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    DDR2 단백질의 티로신 키나아제 활성 저해 화합물
    2.
    发明授权
    DDR2 단백질의 티로신 키나아제 활성 저해 화합물 失效
    用于抑制DDR2蛋白的酪氨酸激酶活性的化合物

    公开(公告)号：KR100883909B1

    公开(公告)日：2009-02-17

    申请号：KR1020067018588

    申请日：2005-01-05

    Applicant: 한국과학기술연구원

    Inventor： 양범석 ,  양경미 ,  김해종 ,  박인성 ,  박성대 ,  이장혁 ,  권혁만 ,  우병영

    IPC: C07D491/048 ,  A61K31/5025

    CPC classification number: C07D491/04

    Abstract: 본 발명은 신규한 푸로피리미딘 화합물, 이들의 약학적으로 허용되는 염, 또는 이들을 포함하는 DDR2(Discoidin Domain Receptor 2) 티로신 키나아제 활성 저해제에 관한 것이다. 상기 푸로피리미딘 화합물은 화학식 1, 화학식 2, 화학식 3 또는 화학식 4로 정의되는 화합물, 이들의 전구체일 수 있으며, 유리 형태 또는 산 부가염 형태로 존재할 수 있다. 본 발명의 푸로피리미딘 화합물은 DDR2 티로신 키나아제의 활성을 억제하는 효과를 갖기 때문에, 간경화, 류마티스 관절염, 암 등과 같이, DDR2 티로신 키나아제 활성이 관여하여 발생하는 질환의 치료에 유용하다.

    증가 된 키나아제 활성을 갖는 ＤＤＲ２ 단백질 및 그제조방법
    4.
    发明授权
    증가 된 키나아제 활성을 갖는 ＤＤＲ２ 단백질 및 그제조방법 有权
    具有活性激酶活性的DDR2蛋白及其制备方法

    公开(公告)号：KR101201902B1

    公开(公告)日：2012-11-16

    申请号：KR1020067010740

    申请日：2004-11-01

    Applicant: 한국과학기술연구원 ,  제일파마홀딩스 주식회사

    Inventor： 양범석 ,  박성대

    IPC: C07K14/705

    CPC classification number: C07K14/705 ,  C07K2319/00 ,  C07K2319/21 ,  C07K2319/23 ,  C07K2319/35 ,  C12N9/1205

    Abstract: 본 발명은 증가 된 자가 인산화 및 키나아제 활성을 갖는 변형된 DDR2(디스코이딘 도메인 리셉터 2) 세포질 티로신 키나아제 도메인을 함유하는 단백질에 관한 것으로서, i) 숙주세포에서 Src나 Src 연관 단백질과 동시 발현에 의하여, 또는 숙주세포의 H
    2 O
    2 처리에 의하여 티로신의 자가 인산화를 유도함으로써, 또는 ii) 적어도 1개의 티로신 잔기를 다른 아미노산으로 특정 부위 돌연 변이 변형하는 방법에 의함으로써 자가 인산화 및 키나아제 활성이 증가 된 DDR2 세포질 티로신 키나아제 도메인을 함유하는 단백질을 제조하는 방법, 및 DDR2 자가 인산화 및 키나아제 작용이 과다 활성화된 것을 원인으로 하는 질환에 대한 의학적 치료제 개발을 위한 표적 물질로서의 용도에 관한 것이다.
    자가 인산화, DDR, 특정부위 돌연 변이, 바큐로바이러스

    증가 된 키나아제 활성을 갖는 ＤＤＲ２ 단백질 및 그제조방법
    5.
    发明公开
    증가 된 키나아제 활성을 갖는 ＤＤＲ２ 단백질 및 그제조방법 有权
    具有活性激酶活性的DDR2蛋白及其制备方法

    公开(公告)号：KR1020070029119A

    公开(公告)日：2007-03-13

    申请号：KR1020067010740

    申请日：2004-11-01

    Applicant: 한국과학기술연구원 ,  제일파마홀딩스 주식회사

    Inventor： 양범석 ,  박성대

    IPC: C07K14/705

    CPC classification number: C07K14/705 ,  C07K2319/00 ,  C07K2319/21 ,  C07K2319/23 ,  C07K2319/35 ,  C12N9/1205

    Abstract: A DDR2(discoidin domain receptor 2) protein having increased kinase activity and a preparation method thereof are provided to offer a target protein so as to develop medicines for treating diseases caused by excessive activation of DDR2 autophosphorylation and kinase activity such as liver cirrhosis, arteriosclerosis, arthritis and cancer. A protein containing a modified human DDR2 cytosolic tyrosine kinase domain having increased autophosphorylation and tyrosine kinase activity is provided, wherein the modified human DDR2 cytosolic tyrosine kinase domain is prepared by modifying at least one of tyrosines 736, 740 and 741 in the activation loop of human DDR2 cytosolic tyrosine kinase domain through induction of tyrosine phosphorylations, or through independent mutation to phenylalanine, alanine or glycine by site-directed mutation. The method for preparing the protein containing modified human DDR2 cytosolic tyrosine kinase domain having increased autophosphorylation and tyrosine kinase activity comprises the steps of: amplifying a DNA fragment encoding the DDR2 cytosolic tyrosine kinase domain protein, and introducing the amplified DNA fragment into a viral expression vector to construct a recombinant viral expression vector for DDR2 cytosolic tyrosine kinase domain protein and to generate a recombinant virus containing the DDR2 cytosolic tyrosine kinase domain protein; amplifying a DNA fragment encoding a full-length c-Src or c-Src related protein, and introducing the amplified DNA fragment into another separate virus expression vector genome to construct a recombinant virus expression vector for the c-Src or c-Src related protein and to generate a recombinant virus containing the c-Src or c-Src related protein; infecting the DDR2 cytosolic tyrosine kinase domain-containing virus and the c-Src or c-Src related protein-containing virus into a host cell, expressing both proteins simultaneously, and inducing the tyrosine phosphorylation at the DDR2 cytosolic tyrosine kinase domain by the tyrosine kinase activity of c-Src or c-Src related protein to produce a large quantity of the protein containing the DDR2 cytosolic tyrosine kinase domain with increased tyrosine phosphorylation; and isolating and purifying the obtained protein containing the DDR2 cytosolic tyrosine kinase domain with increased tyrosine phosphorylation.

    Abstract translation: 提供具有增加的激酶活性的DDR2（盘状结构域受体2）蛋白及其制备方法，以提供靶蛋白，以开发用于治疗由DDR2自磷酸化过度激活和激酶活性引起的疾病的药物，例如肝硬化，动脉硬化， 关节炎和癌症。 提供了含有增加的自磷酸化和酪氨酸激酶活性的修饰的人DDR2胞质酪氨酸激酶结构域的蛋白质，其中通过修饰人类激活环中的酪氨酸736,740和741中的至少一种来制备修饰的人DDR2胞质酪氨酸激酶结构域 通过诱导酪氨酸磷酸化，或通过定点突变，通过独立突变成苯丙氨酸，丙氨酸或甘氨酸来解决DDR2胞质酪氨酸激酶结构域。 制备具有增加的自磷酸化和酪氨酸激酶活性的修饰的人DDR2胞质酪氨酸激酶结构域的蛋白质的方法包括以下步骤：扩增编码DDR2胞质酪氨酸激酶结构域蛋白的DNA片段，并将扩增的DNA片段引入病毒表达载体 构建DDR2胞质酪氨酸激酶结构域蛋白的重组病毒表达载体，并产生含有DDR2胞质酪氨酸激酶结构域蛋白的重组病毒; 扩增编码全长c-Src或c-Src相关蛋白质的DNA片段，并将扩增的DNA片段引入另一个单独的病毒表达载体基因组，构建c-Src或c-Src相关蛋白的重组病毒表达载体 并产生含有c-Src或c-Src相关蛋白的重组病毒; 将含有DDR2胞质酪氨酸激酶结构域的病毒和c-Src或c-Src相关蛋白的病毒感染到宿主细胞中，同时表达两种蛋白质，并通过酪氨酸激酶诱导DDR2细胞溶质酪氨酸激酶结构域的酪氨酸磷酸化 c-Src或c-Src相关蛋白的活性产生大量含有DDR2胞质酪氨酸激酶结构域的蛋白质，酪氨酸磷酸化程度增加; 并分离和纯化所获得的含有DDR2细胞溶质酪氨酸激酶结构域的蛋白质，酪氨酸磷酸化程度增加。

    DDR2 단백질의 티로신 키나아제 활성 저해 화합물
    6.
    发明公开
    DDR2 단백질의 티로신 키나아제 활성 저해 화합물 失效
    用于抑制DDR2蛋白的酪氨酸激酶活性的化合物

    公开(公告)号：KR1020070012648A

    公开(公告)日：2007-01-26

    申请号：KR1020067018588

    申请日：2005-01-05

    Applicant: 한국과학기술연구원

    Inventor： 양범석 ,  양경미 ,  김해종 ,  박인성 ,  박성대 ,  이장혁 ,  권혁만 ,  우병영

    IPC: C07D491/048 ,  A61K31/5025

    CPC classification number: C07D491/04

    Abstract: A novel furopyrimidine compound is provided to show the DDR2 tyrosine kinase inhibition activity, thereby being usefully used for treating a disease caused by tyrosine kinase activity of DDR2 protein such as a tissue fibrosis, rheumatism and cancer. The furopyrimidine compound is represented by one of the formulae(1), (2), (3), (4), (XI) and (XII), where Z is O, S or NH, Y is C or N, X is O, S or NH, n is an integer between 0 and 4, n' is an integer between 0 and 4, each R1, R3 and R3' is single-substituted or independently double-substituted by H, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-4 alkyl, C1-4 halo alkyl, C1-7 alkoxy, C1-4 alkyl amino, C1-4 alkylthio, C1-4 alkyl amide, C1-4 acyl amino, C1-4 acyl oxy, C1-4 alkyl sulfone amide, C1-4 alkyl sulfonate, imidic acid C1-4 alkyl ester, thioimidic acid C1-4 alkyl ester, hydroxy or amino, morpholine, acetate, acetamide, methanesulfoneamide group-substituted methyl, C1-4 halo alkyl, C1-4 alkoxy, or a halogen-substituted benzyl oxy, R" is H, C1-4 alkyl, C1-4 halo alkyl, C1-7 alkoxy, C1-4 alkyl amino, C1-4 alkyl thio, C1-4 alkyl amide, C1-4 acyl amino, C1-4 acyl oxy, imidic acid C1-4 alkyl ester, thiol-imidic acid C1-4 alkyl ester, hydroxy or amino, morpholine, acetate, acetamide, methanesulfoneamide group-substituted methyl, C1-4 halo alkyl, C1-4 alkoxy, or a halogen-substituted phenyl, A ring is benzene, pyrrole, furan, thiophene, imidazole, oxazol, thiazole, triazole, pyrazol, pyrazine, pyridazine, pyrimidine, cyclo hexyl, piperidine or morpholine, R2 is H, halogen, cyano, nitro, hydroxy, amino, C02H, CONH2, CSNH2, C1-5 alkyl, C1-5 haloalkyl, alkylester, phenyl, halogen-substituted phenyl, C1-4 alkoxy group-substituted phenyl or C1-4 haloalkoxy group-substituted phenyl, and R is single-substituted or independently double-substituted by H, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-4 alkyl, C1-4 haloalkyl, C1-7 alkoxy, C1-4 alkylamino, C1-4 alkylthio, C1-4 alkylamide, C1-4 acylamino, C1-4 acyloxy, or C1-4 alkylsufonamide.

    Abstract translation: 提供了一种新的呋喃嘧啶化合物以显示DDR2酪氨酸激酶抑制活性，从而有效地用于治疗由DDR2蛋白的酪氨酸激酶活性引起的疾病，例如组织纤维化，风湿病和癌症。 呋喃并嘧啶化合物由式（1），（2），（3），（4），（XI）和（XII）之一表示，其中Z为O，S或NH，Y为C或N，X 是O，S或NH，n是0和4之间的整数，n'是0和4之间的整数，每个R 1，R 3和R 3'被H，卤素，氰基，硝基的单取代或独立地被双取代 ，羟基，氨基，CO 2 H，CONH 2，CSNH 2，脒，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1-4烷硫基，C 1-4烷基酰胺，C 1-4酰基 氨基，C 1-4酰氧基，C 1-4烷基砜酰胺，C 1-4烷基磺酸酯，酰亚胺酸C 1-4烷基酯，硫代亚氨酸C 1-4烷基酯，羟基或氨基，吗啉，乙酸酯，乙酰胺，甲磺酰胺基 - 取代的甲基，C 1-4卤代烷基，C 1-4烷氧基或卤素取代的苄氧基，R“是H，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1 -4-烷基硫代，C 1-4烷基酰胺，C 1-4酰基氨基，C 1-4酰氧基，酰亚胺酸C 1-4烷基酯，硫醇 - 酰亚胺酸C 1-4烷基酯，羟基或氨基， 乙酰胺，甲磺酰胺基取代的甲基，C 1-4卤代烷基，C 1-4烷氧基或卤素取代的苯基，A环为苯，吡咯，呋喃，噻吩，咪唑，恶唑，噻唑，三唑，吡唑 吡嗪，哒嗪，嘧啶，环己基，哌啶或吗啉，R2是H，卤素，氰基，硝基，羟基，氨基，CO2H，CONH2，CSNH2，C1-5烷基，C1-5卤代烷基，烷基酯，苯基， 取代的苯基，C 1-4烷氧基取代的苯基或C 1-4卤代烷氧基取代的苯基，R是被H，卤素，氰基，硝基，羟基，氨基，CO 2 H，CONH 2，CSNH 2单取代或独立地双取代的 ，脒，C 1-4烷基，C 1-4卤代烷基，C 1-7烷氧基，C 1-4烷基氨基，C 1-4烷硫基，C 1-4烷基酰胺，C 1-4酰氨基，C 1-4酰氧基或C 1-4烷基磺酰胺。

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