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    PROCESS FOR PREPARING AMORPHOUS RIFAXMIN AND THE AMORPHOUS RIFAXIMIN THUS OBTAINED
    72.
    发明申请
    PROCESS FOR PREPARING AMORPHOUS RIFAXMIN AND THE AMORPHOUS RIFAXIMIN THUS OBTAINED 有权
    制备不规则的生物素和获得的非晶体RIFAXIMIN的方法

    公开(公告)号：US20150011750A1

    公开(公告)日：2015-01-08

    申请号：US14261138

    申请日：2014-04-24

    申请人： Emilio Vecchio ,  Roberta Pizzocaro

    发明人： Emilio Vecchio ,  Roberta Pizzocaro

    IPC分类号： C07D491/22

    CPC分类号： C07D491/22 ,  C07D498/22

    摘要： A process is described which enables Rifaximin in a completely amorphous form to be obtained. Said process comprises the steps of dissolving crude Rifaximin in absolute ethanol while hot and then collecting after precipitation by—cooling the title compound under amorphous form.

    摘要翻译： 描述了能够获得完全无定形形式的利福昔明的方法。 所述方法包括以下步骤：在热的同时将粗Rifaximin溶解在无水乙醇中，然后沉淀后通过无定形形式冷却标题化合物进行收集。

    MORPHINAN DERIVATIVE
    74.
    发明申请
    MORPHINAN DERIVATIVE 有权
    莫宁衍生物

    公开(公告)号：US20140343015A1

    公开(公告)日：2014-11-20

    申请号：US14343218

    申请日：2012-09-07

    申请人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    发明人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

    IPC分类号： C07D491/18 ,  C07F7/18 ,  C07D487/08

    CPC分类号： C07D491/18 ,  C07D471/08 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07F7/1804

    摘要： A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like,R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like,X represents O or CH2, andY represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

    摘要翻译： 由以下通式（I）表示的吗啡喃衍生物（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子） 芳烷基（芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基，C 6-10芳基，芳烷基（芳基 部分具有6至10个碳原子，并且亚烷基部分具有1至5个碳原子）等，R3，R4和R5表示氢，羟基，氨基甲酰基，C1-6烷氧基，C6-10芳氧基等，R6a， R6b，R7，R8，R9和R10表示氢等，X表示O或CH2，Y表示C = O，SO2，原子键等）或其酸加成盐作为止痛剂 。

    Compositions and methods of making a photoactive agent
    76.
    发明授权
    Compositions and methods of making a photoactive agent 有权
    制备光敏剂的组合物和方法

    公开(公告)号：US08822677B2

    公开(公告)日：2014-09-02

    申请号：US13473395

    申请日：2012-05-16

    申请人： Leon Xu ,  Alexander J. Pallenberg

    发明人： Leon Xu ,  Alexander J. Pallenberg

    IPC分类号： C07D487/22

    CPC分类号： C07D491/22

    摘要： An improved two stage reaction process for production of mono-L-aspartyl chlorin e6. In a first stage, the activation reaction between chlorin e6 and a carbodiimide produces a previously unknown anhydride in an activation reaction product (Formula I). This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e6. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture.

    摘要翻译： 用于生产单-L-天冬氨酰二氢卟酚e6的改进的两阶段反应方法。 在第一阶段，二氢卟酚e6与碳二亚胺之间的活化反应在活化反应产物中产生以前未知的酸酐（式I）。 将该反应产物纯化以除去相当大比例的二-L-天冬氨酰二氢卟酚e6的前体。 纯化的活化反应产物含有较高浓度的先前未知的酸酐。 该纯化的反应产物用于第二阶段：纯化的活化反应产物与天冬氨酸的偶联反应。 偶联反应产生显着降低二-L-天冬氨酰二氢卟吩e6浓度的偶联反应产物。 这种减少的二-L-天冬氨酰二氢卟吩e6浓度有助于从偶联反应混合物中纯化单-L-天冬氨酰二ine素e6。