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11 条记录 (耗时 0.018 秒)

    Thiazole-substituted β-lactams
    1.
    发明授权
    Thiazole-substituted β-lactams 失效
    噻唑取代的β-内酰胺

    公开(公告)号：US06900312B2

    公开(公告)日：2005-05-31

    申请号：US10196052

    申请日：2002-07-16

    申请人： Juergen Kolb ,  Alexander Doemling

    发明人： Juergen Kolb ,  Alexander Doemling

    IPC分类号： A01N43/78 ,  C07C327/06 ,  C07D417/06 ,  A61P31/04

    CPC分类号： C07D417/06 ,  A01N43/78 ,  C07C327/06

    摘要： The present discovery consists in new thiazole-substituted β-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen atom, a halogen, a hydroxy, amino, nitro, or thiol group, an optionally substituted alkyl, heteroalkyl, aryl, aralkyl, cycloalkyl, cycloaralkyl, heterocycloalkyl, heteroaralkyl, or heteroaryl rest.

    摘要翻译： 本发现包括通式（I）的新的噻唑取代的β-内酰胺以及它们的制备方法。 R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8彼此独立地为氢原子，卤素，羟基，氨基，硝基或硫醇基，任选取代的烷基，杂烷基，芳基， 芳烷基，环烷基，环烷基，杂环烷基，杂芳烷基或杂芳基。

    Selective and dual-action p53/MDM2/MDM4 antagonists
    5.
    发明授权
    Selective and dual-action p53/MDM2/MDM4 antagonists 有权
    选择性和双作用p53 / MDM2 / MDM4拮抗剂

    公开(公告)号：US08163789B2

    公开(公告)日：2012-04-24

    申请号：US12106280

    申请日：2008-04-19

    申请人： Alexander Doemling

    发明人： Alexander Doemling

    IPC分类号： A61K31/4174 ,  A61K31/4178 ,  C07D233/64

    CPC分类号： G01N33/6872 ,  G01N2333/4704 ,  G01N2333/4748 ,  G01N2500/02

    摘要： A fragment-based strategy, involving “multicomponent reaction chemistry” (MCR), can identify novel chemotypes that disrupt the p53/MDM2 or p53/MDM4 complex employs. This approach uses high resolution structural information to delineate the region of a first protein or a ligand that is nestled within the binding pocket of a second target protein. The identified region is imported into a database containing MCR scaffolds to generate a virtual library of compounds, which subsequently are docked into the binding pocket of the target protein. Results from docking then are used to select compounds for synthesis and screening. A complementary, NMR-based methodology allows for screening the ability of compounds, selected using MCR, to disrupt the p53/MDM2 or p53/MDM4 complex.

    摘要翻译： 涉及“多组分反应化学”（MCR）的基于片段的策略可以鉴定破坏p53 / MDM2或p53 / MDM4复合物的新型化学型。 该方法使用高分辨率结构信息来描绘嵌合在第二靶蛋白的结合口袋中的第一蛋白质或配体的区域。 识别的区域被导入到含有MCR支架的数据库中，以生成化合物的虚拟文库，随后将它们对接到目标蛋白质的结合口袋中。 对接结果用于选择合成和筛选的化合物。 基于NMR的互补的方法允许筛选使用MCR选择的化合物破坏p53 / MDM2或p53 / MDM4复合物的能力。

    SUBSTITUTED HETEROCYCLES AS THERAPEUTIC AGENTS FOR TREATING CANCER
    6.
    发明申请
    SUBSTITUTED HETEROCYCLES AS THERAPEUTIC AGENTS FOR TREATING CANCER 审中-公开
    作为治疗癌症的治疗药物的替代治疗剂

    公开(公告)号：US20130211079A1

    公开(公告)日：2013-08-15

    申请号：US13841648

    申请日：2013-03-15

    申请人： Alexander DOEMLING

    发明人： Alexander DOEMLING

    IPC分类号： C07D233/28 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    CPC分类号： C07D233/28 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    摘要： MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.

    摘要翻译： MDM2和MDM4蛋白通过负调节转录因子p53阻止癌细胞的凋亡。 根据式I的化合物是MDM2和MDM4蛋白的选择性拮抗剂，破坏p53 / MDM2和p53 / MDM4复合物。 因此，这些化合物是用于治疗癌症以及其它细胞增殖性疾病状态的候选治疗剂。

    Substituted Heterocycles as Therapeutic agents for treating cancer
    7.
    发明申请
    Substituted Heterocycles as Therapeutic agents for treating cancer 审中-公开
    取代的杂环作为治疗癌症的治疗剂

    公开(公告)号：US20110313167A1

    公开(公告)日：2011-12-22

    申请号：US13067700

    申请日：2011-06-21

    申请人： Alexander Doemling

    发明人： Alexander Doemling

    IPC分类号： C07D401/12

    CPC分类号： C07D233/28 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    摘要： MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.

    摘要翻译： MDM2和MDM4蛋白通过负调节转录因子p53阻止癌细胞的凋亡。 根据式I的化合物是MDM2和MDM4蛋白的选择性拮抗剂，破坏p53 / MDM2和p53 / MDM4复合物。 因此，这些化合物是用于治疗癌症以及其它细胞增殖性疾病状态的候选治疗剂。

    SELECTIVE AND DUAL-ACTION P53/MDM2/MDM4 ANTAGONISTS
    8.
    发明申请
    SELECTIVE AND DUAL-ACTION P53/MDM2/MDM4 ANTAGONISTS 有权
    选择和双重作用P53 / MDM2 / MDM4 ANTAGONISTS

    公开(公告)号：US20080280769A1

    公开(公告)日：2008-11-13

    申请号：US12106280

    申请日：2008-04-19

    申请人： Alexander Doemling

    发明人： Alexander Doemling

    IPC分类号： C40B20/00 ,  G01N33/68 ,  C07D233/54 ,  C07D233/04 ,  C07D215/00 ,  C07C215/00 ,  C07D213/02 ,  C07D295/00

    CPC分类号： G01N33/6872 ,  G01N2333/4704 ,  G01N2333/4748 ,  G01N2500/02

    摘要： A fragment-based strategy, involving “multicomponent reaction chemistry” (MCR), can identify novel chemotypes that disrupt the p53/MDM2 or p53/MDM4 complex employs. This approach uses high resolution structural information to delineate the region of a first protein or a ligand that is nestled within the binding pocket of a second target protein. The identified region is imported into a database containing MCR scaffolds to generate a virtual library of compounds, which subsequently are docked into the binding pocket of the target protein. Results from docking then are used to select compounds for synthesis and screening. A complementary, NMR-based methodology allows for screening the ability of compounds, selected using MCR, to disrupt the p53/MDM2 or p53/MDM4 complex.

    摘要翻译： 涉及“多组分反应化学”（MCR）的基于片段的策略可以鉴定破坏p53 / MDM2或p53 / MDM4复合物的新型化学型。 该方法使用高分辨率结构信息来描绘嵌合在第二靶蛋白的结合口袋中的第一蛋白质或配体的区域。 识别的区域被导入到含有MCR支架的数据库中，以生成化合物的虚拟文库，随后将它们对接到目标蛋白质的结合口袋中。 对接结果用于选择合成和筛选的化合物。 基于NMR的互补的方法允许筛选使用MCR选择的化合物破坏p53 / MDM2或p53 / MDM4复合物的能力。

    Pyrroloimidazole derivatives and their use as medicaments
    10.
    发明授权
    Pyrroloimidazole derivatives and their use as medicaments 失效
    吡咯并咪唑衍生物及其用作药物

    公开(公告)号：US06699883B1

    公开(公告)日：2004-03-02

    申请号：US10089917

    申请日：2002-04-04

    申请人： Alexander Doemling ,  Barbara Beck

    发明人： Alexander Doemling ,  Barbara Beck

    IPC分类号： A61K31445

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D471/04

    摘要： The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I) wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each independently of the others, carbon or nitrogen atoms, the radicals Z denote, each independently of the others, a hydrogen atom, a halogen atom, a pseudohalogen, an optionally substituted alkyl, alkenyl, alkynyl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloaralkyl, cycloaralkenyl, cycloaralkynyl, aryl or alkoxy radical or an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and/or at least two of the radicals Z may be part of an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and to pharmaceutical compositions comprising at least one of the above-mentioned compounds, optionally in combination with carriers and/or adjuvants and/or excipients customary per se.

    摘要翻译： 本发明涉及通式（I）的3-吡咯并咪唑衍生物，其中咪唑基为任选取代的咪唑环，X，Y，A和B各自独立地为碳原子或氮原子，基团Z 表示氢原子，卤素原子，假卤素，任意取代的烷基，烯基，炔基，芳烷基，芳烯基，芳炔基，环烷基，环烯基，环炔基，环烷基，环烯基，环烷基炔基，芳基或烷氧基 或任选取代的环，其中一个或两个另外的任选取代的环可以被稠合，和/或至少两个基团Z可以是任选取代的环的一部分，一个或两个另外的任选取代的环可以 并且包含至少一种上述化合物的药物组合物，任选地与本身常规的载体和/或佐剂和/或赋形剂组合。