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    Process for the Preparation of Doxorubicin Conjugates with Lactosaminated Human Albumin
    1.
    发明申请
    Process for the Preparation of Doxorubicin Conjugates with Lactosaminated Human Albumin 失效
    用乳糖胺化人白蛋白制备多柔比星缀合物的方法

    公开(公告)号：US20070219351A1

    公开(公告)日：2007-09-20

    申请号：US11579857

    申请日：2005-05-04

    申请人： Luigi Fiume ,  Giuseppina Distefana ,  Marcella Lanza

    发明人： Luigi Fiume ,  Giuseppina Distefana ,  Marcella Lanza

    IPC分类号： C07K14/765 ,  G01N33/53

    CPC分类号： A61K47/6809

    摘要： A procedure is described for conjugating the hydrazone derivatives of doxorubicin having a maleimide terminal group to lactosaminated human albumin (L-HAS). The procedure is based on the use of trialkylphosphines to reduce the disulfide bonds of the protein and make its SH groups available for the formation of the thioether bond. In comparison with the conjugation obtained by using thiol reducing agents, such as dithiothreitol, this has the advantage that even when it is performed under very simple conditions, specifically without using an inert atmosphere, in the absence of oxygen, and without preliminary purification of the “reduced” L-HAS, it does not bring about the formation of a precipitate in the reaction means. In comparison with conjugation to L-HAS thiolated by using iminothiolane, the novel procedure has the advantage of greater simplicity and of not introducing exogenous molecules into the L-HAS in order to make the SH groups available.

    摘要翻译： 描述了将具有马来酰亚胺端基的多柔比星的腙衍生物与乳糖胺化的人白蛋白（L-HAS）缀合的方法。 该方法基于使用三烷基膦来降低蛋白质的二硫键并使其SH基团可用于形成硫醚键。 与通过使用硫醇还原剂（例如二硫苏糖醇）获得的缀合相比，这具有的优点是即使在非常简单的条件下进行，特别是在不使用惰性气氛的情况下，在不存在氧的情况下， “减少”L-HAS，不会在反应装置中形成沉淀物。 与通过使用亚氨基硫醇硫醇化的L-HAS的缀合相比，该新方法具有更大的简单性和不将外源分子引入L-HAS以使SH基团可用的优点。

    Use of Conjugates of Doxorubicin with Lactosaminated Albumin
    3.
    发明申请
    Use of Conjugates of Doxorubicin with Lactosaminated Albumin 审中-公开
    使用多柔比星与乳糖白蛋白的缀合物

    公开(公告)号：US20080227710A1

    公开(公告)日：2008-09-18

    申请号：US12067211

    申请日：2006-09-19

    申请人： Luigi Fiume ,  Giuseppina Di Stefano

    发明人： Luigi Fiume ,  Giuseppina Di Stefano

    IPC分类号： A61K38/38 ,  A61P35/00

    CPC分类号： A61K47/643

    摘要： The present invention refers to the use of a conjugate of doxorubicin with lactosaminated human albumin for the preparation of a pharmaceutical composition useful in the treatment of hepatocellular carcinomas (HCCs) which do not express the asialoglycoprotein receptor (ASGP-R). The conjugate which was previously prepared and studied only for the treatment of HCCs expressing the ASGP-R, has now been shown to possess the potentiality of a beneficial use also in the treatment of the HCCs which do not have the receptor. Therefore, compositions containing the conjugate could be administered for treatment of all HCCs, without the need of a preliminary tumor biopsy to demonstrate the presence or the absence of the receptor.

    摘要翻译： 本发明涉及多柔比星与乳糖胺化人白蛋白的缀合物在制备用于治疗不表达唾液酸糖蛋白受体（ASGP-R）的肝细胞癌（HCC））的药物组合物中的用途。 预先制备和研究仅用于治疗表达ASGP-R的HCC的缀合物现已显示具有有益用途的潜力，也用于治疗不具有该受体的HCC。 因此，可以施用含有缀合物的组合物来治疗所有HCC，而不需要进行初步的肿瘤活检来证实受体的存在或不存在。

    Process of conjugation of antiviral nucleosides with lactosaminated human albumin
    4.
    发明授权
    Process of conjugation of antiviral nucleosides with lactosaminated human albumin 失效
    抗病毒核苷与乳糖胺化人白蛋白共轭的方法

    公开(公告)号：US5594110A

    公开(公告)日：1997-01-14

    申请号：US256415

    申请日：1994-09-30

    申请人： Luigi Fiume ,  Corrado Busi ,  Giuseppina D. Stefano ,  Alessandro Mattioli

    发明人： Luigi Fiume ,  Corrado Busi ,  Giuseppina D. Stefano ,  Alessandro Mattioli

    IPC分类号： A61K47/48 ,  C07K1/00 ,  A61K38/16

    CPC分类号： A61K47/48284

    摘要： A conjugate of an antiviral nucleoside with a lactosaminated human albumin (L-HSA) and its method of preparation is described. The method of preparation involves the reaction of an antiviral phosphorylated nucleoside in the form of an imidizolide with L-HSA at a pH above 7.5 and running the reaction until the desired molar ratio of drug to L-HSA is obtained.

    摘要翻译： PCT No.PCT / EP93 / 03261 Sec。 371日期1994年9月30日 102（e）1994年9月30日PCT PCT 1993年11月20日PCT公布。 公开号WO94 / 12218 PCT 日期1994年6月9日描述了抗病毒核苷与乳糖胺化人白蛋白（L-HSA）的缀合物及其制备方法。 制备方法涉及在高于7.5的pH下将咪唑来酰胺与L-HSA形式的抗病毒磷酸化核苷酸反应，并进行反应直到获得所需的药物与L-HSA的摩尔比。

    Process for the preparation of doxorubicin conjugates with lactosaminated human albumin
    7.
    发明授权
    Process for the preparation of doxorubicin conjugates with lactosaminated human albumin 失效
    用乳糖胺化人白蛋白制备多柔比星缀合物的方法

    公开(公告)号：US07528234B2

    公开(公告)日：2009-05-05

    申请号：US11579857

    申请日：2005-05-04

    申请人： Luigi Fiume ,  Giuseppina Di Stefano ,  Marcella Lanza

    发明人： Luigi Fiume ,  Giuseppina Di Stefano ,  Marcella Lanza

    IPC分类号： C07K14/765 ,  C07K1/02 ,  C07K1/06

    CPC分类号： A61K47/6809

    摘要： A procedure is described for conjugating the hydrazone derivatives of doxorubicin having a maleimide terminal group to lactosaminated human albumin (L-HSA). The procedure is based on the use of trialkyiphosphines to reduce the disulfide bonds of the protein and make its SH groups available for the formation of the thioether bond. In comparison with the conjugation obtained by using thiol reducing agents, such as dithiothreitol, this has the advantage that even when it is performed under very simple conditions, specifically without using an inert atmosphere, in the absence of oxygen, and without preliminary purification of the “reduced” L-HSA, it does not bring about the formation of a precipitate in the reaction means. In comparison with conjugation to L-HSA thiolated by using iminothiolane, the novel procedure has the advantage of greater simplicity and of not introducing exogenous molecules into the L-HSA in order to make the SH groups available.

    摘要翻译： 描述了将具有马来酰亚胺端基的多柔比星的腙衍生物与乳糖胺化的人白蛋白（L-HSA）结合的方法。 该方法基于使用三烷基膦来降低蛋白质的二硫键并使其SH基团可用于形成硫醚键。 与通过使用硫醇还原剂（例如二硫苏糖醇）获得的缀合相比，这具有的优点是即使在非常简单的条件下进行，特别是在不使用惰性气氛的情况下，在不存在氧的情况下， “还原”的L-HSA，不会在反应装置中形成沉淀。 与使用亚氨基硫醇硫醇化的L-HSA的缀合相比，该新方法具有更大的简单性和不将外源分子引入L-HSA以使SH基团可用的优点。