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    Pharmaceutical compositions of pyrimidine-2,4,6-triones
    3.
    发明申请
    Pharmaceutical compositions of pyrimidine-2,4,6-triones 审中-公开
    嘧啶-2,4,6-三硝基苯胺的药物组合物

    公开(公告)号：US20070191404A1

    公开(公告)日：2007-08-16

    申请号：US10594162

    申请日：2005-03-31

    申请人： Pierre Bartsch ,  Didier Cataldo ,  Richard Endele ,  Brigitte Evrard ,  Jean-Michel Foidart ,  Hans-Willi Krell ,  Gerd Zimmermann

    发明人： Pierre Bartsch ,  Didier Cataldo ,  Richard Endele ,  Brigitte Evrard ,  Jean-Michel Foidart ,  Hans-Willi Krell ,  Gerd Zimmermann

    IPC分类号： A61K31/515

    CPC分类号： A61K9/0075 ,  A61K9/0078 ,  A61K31/198 ,  A61K31/515 ,  A61K47/183 ,  A61K47/6951 ,  B82Y5/00 ,  A61K2300/00

    摘要： It was surprisingly found that a-trioxopyrimidine-cyclodextrin-complex formed of a trioxopyrimidine derivative represented by the below-described formula (I) and a water-soluble cyclodextrin (further abbreviated as CD) exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent. Accordingly, the present invention provides a trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a cyclodextrin, preferably α-, β- or γ-cyclodextrin or a water-soluble cyclodextrin derivative (water-soluble being defined as a solubility of at least 0.5 gr/100 ml water at 25° C.), wherein the trioxopyrimidine derivative is represented by formula (I). It was furthermore found that such a trioxopyrimidine complex with cyclodextrin and an adjuvant such as L-lysine or L-arginine show improved water solubility and bioavailability, excellent stability, and low topical stimulation and is useful as a therapeutic agent.

    摘要翻译： 令人惊奇地发现由下式（I）表示的三氧嘧啶衍生物和水溶性环糊精（进一步缩写为CD）形成的α-三氧嘧啶 - 环糊精复合物显示出增强的水溶性，优异的稳定性和低的局部 刺激并且可用作治疗剂。 因此，本发明提供由三氧嘧啶衍生物或其盐与环糊精形成的三氟嘧啶 - 环糊精复合物，优选α-，β-或γ-环糊精或水溶性环糊精衍生物（水溶性定义为溶解度 在25℃下为至少0.5gr / 100ml水），其中三氧嘧啶衍生物由式（I）表示。 此外，发现这种与环糊精和L-赖氨酸或L-精氨酸等佐剂的三氧嘧啶配合物显示改善的水溶性和生物利用度，优异的稳定性和低的局部刺激，并且可用作治疗剂。

    Water soluble curcumin compositions for use in anti-cancer and anti-inflammatory therapy
    8.
    发明授权
    Water soluble curcumin compositions for use in anti-cancer and anti-inflammatory therapy 有权
    用于抗癌和抗炎治疗的水溶性姜黄素组合物

    公开(公告)号：US08772265B2

    公开(公告)日：2014-07-08

    申请号：US12995126

    申请日：2009-05-26

    申请人： Philippe Neven ,  Didier Serteyn ,  Robert Kiss ,  Veronique Mathieu ,  Didier Cataldo ,  Natacha Rocks ,  Eva Scheer

    发明人： Philippe Neven ,  Didier Serteyn ,  Jacques Delarge ,  Robert Kiss ,  Veronique Mathieu ,  Didier Cataldo ,  Natacha Rocks

    IPC分类号： A01N43/04 ,  A61K31/715

    CPC分类号： B82Y5/00 ,  A61K31/724 ,  A61K45/06 ,  A61K47/6951 ,  A61K2300/00

    摘要： The present invention relates to the medical field. In a first aspect the present invention relates to novel water soluble cyclodextrin-curcumin complexes having a pharmacological activity, in particular an anti-tumor and/or anti-inflammatory activity, and improved physico-chemical properties. In a second aspect, the present invention relates to a method for preparation of said water soluble curcumin derivatives. The invention further relates in a third aspect to a pharmaceutical composition comprising an effective amount of said water soluble curcumin derivatives. In a fourth aspect, the present invention concerns the use of said water soluble cucumin derivatives as a medicament and the use of said water soluble curcumin derivatives for the preparation of a medicament for the treatment of cancer and inflammatory diseases. In a fifth aspect, the present invention relates to the use of a pharmaceutical composition comprising said water soluble curcumin derivatives in the treatment of cancer and inflammatory diseases and to a new pharmaceutical composition comprising said water soluble curcumin derivatives.

    摘要翻译： 本发明涉及医疗领域。 在第一方面，本发明涉及具有药理活性，特别是抗肿瘤和/或抗炎活性以及改善的物理化学性质的新的水溶性环糊精 - 姜黄素复合物。 在第二方面，本发明涉及一种制备所述水溶性姜黄素衍生物的方法。 本发明在第三方面进一步涉及包含有效量的所述水溶性姜黄素衍生物的药物组合物。 在第四方面，本发明涉及所述水溶性姜黄素衍生物作为药物的用途，以及所述水溶性姜黄素衍生物在制备用于治疗癌症和炎性疾病的药物中的用途。 在第五方面，本发明涉及包含所述水溶性姜黄素衍生物的药物组合物在治疗癌症和炎性疾病中的用途以及包含所述水溶性姜黄素衍生物的新药物组合物的用途。

    WATER SOLUBLE CURCUMIN COMPOSITIONS FOR USE IN ANTI-CANCER AND ANTI-INFLAMMATORY THERAPY
    9.
    发明申请
    WATER SOLUBLE CURCUMIN COMPOSITIONS FOR USE IN ANTI-CANCER AND ANTI-INFLAMMATORY THERAPY 有权
    用于抗癌和抗炎治疗的水溶性曲霉素组合物

    公开(公告)号：US20110257126A1

    公开(公告)日：2011-10-20

    申请号：US12995126

    申请日：2009-05-26

    申请人： Philippe Neven ,  Didier Serteyn ,  Jacques Delarge ,  Eva Scheer ,  Robert Kiss ,  Veronique Mathieu ,  Didier Cataldo ,  Natacha Rocks

    发明人： Philippe Neven ,  Didier Serteyn ,  Jacques Delarge ,  Eva Scheer ,  Robert Kiss ,  Veronique Mathieu ,  Didier Cataldo ,  Natacha Rocks

    IPC分类号： A61K31/724 ,  A61P35/00 ,  A61P29/00 ,  A61P35/02 ,  A61P17/06 ,  A61P25/00 ,  A61P1/00 ,  A61P25/28 ,  A61P25/16 ,  A61P9/10 ,  A61P3/10 ,  A61P19/02 ,  A61P37/06 ,  A61P37/08 ,  C08B37/16

    CPC分类号： B82Y5/00 ,  A61K31/724 ,  A61K45/06 ,  A61K47/6951 ,  A61K2300/00

    摘要： The present invention relates to the medical field. In a first aspect the present invention relates to novel water soluble cyclodextrin-curcumin complexes having a pharmacological activity, in particular an anti-tumour and/or anti-inflammatory activity, and improved physico-chemical properties. In a second aspect, the present invention relates to a method for preparation of said water soluble curcumin derivatives. The invention further relates in a third aspect to a pharmaceutical composition comprising an effective amount of said water soluble curcumin derivatives. In a fourth aspect, the present invention concerns the use of said water soluble cucumin derivatives as a medicament and the use of said water soluble curcumin derivatives for the preparation of a medicament for the treatment of cancer and inflammatory diseases. In a fifth aspect, the present invention relates to the use of a pharmaceutical composition comprising said water soluble curcumin derivatives in the treatment of cancer and inflammatory diseases and to a new pharmaceutical composition comprising said water soluble curcumin derivatives.

    摘要翻译： 本发明涉及医疗领域。 在第一方面，本发明涉及具有药理活性，特别是抗肿瘤和/或抗炎活性以及改善的物理化学性质的新的水溶性环糊精 - 姜黄素复合物。 在第二方面，本发明涉及一种制备所述水溶性姜黄素衍生物的方法。 本发明在第三方面进一步涉及包含有效量的所述水溶性姜黄素衍生物的药物组合物。 在第四方面，本发明涉及所述水溶性姜黄素衍生物作为药物的用途，以及所述水溶性姜黄素衍生物在制备用于治疗癌症和炎性疾病的药物中的用途。 在第五方面，本发明涉及包含所述水溶性姜黄素衍生物的药物组合物在治疗癌症和炎性疾病中的用途以及包含所述水溶性姜黄素衍生物的新药物组合物的用途。

    Use of a trioxopyrimidine for the treatment and prevention of bronchial inflammatory diseases
    10.
    发明申请
    Use of a trioxopyrimidine for the treatment and prevention of bronchial inflammatory diseases 审中-公开
    使用三氧嘧啶治疗和预防支气管炎症性疾病

    公开(公告)号：US20070225253A1

    公开(公告)日：2007-09-27

    申请号：US10594101

    申请日：2005-03-31

    申请人： Didier Cataldo

    发明人： Didier Cataldo

    IPC分类号： A61K31/724 ,  A61K31/506

    CPC分类号： A61K31/724 ,  A61K31/515

    摘要： The invention provides the use of a trioxopyrimidine compound having an inhibitory activity against MMP-1, MMP-2, MMP-3, MMP-9 and MMP-14 defined as a) an IC50 value of less than 5 μM for MMP-2, MMP-9 and MMP-14 each; b) a ratio of more than 100 for the IC50 values of MMP-1:MMP-2, MMP-1: MMP-9, MMP-1:MMP-14; and c) a ratio of more than 10 for the IC50 values of MMP-3:MMP-2, MMP-3:MMP-9, MMP-3:MMP-14, for the manufacturing of a medicament for the treatment or prevention of bronchial inflammatory diseases.

    摘要翻译： 本发明提供了具有对MMP-1，MMP-2，MMP-3，MMP-9和MMP-14具有抑制活性的三氧嘧啶化合物的用途，其定义为a）较小的IC 50 MMP-2，MMP-9和MMP-14各为5μM; b）MMP-1：MMP-2，MMP-1：MMP-9，MMP-1：MMP-14的IC 50值的比值大于100; 和c）对于MMP-3：MMP-2，MMP-3：MMP-9，MMP-3：MMP-14的IC 50值的超过10的比例用于制造 用于治疗或预防支气管炎症疾病的药物。