USE OF LEVOCETIRIZINE FOR THE PREPARATION OF A DRUG
    12.
    发明申请
    USE OF LEVOCETIRIZINE FOR THE PREPARATION OF A DRUG 审中-公开
    用于制备药物的乙酰胆碱酯酶的使用

    公开(公告)号:WO2005077371A1

    公开(公告)日:2005-08-25

    申请号:PCT/EP2005/050543

    申请日:2005-02-08

    Inventor: KOUZAN, Serge

    CPC classification number: A61K31/495

    Abstract: The present invention relates to a pharmaceutical use of levocetirizine for the prevention of symptoms or exacerbation of allergic asthma.

    Abstract translation: 本发明涉及左西替利嗪的药物用途,用于预防过敏性哮喘的症状或加重。

    PYROGLUTAMATE SALTS AND THEIR USE IN THE OPTICAL RESOLUTION OF INTERMEDIATES FOR THE SYNTHESIS OF DEXTROCETIRIZINE AND LEVOCETIRIZINE
    14.
    发明申请
    PYROGLUTAMATE SALTS AND THEIR USE IN THE OPTICAL RESOLUTION OF INTERMEDIATES FOR THE SYNTHESIS OF DEXTROCETIRIZINE AND LEVOCETIRIZINE 审中-公开
    吡咯烷酮盐及其在中间体光合作用中的用途,用于合成去氧胆酸酯酶和左旋胆碱酯酶

    公开(公告)号:WO2006094648A1

    公开(公告)日:2006-09-14

    申请号:PCT/EP2006/001676

    申请日:2006-02-23

    CPC classification number: C07D295/088 C07D207/28

    Abstract: The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]- ethoxyacetamide - (S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide - (S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide - (R)-pyrrolidone-5-carboxylic acid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide - (R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.

    Abstract translation: 本发明涉及(S)-2- [4-(4-氯二苯甲基)哌嗪-1-基] - 乙氧基乙酰胺 - (S) - 吡咯烷酮-5-羧酸盐; (R)-2- [4-(4-氯二苯甲基)哌嗪-1-基] - 乙氧基乙酰胺 - (S) - 吡咯烷酮-5-羧酸盐; (S)-2- [4-(4-氯二苯甲基)哌嗪-1-基] - 乙氧基乙酰胺 - (R) - 吡咯烷酮-5-羧酸盐; 或(R)-2- [4-(4-氯二苯甲基)哌嗪-1-基] - 乙氧基己酰胺 - (R) - 吡咯烷酮-5-羧酸盐。 本发明还涉及制备(S)-2- [4-(4-氯二苯甲基)哌嗪-1-基] - 乙氧基乙酰胺(I)和(R)-2- [4-(4-氯二苯甲基) 哌嗪-1-基] - 乙氧基乙酰胺(II)。 这些化合物分别是合成右旋西西替丁和左西替利嗪的中间体。

    NEW PIPERAZINE DERIVATIVES AND THEIR USE AS SYNTHESIS INTERMEDIATES
    16.
    发明申请
    NEW PIPERAZINE DERIVATIVES AND THEIR USE AS SYNTHESIS INTERMEDIATES 审中-公开
    新的哌嗪衍生物及其作为合成中间体的用途

    公开(公告)号:WO2004065360A2

    公开(公告)日:2004-08-05

    申请号:PCT/EP2004/000399

    申请日:2004-01-20

    IPC: C07D

    CPC classification number: C07D271/07 C07D295/15

    Abstract: The present invention relates to new enantiomerically pure piperazine derivatives of formula (I) wherein Y represents hydroxy or a leaving group and n is 1, 2, 3, 4 or 5, and to their use as synthesis intermediates, especially for the preparation of pharmaceutically active compounds.

    Abstract translation: 本发明涉及式(I)的新的对映体纯的哌嗪衍生物,其中Y代表羟基或离去基团,n是1,2,3,4或5,并且它们用作合成中间体,特别是用于制备药学上 活性化合物。

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