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    MANGANESE CHELATES WITH HIGH RELAXIVITY IN SERUM
    1.
    发明公开
    MANGANESE CHELATES WITH HIGH RELAXIVITY IN SERUM 有权
    锰在血清中高度放松

    公开(公告)号：EP1061957A1

    公开(公告)日：2000-12-27

    申请号：EP99910336.9

    申请日：1999-03-09

    申请人： BRACCO S.p.A. ,  DIBRA S.p.A.

    发明人： BROCCHETTA, Marino ,  CALABI, Luisella ,  FEDELI, Franco ,  MANFREDI, Giuseppe ,  PALEARI, Lino ,  UGGERI, Fulvio

    IPC分类号： A61K49/00 ,  C07C229/28 ,  C07C229/36 ,  C07C233/83 ,  C07D209/20 ,  C07C229/22

    CPC分类号： A61K49/06 ,  C07C229/36

    摘要： Compounds of formula (I) wherein: R1, R2 which are the same or different, are a hydrogen atom, or a -(CH2)m-O-(CH2)n-R3 group, wherein R3 is an aryl residue, m is an integer 1 to 5 and n is an integer 1 to 4, with the proviso that R1 and R2 cannot be at the same time hydrogen, as well as the optically active forms of the chelates thereof with Mn(II) and the salts thereof with physiologically compatible organic bases selected from primary, secondary, tertiary amines or basic amino acids, or with inorganic bases whose cations are sodium, potassium, magnesium, calcium, or mixtures thereof, are disclosed.

    摘要翻译： 其中：R 1，R 2相同或不同，为氢原子或 - （CH 2）m -O-（CH 2）n -R 3基团的式（I）化合物，其中R 3为芳基，m为整数 1至5，并且n是整数1至4，条件是R 1和R 2不能同时为氢，以及其与Mn（II）螯合物的光学活性形式及其盐与生理相容 公开了选自伯，仲，叔胺或碱性氨基酸的有机碱或其阳离子为钠，钾，镁，钙或其混合物的无机碱。

    DIAGNOSTIC IMAGING CONTRAST AGENT WITH IMPROVED IN-SERUM-RELAXIVITY
    4.
    发明公开
    DIAGNOSTIC IMAGING CONTRAST AGENT WITH IMPROVED IN-SERUM-RELAXIVITY 失效
    诊断剂BILDERZEUGUNGIS KONTRASTMITTEL MIT VERBESSERTER IN-SERUM-RELAXATION

    公开(公告)号：EP0920411A1

    公开(公告)日：1999-06-09

    申请号：EP97938855.0

    申请日：1997-07-24

    申请人： BRACCO S.p.A. ,  DIBRA S.p.A.

    发明人： ANELLI, Pier, Lucio ,  LOLLI, Marco ,  FEDELI, Franco ,  VIRTUANI, Mario

    IPC分类号： A61K49 ,  C07C229 ,  C07C233 ,  C07C237 ,  C07D209 ,  C07D263 ,  C07F5

    CPC分类号： A61K49/06 ,  C07C229/26 ,  C07C229/36 ,  C07C233/48 ,  C07C233/51 ,  C07C237/06 ,  C07C2601/14 ,  C07D209/20 ,  C07D263/26

    摘要： Compounds of formula (I), both in the racemic and optically active forms in which R is H, or a linear or branched, saturated or unsaturated C1-C20 alkyl, optionally interrupted by one or more -CH(OH)-, -CONH-, -NHCO-, -CO-, -CH(NH2)-, -SO-, -SO2-, SO2NH- groups and/or one or more N, O, S atoms optionally substituted with one or more -COOH groups and/or amide or ester derivatives thereof, and in which said alkyl chain is interrupted or substituted by at least 2, which are independently the same or different, isolated or fused, cyclic L residues, with the proviso that, when some L residues are fused together, the resulting polycyclic unit comprises no more than 3 cyclic group, and in which L is a carbocyclic or heterocyclic, saturated or unsaturated or aromatic cyclic unit, comprising from 5 to 6 atoms, optionally substituted by one or more X groups, which are independently the same or different, in which X is OH, halogen, NH2, NHZ, N(Z)2, -OZ-, -SZ-, COZ, where the Z groups can independently be a C1-C5 linear or branched alkyl, optionally substituted with one or more -OH, -COOH or alkoxy groups, or said X group is a -COOH group or a derivative thereof, such as an ester or an amido group, or -SOZH group or an amino derivative of the same; R1 is the same as R with the provisos that: R and R1 cannot be at the same time H; when R is different from H, R1 is H; when R1 is different from H, R is H; as well as the complexes of the compounds of fomula (I) with metal ions of atomic number from 20 to 31, 39, from 42 to 44, 49 and from 57 to 83 and the salts thereof with physiologically acceptable organic bases selected from primary, secondary or tertiary amines, or basic amino acids, or with inorganic bases the cations of which are sodium, potassium, magnesium, calcium or the mixtures thereof. Said compounds are useful as contrast agents in Magnetic Resonance Imaging and have improved relaxivitty in human serum.

    摘要翻译： 式（I）的化合物，其外消旋和旋光活性，其中R是H，或直链或支链饱和或不饱和的C 1 -C 20烷基，任选被一个或多个-CH（OH） - ，-CONH - ， - NHCO - ， - SO - ， - SO 2 - ，SO 2 NH - 基团和/或一个或多个任选被一个或多个-COOH基团取代的N，O， 或其酰胺或酯衍生物，其中所述烷基链被至少2个间隔或取代，其独立地是相同或不同的分离或稠合的环状L残基，条件是当一些L残基融合时 所得的多环单元一起包含不超过3个环状基团，其中L是碳环或杂环的饱和或不饱和或芳族环状单元，其包含5至6个原子，任选被一个或多个X基团取代， 独立地相同或不同，其中X是OH，卤素，NH 2，NHZ，N（Z）2，-OZ-，-SZ-，COZ，其中Z基团可以独立地 本发明是一个C1-C5直链或支链烷基，任选被一个或多个-OH，-COOH或烷氧基取代，或所述X基团是-COOH基团或其衍生物，如酯或酰胺基，或 -SOZH基或其氨基衍生物; R1与R相同，条件是：R和R1不能同时为H; 当R不同于H时，R 1为H; 当R1不同于H时，R为H; 以及式（I）化合物与原子序数为20-31,39,42,49和57至83的金属离子的络合物，以及其盐与生理上可接受的有机碱选自伯， 仲胺或叔胺或碱性氨基酸，或其阳离子为钠，钾，镁，钙或其混合物的无机碱。 所述化合物可用作磁共振成像中的造影剂，并且在人血清中具有改善的松弛度。

    PROCESS FOR THE PURIFICATION OF AN AMINOALCOHOL
    7.
    发明公开
    PROCESS FOR THE PURIFICATION OF AN AMINOALCOHOL 失效
    清理方法的氨基醇

    公开(公告)号：EP0883597A1

    公开(公告)日：1998-12-16

    申请号：EP97952845.0

    申请日：1997-12-01

    申请人： DIBRA S.p.A.

    发明人： DESANTIS, Nicola ,  FEDELI, Franco

    IPC分类号： A61K49 ,  C07C213 ,  C07C215 ,  C07C231 ,  C07C237

    CPC分类号： C07C213/02 ,  C07C213/10

    摘要： The present invention relates to a process for the preparation of 2-amino-1,3-propanediol, having a content of organic impurities lower than 0.1 % and inorganic impurities lower than 0.05 %, comprising the following steps: a) formation of a 2-amino-1,3-propanediol salt with an acid; b) crystallization of the salt resulting from step a) from an aqueous or a hydro-organic mixture with a solvent selected from the group consisting of an alcohol of the general formula R-OH, wherein R is a C1-C6 straight or branched alkyl chain, and a mono (C1-C3)alkylether of the (C3-C7)alkylcellosolve group; c) elution of the free base by using ion exchangers to give an aqueous solution of said base; d) precipitation or crystallization of the solid 2-amino-1,3-propanediol from a solvent as defined in step b).