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    Pharmaceutical composition
    1.
    发明申请
    Pharmaceutical composition 审中-公开
    药物组成

    公开(公告)号：US20070155685A1

    公开(公告)日：2007-07-05

    申请号：US10591048

    申请日：2005-02-28

    申请人： Karl-Hermann Schlingensiepen ,  Relmar Schlingensiepen ,  Piotr Jachimczak ,  Gerhard Stauder ,  Astrid Bischof ,  Michael Hafner ,  Tamara Egger

    发明人： Karl-Hermann Schlingensiepen ,  Relmar Schlingensiepen ,  Piotr Jachimczak ,  Gerhard Stauder ,  Astrid Bischof ,  Michael Hafner ,  Tamara Egger

    IPC分类号： A61K48/00 ,  C07H21/02

    CPC分类号： A61K31/713 ,  C12N15/1136 ,  C12N15/1137 ,  C12N15/1138 ,  C12N2310/11

    摘要： The present invention is related to pharmaceutical compositions for the inhibition of metastases and treatment of cancer such as bladder carcinoma, colon cancer, endometrial cancer, hepatocellular carcinoma, leukemia, lymphoma, melanoma, non-small cell lung cancer (NSCLC), ovarian cancer, pancreatic cancer, prostate cancer, soft tissue cancer, renal cancer, osteosarcoma, mesothelioma, myeloma multiple, bladder carcinoma and esophagcal cancer as well as the use of these pharmaceutical compositions for the treatment of said metastases and cancers. Another aspect of this invention are new antisense oligonucleotides inhibiting the formation of human interleukin 10 and their synthesis. A further aspect of this invention is the use IL-10 antisense oligonucleotides for the preparation of pharmaceutical compositions and for the treatment of cancer and metastases.

    摘要翻译： 本发明涉及用于抑制转移和治疗癌症的药物组合物，例如膀胱癌，结肠癌，子宫内膜癌，肝细胞癌，白血病，淋巴瘤，黑素瘤，非小细胞肺癌（NSCLC），卵巢癌， 胰腺癌，前列腺癌，软组织癌，肾癌，骨肉瘤，间皮瘤，骨髓瘤多发，膀胱癌和食道癌，以及这些药物组合物用于治疗所述转移和癌症的用途。 本发明的另一方面是抑制人白介素10的形成及其合成的新的反义寡核苷酸。 本发明的另一方面是使用IL-10反义寡核苷酸用于制备药物组合物和用于治疗癌症和转移瘤。

    Pharmaceutical composition
    8.
    发明申请
    Pharmaceutical composition 审中-公开
    药物组成

    公开(公告)号：US20100160208A1

    公开(公告)日：2010-06-24

    申请号：US12585086

    申请日：2009-09-02

    申请人： Karl-Hermann Schlingensiepen ,  Reimar Schlinensiepen

    发明人： Karl-Hermann Schlingensiepen ,  Reimar Schlinensiepen

    IPC分类号： A61K38/00 ,  A61K31/7088 ,  A61K31/7125 ,  A61K31/712

    CPC分类号： A61K31/04 ,  A61K31/166 ,  A61K31/52 ,  A61K31/7048 ,  A61K31/7125 ,  A61K38/08 ,  A61K38/16 ,  A61K38/1841 ,  A61K45/06 ,  C07K14/495 ,  C12N15/111 ,  C12N15/1136 ,  C12N2310/315 ,  C12N2310/346 ,  C12N2320/31 ,  A61K2300/00

    摘要： The invention concerns a pharmaceutical composition comprising at least one stimulator of the immune cell functions and at least one substance inhibiting the cell proliferation and/or inducing cell death. In a preferred embodiment the stimulator of the function of the immune system and/or the immune cells are antagonists of TGF-beta selected from the group of oligonucleotides hybridizing with an area of the messenger RNA and or DNA encoding TGF-beta and the at least one substance inhibiting cell proliferation and/or inducing cell death is selected from the group of temozolomide, nitrosoureas, Vinca alkaloids, antagonists of the purine and pyrimidines bases, cytoststatic active antibiotics, caphthotecine derivatives, anti estrogens, anti-androgens and analogs of gonadotropin releasing hormone.

    摘要翻译： 本发明涉及包含免疫细胞功能的至少一种刺激剂和抑制细胞增殖和/或诱导细胞死亡的至少一种物质的药物组合物。 在优选的实施方案中，免疫系统和/或免疫细胞的功能的刺激物是选自与信使RNA的区域杂交的寡核苷酸和/或至少编码TGF-β的DNA的TGF-β的拮抗剂 一种抑制细胞增殖和/或诱导细胞死亡的物质选自替莫唑胺，亚硝基脲，长春花生物碱，嘌呤和嘧啶碱的拮抗剂，抑菌活性抗生素，萘普生衍生物，抗雌激素，促雄激素和促性腺激素释放的类似物 激素。

    Antisense oligonucleotide preparation method
    9.
    发明申请
    Antisense oligonucleotide preparation method 失效
    反义寡核苷酸制备方法

    公开(公告)号：US20050130927A1

    公开(公告)日：2005-06-16

    申请号：US10984919

    申请日：2004-11-10

    申请人： Karl-Hermann Schlingensiepen ,  Wolfgang Brysch

    发明人： Karl-Hermann Schlingensiepen ,  Wolfgang Brysch

    IPC分类号： C12N15/09 ,  A61K31/70 ,  A61K31/7088 ,  A61K31/7125 ,  A61K38/00 ,  A61K48/00 ,  A61P3/00 ,  A61P9/10 ,  A61P25/28 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C12P19/34 ,  C12Q1/68

    CPC分类号： C12N15/1136 ,  A61K38/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C12N15/1135 ,  C12N15/1138 ,  C12N2310/11 ,  C12N2310/3125 ,  C12N2310/3145 ,  C12N2310/315 ,  C12N2310/3181 ,  C12N2310/351

    摘要： A method for the preparation of an antisense oligonucleotide or derivative thereof comprising the steps of: selecting a target nucleic acid, if necessary elucidating its sequence; generating the antisense oligonucleotide with the proviso that: the oligonucleotide comprises at least 8 residues; the oligonucleotide comprises at maximum twelve elements, which are capable of forming three hydrogen bonds each to cytosine bases; the oligonucleotide does not contain four or more consecutive elements, capable of forming three hydrogen bonds each with four consecutive cytosine bases (CCCC) within the target molecule or alternatively four or more consecutive elements of GGGG; the oligonucleotide does also not contain 2 or more series of three consecutive elements, capable of forming three hydrogen bonds each with three consecutive cytosine bases (CCC) within the target molecule, or alternatively 2 or more series of three consecutive elements of GGG; and the ratio between residues forming two hydrogen bonds per residue (2H-bond-R) with the target molecule and those residues forming three hydrogen bonds per residue (3H-bond-R) with the target molecule, is ruled by the following specifications: 3H-bond-R/3H-bond-R+2H-bond-R≧0.29; and synthesizing the oligonucleotide thus generated in a per se known manner.

    摘要翻译： 一种制备反义寡核苷酸或其衍生物的方法，包括以下步骤：如果需要，选择靶核酸阐明其序列; 产生反义寡核苷酸，条件是：寡核苷酸包含至少8个残基; 该寡核苷酸包含最多12个元件，其能够形成各自与胞嘧啶碱基的三个氢键; 寡核苷酸不含有四个或更多个连续的元件，能够在目标分子内形成三个氢键，每个具有四个连续的胞嘧啶碱基（CCCC），或者四个或更多个连续的GGGG元件; 寡核苷酸还不含有两个或更多个三个连续元件的系列，能够在目标分子内形成三个连接的胞嘧啶碱基（CCC）的三个氢键，或者另外两个或更多个三个连续的GGG元件系列; 并且与目标分子形成每个残基（2H-键-R）的两个氢键与每个残基形成三个氢键（3H-键-R）的残基与靶分子之间的比例由下列规格表示： 3H键-R / 3H键-R + 2H-键-R = 0.29; 并以本身已知的方式合成由此产生的寡核苷酸。