Histone Deacetylase Inhibitors
    4.
    发明申请
    Histone Deacetylase Inhibitors 失效
    组蛋白脱乙酰酶抑制剂

    公开(公告)号:US20110287535A1

    公开(公告)日:2011-11-24

    申请号:US12977335

    申请日:2010-12-23

    IPC分类号: C12N5/071

    摘要: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

    摘要翻译: 组蛋白脱乙酰酶是在活性位点具有锌的金属酶。 具有锌结合部分的化合物,例如异羟肟酸基或羧酸基可以抑制组蛋白脱乙酰酶。 组蛋白脱乙酰酶可抑制基因表达,包括与肿瘤抑制有关的基因的表达。 因此,组蛋白脱乙酰酶的抑制可以提供用于治疗癌症,血液学疾病例如血红蛋白病和遗传相关代谢紊乱(例如囊性纤维化和肾上腺嗜甲基营养不良)的替代途径。

    Histone deacetylase inhibitors based on alpha-ketoepoxide compounds
    5.
    发明授权
    Histone deacetylase inhibitors based on alpha-ketoepoxide compounds 失效
    基于α-酮氧化物化合物的组蛋白脱乙酰酶抑制剂

    公开(公告)号:US07579372B2

    公开(公告)日:2009-08-25

    申请号:US11198293

    申请日:2005-08-08

    IPC分类号: A61K31/336

    CPC分类号: C07D303/32

    摘要: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-ketoepoxide group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or to stimulate hematopoietic cells ex vivo.

    摘要翻译: 组蛋白脱乙酰酶是在活性位点具有锌的金属酶。 具有锌结合部分的化合物,例如α-酮氧化物基团,例如α-酮硫基,可以抑制组蛋白脱乙酰酶。 组蛋白脱乙酰酶抑制可抑制基因表达,包括与肿瘤抑制相关的基因的表达。 因此,组蛋白脱乙酰酶的抑制可以提供治疗癌症的替代途径,血液学病症,例如血红蛋白病,常染色体显性疾病,例如常染色体显性疾病。 脊髓性肌肉萎缩和亨廷顿病,遗传相关的代谢紊乱,例如囊性纤维化和肾上腺脑白质营养不良,或离体刺激造血细胞。

    Histone deacetylase inhibitors based on alpha-ketoepoxide compounds
    9.
    发明授权
    Histone deacetylase inhibitors based on alpha-ketoepoxide compounds 失效
    基于α-酮氧化物化合物的组蛋白脱乙酰酶抑制剂

    公开(公告)号:US08138225B2

    公开(公告)日:2012-03-20

    申请号:US12545712

    申请日:2009-08-21

    IPC分类号: A61K31/336

    CPC分类号: C07D303/32

    摘要: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-ketoepoxide group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or to stimulate hematopoietic cells ex vivo.

    摘要翻译: 组蛋白脱乙酰酶是在活性位点具有锌的金属酶。 具有锌结合部分的化合物,例如α-酮氧化物基团,例如α-酮硫基,可以抑制组蛋白脱乙酰酶。 组蛋白脱乙酰酶抑制可抑制基因表达,包括与肿瘤抑制相关的基因的表达。 因此,组蛋白脱乙酰酶的抑制可以提供治疗癌症的替代途径,血液学病症,例如血红蛋白病,常染色体显性疾病,例如常染色体显性疾病。 脊髓性肌肉萎缩和亨廷顿病,遗传相关的代谢紊乱,例如囊性纤维化和肾上腺脑白质营养不良,或离体刺激造血细胞。

    HISTONE DEACETYLASE INHIBITORS
    10.
    发明申请
    HISTONE DEACETYLASE INHIBITORS 审中-公开
    HISTONE脱乙酰酶抑制剂

    公开(公告)号:US20110288168A1

    公开(公告)日:2011-11-24

    申请号:US12955470

    申请日:2010-11-29

    摘要: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, genetic disorders, e.g. Huntington's disease and spinal muscular atrophy and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

    摘要翻译: 组蛋白脱乙酰酶是在活性位点具有锌的金属酶。 具有锌结合部分的化合物,例如异羟肟酸基或羧酸基可以抑制组蛋白脱乙酰酶。 组蛋白脱乙酰酶抑制可抑制基因表达,包括与肿瘤抑制相关的基因的表达。 因此,组蛋白脱乙酰酶的抑制可以提供治疗癌症的替代途径,血液病症,例如血红蛋白病,遗传疾病, 亨廷顿氏病和脊髓性肌肉萎缩以及遗传相关的代谢紊乱,例如囊性纤维化和肾上腺脑白质营养不良。