公开(公告)号：KR102129367B1

公开(公告)日：2020-07-03

申请号：KR1020180119161

申请日：2018-10-05

Applicant: 한국화학연구원 ,  한국생명공학연구원

Inventor： 황종연 ,  하재두 ,  조성윤 ,  김필호 ,  박병철 ,  김선홍 ,  김정훈 ,  박성구

IPC: C07D417/14 ,  A61K31/4035 ,  A61K31/454 ,  C07D401/14

公开(公告)号：KR101825065B1

公开(公告)日：2018-02-05

申请号：KR1020160063391

申请日：2016-05-24

Applicant: 한국화학연구원

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

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  A61K31/506 ,  A61K31/4035

CPC classification number: A61K31/4035 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

Abstract: ALK 단백질의분해를유도하는약물의제조방법및 이를유효성분으로합유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에따른화학식 1로표시되는화합물은역형성림프종키나제(ALK)를억제하거나분해시킬수 있어, 역형성림프종키나제(ALK) 관련질환, 예를들어암의예방및 치료에유용한효과가있다.

Abstract translation: 相关的是用于制备诱导ALK蛋白分解的药物的方法，以及用于癌症预防或治疗并包含其作为活性成分的药物组合物。 根据本发明的由化学式1表示的化合物可以抑制或分解间变性淋巴瘤激酶（ALK），因此对于预防或治疗诸如癌症的间变性淋巴瘤激酶相关疾病具有有用的效果。

公开(公告)号：KR1020170027757A

公开(公告)日：2017-03-10

申请号：KR1020170025934

申请日：2017-02-28

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: 本发明涉及嘧啶-2,4-二胺衍生物或其药学上可接受的盐，以及用于预防或治疗癌症的药物组合物，其包含其作为有效成分。 根据本发明的化合物具有抑制间变性淋巴瘤激酶（ALK）活性的良好效果，从而对具有间变性淋巴瘤激酶（ALK）融合蛋白如EML4-ALK，NPM-ALK等的癌细胞具有治疗作用 可以加强，预计会有效地抑制癌症复发。 因此，该化合物可以有效地用于预防或治疗癌症的药物组合物中。

公开(公告)号：KR101577430B1

公开(公告)日：2015-12-14

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: 본발명은피페리딘-3,5-디카복시아마이드유도체또는이의약학적으로허용가능한염 및이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에의한화합물은역형성림프종키나아제(ALK) 활성을억제하는효과가우수하므로이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가향상될수 있으며, 암의재발을막는데효과적일것으로예상되므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.

公开(公告)号：KR1020130115470A

公开(公告)日：2013-10-22

申请号：KR1020120037775

申请日：2012-04-12

Applicant: 한국화학연구원 ,  주식회사 한독

Inventor： 정희정 ,  하재두 ,  조성윤 ,  김형래 ,  이광호 ,  최상운 ,  박지훈 ,  이정옥

IPC: C07D413/14 ,  C07D413/04 ,  A61K31/5377 ,  A61P35/00

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: PURPOSE: A novel hydrazinone-substituted pyrimidine derivative is provided to effectively suppress the activation of c-Met tyrosine kinase, thereby being used as a therapeutic agent for treating various hyperpoliferative disorders related to hyperproliferation and overgrowth of cells. CONSTITUTION: A hydrazinone-substituted pyrimidine derivative of chemical formula 1 or a pharmaceutically acceptable salt thereof is provided. A pharmaceutical composition for suppressing the activation of c-Met tyrosine kinase contains the pyrimidine derivative or a pharmaceutically acceptable salt or a solvate thereof as an active ingredient. A pharmaceutical composition for preventing or treating hyperproliferative disorders contains the pyrimidine derivative or a pharmaceutically acceptable salt or a solvate thereof as an active ingredient.

Abstract translation: 目的：提供一种新的肼取代嘧啶衍生物，以有效抑制c-Met酪氨酸激酶的活化，从而用作治疗与过度增殖和细胞过度生长有关的各种超增生障碍的治疗剂。 构成：提供化学式1的肼酮取代的嘧啶衍生物或其药学上可接受的盐。 用于抑制c-Met酪氨酸激酶活化的药物组合物含有嘧啶衍生物或其药学上可接受的盐或溶剂化物作为活性成分。 用于预防或治疗过度增殖性疾病的药物组合物含有嘧啶衍生物或其药学上可接受的盐或溶剂化物作为活性成分。

公开(公告)号：KR101242571B1

公开(公告)日：2013-03-20

申请号：KR1020100114874

申请日：2010-11-18

Applicant: 한국화학연구원

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

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

Abstract: 본 발명은 하기 화학식 1로 표시되는 티에노피리미딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 비정상 세포 성장 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 따르면 비정상 세포 성장 질환의 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, 비정상 세포 성장 질환의 예방 또는 치료에 유용하게 사용될 수 있다.
[화학식 1]

(상기 화학식 1에서, R
1 , R
2
, R
3 , R
4 , X 및 n은 본 명세서에서 정의된 바와 같다.)

公开(公告)号：KR1020120100845A

公开(公告)日：2012-09-12

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: PURPOSE: A pharmaceutical composition containing pyridine derivative subsituted with multiple substituted benzoxazole is provided to prevent and treat abnormal cell growth diseases. CONSTITUTION: A pyridine derivative substituted with multiple substituted benzoxazole is denoted by chemical formula 1. A method for preparing the 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 prepare a compound of chemical formula 5; a step of substituting the compound of chemical formula 5 to prepare a compound of chemical formula 6; a step of 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 hydrogenation of the compound of chemical formula 8 to prepare a compound of chemical formula 9; a step of addition reaction of the compound of chemical formula 9 with a compound of chemical formula 10 to prepare a compound of chemical formula 11; and a step of deprotecting the compound of chemical formula 11.

Abstract translation: 目的：提供含有由多取代苯并恶唑取代的吡啶衍生物的药物组合物，以预防和治疗异常的细胞生长疾病。 构成：用多取代的苯并恶唑取代的吡啶衍生物由化学式1表示。制备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化合物的步骤; 使化学式4的化合物环化以制备化学式5的化合物的步骤; 用化学式5的化合物代替化学式6化合物的步骤; 化学式6的化合物与化学式7化合物的Suzuki偶联反应步骤，制备化学式8的化合物; 化学式8的化合物的氢化步骤，以制备化学式9的化合物; 化学式9的化合物与化学式10的化合物的加成反应步骤，制备化学式11的化合物; 以及使化学式11的化合物脱保护的工序。

公开(公告)号：KR1020110006173A

公开(公告)日：2011-01-20

申请号：KR1020090063681

申请日：2009-07-13

Applicant: 한국화학연구원

Inventor： 한선영 ,  하재두

IPC: C07D333/58 ,  C07D333/54

Abstract: PURPOSE: A method for preparing a novel benzothiophene compound is provided to suppress tyrosine kinase and to treat abnormal cell growth diseases. CONSTITUTION: A benxothiophene is denoted by chemical formula 1. A method for preparing the benzothiophene compound comprises: a step of hydrolyzing est compound of chemical formula 1-a to obtain an acid compound of chemical formula 1-b; and a step of reacting the acid compound of chemical formula 1-b with diphenylphosphorylazide(DPPA) under the presence of base and binding with an amine compound(NHR10R11) to obtain urea compound of chemical formula 1-c. A pharmaceutical composition for treating tumor, psoriasis, rheumatism, and diabetic retinosis contains the compound of chemciail formula 1. The pharmaceutical composition is used in the form of oral administration, injection, tablet, capsule, or powder.

Abstract translation: 目的：提供一种制备新型苯并噻吩化合物的方法，以抑制酪氨酸激酶和治疗异常的细胞生长疾病。 构成：苯噻吩由化学式1表示。制备苯并噻吩化合物的方法包括：水解化学式1-a的化合物的步骤，得到化学式1-b的酸化合物; 和在碱存在下使化学式1-b的酸化合物与二苯基磷酰基叠氮化物（DPPA）反应并与胺化合物（NHR 10 R 11）结合的步骤，得到化学式1-c的脲化合物。 用于治疗肿瘤，牛皮癣，风湿病和糖尿病性视网膜病变的药物组合物含有化学式1化合物。药物组合物以口服给药，注射，片剂，胶囊或粉末的形式使用。

公开(公告)号：KR1020110006171A

公开(公告)日：2011-01-20

申请号：KR1020090063679

申请日：2009-07-13

Applicant: 한국화학연구원

Inventor： 하재두 ,  한선영 ,  조성윤 ,  이종국 ,  이정옥 ,  김형래 ,  최상운

IPC: C07D403/04 ,  C07D403/02 ,  C07D487/04 ,  C07D487/02

Abstract: PURPOSE: A tetrahydroimidazopyridine group-substituted novel quinolinone compound is provided to suppress vascular endothelial growth factor receptor(VEGFR) and flit 3(Flt3) and to treat abnormal cell growth diseases. CONSTITUTION: A tetrahydroimidazopyridine group-substituted quinolinone compound is denoted by chemical formula 1. The compound of chemical formula 1 is obtained by binding (4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-2-yl)-acetic acid ethyl est compound of chemical formula 3 with 2-aminobenzaldehyde compound of chemical formula 2 under the presence of tertiary amine base. A pharmaceutical composition for treating tumor, psoriasis, rheumatism, diabetic retinosis contains the compound of chemical formula 1. The pharmaceutical composition is used in the form of oral administration or injection. The pharmaceutical composition is also used in the form of tablet, capsule, or powder. A therapeutic agent for psoriasis contains the compound of chemical formula 1.

Abstract translation: 目的：提供四氢咪唑并吡啶基取代的新型喹啉酮化合物，以抑制血管内皮生长因子受体（VEGFR）和flit 3（Flt3），并治疗异常细胞生长疾病。 组成：化学式1表示四氢咪唑并吡啶基取代的喹啉酮化合物。化学式1化合物是通过将（4,5,6,7-四氢-1H-咪唑并[4,5-c]吡啶-2 - 基） - 乙酸乙酯，化学式3化合物与化学式2的2-氨基苯甲醛化合物在叔胺碱存在下反应。 用于治疗肿瘤，牛皮癣，风湿病，糖尿病性视网膜病变的药物组合物含有化学式1的化合物。药物组合物以口服给药或注射的形式使用。 药物组合物也以片剂，胶囊剂或粉剂的形式使用。 牛皮癣治疗剂含有化学式1的化合物。

公开(公告)号：KR1020090107807A

公开(公告)日：2009-10-14

申请号：KR1020080033282

申请日：2008-04-10

Applicant: 한국화학연구원 ,  한국생명공학연구원 ,  한국과학기술연구원

Inventor： 고종성 ,  이종국 ,  조성윤 ,  한선영 ,  이정옥 ,  류재욱 ,  박경찬 ,  한동초 ,  하재두 ,  박성규 ,  정희정 ,  권병목 ,  유경호 ,  심태보

IPC: C07D413/14

CPC classification number: C07D413/14

Abstract: PURPOSE: A pyridine derivative substituted with a novel pyrazole and benzoxide or a pharmaceutically acceptable salt is provided to prevent and treat idioblast growth diseases. CONSTITUTION: A pyridine derivative substituted with a pyrazol and benzoxazole or its pharmaceutically acceptable salt is denoted by the chemical formula 1. In the chemical formula 1, R1 is hydrogen or NHR4, R4 is hydrogen, straight or branched alkyl or benzyl of C1-C4, and R2 is hydrogen or halogen, straight or branched alkyl of C1-C4, -NHR5, -NR6R7, OR5, -CN, -NHC(O)R6, -SO2R6, -OS(O)2R6, pyrrolidine, piperidine and morpholine.

Abstract translation: 目的：提供一种吡唑衍生物，其被新的吡唑和苯甲醛或其药学上可接受的盐所取代，以预防和治疗成年细胞生长疾病。 构成：由吡唑和苯并恶唑或其药学上可接受的盐取代的吡啶衍生物由化学式1表示。在化学式1中，R1是氢或NHR4，R4是氢，C1-C4的直链或支链烷基或苄基 ，R 2是氢或卤素，C 1 -C 4，-NHR 5，-NR 6 R 7，OR 5，-CN，-NHC（O）R 6，-SO 2 R 6，-OS（O）2 R 6，吡咯烷，哌啶和吗啉的直链或支链烷基 。