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207 条记录 (耗时 0.02 秒)

    PALIPERIDONE DERIVATIVES
    21.
    发明公开
    PALIPERIDONE DERIVATIVES 审中-公开
    PALIPERIDONE衍生物

    公开(公告)号：EP2178872A1

    公开(公告)日：2010-04-28

    申请号：EP08785075.6

    申请日：2008-07-25

    申请人： Synthon B.V.

    发明人： BARTL, Jiri ,  PICHA, Frantisek

    IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P25/18

    CPC分类号： C07D471/04

    摘要： A compound of formula (1) is useful as a pharmaceutical and as an intermediate in making paliperidone, wherein Y is an acid-sensitive group of the formula (A') in which X represents an oxygen atom, a sulfur atom, or an -NH- group; Z represents a C2-C7 alkylene bridge; and R represents hydrogen or a C1-C4 alkyl group.

    摘要翻译： 式（1）化合物可用作制备帕潘立酮的药物和中间体，其中Y是式（A'）的酸敏感性基团，其中X表示氧原子，硫原子或 - NH-组; Z代表C2-C7亚烷基桥; 并且R表示氢或C1-C4烷基。

    PROCESS FOR MAKING AMINOALKYLPHENYL CARBAMATES AND INTERMEDIATES THEREFOR
    24.
    发明公开
    PROCESS FOR MAKING AMINOALKYLPHENYL CARBAMATES AND INTERMEDIATES THEREFOR 有权
    用于生产AMINOALKYLPHENYL，氨基甲酸酯及其中间体

    公开(公告)号：EP2076485A2

    公开(公告)日：2009-07-08

    申请号：EP07846670.3

    申请日：2007-09-27

    申请人： Synthon B.V.

    发明人： HENAR TEJEDOR, Vinent ,  OVEREEM Arjanne ,  LAMBERTUS Thijs

    IPC分类号： C07C219/28 ,  C07C269/04 ,  C07C271/44

    CPC分类号： C07C269/04 ,  C07C219/28 ,  C07C271/44

    摘要： The invention relates to a process for making the compound of general formula (I), or an acid addition salt wherein the dotted line indicates a carbon-carbon bond on the asymmetric carbon, which process comprises the steps of a) the reaction of the compound of formula (II), wherein the dotted line has the same meaning, with bis(p-nitrophenyl)carbonate of the formula (IX) preferably at the temperature between -20 to 50°C and in an inert solvent, followed by b) the reaction of the so formed intermediate of the formula (VII-1) with ethylmethylamine of the formula (III), preferably at the temperature between -20 to 50°C and in an inert solvent, and to novel compounds and their use in the synthesis of rivastigmine.

    N-FORMYL DERIVATIVES OF PAROXETINE
    29.
    发明公开
    N-FORMYL DERIVATIVES OF PAROXETINE 有权
    帕罗西汀N-甲酰基衍生物

    公开(公告)号：EP1440067A1

    公开(公告)日：2004-07-28

    申请号：EP02768169.1

    申请日：2002-10-15

    申请人： Synthon B.V.

    发明人： HOORN, Hans, Jan ,  PETERS, Theodorus, Hendricus, Antonius ,  PICHA, Frantisek

    IPC分类号： C07D405/12 ,  A61P39/00

    CPC分类号： C07D405/12 ,  C07D211/22

    摘要： The invention relates to a compound or composition comprising N-formyl paroxetine of formula (1) and 0 to 99.97% of a paroxetine compound, based on the combined weight of said N­-formyl paroxetine and said paroxetine compound, to a pharmaceutical composition, for treating a selective serotonin reuptake inhibitor-treatable disease or condition, comprising an effective amount of a paroxetine agent and at least one pharmaceutically acceptable excipient, wherein said paroxetine agent comprises of an N-formyl paroxetine compound of formula (1) and optionally a paroxetine compound, and to a process for producing a paroxetine compound which comprises treating an N-formyl paroxetine compound of formula (1) with a de-formylation agent, to a compound having the formula (2), to a process for determining the stability or purity of a paroxetine substance or composition, which comprises assaying a paroxetine substance or composition for the presence of an N-formyl paroxetine compound of formula (1), and to a process assaying the quality of paroxetine, which comprises forming a production lot of paroxetine pharmaceutical solid dosage forms wherein each dosage form comprises paroxetine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable exipient; removing a sample of said paroxetine pharmaceutical solid dosage forms from said production lot; assaying said sample for the presence and/or amount of N-formyl paroxetine; and selling or releasing said production lot if said sample passes said assay with respect to the presence or amount of N-formyl paroxetine.