公开(公告)号：KR101147550B1

公开(公告)日：2012-05-17

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: Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.

公开(公告)号：KR1020120040980A

公开(公告)日：2012-04-30

申请号：KR1020100102522

申请日：2010-10-20

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  정명호 ,  엘가말모하메드 ,  유경호 ,  심태보 ,  최원경 ,  조정혁

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: PURPOSE: A pyrrolo[3,2-c]pyridine derivative and a pharmaceutical composition containing the same are provided to ensure anti-proliferatioin activity of melanoma and to prevent or treat melanoma. CONSTITUTION: A pyrrolo[3,2-c]pyridine derivative is denoted by chemical formula I. A method for preparing the pyrrolo[3,2-c]pyridine derivative of chemical formula I' or pharmaceutically acceptable salt thereof comprises: a step of reacting 4-chloro-1-pyrrolo[2,3-b]pyridine of chemical formula II with nitroaniline to prepare a compound of chemical formula III; a step of reacting a compound of chemical formula III with benzoyl chloride to prepare a compound of chemical formula IV; a step of reducing the compound of chemical formula IV to prepare a compound of chemical formula V; and a step of reacting the compound of chemical formula V with a compound of chemical formula VI or formula VII.

Abstract translation: 目的：提供吡咯并[3,2-c]吡啶衍生物和含有它们的药物组合物，以确保黑色素瘤的抗增殖活性并预防或治疗黑素瘤。 构成：化学式I表示吡咯并[3,2-c]吡啶衍生物。制备化学式I'吡咯并[3,2-c]吡啶衍生物或其药学上可接受的盐的方法包括： 使化学式II的4-氯-1-吡咯并[2,3-b]吡啶与硝基苯胺反应制备化学式Ⅲ化合物; 使化学式III的化合物与苯甲酰氯反应以制备化学式IV的化合物的步骤; 降低化学式IV化合物以制备化学式V的化合物的步骤; 以及使化学式V的化合物与化学式VI或式VII的化合物反应的步骤。

公开(公告)号：KR101083421B1

公开(公告)日：2011-11-14

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: (상기화학식 1에서, R, R, R, R및 R는본 명세서에서정의된바와같다)

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。

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。