公开(公告)号：KR101733733B1

公开(公告)日：2017-05-11

申请号：KR1020150071257

申请日：2015-05-21

Applicant: 한국화학연구원

Inventor： 윤창수 ,  김형래 ,  조성윤 ,  정희정 ,  이광호 ,  채종학 ,  이정옥 ,  박지훈 ,  김필호 ,  황종연 ,  하재두 ,  안선주

IPC: C07D403/12 ,  C07D209/04 ,  C07D239/12 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/506 ,  C07D209/04 ,  C07D239/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

Abstract: 본발명은피리미딘-2,4-디아민유도체또는이의약학적으로허용가능한염 및이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에의한화합물은역형성림프종키나아제(ALK) 활성을억제하는효과가우수하므로이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가향상될수 있으며, 암의재발을막는데효과적일것으로예상되므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.

Abstract translation: 本发明涉及用于预防或治疗嘧啶-2,4-二胺衍生物或其药学上可接受的盐的药物组合物以及含有该化合物作为有效成分的癌症，本发明的化合物用于治疗反向淋巴瘤激酶 （ALK）融合蛋白在抑制癌症复发方面是有效的，因此可以提高具有淋巴瘤激酶（ALK）融合蛋白如EML4-ALK和NPM-ALK的癌细胞的治疗效果 因此可以有效地用作预防或治疗癌症的药物组合物。

公开(公告)号：KR1020160123231A

公开(公告)日：2016-10-25

申请号：KR1020160041920

申请日：2016-04-05

Applicant: 한국화학연구원

Inventor： 김필호 ,  김형래 ,  조성윤 ,  하재두 ,  정희정 ,  윤창수 ,  황종연 ,  박지훈 ,  이정옥 ,  안선주 ,  채종학

IPC: C07D239/48 ,  A61K31/505 ,  A23L1/30

CPC classification number: C07D239/48 ,  A23L33/10 ,  A23L33/30 ,  A23L33/40 ,  A23V2002/00 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12

Abstract: 본발명은 N2-(2-메톡시페닐)피리미딘유도체, 이의제조방법및 이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에따른 N2-(2-메톡시페닐)피리미딘유도체, 이의광학이성질체, 또는이의약학적으로허용가능한염은역형성림프종키나아제(ALK)를억제하는활성이우수해, 이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가우수하므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.

公开(公告)号：KR1020150104748A

公开(公告)日：2015-09-16

申请号：KR1020140026462

申请日：2014-03-06

Applicant: 한국화학연구원

Inventor： 이광호 ,  김형래 ,  조성윤 ,  정희정 ,  이정옥 ,  채종학 ,  박지훈 ,  윤창수 ,  김필호 ,  라티프무하마드 ,  황종연 ,  하재두

IPC: C07D403/04 ,  A61K31/506 ,  A61P35/00

Abstract: 본 발명은 피페리딘-3,5-디카복시아마이드 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 의한 화합물은 역형성 림프종 키나아제(ALK) 활성을 억제하는 효과가 우수하므로 이에 따른 EML4-ALK, NPM-ALK 등의 역형성 림프종 키나아제(ALK) 융합 단백질을 가진 암세포에 대한 치료효과가 향상될 수 있으며, 암의 재발을 막는데 효과적일 것으로 예상되므로 암의 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.

Abstract translation: 本发明涉及哌啶-3,5-二甲酰胺衍生物或其药学上可接受的盐，以及用于预防或治疗含有其作为活性成分的癌症的药物组合物。 根据本发明的化合物显示出抑制间变性淋巴瘤激酶（ALK）的优异效果，结果可以提高对具有间变性淋巴瘤激酶（ALK）融合蛋白（例如EML4-ALK）的癌细胞的治疗效果，以及 NPM-ALK。 此外，化合物可用于预防或治疗癌症的药物组合物，因为预期有效地预防癌症复发。

公开(公告)号：KR101245559B1

公开(公告)日：2013-03-22

申请号：KR1020120070944

申请日：2012-06-29

Applicant: 한국화학연구원

Inventor： 김형래 ,  이정옥 ,  류재욱 ,  하재두 ,  조성윤 ,  정희정 ,  한선영 ,  이종국

IPC: C07D413/14 ,  A61K31/423 ,  A61K31/4427 ,  A61P35/00

Abstract: 본 발명은 하기 화학식 1로 표시되는 신규 다중치환 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 이상세포 성장 질환의 예방 및 치료용 약학적 조성물에 관한 것으로, 본 발명에 따르면 이상 세포 성장질환의 치료에 유용한 다양한 단백질 키나아제, 예를 들면 c-Met, Ron, KDR, Lck, Flt1, Flt3, Tie2, TrkA, TrkB, b-Raf, Aurora-A 등에 대하여 우수한 억제효과를 나타내므로, 이상 세포 성장 질환의 예방 및 치료에 유용하게 사용될 수 있다.
[화학식 1]

(상기 화학식 1에서, R
1 ~R
4 는 본 명세서에서 정의된 바와 같다.)

公开(公告)号：KR101109122B1

公开(公告)日：2012-06-12

申请号：KR1020090105096

申请日：2009-11-02

Applicant: 한국화학연구원

Inventor： 정희정 ,  이철해 ,  김재학 ,  정원장 ,  김비치 ,  박선필

IPC: C07C239/14 ,  C07C231/14 ,  A61K31/165 ,  A61P35/00

Abstract: PURPOSE: A 6-amido-n-hydroxyhexanamide compound is provided to selectively induce the terminal differentiation of tumor cell by effectively inhibiting enzyme activity of histone deacetylase, and to inhibit the proliferation of tumor cell. CONSTITUTION: A compound is selected from a 6-amido-n-hydroxyhexanamide compound represented by chemical formula 1 and pharmaceutically acceptable salts thereof. In chemical formula 1, X is selected from a single bond or the group of C1-6 alkylenyl; R is amino, C1-6 alkylamino, di(C1-6 alkyl)amino, 5-9-membered aryl, 5-9-membered aryl C1-6 alkyl, 5-9-membered aryl C1-6 alkyloxy, 5-9-membered heteroaryl including 1-3 hetero atoms selected from N and O, and 5-7-membered heterocycloalkyl including 1-3 hetero atoms selected from N and O.

公开(公告)号：KR1020120046505A

公开(公告)日：2012-05-10

申请号：KR1020100108192

申请日：2010-11-02

Applicant: 한국화학연구원

Inventor： 김형래 ,  류재욱 ,  이종국 ,  하재두 ,  조성윤 ,  이정옥 ,  한선영 ,  정희정

IPC: C07D487/04 ,  A61K31/5025 ,  A61P35/00

Abstract: PURPOSE: A pharmaceutical composition containing a novel methyl isoquinolinone-substituted triazolopyridazine derivative and a pharmaceutical composition containing the same are provided to prevent or treat abnormal cell growth diseases. CONSTITUTION: A method for preparing a methyl isoquinolinone-substituted triazolopyridazine derivative or pharmaceutically acceptable salt thereof comprises: a step of performing heck reaction of a compound of chemical formula 2 and a compound of chemical formula 3 to prepare a compound of chemical formula 4; a step of coupling the compound of chemical formula 4 with a compound of chemical formula 5 to prepare a compound of chemical formula 6; a step of cyclizing the compound of chemical formula 6 to prepare a compound of chemical formula 7; a step of substituting the compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of performing azidation of the compound of chemical formula 8 to prepare a compound of chemical formula 9; a step of cyclizing the compound of chemical formula 9 to prepare a compound of chemical formula 10; a step of performing Suzuki coupling reaction of the compound of chemical formula 10 to prepare a compound of chemical formula 1A.

Abstract translation: 目的：提供含有新的甲基异喹啉酮取代的三唑并哒嗪衍生物的药物组合物和含有它们的药物组合物，以预防或治疗异常的细胞生长疾病。 构成：制备甲基异喹啉酮取代的三唑并哒嗪衍生物或其药学上可接受的盐的方法包括：化学式2的化合物与化学式3的化合物进行反应以制备化学式4化合物的步骤; 将化学式4的化合物与化学式5的化合物偶联以制备化学式6的化合物的步骤; 使化学式6的化合物环化以制备化学式7的化合物的步骤; 用化学式7的化合物代替化学式8的化合物的步骤; 进行化学式8的化合物的叠氮化以制备化学式9的化合物的步骤; 使化学式9的化合物环化以制备化学式10的化合物的步骤; 进行化学式10的化合物的Suzuki偶联反应以制备化学式1A的化合物的步骤。

公开(公告)号：KR101117129B1

公开(公告)日：2012-02-24

申请号：KR1020090086575

申请日：2009-09-14

Applicant: 한국화학연구원

Inventor： 최상운 ,  안진희 ,  김광록 ,  정희정 ,  강승규 ,  김성수

IPC: C07D241/36 ,  C07D241/44 ,  A61K31/495 ,  A61P25/28

Abstract: 본 발명은 하기 화학식 1의 신규한 퀴녹살린 유도체 및 이를 포함하는 줄기세포의 신경세포로의 분화유도용 조성물에 관한 것으로, 본 발명에 따른 퀴녹살린 유도체는 신경 손상 질환의 치료에 효과적으로 사용될 수 있다:


퀴녹살린 유도체, 줄기세포, 신경세포, 분화

公开(公告)号：KR1020110033395A

公开(公告)日：2011-03-31

申请号：KR1020090090879

申请日：2009-09-25

Applicant: 한국화학연구원

Inventor： 김형래 ,  이정옥 ,  류재욱 ,  하재두 ,  조성윤 ,  정희정 ,  한선영 ,  이종국

IPC: C07D403/14 ,  C07D401/14 ,  A61K31/44 ,  A61P35/00

Abstract: PURPOSE: A novel multiple substituted-benzoxazole-substituted pyridine derivative is provided to suppress c-Met, Ron, KDR, Lck, Flt1, Flt3, Tie2, TrkA, TrkB, b-Raf, and Aurora-A and to prevent and treating abnormal cell growth diseases. CONSTITUTION: A multiple substituted-benzoxazole-substituted pyridine derivative is denoted by chemical formula 1. A method for preparing the pyridine derivative or pharmaceutically acceptable salt thereof comprises: a step of substituting a compound of chemical formula 2 to prepare a compound of chemical formula 4; a step of cyclizing the compound of chemical formula 4 to obtain a compound of chemical formula 5; a step of substituting amine compound with the compound of chemical formula 5 to obtain a compound of chemical formula 6; a step of performing Suzuki coupling reaction of the compound of chemical formula 6 with a compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of hydrogenating the compound of chemical formula 8 to obtain a compound of chemical formula 9; a step of adding the compound of chemical formula 9 with a compound of chemical formula 10 to obtain a compound of chemical formula 11; and a step of deprotecting the compound of chemical formula 11 to obtain a compound of chemical formula 1a.

Abstract translation: 目的：提供一种新的多取代苯并恶唑取代的吡啶衍生物，以抑制c-Met，Ron，KDR，Lck，Flt1，Flt3，Tie2，TrkA，TrkB，b-Raf和Aurora-A，并预防和治疗异常 细胞生长疾病。 构成：化学式1表示多取代苯并恶唑取代的吡啶衍生物。制备吡啶衍生物或其药学上可接受的盐的方法包括：用化学式2的化合物代替化学式4的化合物 ; 环化化学式4的化合物以获得化学式5的化合物的步骤; 用化学式5的化合物代替胺化合物以获得化学式6化合物的步骤; 化学式6的化合物与化学式7的化合物进行Suzuki偶联反应以制备化学式8的化合物的步骤; 氢化化学式8的化合物以获得化学式9的化合物的步骤; 将化学式9的化合物与化学式10化合物相加的步骤，得到化学式11的化合物; 和使化学式11的化合物脱保护以获得化学式1a的化合物的步骤。

公开(公告)号：KR1020110028932A

公开(公告)日：2011-03-22

申请号：KR1020090086575

申请日：2009-09-14

Applicant: 한국화학연구원

Inventor： 최상운 ,  안진희 ,  김광록 ,  정희정 ,  강승규 ,  김성수

IPC: C07D241/36 ,  C07D241/44 ,  A61K31/495 ,  A61P25/28

Abstract: PURPOSE: A composition containing a novel quinoxaline derivative for inducing stem cells to nerve cells is provided to treat nerve damage including stroke, Alzheimer's disease, Parkinson's disease, and spiral injury. CONSTITUTION: A novel quinoxaline derivative is denoted by chemical formula 1. A composition for inducing stem cells to nerve cells contains 0.1-100 uM of quinoxaline derivative or salt thereof as an active ingredient. The stem cells are embryonic stem cells, adult stem cells, or embryonic carcinoma stem cells. A pharmaceutical composition for treating nerve damage contains the quinoxaline derivative or salt thereof as an active ingredient. The nerve damage includes stroke, Alzheimer's disease, Parkinson's disease, spinal cord injury disease, or dementia.

Abstract translation: 目的：提供含有用于诱导神经细胞干细胞的新型喹喔啉衍生物的组合物，用于治疗神经损伤，包括中风，阿尔茨海默病，帕金森病和螺旋损伤。 构成：一种新颖的喹喔啉衍生物由化学式1表示。用于向神经细胞诱导干细胞的组合物含有0.1-100μM的喹喔啉衍生物或其盐作为活性成分。 干细胞是胚胎干细胞，成体干细胞或胚胎干细胞。 用于治疗神经损伤的药物组合物含有喹喔啉衍生物或其盐作为活性成分。 神经损伤包括中风，阿尔茨海默病，帕金森病，脊髓损伤疾病或痴呆。

公开(公告)号：KR1020090055455A

公开(公告)日：2009-06-02

申请号：KR1020080030876

申请日：2008-04-02

Applicant: 한국화학연구원

Inventor： 김문석 ,  안현희 ,  조미희 ,  정희정 ,  이해방 ,  이정화

IPC: C12N5/071 ,  C12N5/02 ,  C12N5/00

Abstract: A method for differentiating an adult stem cell to a nerve cell using a small molecule compound is provided to treat central nervous disease such as Parkinson disease, dementia, alzheimer disease, and spinal cord injury. An adult stem cell is differentiated to a nerve cell using a small molecule compound as an inducer. The adult stem cell is derived from a bone marrow, skeletal muscle or adipose tissue. A small compound is a histon deacetylase inhibitor and comprises alkylthiobenximidazole compound, benzhydroxyamide compound, quinozaline hydrozamide compound, or acylaminomethyl hydroximide. A composition for treating the nerve disease comprises a differentiated nerve cell using the inducer. The nerve disease is Parkinson disease, dementia, Alzheimer disease, or spinal cord injury.

Abstract translation: 提供使用小分子化合物将成体干细胞分化为神经细胞的方法，用于治疗中枢神经疾病如帕金森病，痴呆，阿尔茨海默病和脊髓损伤。 使用小分子化合物作为诱导剂将成体干细胞分化成神经细胞。 成体干细胞衍生自骨髓，骨骼肌或脂肪组织。 一种小化合物是一种组蛋白脱乙酰酶抑制剂，它包括烷基硫代噻肟化合物，苯甲酰胺化合物，喹喔啉氢化物酰胺化合物或酰氨基甲基氢化物。 用于治疗神经疾病的组合物包括使用诱导剂的分化神经细胞。 神经疾病是帕金森病，痴呆，阿尔茨海默病或脊髓损伤。