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71.发明公开신규한 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 有权新型嘧啶-24-二胺衍生物和用于预防或治疗癌症的药物组合物，所述癌症含有其作为活性成分
公开(公告)号：KR20180012352A
公开(公告)日：2018-02-06
申请号：KR20160094560
申请日：2016-07-26
IPC: C07D403/12 , A61K31/506 , A61K31/53 , A61K31/5395 , C07D403/10 , C07D413/10 , C07D413/12
CPC classification number: A23L33/10 , A61K31/506 , A61K31/53 , A61K31/5395 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/12
Abstract: 본발명은신규한피리미딘-2,4-디아민유도체또는이의약학적으로허용가능한염 및이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에의한화합물은역형성림프종키나아제(ALK) 활성을억제하는효과가우수하므로이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가향상될수 있으며, 암의재발을막는데효과적일것으로예상되므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.
Abstract translation: 嘧啶-2,4-二胺衍生物或其药学上可接受的盐以及含有该化合物作为有效成分的用于预防或治疗癌症的药物组合物技术领域本发明涉及新的嘧啶-2,4- 根据本发明的化合物具有优异的抑制逆转形成淋巴瘤激酶（ALK）活性的作用，由此改善对具有逆转形成淋巴瘤激酶（ALK）融合蛋白的癌细胞的治疗效果，例如EML4- ALK或NPM-ALK，预计本发明在防止癌症复发方面是有效的，因此可以有效地用作预防或治疗癌症的药物组合物。
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公开(公告)号：KR101656382B1
公开(公告)日：2016-09-09
申请号：KR1020140023897
申请日：2014-02-28
Applicant: 한국화학연구원
IPC: C07D401/12 , A61K31/506 , A61P35/00
CPC classification number: A61K31/506 , C07D401/12
Abstract: 본발명은피리미딘-2,4-디아민유도체또는이의약학적으로허용가능한염 및이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에의한화합물은역형성림프종키나아제(ALK) 활성을억제하는효과가우수하므로이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가향상될수 있으며, 암의재발을막는데효과적일것으로예상되므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.
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73.发明授权4-(1-퍼롤-3,4-디카르복시아미드)피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 有权4-1-34- 4-1-吡咯-34-二甲酰胺嘧啶衍生物的制备方法和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
公开(公告)号：KR101633722B1
公开(公告)日：2016-06-28
申请号：KR1020140135844
申请日：2014-10-08
Applicant: 한국화학연구원
IPC: C07D403/04 , A61K31/506 , A61P35/00
Abstract: 본발명은 4-(1-퍼롤-3,4-디카르복시아미드)피리미딘유도체, 이의제조방법및 이를유효성분으로함유하는암의예방또는치료용약학적조성물에관한것으로, 본발명에따른 4-(1-퍼롤-3,4-디카르복시아미드)피리미딘유도체, 이의광학이성질체, 또는이의약학적으로허용가능한염은역형성림프종키나아제(ALK)를억제하는활성이우수하므로, 이에따른 EML4-ALK, NPM-ALK 등의역형성림프종키나아제(ALK) 융합단백질을가진암세포에대한치료효과가우수하고, 암의재발을막는데효과적일것으로예상되므로암의예방또는치료용약학적조성물로유용하게사용될수 있다.
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公开(公告)号：KR1020150145176A
公开(公告)日：2015-12-29
申请号：KR1020150071257
申请日：2015-05-21
Applicant: 한국화학연구원
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含有嘧啶-2,4-二胺衍生物作为活性成分的癌症的药物组合物。 根据本发明的化合物具有抑制间变性淋巴瘤激酶（ALK）活性的优异效果。 因此，可以改善对具有ALK融合蛋白（例如EML4-ALK和NPM-ALK等）的癌细胞的治疗效果。 预期该组合物可有效预防癌症的复发，因此可用作预防或治疗癌症的药物组合物。
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公开(公告)号：KR1020150102252A
公开(公告)日：2015-09-07
申请号：KR1020140023897
申请日：2014-02-28
Applicant: 한국화학연구원
IPC: C07D401/12 , A61K31/506 , A61P35/00
CPC classification number: A61K31/506 , C07D401/12
Abstract: 본 발명은 피리미딘-2,4-디아민 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。
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Patent Agency Ranking
公开(公告)号：KR1020140022229A
公开(公告)日：2014-02-24
申请号：KR1020120088577
申请日：2012-08-13
IPC: C07D487/04 , C07D403/14 , A61K31/4985 , A61K31/506 , A61K31/5377
CPC classification number: C07D487/04 , A61K31/4985 , A61K31/506 , A61K31/5377 , C07D403/14
Abstract: The present invention relates to novel triazolopyrazine derivatives or a pharmaceutically acceptable salt, and a pharmaceutical composition for inhibiting c-Met tyrosine kinase activity and a pharmaceutical composition for preventing or treating hyperproliferative disorders, containing the same as active ingredients. The present invention effectively inhibits c-Met tyrosine kinase activity, thereby being able to be useful as a drug for various hyperproliferative disorders such as cancers, psoriasis, rheumatoid arthritis, diabetic retinitis, etc. related to excessive cell proliferation and growth by abnormal kinase activation.
Abstract translation: 本发明涉及新的三唑并吡嗪衍生物或其药学上可接受的盐，以及用于抑制c-Met酪氨酸激酶活性的药物组合物和用于预防或治疗含有与活性成分相同的过度增殖性疾病的药物组合物。 本发明有效地抑制c-Met酪氨酸激酶活性，从而能够用作各种过度增殖性疾病如癌症，牛皮癣，类风湿性关节炎，糖尿病性视网膜炎等与异常激酶激活相关的过度细胞增殖和生长相关的药物 。
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77.发明公开Ｎ2,Ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 有权N2，N4-BIS（4-（哌嗪-1-基）苯基）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包含其作为活性成分的癌症的药物组合物
公开(公告)号：KR1020140021350A
公开(公告)日：2014-02-20
申请号：KR1020120087716
申请日：2012-08-10
Applicant: 한국화학연구원
IPC: C07D403/14 , C07D403/12 , A61K31/506 , A61P35/00
CPC classification number: C07D239/48 , A61K31/506 , C07D403/12 , C07D403/14
Abstract: The present invention relates to N2,N4-bis(4-(piperazine-1-yl)phenyl)pyrimidine-2,4-diamine derivatives or pharmaceutically acceptable salts thereof, and pharmaceutical compositions for cancer prevention or treatment containing the same as an active ingredient. The compounds of the present invention have an excellent effect in inhibiting anaplastic lymphoma kinase (ALK) and activated Cdc42-associated kinase (ACK1), and thus can improve the effect in treating cancer cells having ALK fusion proteins such as EML4-ALK and NPM-ALK. Further, the compounds of the present invention are expected to be effective in preventing cancer recurrence, and thus are useful as pharmaceutical compositions for cancer prevention or treatment.
Abstract translation: 本发明涉及N 2，N 4 - 双（4-（哌嗪-1-基）苯基）嘧啶-2,4-二胺衍生物或其药学上可接受的盐，以及用于癌症预防或治疗的药物组合物，其含有活性物质 成分。 本发明的化合物在抑制间变性淋巴瘤激酶（ALK）和活化的Cdc42相关激酶（ACK1）中具有优异的效果，从而可以改善治疗具有ALK融合蛋白如EML4-ALK和NPM- ALK。 此外，预期本发明的化合物可有效预防癌症复发，因此可用作癌症预防或治疗的药物组合物。
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公开(公告)号：KR1020130101408A
公开(公告)日：2013-09-13
申请号：KR1020120022541
申请日：2012-03-05
IPC: C07D498/04 , C07D487/04 , A61K31/5025 , A61P35/00
CPC classification number: C07D519/00
Abstract: PURPOSE: A novel triazolo pyridazine derivative is provided to effectively suppress the activity of c-Met tyrosine kinase, thereby being used as a therapeutic agent for treating various hyperproliferative disorders related to excessive cell proliferation and growth caused by abnormal kinase activity. CONSTITUTION: A triazolo pyridazine derivative of chemical formula 1 or a pharmaceutically acceptable salt thereof is provided. A pharmaceutical composition for suppressing c-Met tyrosine kinase contains the triazolo pyridazine derivative or a pharmaceutically acceptable salt or solvate thereof as an active ingredient. A pharmaceutical composition for preventing or treating hyperproliferative disorders contains the triazolo pyridazine derivative, the pharmaceutically acceptable salt, or the solvate as an active ingredient.
Abstract translation: 目的：提供一种新的三唑并噻唑衍生物，以有效抑制c-Met酪氨酸激酶的活性，从而用作治疗与异常激酶活性引起的过度细胞增殖和生长相关的各种过度增殖性疾病的治疗剂。 构成：提供化学式1的三唑并哒嗪衍生物或其药学上可接受的盐。 用于抑制c-Met酪氨酸激酶的药物组合物含有三唑并哒嗪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三唑并哒嗪衍生物，药学上可接受的盐或溶剂化物作为活性成分。
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公开(公告)号：KR1020110048476A
公开(公告)日：2011-05-11
申请号：KR1020100108201
申请日：2010-11-02
Applicant: 서울대학교산학협력단 , 한국화학연구원
IPC: C07D401/12 , C07D239/34 , A61K31/513 , A61P29/00
CPC classification number: C07D239/60 , C07D239/52 , C07D401/12
Abstract: PURPOSE: A composition containing a novel 2,4-pyrimidine derivative is provided to suppress gp96 surface translocation and to prevent and treat SLE(systemic lupus etythematosus). CONSTITUTION: A novel 2,4-pyrimidine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating SLE contains the 2,4-pyrimidine derivative compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A method for screening a therapeutic agent for SLE comprises: a step of contacting a test agent with AIMP1 and gp96; a step of measuring disintegration activity of AIMP1 and gp96 and selecting an agent which changes AIMP1 and gp96 binding ability; and a step of testing the treatment or relief on SLE by the selected agent.
Abstract translation: 目的：提供含有新的2,4-嘧啶衍生物的组合物，以抑制gp96表面易位并预防和治疗SLE（系统性红斑狼疮）。 构成：化学式1表示新的2,4-嘧啶衍生物。用于预防和治疗SLE的药物组合物含有化学式1的2,4-嘧啶衍生物化合物或其药学上可接受的盐作为活性成分。 用于筛选SLE治疗剂的方法包括：使测试试剂与AIMP1和gp96接触的步骤; 测量AIMP1和gp96的分解活性并选择改变AIMP1和gp96结合能力的药剂的步骤; 以及由所选代理测试SLE的治疗或救济的步骤。
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公开(公告)号：KR100535951B1
公开(公告)日：2005-12-09
申请号：KR1020030067964
申请日：2003-09-30
Applicant: 한국화학연구원
IPC: A61K31/4152 , A61P35/00
Abstract: 본 발명은 3-메칠-(O-치환된 옥시이미노)-피라졸린-5-온 유도체를 함유하는 항암제에 관한 것으로서, 더욱 상세하게는 세포분열에 결정적으로 작용하는 CDC25B의 탈인산화효소에 대한 탁월한 저해활성을 가지고 있는 다음 화학식 1로 표시되는 (O-치환된 옥시이미노)-피라졸린-5-온 유도체가 유효활성 성분으로 함유되어 있는 항암제에 관한 것이다.
상기 화학식 1에서, R
1 및 R
2 는 각각 발명의 상세한 설명에서 정의한 바와 같다.
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