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9 条记录 (耗时 0.017 秒)

    Marine Alkalod Makaluvamines and Derivatives Thereof
    2.
    发明申请
    Marine Alkalod Makaluvamines and Derivatives Thereof 审中-公开
    海洋阿卡洛德马卡鲁胺及其衍生物

    公开(公告)号：US20100144779A1

    公开(公告)日：2010-06-10

    申请号：US12528358

    申请日：2008-02-25

    申请人： Sadanandan E. Velu ,  Kevin P. Raisch ,  Ruiwen Zhang ,  Wei Wang

    发明人： Sadanandan E. Velu ,  Kevin P. Raisch ,  Ruiwen Zhang ,  Wei Wang

    IPC分类号： A61K31/437 ,  C07D471/02 ,  A61P35/00

    CPC分类号： A61K31/4745 ,  C07D471/06

    摘要： The present disclosure provides compounds based on the marine alkaloid makaluvamine. Described are compounds of the general formula (I) and (II). Also described are pharmaceutical compositions comprising one or more of the compounds of the general formula (I) and (II). The compounds and pharmaceutical compositions described inhibit the growth of several cancer lines, induce apoptosis and cell cycle arrest, display topoisomerase II inhibitory activity and modulate the activity and/or expression of key proteins involved in the regulation of cell growth. Methods of treatment and prevention using the compounds and pharmaceutical compositions described are also provided.

    摘要翻译： 本公开提供了基于海洋生物碱麦考卢明胺的化合物。 描述了通式（I）和（II）的化合物。 还描述了包含一种或多种通式（I）和（II）的化合物的药物组合物。 所描述的化合物和药物组合物抑制几种癌细胞系的生长，诱导细胞凋亡和细胞周期阻滞，显示拓扑异构酶II抑制活性并调节参与调节细胞生长的关键蛋白质的活性和/或表达。 还提供了使用所述化合物和药物组合物的治疗和预防方法。

    MDM2-specific antisense oligonucleotides
    4.
    发明授权
    MDM2-specific antisense oligonucleotides 失效
    MDM2特异性反义寡核苷酸

    公开(公告)号：US06946447B2

    公开(公告)日：2005-09-20

    申请号：US09541848

    申请日：2000-04-03

    申请人： Jiandong Chen ,  Sudhir Agrawal ,  Ruiwen Zhang

    发明人： Jiandong Chen ,  Sudhir Agrawal ,  Ruiwen Zhang

    IPC分类号： A61K38/00 ,  C12N15/113 ,  A61K41/00 ,  C12Q1/68

    CPC分类号： C12N15/113 ,  A61K38/00 ,  C12N15/1135 ,  C12N2310/315 ,  C12N2310/345 ,  C12N2310/346

    摘要： The invention provides methods to activate tumor suppressors. The invention further provides antisense oligonucleotides complementary to a portion of the MDM2-encoding RNA and methods for using such antisense oligonucleotides as analytical and diagnostic tools, as potentiators of transgenic animal studies and for gene therapy approaches, and as potential therapeutic agents. The invention also provides methods to augment and synergistically activate a tumor suppressor in conjunction with the use of a DNA-damage inducing agent. The invention further provides in vitro and in vivo models to evaluate the therapeutic effectiveness of a recently identified anti-human-MDM2 antisense oligonucleotide in the treatment of human colorectal cancers.

    摘要翻译： 本发明提供激活肿瘤抑制因子的方法。 本发明还提供了与一部分编码MDM2的RNA互补的反义寡核苷酸以及使用这样的反义寡核苷酸作为分析和诊断工具，作为转基因动物研究和基因治疗方法的增效剂以及作为潜在治疗剂的方法。 本发明还提供了与使用DNA损伤诱导剂一起增加和协同激活肿瘤抑制基因的方法。 本发明进一步提供体外和体内模型以评估最近鉴定的抗人MDM2反义寡核苷酸在治疗人结肠直肠癌中的治疗有效性。

    Method of down-regulating gene expression
    5.
    发明授权
    Method of down-regulating gene expression 失效
    降低基因表达的方法

    公开(公告)号：US06608035B1

    公开(公告)日：2003-08-19

    申请号：US09587934

    申请日：2000-06-06

    申请人： Sudhir Agrawal ,  Robert B. Diasio ,  Ruiwen Zhang

    发明人： Sudhir Agrawal ,  Robert B. Diasio ,  Ruiwen Zhang

    IPC分类号： A01N4304

    CPC分类号： C12N15/113 ,  A61K31/7125 ,  A61K38/1709 ,  C12N2310/312 ,  C12N2310/3125 ,  C12N2310/315 ,  C12N2310/345 ,  Y02A50/411 ,  Y02A50/491

    摘要： Disclosed is a method of down-regulating the expression of a gene in an animal, wherein a pharmacological formulation comprising a chimeric oligonucleotide complementary to the gene is orally administered to an animal. The oligonucleotide administered has at least one phosphorothioate internucleotide linkage and at least one alkylphosphonate, phosphorodithioate, alkylphosphonothioate, phosphoramidate, phosphoramidite, phosphate ester, carbamate, carbonate, phosphate triester, acetamidate, or carboxymethyl ester internucleotide linkage.

    摘要翻译： 公开了一种下调动物基因表达的方法，其中将包含与该基因互补的嵌合寡核苷酸的药理学制剂口服给予动物。 所施用的寡核苷酸具有至少一个硫代磷酸酯核苷酸间键和至少一种烷基膦酸盐，二硫代磷酸盐，烷基磷硫酸盐，氨基磷酸盐，亚磷酰胺，磷酸酯，氨基甲酸盐，碳酸盐，磷酸三酯，乙酰胺盐或羧甲基酯核苷酸间键。

    1-aryl-or 1-heteroaryl-pyrido[B]indoles and uses thereof
    7.
    发明申请
    1-aryl-or 1-heteroaryl-pyrido[B]indoles and uses thereof 有权
    1-芳基或1-杂芳基 - 吡啶并[B]吲哚及其用途

    公开(公告)号：US20100317667A1

    公开(公告)日：2010-12-16

    申请号：US12799485

    申请日：2010-04-26

    申请人： John K. Buolamwini ,  Shivaputra Patil ,  James K. Addo ,  D. Parker Suttle ,  Ruiwen Zhang ,  Zhengxiang Zhu ,  Sharma Horrick

    发明人： John K. Buolamwini ,  Shivaputra Patil ,  James K. Addo ,  D. Parker Suttle ,  Ruiwen Zhang ,  Zhengxiang Zhu ,  Sharma Horrick

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61P35/00 ,  C12N5/09

    CPC分类号： A61K45/06 ,  A61K31/437 ,  C07D471/04 ,  A61K2300/00

    摘要： Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a β-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, halogen, thiol, alkylthiol, sulfonyl, sulfomainde, amide, substituted amide, ester, nitrile, OH, amino, substituted amine, haloalkyl, haloalkoxy, acyl, or a hydrogen. Also provided are methods for inhibiting proliferation of a cancer cell or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.

    摘要翻译： 本文提供的是1-芳基或1-杂芳基取代的菲二酮酸化合物。 这些化合物包括在C 1上被芳基或杂芳基部分取代并在C 3 -C 8和N 9与C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4烷氧基苯基，卤素，硫醇 烷基硫醇，磺酰基，磺基汞，酰胺，取代的酰胺，酯，腈，OH，氨基，取代的胺，卤代烷基，卤代烷氧基，酰基或氢。 还提供了通过使包含其的癌细胞或肿瘤与本文提供的化合物接触或通过将化合物给予具有细胞增殖性疾病的受试者来抑制癌细胞增殖或治疗细胞增殖性疾病的方法。

    Method of down-regulating gene expression
    8.
    发明授权
    Method of down-regulating gene expression 失效
    降低基因表达的方法

    公开(公告)号：US06936593B1

    公开(公告)日：2005-08-30

    申请号：US09777526

    申请日：2001-02-06

    申请人： Sudhir Agrawal ,  Robert B. Diasio ,  Ruiwen Zhang

    发明人： Sudhir Agrawal ,  Robert B. Diasio ,  Ruiwen Zhang

    IPC分类号： A01N43/04 ,  A61K31/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/85 ,  C12P19/34 ,  C12Q1/68

    CPC分类号： A61K31/7125 ,  Y02A50/387 ,  Y02A50/402 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/423

    摘要： Disclosed is a method of down-regulating the expression of a gene in an animal, wherein a pharmacological formulation comprising a chimeric oligonucleotide complementary to the gene is orally administered to an animal. The oligonucleotide administered has at least one phosphorothioate internucleotide linkage and at least one alkylphosphonate, phosphorodithioate, alkylphosphonothioate, phosphoramidate, phosphoramidite, phosphate ester, carbamate, carbonate, phosphate triester, acetamidate, or carboxymethyl ester internucleotide linkage.

    摘要翻译： 公开了一种下调动物基因表达的方法，其中将包含与该基因互补的嵌合寡核苷酸的药理学制剂口服给予动物。 所施用的寡核苷酸具有至少一个硫代磷酸酯核苷酸间键和至少一种烷基膦酸盐，二硫代磷酸盐，烷基磷硫酸盐，氨基磷酸盐，亚磷酰胺，磷酸酯，氨基甲酸盐，碳酸盐，磷酸三酯，乙酰胺盐或羧甲基酯核苷酸间键。