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    Stable lyophilized anthracycline glycosides
    3.
    发明申请
    Stable lyophilized anthracycline glycosides 审中-公开
    稳定的冻干蒽环类苷

    公开(公告)号：US20070004653A1

    公开(公告)日：2007-01-04

    申请号：US11433026

    申请日：2006-05-11

    申请人： Roberto Arosio ,  Marco Villa ,  Simonetta Amati

    发明人： Roberto Arosio ,  Marco Villa ,  Simonetta Amati

    IPC分类号： A61K31/7048

    CPC分类号： A61K9/19 ,  A61K31/704 ,  A61K31/7048 ,  A61K47/12 ,  A61K47/34

    摘要： The present invention provides lyophilized and stable lyophilized anthracycline glycoside salts, in particular, the hydrochloride salt. Also, the present invention provides methods of stabilizing these anthracycline glycoside salts, and methods for producing stable lyophilized anthracycline glycoside salts, such as for example the antineoplastic compound idarubicin hydrochloride, or the compounds doxorubicin hydrochloride, and epirubicin hydrochloride.

    摘要翻译： 本发明提供冻干和稳定的冻干蒽环苷糖苷盐，特别是盐酸盐。 此外，本发明提供了稳定这些蒽环苷类糖苷盐的方法，以及用于制备稳定的冻干蒽环苷类糖苷盐的方法，例如抗肿瘤化合物盐酸伊多比星，或盐酸多柔比星化合物和盐酸表柔比星。

    Process for preparing N-methyl-3-(P-trifluoromethylphenoxy)-3-phenyl-propylamine and salts thereof in a highly pure form
    5.
    发明授权
    Process for preparing N-methyl-3-(P-trifluoromethylphenoxy)-3-phenyl-propylamine and salts thereof in a highly pure form 失效
    以高纯度形式制备N-甲基-3-（对三氟甲基苯氧基）-3-苯基 - 丙胺及其盐的方法

    公开(公告)号：US5847214A

    公开(公告)日：1998-12-08

    申请号：US889162

    申请日：1997-07-07

    申请人： Roberto Arosio ,  Stefano Giovanni Vittorio Beratto ,  Vittorio Rossetti

    发明人： Roberto Arosio ,  Stefano Giovanni Vittorio Beratto ,  Vittorio Rossetti

    IPC分类号： C07C213/08 ,  C07C217/48 ,  C07C213/06

    CPC分类号： C07C213/08

    摘要： The present invention relates to a process for preparing N-methyl-3-(p-trifluoromethylphenoxy)-3-phenyl-propylamine and pharmaceutically acceptable acid addition salts thereof. The process in accordance with the present invention comprises reacting 1-phenyl-3-(N-methylamine) propane-1-ol with 1-chloro-4-trifluoromethylbenzene, in the presence of an hydroxide of an alkaline metal in a dipolar aprotic solvent non saponifiable in reaction conditions. The process in accordance with the present invention further comprises a final crystallization step which allows to obtain the active ingredient in a highly pure crystalline form.

    摘要翻译： 本发明涉及N-甲基-3-（对三氟甲基苯氧基）-3-苯基 - 丙胺及其药学上可接受的酸加成盐的制备方法。 根据本发明的方法包括使1-苯基-3-（N-甲胺）丙-1-醇与1-氯-4-三氟甲基苯在偶极非质子溶剂中的碱金属氢氧化物存在下反应 在反应条件下不皂化。 根据本发明的方法还包括最终结晶步骤，其允许获得高纯度结晶形式的活性成分。

    Process for the preparation of taurocholanic acids
    6.
    发明授权
    Process for the preparation of taurocholanic acids 失效
    制备牛磺胆酸的方法

    公开(公告)号：US5565587A

    公开(公告)日：1996-10-15

    申请号：US458618

    申请日：1995-06-02

    申请人： Roberto Arosio ,  Vittorio Rossetti

    发明人： Roberto Arosio ,  Vittorio Rossetti

    IPC分类号： C07J9/00 ,  C07J41/00 ,  C07J75/00

    CPC分类号： C07J9/005 ,  C07J41/0061

    摘要： A process is described for the preparation of taurocholanic acids of formula (I): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid and E is hydrogen or a methyl group, by reacting the corresponding cholanic acid with the chloride of an acid having a tertiary carbon in the alpha-position, and treating the resulting mixed anhydride with taurine.

    摘要翻译： 描述了制备式（I）的牛磺胆酸的方法：其中A完成胆碱酸的5β-环戊烷 - 氢化菲菲结构，E是氢或甲基，通过使相应的胆碱 与α-位上具有叔碳的酸的氯化物酸反应，并用牛磺酸处理得到的混合酸酐。

    Intermediate for use in the preparation of taurocholanic acids
    7.
    发明授权
    Intermediate for use in the preparation of taurocholanic acids 失效
    用于制备牛磺胆酸的中间体

    公开(公告)号：US5508453A

    公开(公告)日：1996-04-16

    申请号：US246148

    申请日：1994-05-19

    申请人： Roberto Arosio ,  Vittorio Rossetti

    发明人： Roberto Arosio ,  Vittorio Rossetti

    IPC分类号： C07J9/00 ,  C07J41/00 ,  C07J75/00

    CPC分类号： C07J9/005 ,  C07J41/0061

    摘要： The present invention relates to intermediates for use in the preparation of taurocholanic acids. The intermediates have the following formula (IV): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid; E is hydrogen or a methyl; and R is a hydrocarbon residue bonded to the carbonyl group by a tertiary carbon.

    摘要翻译： 本发明涉及用于制备牛磺胆酸的中间体。 中间体具有下式（Ⅳ）：胆酸的环戊烷四氢菲结构; E是氢或甲基; 并且R是通过叔碳键合到羰基的烃残基。