公开(公告)号：KR101704386B1

公开(公告)日：2017-02-08

申请号：KR1020130075122

申请日：2013-06-28

Applicant: 한국과학기술연구원

Inventor： 심태보 ,  김환 ,  윤호종

IPC: A61K31/519 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00 ,  A61K47/00

Abstract: 본발명은단백질키나아제의 Bcr-Abl 유전자에서발생하는점돌연변이종에대한저해활성을가지고있는티에노[3,2]피리미딘유도체가활성성분으로포함된글리벡내성항암제에관한것이다.

Abstract translation: 本发明涉及具有对作为蛋白质的激酶Bcr-Abl portein产生的点突变种具有抑制活性的噻吩并[3,2-d]嘧啶衍生物的格列维克耐受性抗癌剂。 本发明的Gleevec耐受性抗癌剂包含选自由化学式1表示的噻吩并[3,2-d]嘧啶衍生物及其药学上可接受的盐，水合物和溶剂合物作为活性成分的化合物。 在化学式1中，格列卫是第一种靶向抗癌剂，广泛用于治疗慢性骨髓性白血病。

公开(公告)号：KR101123071B1

公开(公告)日：2012-03-05

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: (상기화학식 1에서, R및 R는본 명세서에서정의된바와같다.)

公开(公告)号：KR1020110114194A

公开(公告)日：2011-10-19

申请号：KR1020100033695

申请日：2010-04-13

Applicant: 한국과학기술연구원

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

IPC: C07D231/40 ,  C07D231/02 ,  A61K31/415 ,  A61P35/00

Abstract: 본 발명은 하기 신규 아미노피라졸 아릴아마이드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 비정상 세포 성장 질환의 예방 및 치료용 약학적 조성물에 관한 것으로, 본 발명에 따르면 비정상 세포 성장 질환을 유발하는 다양한 단백질 카이네이즈, 예를 들면 ABL1, B-RAF, c-Kit, FMS, LCK, LYN, P38α 및 C-RAF에 대하여 우수한 억제효과를 나타내므로, 비정상 세포 성장 질환의 예방 및 치료에 유용하게 사용될 수 있다.

公开(公告)号：KR1020110088960A

公开(公告)日：2011-08-04

申请号：KR1020100008720

申请日：2010-01-29

Applicant: 한미약품 주식회사 ,  한국과학기술연구원

Inventor： 정승현 ,  정영희 ,  최화일 ,  손정범 ,  전은주 ,  양인호 ,  송태헌 ,  이미경 ,  고명실 ,  안영길 ,  김맹섭 ,  함영진 ,  심태보 ,  최환근 ,  하정미 ,  박동식 ,  김환

IPC: C07D487/04 ,  C07D495/04 ,  A61K31/519 ,  A61P43/00

CPC classification number: C07D495/04

Abstract: PURPOSE: A bicyclic derivative having an activity of suppressing protein kinase is provided to prevent and treat abnormal cell growth diseases. CONSTITUTION: A bicyclic heteroaryl derivative with an activity of suppressing protein kinase has a structure of chemical formula 1. A pharmaceutical composition for preventing and treating abnormal cell growth disease due to excessive activation of protein kinase contains the compound of chemical formula 1 as an active ingredient.

Abstract translation: 目的：提供具有抑制蛋白激酶活性的双环衍生物，以预防和治疗异常细胞生长疾病。 构成：具有抑制蛋白激酶活性的双环杂芳基衍生物具有化学式1的结构。用于预防和治疗由蛋白激酶过度激活引起的异常细胞生长疾病的药物组合物含有化学式1的化合物作为活性成分 。

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。

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。

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。

公开(公告)号：KR1020140069421A

公开(公告)日：2014-06-10

申请号：KR1020120136617

申请日：2012-11-29

Applicant: 한국과학기술연구원

Inventor： 심태보 ,  김환

IPC: A61K31/13 ,  A61K31/136 ,  A61P35/00

CPC classification number: A61K31/136

Abstract: The present invention relates to a methyl violet derivative used as an antitumor agent by inhibiting activity of allosteric focal adhesion kinase (FAK). The methyl violet derivative can be used as an active ingredient of a pharmaceutical composition for preventing or treating various cancer diseases by having the FAC inhibitory activity.

Abstract translation: 本发明涉及通过抑制变构粘着斑激酶（FAK）的活性而用作抗肿瘤剂的甲基紫衍生物。 甲基紫衍生物可以用作通过具有FAC抑制活性来预防或治疗各种癌症疾病的药物组合物的活性成分。

公开(公告)号：KR101347303B1

公开(公告)日：2014-01-06

申请号：KR1020110009687

申请日：2011-01-31

Applicant: 한미사이언스 주식회사 ,  한국과학기술연구원 ,  가톨릭대학교 산학협력단

Inventor： 손정범 ,  정승현 ,  최화일 ,  정영희 ,  최재율 ,  송지연 ,  이규항 ,  이재철 ,  김은영 ,  안영길 ,  김맹섭 ,  최환근 ,  심태보 ,  함영진 ,  박동식 ,  김환 ,  김동욱

IPC: C07D495/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D495/04

Abstract: 본 발명에 따르는 신규한 티에노[3,2-d]피리미딘 유도체, 이의 약학적으로 허용가능한 염, 수화물 또는 용매화물은 단백질 키나아제에 대한 저해 활성이 우수하며, 이를 포함하는 약학적 조성물은 비정상 세포 성장 질환의 예방제 또는 치료제로서 효과가 우수하다.

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.