Drechsleranol derivatives, processes for their preparation and their use
    15.
    发明授权
    Drechsleranol derivatives, processes for their preparation and their use 失效
    德舒辛醇衍生物,其制备方法及其用途

    公开(公告)号:US06794408B2

    公开(公告)日:2004-09-21

    申请号:US10351773

    申请日:2003-01-27

    IPC分类号: A61K3134

    摘要: The present invention provides novel drechsleranol compounds of formula (I) which are formed by the microorganism Drechslera australlensis, ST 003360, DSM 14093, or a fungus ST 004112, DSM 14524, during fermentation. A process for their preparation, pharmaceutical compositions containing said drechsleranols their use for the treatment and/or prophylaxis of degenerative neuropathies, such as, Alzheimeu's disease, or psychiatric disorders, such as depression, sleep disturbance or seasonal affective disorder, and their use as chelating agents or antioxidants are also disclosed and claimed.

    摘要翻译: 本发明提供了在发酵期间由微生物Drechslera australlensis,ST 003360,DSM14093或真菌ST 004112,DSM14524形成的式(I)的新颖的德劳克醇化合物。 它们的制备方法,含有所述的drechsleranols的药物组合物,它们用于治疗和/或预防退行性神经病,例如阿尔茨海默病,或精神疾病如抑郁症,睡眠障碍或季节性情感障碍,以及它们作为螯合剂的用途 还公开并要求保护剂或抗氧化剂。

    Eurotinones, and derivatives thereof, processes for preparing them, and their use
    17.
    发明授权
    Eurotinones, and derivatives thereof, processes for preparing them, and their use 有权
    欧卡因及其衍生物,其制备方法及其应用

    公开(公告)号:US06818667B2

    公开(公告)日:2004-11-16

    申请号:US10180003

    申请日:2002-06-26

    IPC分类号: A61K31335

    CPC分类号: C07D313/12

    摘要: The present invention relates to novel compounds of the formula I in which R(1), R(2), R(3) and R(4) are, independently of each other, hydrogen or an alkyl radical. The compounds of the formula I are inhibitors of KDR kinase and, due to their antiangiogenic effect, are suitable for preventing and/or treating malignant diseases. The compounds of the formula I can be obtained by fermenting the microorganism Eurotium echinulatum Delacroix (DSM 13872) or by chemically derivatizing the compounds which are obtained after fermenting said microorganism. The invention consequently also relates to a process for preparing the compounds of the formula I, to the use of the compounds of the formula I for preparing a pharmaceutical for treating malignant diseases and diseases which can be treated by inhibiting KDR kinase, and also to pharmaceutical preparations which have a content of at least one compound of the formula I.

    摘要翻译: 本发明涉及式Iin的新化合物,其中R(1),R(2),R(3)和R(4)彼此独立地为氢或烷基。 式I的化合物是KDR激酶的抑制剂,并且由于其抗血管生成作用,适用于预防和/或治疗恶性疾病。 式I的化合物可以通过发酵微生物欧氏螺旋体(DSM 13872)或通过化学衍生在发酵所述微生物后获得的化合物而获得。 因此,本发明还涉及制备式I化合物的方法,使用式I化合物来制备治疗可通过抑制KDR激酶治疗的恶性疾病和疾病的药物,还涉及药物 具有至少一种式I化合物含量的制剂。