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：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：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：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：KR1020100004797A

公开(公告)日：2010-01-13

申请号：KR1020080065147

申请日：2008-07-04

Applicant: 한국과학기술연구원

Inventor： 김창삼 ,  정경윤 ,  황성익 ,  이정헌 ,  신호철

IPC: H01M4/04 ,  H01M4/48 ,  H01M4/58 ,  C01B25/26

CPC classification number: H01M4/366 ,  C01B25/375 ,  H01M4/5825 ,  H01M4/583 ,  H01M4/624 ,  H01M2004/028 ,  Y02E60/122

Abstract: PURPOSE: A method for manufacturing olivine-type positive electrode powder is provided to improve electric conductivity of a positive active material powder and to effectively control the growth of particles during thermal treatment of the active material. CONSTITUTION: A method for manufacturing a LiFePO4 compound of an olivine structure comprises the steps of: (i) mixing a lithium compound, iron compound and phosphorus compound, and heat-treating the mixture to prepare precursor powder; (ii) impregnating carbon source in the powder and drying the impregnated powder; (iii) dry milling the dried powder; and (iv) heat-treating the powder in an inactivation or reducing atmosphere.

Abstract translation: 目的：提供橄榄石型正极粉末的制造方法，以提高正极活性物质粉末的导电性，并有效控制活性物质热处理过程中颗粒的生长。 构成：一种橄榄石结构的LiFePO 4化合物的制造方法，其特征在于，包括：（i）将锂化合物，铁化合物与磷化合物混合，对该混合物进行热处理，制备前体粉末; （ii）将碳源浸渍在粉末中并干燥浸渍的粉末; （iii）将干粉干燥研磨; 和（iv）在灭活或还原气氛中对粉末进行热处理。

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