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    APTAMER LABELED WITH F-19 NUCLEUS FOR TARGETED MOLECULAR IMAGING BY MRI
    1.
    发明申请
    APTAMER LABELED WITH F-19 NUCLEUS FOR TARGETED MOLECULAR IMAGING BY MRI 审中-公开
    标有F-19核子的APTAMER通过MRI进行靶向分子成像

    公开(公告)号：WO2012076191A1

    公开(公告)日：2012-06-14

    申请号：PCT/EP2011/006255

    申请日：2011-12-12

    Applicant: MERCK PATENT GMBH ,  GUENTHER, Ralf ,  HOCK, Bjoern ,  GOODMAN, Simon ,  PIATER, Birgit

    Inventor： GUENTHER, Ralf ,  HOCK, Bjoern ,  GOODMAN, Simon ,  PIATER, Birgit

    IPC: A61K49/12

    CPC classification number: C12N15/115 ,  A61K49/12 ,  A61K49/126

    Abstract: Magnetic Resonance Imaging, usually based on 1 H as the magnetic nucleus, is an important diagnostic technique that is commonly used in hospitals for the diagnosis of disease. MRI allows for the non- invasive imaging of soft tissue with a superb spatial resolution. Magnetic Resonance Imaging based on 19 F instead of 1 H opens up new diagnostic possibilities. The 19 F nucleus has a high gyromagnetic ratio (40 MHz/T) and a natural isotopic abundance ratio of 100%. In the human body, 19 F containing structures are exclusively present in the form of solid salts in e.g. teeth and bones. As a consequence, the J2 relaxation times of the endogenous 19 F atoms are extremely short and the MR signal is hardly detectable, in other words, the lack of endogenous, 19 F-based structures with relatively high transverse relaxation times assures a very low background MR signal. Therefore, exogenous 19 F-based MRI contrast agents allow for "hot spot" imaging in a way similar to other techniques such as PET (positron emission tomography). As a useful extension of its diagnostic use, MRI is also proposed for the monitoring of the delivery of bio-active agents such as therapeutic or diagnostic agents. I.e., MRI can not only be used for treatment planning, but also to control local drug delivery under image guidance.

    Abstract translation: 磁共振成像通常以1H为磁核，是医院常用于诊断疾病的重要诊断技术。 MRI允许具有极好的空间分辨率的软组织的非侵入性成像。 基于19F而不是1H的磁共振成像开辟了新的诊断可能性。 19F核具有高回旋比（40MHz / T）和100％的天然同位素丰度比。 在人体中，含有19F的结构仅以例如固体盐的形式存在。 牙齿和骨头。 因此，内源性19F原子的J2松弛时间非常短，并且MR信号几乎不可检测，换句话说，缺乏具有相对较高的横向弛豫时间的内源性19F基结构，确保非常低的背景MR信号 。 因此，外源性基于19F的MRI造影剂允许以与PET（正电子发射断层摄影）等其他技术相似的方式进行“热点”成像。 作为其诊断用途的有用扩展，还提出了用于监测生物活性剂如治疗剂或诊断剂的递送的MRI。 即，MRI不仅可以用于治疗计划，还可以在图像引导下控制局部药物传播。

    ANTIBODIES FOR THE DETECTION OF INTEGRIN COMPLEXES IN FFPE MATERIAL
    2.
    发明申请
    ANTIBODIES FOR THE DETECTION OF INTEGRIN COMPLEXES IN FFPE MATERIAL 审中-公开
    用于检测FFPE材料中的整合复合物的抗体

    公开(公告)号：WO2011020529A3

    公开(公告)日：2011-06-16

    申请号：PCT/EP2010004313

    申请日：2010-07-15

    Applicant: MERCK PATENT GMBH ,  GOODMAN SIMON ,  WILM CLAUDIA ,  MITJANS FRANCESC

    Inventor： GOODMAN SIMON ,  WILM CLAUDIA ,  MITJANS FRANCESC

    IPC: C07K16/28 ,  C07K16/00 ,  C12N15/13 ,  G01N33/53

    CPC classification number: C07K16/2839 ,  C07K16/00 ,  G01N33/566 ,  G01N2333/70546

    Abstract: The invention relates to antibodies that are capable to bind the extracellular domain of integrin. Another object of the invention concerns the use of said antibodies for detecting integrins in archival formalin fixed paraffin embedded (FFPE) tissue. The invention also relates to methods for preparing monoclonal rabbit antibodies, wherein the immunogen is an insect expression culture-derived recombinant extracellular integrin domain, and another method for screening anti-integrin antibodies that discriminate between closest integrin homologues and that are especially suited for immunohistochemistry in FFPE material.

    Abstract translation: 本发明涉及能够结合整联蛋白的细胞外结构域的抗体。 本发明的另一个目的涉及所述抗体用于检测归档福尔马林固定石蜡包埋（FFPE）组织中的整联蛋白的用途。 本发明还涉及用于制备单克隆兔抗体的方法，其中所述免疫原是来自昆虫表达培养物的重组细胞外整联蛋白结构域，以及用于筛选抗整联蛋白抗体的另一种方法，所述抗整联蛋白抗体区分最接近的整联蛋白同源物并且特别适用于免疫组织化学 FFPE材料。

    ANTIBODIES FOR THE DETECTION OF INTEGRIN COMPLEXES IN FFPE MATERIAL
    3.
    发明申请
    ANTIBODIES FOR THE DETECTION OF INTEGRIN COMPLEXES IN FFPE MATERIAL 审中-公开

    公开(公告)号：WO2011020529A8

    公开(公告)日：2011-02-24

    申请号：PCT/EP2010/004313

    申请日：2010-07-15

    Applicant: MERCK PATENT GMBH ,  GOODMAN, Simon ,  WILM, Claudia ,  MITJANS, Francesc

    Inventor： GOODMAN, Simon ,  WILM, Claudia ,  MITJANS, Francesc

    IPC: C07K16/10

    Abstract: The invention relates to antibodies that are capable to bind the extracellular domain of integrin. Another object of the invention concerns the use of said antibodies for detecting integrins in archival formalin fixed paraffin embedded (FFPE) tissue. The invention also relates to methods for preparing monoclonal rabbit antibodies, wherein the immunogen is an insect expression culture-derived recombinant extracellular integrin domain, and another method for screening anti-integrin antibodies that discriminate between closest integrin homologues and that are especially suited for immunohistochemistry in FFPE material.

    ISOLATED ORGAN PERFUSION COMBINATION THERAPY OF CANCER
    6.
    发明申请
    ISOLATED ORGAN PERFUSION COMBINATION THERAPY OF CANCER 审中-公开
    分离的器官灌注组合治疗癌症

    公开(公告)号：WO2007082742A1

    公开(公告)日：2007-07-26

    申请号：PCT/EP2007/000408

    申请日：2007-01-18

    Applicant: MERCK PATENT GMBH ,  GOODMAN, Simon ,  GRELL, Matthias ,  TEN HAGEN, Timo, L., M. ,  EGERMONT, Alexander, M., M.

    Inventor： GOODMAN, Simon ,  GRELL, Matthias ,  TEN HAGEN, Timo, L., M. ,  EGERMONT, Alexander, M., M.

    IPC: A61K38/17 ,  A61P35/00

    CPC classification number: A61K38/12 ,  A61K41/00 ,  A61K45/06 ,  A61K2300/00

    Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agents or therapy forms that have synergistic efficacy when administered together with said ligands, such as chemotherapeutic agents and/or radiation therapy, in isolated organ perfusion. The therapy results in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone.

    Abstract translation: 本发明涉及用于治疗肿瘤和肿瘤转移的组合疗法，其包括将整联蛋白配体，优选整联蛋白拮抗剂，以及当与所述配体如化学治疗剂一起施用时具有协同疗效的共同治疗剂或治疗形式， /或放射治疗，分离器官灌注。 治疗导致每个单独治疗剂对肿瘤细胞增殖的抑制作用的协同增加潜力，产生比通过单独施用单独组分发现的更有效的治疗。

    COMBINATION THERAPY USING RECEPTOR TYROSINE KINASE INHIBITORS AND ANGIOGENESIS INHIBITORS
    9.
    发明申请
    COMBINATION THERAPY USING RECEPTOR TYROSINE KINASE INHIBITORS AND ANGIOGENESIS INHIBITORS 审中-公开
    使用受体酪氨酸激酶抑制剂和血管生成抑制剂的联合治疗

    公开(公告)号：WO02055106A3

    公开(公告)日：2003-03-06

    申请号：PCT/EP0115241

    申请日：2001-12-21

    Applicant: MERCK PATENT GMBH ,  GOODMAN SIMON ,  KREYSCH HANS-GEORG

    Inventor： GOODMAN SIMON ,  KREYSCH HANS-GEORG

    IPC: A61K45/06 ,  A61K31/337 ,  A61K31/704 ,  A61K31/7064 ,  A61K31/7068 ,  A61K33/24 ,  A61K38/00 ,  A61K38/08 ,  A61K39/395 ,  A61K41/00 ,  A61K47/48 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07K16/30

    CPC classification number: C07K16/30 ,  A61K38/08 ,  A61K39/39558 ,  A61K41/0038 ,  A61K2039/505 ,  A61K2300/00

    Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of receptor tyrosine kinase antagonists/inhibitors, especially ErbB receptor antagonists, more preferably EGF receptor (Her 1) antagonists and anti-angiogenic agents, preferably integrin antagonists, optionally together with agents or therapy forms that have additive or synergistic efficacy when administered together with said combination of antagonists/inhibitors, such as chemotherapeutic agents and or radiation therapy. The therapy can result in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone.

    Abstract translation: 本发明涉及用于治疗肿瘤和肿瘤转移的组合疗法，其包括施用受体酪氨酸激酶拮抗剂/抑制剂，特别是ErbB受体拮抗剂，更优选EGF受体（Her1）拮抗剂和抗血管生成剂，优选整联蛋白拮抗剂，任选地 以及当与所述拮抗剂/抑制剂如化学治疗剂和/或放射治疗的组合一起施用时具有添加或协同效力的药剂或治疗形式。 该治疗可以导致每个单独治疗剂对肿瘤细胞增殖的抑制作用的协同增加，产生比通过单独施用单独组分所发现的更有效的治疗。

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