公开(公告)号：EP1061957B1

公开(公告)日：2002-10-30

申请号：EP99910336.9

申请日：1999-03-09

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

公开(公告)号：EP2408735B1

公开(公告)日：2013-06-05

申请号：EP10708209.1

申请日：2010-03-12

申请人： Bracco Imaging S.p.A

发明人： ANELLI, Pier Lucio ,  BROCCHETTA, Marino ,  FRETTA, Roberta ,  LATTUADA, Luciano ,  MORTILLARO, Armando

IPC分类号： C07C231/10 ,  C07C231/02 ,  C07C235/16 ,  C07C237/46

CPC分类号： C07C237/46 ,  C07C231/02 ,  C07C231/10 ,  C07C235/16

公开(公告)号：EP1337505B1

公开(公告)日：2008-10-15

申请号：EP01995673.9

申请日：2001-11-28

申请人： BRACCO IMAGING S.p.A.

发明人： ANELLI, Pier, Lucio ,  BROCCHETTA, Marino ,  LUX, Giovanna ,  CAPPELLETTI, Enrico

IPC分类号： C07C231/02 ,  C07C237/32 ,  C07C227/04 ,  C07C227/18 ,  C07C237/42

CPC分类号： C07C231/02 ,  C07C227/04 ,  C07C227/18 ,  C07C231/12 ,  C07C231/14 ,  C07C237/32 ,  C07C237/42

摘要： The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein R1 represents a straight or branched (C1-C4)-alkyl group, with at least the stoichiometric amount of an amine of formula H2NR.

公开(公告)号：EP2408735A1

公开(公告)日：2012-01-25

申请号：EP10708209.1

申请日：2010-03-12

申请人： Bracco Imaging S.p.A

发明人： ANELLI, Pier Lucio ,  BROCCHETTA, Marino ,  FRETTA, Roberta ,  LATTUADA, Luciano ,  MORTILLARO, Armando

IPC分类号： C07C231/10 ,  C07C235/16 ,  C07C237/52

CPC分类号： C07C237/46 ,  C07C231/02 ,  C07C231/10 ,  C07C235/16

摘要： The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available α-hydroxyacid or a salt thereof.

公开(公告)号：EP1358201B1

公开(公告)日：2009-10-07

申请号：EP02718087.6

申请日：2002-02-04

申请人： BRACCO IMAGING S.p.A.

发明人： BROCCHETTA, Marino ,  ANELLI, Pier, Lucio ,  MANFREDI, Giuseppe ,  VISIGALLI, Massimo ,  PALANO, Daniela ,  ALESSANDRONI, Laura

IPC分类号： C07J41/00

CPC分类号： C07J41/0005 ,  C07J41/0011 ,  C07J41/0055 ,  Y02P20/55

摘要： The present invention relates to a novel process for the preparation of bile esters derivatives of general formula (I), in which R0 is H or OH; R1 is H, α-OH or β-OH; R2 and R3 are independently hydrogen, straight or branched (C1-C20) alkyl optionally substituted with aryl; R5 is a straight or branched (C1-C4) alkyl and R6 is a straight or branched (C1-C4) alkyl or a benzyl group, via transamidation of the amine (V) with the 5-ocoproline derivative (II), wherein R4 is selected from the group consisting of tertbutoxycarbonyl, methoxycarbonyl, ethoxycarbonyl, 2-trimethylsilylethoxycarbonyl, cyclobutoxycarbonyl and 1-methylcyclobutoxy carbonyl, followed by the selective cleavage of the protecting group R4 under acidic conditions.

公开(公告)号：EP1140209B1

公开(公告)日：2008-08-20

申请号：EP99963556.8

申请日：1999-12-16

申请人： BRACCO IMAGING S.p.A.

发明人： ANELLI, Pier Lucio ,  BROCCHETTA, Marino ,  DE HAËN, Christoph ,  GAZZOTTI, Ornella ,  LATTUADA, Luciano ,  LUX, Giovanna ,  MANFREDI, Giuseppe ,  MOROSINI, Pierfrancesco ,  PALANO, Daniela ,  SERLETI, Michele ,  UGGERI, Fulvio ,  VISIGALLI, Massimo

IPC分类号： A61K49/00

CPC分类号： A61K49/10 ,  A61K49/085 ,  Y10S977/928 ,  Y10S977/929 ,  Y10S977/93

摘要： The use of the complexes of the compounds of general formula (I) with paramagnetic bi-trivalent metal ions selected from the group consisting of Fe?(2+), Fe(3+), Cu(2+), Cr(3+), Gd(3+), Eu(3+), Dy(3+), Yb(3+) or Mn(2+)¿, as well as 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. In formula (I) X-L-Y wherein: X is the residue of a polyaminopolycarboxylic ligand and the derivatives thereof, selected from the group consisting of: EDTA, DTPA, DOTA, DO3A, BOPTA; Y is the derivative of a bile acid selected from the group consisting of residues of cholic, chenodeoxycholic, deoxycholic, ursodeoxycholic, lithocholic acids, both as they are and functionalized at the positions having the hydroxy group as the reactive group; L is a chain linked at any position of X and the C-3, C-7, C-12 positions of Y, for the preparation of diagnostic formulations for the imaging of the blood system of the human and animal body, by means of nuclear magnetic resonance; novel compounds of general formula (I) and the diagnostic compositions containing them.

公开(公告)号：EP1358201A1

公开(公告)日：2003-11-05

申请号：EP02718087.6

申请日：2002-02-04

申请人： BRACCO IMAGING S.p.A.

发明人： BROCCHETTA, Marino ,  ANELLI, Pier, Lucio ,  MANFREDI, Giuseppe ,  VISIGALLI, Massimo ,  PALANO, Daniela ,  ALESSANDRONI, Laura

IPC分类号： C07J41/00

CPC分类号： C07J41/0005 ,  C07J41/0011 ,  C07J41/0055 ,  Y02P20/55

摘要： The present invention relates to a novel process for the preparation of bile esters derivatives of general formula (I), in which R0 is H or OH; R1 is H, α-OH or β-OH; R2 and R3 are independently hydrogen, straight or branched (C1-C20) alkyl optionally substituted with aryl; R5 is a straight or branched (C1-C4) alkyl and R6 is a straight or branched (C1-C4) alkyl or a benzyl group, via transamidation of the amine (V) with the 5-ocoproline derivative (II), wherein R4 is selected from the group consisting of tertbutoxycarbonyl, methoxycarbonyl, ethoxycarbonyl, 2-trimethylsilylethoxycarbonyl, cyclobutoxycarbonyl and 1-methylcyclobutoxy carbonyl, followed by the selective cleavage of the protecting group R4 under acidic conditions.

公开(公告)号：EP1337505A1

公开(公告)日：2003-08-27

申请号：EP01995673.9

申请日：2001-11-28

申请人： Bracco Imaging S.p.A.

发明人： ANELLI, Pier, Lucio ,  BROCCHETTA, Marino ,  LUX, Giovanna ,  CAPPELLETTI, Enrico

IPC分类号： C07C231/02 ,  C07C237/32 ,  C07C227/04 ,  C07C227/18 ,  C07C237/42

CPC分类号： C07C231/02 ,  C07C227/04 ,  C07C227/18 ,  C07C231/12 ,  C07C231/14 ,  C07C237/32 ,  C07C237/42

摘要： The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein R1 represents a straight or branched (C1-C4)-alkyl group, with at least the stoichiometric amount of an amine of formula H2NR.

摘要翻译： 本发明涉及制备式（I）化合物的方法，其中R表示2,3-二羟基-1-丙基或1,3-二羟基-2-丙基，通过直接酰胺化二烷基 （V）的5-氨基-1,3-苯二甲酸的酯，其中R 1表示直链或支链（C 1 -C 4） - 烷基，并且至少化学计量的式H 2 NR的胺。

公开(公告)号：EP1061956B1

公开(公告)日：2002-12-11

申请号：EP99910335.1

申请日：1999-03-08

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

发明人： BROCCHETTA, Marino ,  CALABI, Luisella ,  PALANO, Daniella ,  PALEARI, Lino ,  UGGERI, Fulvio

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

CPC分类号： C07C229/16 ,  A61K49/06 ,  C07C233/83 ,  C07C2603/24 ,  Y10S977/915

摘要： Compounds of formula (I), both in the racemic and optically active forms, wherein the groups are as defined in the disclosure, are disclosed.

摘要翻译： 以外消旋和旋光形式的式（I）化合物用于MRI诊断成像。

公开(公告)号：EP2593423B1

公开(公告)日：2014-09-03

申请号：EP11731379.1

申请日：2011-07-14

申请人： Bracco Imaging S.p.A

发明人： ANELLI, Pier Lucio ,  BROCCHETTA, Marino ,  CAPPELLETTI, Enrico ,  GAZZOTTI, Ornella

IPC分类号： C07C231/10

CPC分类号： C07C231/12 ,  C07C231/10 ,  C07C237/46