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1. 发明公开

KR1020130006417A 키나아제 억제제 有权
标题翻译：激酶抑制剂
公开(公告)号：KR1020130006417A
公开(公告)日：2013-01-16
申请号：KR1020127011751
申请日：2010-11-12
申请人： 제노스코 , 주식회사 오스코텍
发明人： 이재규 , 송호준 , 고종성 , 이희규 , 김영삼 , 김홍우 , 장선화 , 임선희 , 최장식 , 김중호 , 김세원
IPC分类号： C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： A61K31/505 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D487/08
摘要： PURPOSE: A novel protein kinase inhibitor is provided to treat cancer, autoimmune diseases, infection, cardiovascular diseases, neurodegenerative diseases. CONSTITUTION: A kinase inhibitor compound is denoted by chemical formula I. A pharmaceutical formulation contains the compound of chemical formula I with a pharmaceutically acceptable carrier, diluents, or excipient. A method for treating protein kinase-mediated diseases comprises a step of administering therapeutically effective amount of the compound of chemical formula I or pharmaceutically acceptable salt to a subject to be treated. The kinase inhibitor compound is used by intravenous, subcutaneous, colorectal, parenteral intramuscular, nasal, skin, topical, ear, oral, ocular, or sublingual administration or inhalation. A method for suppressing SYK, PYK2, FAK, ZAP70, PIM1, FLT3, RET, JAK2, JAK3, LRRK2, LRRK2(G2019S), ABL1(T315I), AURKB, AXL, FLT3, KIT, KIT(D816V), KIT(V559D,T670I), MKNK2, MLK1, PDGFRB, PLK3, RET, SNARK, SRPK3, TAK1, or TYK2 signal transduction in the subject comprises a step of administering effective amount of the compound of chemical formula I.
摘要翻译：目的：提供一种新的蛋白激酶抑制剂，用于治疗癌症，自身免疫疾病，感染，心血管疾病，神经变性疾病。构成：激酶抑制剂化合物由化学式I表示。药物制剂含有化学式I化合物和药学上可接受的载体，稀释剂或赋形剂。用于治疗蛋白激酶介导的疾病的方法包括向受治疗对象施用治疗有效量的化学式I化合物或其药学上可接受的盐的步骤。激酶抑制剂化合物通过静脉内，皮下，结肠直肠，肠胃外，肌内，鼻腔，皮肤，局部，耳朵，口服，眼部或舌下给药或吸入使用。一种抑制SYK，PYK2，FAK，ZAP70，PIM1，FLT3，RET，JAK2，JAK3，LRRK2，LRRK2（G2019S），ABL1（T315I），AURKB，AXL，FLT3，KIT，KIT（D816V），KIT（V559D ，T670I），MKNK2，MLK1，PDGFRB，PLK3，RET，SNARK，SRPK3，TAK1或TYK2信号转导的方法包括施用有效量的化学式I的化合物的步骤。

2. 发明授权

KR101690358B1 키나아제 억제제 有权
标题翻译：激酶抑制剂
公开(公告)号：KR101690358B1
公开(公告)日：2017-01-09
申请号：KR1020127011750
申请日：2010-10-29
申请人： 제노스코 , 주식회사 오스코텍
发明人： 김홍우 , 고종성 , 이재규 , 송호준 , 김영삼 , 이희규 , 최장식 , 임선희 , 장선화
IPC分类号： C07D471/04 , C07D401/04 , A61K31/519 , A61P11/00
CPC分类号： A61K31/519 , C07D471/04
摘要： 본발명은암, 자가면역질환, 감염, 심혈관질환및 퇴행성신경질환과장애와같은세포증식성질환과장애를치료하기위해유용한신규한일군의단백질키나아제억제제, 피리도[4,3,-d]피리미딘-5-온유도체및 이의약제학적으로허용되는염을제공한다. 본발명은상기단백질키나아제억제제화합물을합성및 투여하기위한방법을제공한다. 본발명은또한상기단백질키나아제억제제화합물중 적어도하나이상과이를위한약제학적으로허용되는담체, 희석제또는부형제를함께포함하는약제학적제형을제공한다. 본발명은또한피리도[4,3,-d]피리딘-5-온유도체합성중에생성되는유용한중간체를제공한다.
摘要翻译：本发明提供了一组新的蛋白激酶抑制剂，吡啶并[4,3，-d]嘧啶-5-酮衍生物及其药学上可接受的盐，其可用于促进细胞增殖性疾病和病症如癌症，自身免疫性疾病，感染，心血管疾病和神经退行性疾病和障碍。本发明提供了合成和施用蛋白激酶抑制剂化合物的方法。本发明还提供了包含蛋白激酶抑制剂化合物中的至少一种与药学上可接受的载体，稀释剂或赋形剂的药物制剂。本发明还提供了在吡啶并[4,3， - d]嘧啶-5-酮衍生物的合成过程中产生的有用的中间体。

3. 发明公开

KR1020120140643A 키나아제 억제제 有权
标题翻译：激酶抑制剂
公开(公告)号：KR1020120140643A
公开(公告)日：2012-12-31
申请号：KR1020127011750
申请日：2010-10-29
申请人： 제노스코 , 주식회사 오스코텍
发明人： 김홍우 , 고종성 , 이재규 , 송호준 , 김영삼 , 이희규 , 최장식 , 임선희 , 장선화
IPC分类号： C07D471/04 , C07D401/04 , A61K31/519 , A61P11/00
CPC分类号： A61K31/519 , C07D471/04
摘要： PURPOSE: Pharmaceutically allowed salt is produced by using a derivate of pyrido(4,3,-d) pyrimidine-5-on and a protein kinase inhibitor useful for treating cell proliferative disorders such as cancer, autoimmune disease, infection, cardiovascular disease, neurogenerative disease and disability. CONSTITUTION: A protein kinase inhibitor is marked structural formula(I). A pharmaceutical formulation comprises a pharmaceutically allowed carrier, a diluting agent and a compound of structural formula(I). A method of treating protein kinase infected disease comprises a step to inject an effective dose of a compound of structural formula(I) and pharmaceutically allowed salt of the same into the object to be treated. A compound of structural formula(I) is injected one or more than one additional medicine. A compound of structural formula(I) is injected through intravenous injection, subcutaneous injection, suction, oral administration, colorectal administration, non-oral administration, injection into vitneous body, intramuscular medication, nasal administration, skin dose, topical administration, ear administration, ocular medication, oral administration, tracheal administration, bronchus administration or injection in hypoglotis. A method of suppressing of the growth of cancer cells comprises a step to touch cancer cells with a compound of structural formula(I) and pharmaceutically allowed salt. Neurogenerative disease is parkinson's disease or Alzheimer disease.
摘要翻译：目的：通过使用可用于治疗细胞增殖性疾病如癌症，自身免疫性疾病，感染，心血管疾病，神经生长因子的吡啶并（4,3，-d）嘧啶-5-酮和蛋白激酶抑制剂的衍生物来产生药学上允许的盐疾病和残疾构成：蛋白激酶抑制剂为结构式（I）。药物制剂包含药学上允许的载体，稀释剂和结构式（I）的化合物。治疗蛋白激酶感染疾病的方法包括将有效剂量的结构式（I）化合物及其药学上允许的盐注入待治疗对象的步骤。结构式（I）的化合物注射一种或多于一种另外的药物。通过静脉注射，皮下注射，抽吸，口服给药，结肠直肠给药，非口服给药，注射到维生素体内，肌肉内用药，鼻内给药，皮肤剂量，局部给药，耳部给药，注射结构式（I）眼药物，口服给药，气管给药，支气管给药或低血糖注射。抑制癌细胞生长的方法包括用结构式（I）化合物和药学上允许的盐接触癌细胞的步骤。神经生殖疾病是帕金森病或阿尔茨海默病。

4. 发明授权

KR101663637B1 키나아제 억제제 有权
公开(公告)号：KR101663637B1
公开(公告)日：2016-10-07
申请号：KR1020127011751
申请日：2010-11-12
申请人： 제노스코 , 주식회사 오스코텍
发明人： 이재규 , 송호준 , 고종성 , 이희규 , 김영삼 , 김홍우 , 장선화 , 임선희 , 최장식 , 김중호 , 김세원
IPC分类号： C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： A61K31/505 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D487/08
摘要： 본발명은암, 자가면역질환, 감염, 심혈관질환및 퇴행성신경질환과장애와같은세포증식성질환과장애를치료하기에유용한신규한일군의단백질키나아제억제제, 피로피리미딘과피라졸로피리미딘유도체및 이의약제학적으로허용되는염 및프로드러그를제공한다. 본발명은상기단백질키나아제억제제화합물을합성하고투여하기위한방법을제공한다. 본발명은또한상기단백질키나아제억제제화합물중 적어도하나이상과이를위한약제학적으로허용되는담체, 희석제또는부형제를함께포함하는약제학적제형을제공한다. 본발명은또한피로피리미딘과피라졸로피리미딘유도체합성중에생성되는유용한중간체를제공한다.

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