놀린 화합물, 이의 제조 방법 및 이를 함유하는 의약 조성물
    5.
    发明公开
    아미노퀴놀린 화합물, 이의 제조 방법 및 이를 함유하는 의약 조성물 失效
    氨基喹啉衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：KR1020100107326A

    公开(公告)日：2010-10-05

    申请号：KR1020090025560

    申请日：2009-03-25

    Applicant: 한국과학기술연구원

    Inventor： 유경호 ,  김동진 ,  남봉수 ,  오창현 ,  이소하 ,  조승주 ,  심태보 ,  하정미

    IPC: C07D215/54 ,  C07D215/44

    CPC classification number: C07D215/233 ,  A61K31/47 ,  C07D401/12 ,  C07D413/12

    Abstract: PURPOSE: A novel aminoquinoline compound or pharmaceutically acceptable salt thereof are provided to ensure anti-proliferative efficiency with respect to melanoma and to prevent or treat skin cancer. CONSTITUTION: An amino quinoline compound is denoted by chemical formula 1. A method for preparing the amino quinoline compound or pharmaceutically acceptable salt thereof comprises: a step of performing nitration of a compound of chemical formula 2 to obtain a compound of chemical formula 3; a step of substituting the compound of chemical formula 3 to amino phenol compound to obtain a compound of chemical formula 4; a step of coupling the compound of chemical formula 4 with carboxylic acid compound of general formula R^5-CO_2H or isocyanate of general formula R^5-NCO to obtain a compound of chemical formula 5; a step of reducing the compound of chemical formula 5 to obtain a compound of chemical formula 6; a step of performing amidation of the compound of chemical formula 6 with carboxylic acid of general formula R^4-CO_2H. A pharmaceutical composition for preventing or treating skin cancer contains aminoquinoline compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的：提供一种新的氨基喹啉化合物或其药学上可接受的盐以确保相对于黑素瘤的抗增殖效能并预防或治疗皮肤癌。 构成：氨基喹啉化合物由化学式1表示。氨基喹啉化合物或其药学上可接受的盐的制备方法包括：对化学式2的化合物进行硝化以获得化学式3的化合物的步骤; 将化学式3的化合物代替氨基酚化合物以获得化学式4的化合物的步骤; 将化学式4的化合物与通式为R 5，-CO 2 H的羧酸化合物或通式为R 5，NCO的异氰酸酯偶联，得到化学式5化合物的步骤; 还原化学式5的化合物以获得化学式6的化合物的步骤; 用通式为R 4 -OR-CO 2 H的羧酸进行化学式6的化合物的酰胺化反应的步骤。 用于预防或治疗皮肤癌的药物组合物含有化学式1的氨基喹啉化合物或其药学上可接受的盐作为活性成分。

    단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
    8.
    发明公开
    단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 有权
    具有蛋白激酶抑制活性的1,3,6-取代的吲哚衍生物

    公开(公告)号：KR1020110019584A

    公开(公告)日：2011-02-28

    申请号：KR1020090077185

    申请日：2009-08-20

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  함영진 ,  유경호 ,  오창현 ,  하정미 ,  김환 ,  최환근 ,  이정헌

    IPC: C07D209/04 ,  C07D403/04 ,  A61K31/40 ,  A61P29/00

    CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

    Abstract: PURPOSE: A 1,3,6-substituted indole compound having an activity of suppressing protein kinase is provided to suppress various protein kinases and to prevent and treat abnormal cell growth diseases. CONSTITUTION: A 1,3,6-substituted indole compound is denoted by chemical formula 1. A pharmaceutical composition contains 1,3,6-substituted indole compound of chemical formula 1 as an active ingredient. The pharmaceutical composition prevents and treats abnormal cell growth diseases through protein kinase suppression mechanism selected from Raf, KDR, Fms, Tie2, SAPK2a, Ret, Abl, Abl(T315I), ALK, Aurora A, Bmx, CDK/cyclinE, Kit, Src, EGFR, EphA1, FGFR3, Flt3, Fms, IGF-1R, IKKb, IR, Itk, JAK2, KDR, Met, mTOR, PDGFRa, Plk1, Ret, Syk, Tie2, and TrtB. An agent for preventing and treating tumor contains 1,3,6-substituted indole compound of chemical formula 1.

    Abstract translation: 目的：提供具有抑制蛋白激酶活性的1,3,6-取代的吲哚化合物以抑制各种蛋白激酶并预防和治疗异常的细胞生长疾病。 构成：1,3,6-取代的吲哚化合物由化学式1表示。药物组合物含有化学式1的1,3,6-取代的吲哚化合物作为活性成分。 药物组合物通过选自Raf，KDR，Fms，Tie2，SAPK2a，Ret，Abl，Abl（T315I），ALK，Aurora A，Bmx，CDK / cyclinE，Kit，Src的蛋白激酶抑制机制预防和治疗异常细胞生长疾病 ，EGFR，EphA1，FGFR3，Flt3，Fms，IGF-1R，IKKb，IR，Itk，JAK2，KDR，Met，mTOR，PDGFRa，Plk1，Ret，Syk，Tie2和TrtB。 用于预防和治疗肿瘤的药物含有化学式1的1,3,6-取代的吲哚化合物。

    신규 피롤로[3,2-ｂ]피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종 예방 또는 치료용 약학적 조성물
    9.
    发明公开
    신규 피롤로[3,2-ｂ]피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 흑색종 예방 또는 치료용 약학적 조성물 失效
    新型吡咯并[3,2-B]吡啶衍生物或其药学上可接受的盐，其制备方法和药物组合物，用于预防或治疗含有作为活性成分的梅毒

    公开(公告)号：KR1020100047998A

    公开(公告)日：2010-05-11

    申请号：KR1020080106962

    申请日：2008-10-30

    Applicant: 한국과학기술연구원

    Inventor： 오창현 ,  유경호 ,  심태보 ,  이소하 ,  하정미 ,  김희진 ,  정명호

    IPC: C07D487/04

    Abstract: PURPOSE: A novel pyrollo[3,2-b]pyridine derivative and a pharmaceutical composition for preventing or treating melanoma containing the same are provided to ensure high anti-proliferative activity to melanoma cells. CONSTITUTION: A pyrollo(3,2-b)pyridine derivative is denoted by chemical formula 1. A method for preparing the pirrolo(3,2,-b)pyridine derivative comprises: a step of coupling 1-iodine-4-nitrobenze to a compound of chemical formula 2 to obtain a compound of chemical formula 3; a step of reducing the compound of chemical formula 3 to obtain a compound of chemical formula 4; and a step of coupling the compound of chemical formula 4 with a phenylcarboxylic acid or amine derivative which trifluoromethyl, halogen, morpholine, piperazine. A pharmaceutical composition for preventing or treating melanoma contains the pyrollo(3,2-b)pyridine derivative or pharmaceutically acceptable salt as an active ingredient.

    Abstract translation: 目的：提供一种新型的吡咯并[3,2-b]吡啶衍生物和用于预防或治疗含有此类黑色素瘤的药物组合物，以确保对黑素瘤细胞的高抗增殖活性。 构成：吡咯（3,2-b）吡啶衍生物由化学式1表示。制备吡罗咯（3,2，-b）吡啶衍生物的方法包括：将1-碘-4-硝基苯偶联到 化学式2的化合物，得到化学式3的化合物; 还原化学式3的化合物以获得化学式4的化合物的步骤; 以及将化学式4的化合物与三氟甲基，卤素，吗啉，哌嗪的苯基羧酸或胺衍生物偶合的步骤。 用于预防或治疗黑素瘤的药物组合物含有吡罗洛（3,2-b）吡啶衍生物或其药学上可接受的盐作为活性成分。

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