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    AMINOMETHYLENE PYRAZOLONES WITH THERAPEUTIC ACTIVITY
    37.
    发明申请
    AMINOMETHYLENE PYRAZOLONES WITH THERAPEUTIC ACTIVITY 有权

    公开(公告)号：US20170240531A1

    公开(公告)日：2017-08-24

    申请号：US15590797

    申请日：2017-05-09

    Applicant: Compound Handling B.V. ,  Stichting Katholieke Universiteit

    Inventor： Onno Van Hooij ,  Jacobus Antonius Schalken ,  Hendrik Engelbertus Vietor ,  Dennis Patrick Piet ,  Petrus Emmanuel Marie Maas ,  Johann Heinrich Tijhuis ,  Sirik Deerenberg ,  Nanda Elisabeth Sprenkels ,  Siu Ha Tang

    IPC: C07D403/04

    CPC classification number: C07D403/04 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/454 ,  A61K45/06 ,  C07D417/04 ,  C07D417/14

    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring; or R3 and R4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; R5 is H, Cl, F, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; R6 is H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen; R7 is H, F, Cl, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular, to delay, prevent or reverse metastasis in prostate cancer.

    INTRAMEDULLARY DEVICE FOR MID-SHAFT CLAVICLE FRACTURES
    38.
    发明申请
    INTRAMEDULLARY DEVICE FOR MID-SHAFT CLAVICLE FRACTURES 审中-公开
    用于中轴分离器的内置装置

    公开(公告)号：US20160317200A1

    公开(公告)日：2016-11-03

    申请号：US15106152

    申请日：2014-12-03

    Applicant: STICHTING KATHOLIEKE UNIVERSITEIT

    Inventor： Paul HOOGERVORST

    IPC: A61B17/72 ,  A61B17/92 ,  A61B17/86

    CPC classification number: A61B17/7233 ,  A61B17/7225 ,  A61B17/7291 ,  A61B17/863 ,  A61B17/8685 ,  A61B17/921

    Abstract: An intramedullary device for treatment of a mid-shaft clavicle fracture includes a base pin (1) having a primary fixation element (2) and a connection part (3). A secondary fixation element (6) is provided which is attachable to the connection part (3) at a distance along the base pin with respect to the primary fixation element (2). The connection part (3) of the base pin (1) and the secondary fixation element (6) are rotatable with respect to each other when attached, e.g. using an end cap (7).

    Abstract translation: 用于治疗中轴锁骨骨折的髓内装置包括具有主固定元件（2）和连接部分（3）的底销（1）。 提供辅助固定元件（6），该辅助固定元件（6）可相对于主固定元件（2）沿着底销一段距离地附接到连接部分（3）。 基座销（1）和辅助固定元件（6）的连接部分（3）可以在安装时相对于彼此旋转。 使用端盖（7）。

    METHODS FOR THE TREATMENT OR PREVENTION OF SYSTEMIC SCLEROSIS
    40.
    发明申请
    METHODS FOR THE TREATMENT OR PREVENTION OF SYSTEMIC SCLEROSIS 审中-公开
    治疗或预防系统性溃疡的方法

    公开(公告)号：US20160121039A1

    公开(公告)日：2016-05-05

    申请号：US14993814

    申请日：2016-01-12

    Applicant: Stichting Katholieke Universiteit

    Inventor： Timothy Ruben Dirk Jan Radstake

    IPC: A61M1/36

    CPC classification number: A61M1/3618 ,  A61K38/17 ,  A61K39/39541 ,  A61K39/3955 ,  A61K2039/505 ,  C07K16/18 ,  C07K16/24 ,  C07K16/2851 ,  C07K2317/76

    Abstract: The disclosure is in the field of molecular immunology, more in particular, in the field of the prevention or treatment of autoimmune diseases, more in particular, systemic sclerosis or scleroderma. The disclosure is based on the observation that SSC patients have an elevated plasma level of CXCL4. This was found to contribute to the pathogenesis of SSc, in particular, fibrosis. When CXCL4 was neutralized in in vitro experiments, the fibrotic effects could be neutralized. This led us to conclude that SSc may be cured by reducing the plasma level of CXCL4. The disclosure, therefore, relates to a method for treatment or prevention of fibrosis in patients with scleroderma, wherein the plasma level of CXCL4 is reduced.

    Abstract translation: 本发明涉及分子免疫学领域，特别是在预防或治疗自身免疫性疾病，特别是系统性硬化症或硬皮病领域。 该披露是基于SSC患者血浆CXCL4水平升高的观察。 这被发现有助于SSc的发病机制，特别是纤维化。 当CXCL4在体外实验中被中和时，可以中和纤维化作用。 这导致我们得出结论，通过降低CXCL4的血浆水平可以治愈SSc。 因此，本发明涉及用于治疗或预防硬皮病患者纤维化的方法，其中CXCL4的血浆水平降低。

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