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    Anesthetic trifluoromethylcyclobutanes
    81.
    发明授权
    Anesthetic trifluoromethylcyclobutanes 失效
    麻醉三氟甲磺酰氯

    公开(公告)号：US3852474A

    公开(公告)日：1974-12-03

    申请号：US17839871

    申请日：1971-09-07

    申请人： GRACE W R & CO

    发明人： SIMONS C ,  HOLDSWORTH R

    IPC分类号： A61K31/025 ,  A61K27/00

    CPC分类号： A61K31/025

    摘要： Certain trifluoromethylcyclobutanes are disclosed which possess utility as inhalation anesthetics. They are: 1-chloro-2trifluoromethyl-2,3,3-trifluorocyclobutane, 1-bromo-2trifluoromethyl-2,3,3-trifluorocyclobutane, 1-methyl-2trifluoromethyl-2,3,3-trifluorocyclobutane and 1,2,3,3tetrafluoro-2-trifluoromethylcyclobutane.

    摘要翻译： 公开了一些可用作吸入麻醉剂的三氟甲基环丁烷。 它们是：1-氯-2-三氟甲基-2,3,3-三氟环丁烷，1-溴-2-三氟甲基-2,3,3-三氟环丁烷，1-甲基-2-三氟甲基-2,3,3-三氟环丁烷 和1,2,3,3-四氟-2-三氟甲基环丁烷。

    Fluorocyclopropane anesthetics
    82.
    发明授权
    Fluorocyclopropane anesthetics 失效
    氟代环丙沙星

    公开(公告)号：US3839589A

    公开(公告)日：1974-10-01

    申请号：US39530373

    申请日：1973-09-07

    申请人： GRACE W R & CO

    发明人： O NEILL G ,  SIMONS C ,  BILLINGS C

    IPC分类号： A61K31/025 ,  A61K27/00

    CPC分类号： A61K31/025

    摘要： THE PROCESS OF INDUCING ANESTHESIA IN A MAMMAL WHICH COMPRISES ADMINSTERING TO SAID MAMMAL BY INHALATION AN EFFECTIVE QUANTITY FOR INDUCING ANSETHESIA OF A CYCLOPROPANE SELECTED FFROM THE GROUP CONSISTING OF 1CHLORO-1,2,2-TRIFLUOROCYCLOPROPANE, 1-BROMO-2,2-DIFFUOROCYCLOPROPANE AND 1,1-DIBROMO-2,2-DIFLUOROCYCLOPROPANE.

    Small molecule inhibitors of replication protein A that also act synergistically with cisplatin
    90.
    发明授权
    Small molecule inhibitors of replication protein A that also act synergistically with cisplatin 有权
    复制蛋白A的小分子抑制剂也与顺铂协同作用

    公开(公告)号：US08980955B2

    公开(公告)日：2015-03-17

    申请号：US13824318

    申请日：2011-09-19

    申请人： John J. Turchi ,  Richard Fitch

    发明人： John J. Turchi ,  Richard Fitch

    IPC分类号： A61K31/025 ,  A61K31/22 ,  C07D307/93 ,  A61K31/343

    CPC分类号： A61K31/22 ,  A61K31/343 ,  A61K33/24 ,  C07D307/93

    摘要： Replication protein A (RPA) is a single-strand DNA-binding protein with essential roles in DNA replication, recombination and repair. Small molecule inhibitors (SMIs) with the ability to disrupt RPA binding activity to ssDNA have been identified and assessed using both lung and ovarian cancer cell lines. Lung cancer cell lines demonstrated increased apoptotic cell death following treatment with the SMI MCI13E, with IC50 values of ˜5 μM. The A2780 ovarian cancer cell line and the p53-null lung cancer cell line HI 299 were particularly sensitive to MCI13E treatment with IC50 values below 3 μM. Sequential treatment with MCI13E and cisplatin resulted in synergism, suggesting that decreasing RPA's DNA binding activity via a SMI may disrupt RPA's role in cell cycle regulation. Thus, RPA SMIs hold the potential to be used as single agent chemotherapeutics or in combination with current chemotherapeutic regimens to increase their efficacy.

    摘要翻译： 复制蛋白A（RPA）是一种单链DNA结合蛋白，在DNA复制，重组和修复中具有重要作用。 已经使用肺和卵巢癌细胞系鉴定和评估了具有破坏对ssDNA的RPA结合活性的能力的小分子抑制剂（SMI）。 在用SMI MCI13E处理后，肺癌细胞株表现出凋亡细胞死亡增加，IC50值约为5μM。 A2780卵巢癌细胞系和p53无肺癌细胞系HI 299对MCI13E治疗特别敏感，IC 50值低于3μM。 用MCI13E和顺铂进行顺序治疗可以产生协同作用，这表明通过SMI降低RPA的DNA结合活性可能会破坏RPA在细胞周期调控中的作用。 因此，RPA SMI可能被用作单一化学药物治疗剂或与目前的化学治疗方案结合使用，以提高其疗效。