FIVE CRYSTAL FORMS, METHODS OF PREPARATION, PHARMACEUTICAL COMPOSITIONS AND APPLICATIONS OF XLF-III-43
    2.
    发明申请
    FIVE CRYSTAL FORMS, METHODS OF PREPARATION, PHARMACEUTICAL COMPOSITIONS AND APPLICATIONS OF XLF-III-43 有权
    五水晶形态,制备方法,药物组合物和XLF-III-43的应用

    公开(公告)号:US20110319401A1

    公开(公告)日:2011-12-29

    申请号:US13131492

    申请日:2009-11-28

    CPC classification number: C07D311/16 A61K31/37

    Abstract: This invention discloses that the five crystal forms of XLF-III-43 can be used as crude drugs. The invention also relates to the preparation methods of the five crystal forms of XLF-III-43 as crude drugs, to the applications of the sterling of the five crystal forms of XLF-III-43 and mixed crystals in different proportions as medicinally active components to develop various kinds of medicines and compound medicines. In addition, this invention also relates to applying the crystal samples of XLF-III-43 as crude drugs to treat kidney dysfunction, cardiocerebral vessel diseases, hypertension, type II diabetic mellitus, complications of hypertension and diabetic mellitus, tumor, precancerosis, edema, and achieves therapeutic effects by enhancing blood drug levels resulted from effects of crystal forms in the processes of treating all kinds of diseases.

    Abstract translation: 本发明公开了XLF-III-43的五种晶体形式可用作生药。 本发明还涉及作为生药的XLF-III-43的五种结晶形式的制备方法,将XLF-III-43的五种晶型和不同比例的混晶的英制应用作为药物活性成分 开发各种药品和复合药物。 此外,本发明还涉及将XLF-III-43的晶体样品作为生药用于治疗肾功能障碍,心脑血管疾病,高血压,II型糖尿病,高血压和糖尿病并发症,肿瘤,癌前病变,水肿, 并且通过在治疗各种疾病的过程中增强由结晶形式的作用引起的血药浓度来达到治疗效果。

    Nucleophile substituted ecteinascidins and N-oxide ecteinascidins
    3.
    发明授权
    Nucleophile substituted ecteinascidins and N-oxide ecteinascidins 失效
    亲核取代的ecteinascidins和N-氧化物ecteinascidins

    公开(公告)号:US5985876A

    公开(公告)日:1999-11-16

    申请号:US58499

    申请日:1998-04-10

    CPC classification number: C07D515/22

    Abstract: Five new nucleophile substituted ecteinascidin (Et) compounds have been isolated from extracts of Ecteinascidia turbinata. These compounds have been purified by chromatographic techniques and their structures and bioactivities have been determined. The five nucleophile substituted Et compounds have been designated herein as Et 802 (1), Et 788 (2), Et 760 (3), Et 858 (4) and Et 815 (5). Also obtained were three new N-oxide ecteinascidin compounds, which have been designated herein as Et 717 (6), Et 775 (7) and Et 789 (8). Some of these newly discovered Et compounds show exceedingly potent cytotoxicity against L1210.

    Abstract translation: 五种新的亲核取代的ecteinascidin(Et)化合物已从Ecteinascidia turbinata的提取物中分离出来。 这些化合物已经通过色谱技术纯化,并且已经确定了它们的结构和生物活性。 本文将五种亲核取代的Et化合物定义为Et 802(1),Et 788(2),Et 760(3),Et 858(4)和Et 815(5)。 还获得了三种新的N-氧化物角叉菜胶化合物,其在本文中被称为Et 717(6),Et 775(7)和Et 789(8)。 这些新发现的Et化合物中的一些对L1210显示出极强的细胞毒性。

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