Abstract: Injectable aqueous composition intended for opacifying certain organs with a view to examination by X-rays. This composition is based on liposomes containing, encapsulated therein, an aqueous solution of an iodinated opacifying agent. The ratio between the weight of iodine encapsulated by the liposomes and the weight of the lipids from which their membrane is formed is not lower than 1.5 mg/mg.
Type:
Grant
Filed:
January 19, 1989
Date of Patent:
May 17, 1994
Assignee:
Bracco - Industria Chimica S.p.A.
Inventors:
Michel Schneider, Herve Tournier, Bernard Lamy
Abstract: Comounds having the formula ##STR1## wherein: a is 2 or 3; b is an integer from 0 to 4;Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44;E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;S is the group --A--O--R wherein:A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --; m is an integer from 1 to 5; R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hyroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms;R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.
Type:
Grant
Filed:
December 13, 1989
Date of Patent:
January 26, 1993
Assignee:
Bracco Industria Chimica S.p.A.
Inventors:
Ernst Felder, Luciano Fumagalli, Fulvio Uggeri, Giorgio Vittadini
Abstract: Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.
Type:
Grant
Filed:
November 27, 1989
Date of Patent:
July 21, 1992
Assignee:
Bracco Industria Chimica S.p.A.
Inventors:
Ernst Felder, Carlo Musu, Luciano Fumagalli, Fulvio Uggeri
Abstract: Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH; R.sub.1 is the same as R.sub.2 oris --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.
Type:
Grant
Filed:
September 25, 1989
Date of Patent:
December 25, 1990
Assignee:
Bracco Industria Chimica, S.p.A.
Inventors:
Ernst Felder, Fulvio Uggeri, Luciano Fumagalli, Giorio Vittadini
Abstract: Barium sulfate suitable for the preparation of radiographic contrast agents of increased flowability and density is obtained by a high temperature treatment at 700.degree. to 1,200.degree. C. and preferably at 800.degree. to 1,000.degree. C. The barium sulfate so sintered is distinguished by a bulk density of 2.5 to 3 g/ml and its aqueous suspension, containing 200 g of barium sulfate per 100 ml, is distinguished by a viscosity of no more than 1,000 mPas. Radiographic contrast agents containing at least 200 g of sintered barium sulfate per 100 ml are outstandingly suitable for the difficult double contrast visualization of the stomach and gastric mucosa.
Abstract: Compounds for use in non-ionic X-ray contrasting materials having the formula ##STR1## in which (H0).sub.2-3 alkyl is 1,3-dihydroxyisopropyl, 2,3-dihydroxypropyl or 1,3-dihydroxy-2-hydroxymethylisopropyl,R is hydrogen or methyl, andR.sub.1 is an alkyl residue with 1 to 5 carbon atoms.These compounds possess high water-solubility as well as excellent stability against hydrolysis. Methods for preparation and use of the compounds are also disclosed.
Abstract: Novel, radio-opaque compounds comprising water-soluble bis-[N-{3,5-bis-(hydroxyalkylaminocarbonyl)-2,4,6-triiodo-phenyl}-N-(.alph a.-hydroxyacyl)-amino]-alkanes are disclosed for use as X-ray contrast agents. These compounds are relatively simple to synthesize, possess low toxicity and have good stability as well as resistance to hydrolysis. Methods for preparation and use of the compounds are also disclosed.
Abstract: 3-Alkoxy-2-alkyl-propionic acid derivatives are prepared by catalytic hydrogenation of the acrylic acid analogs. The latter are obtained by CO treatment of lower alkyl esters of alkanoic acids having 3-6 carbon atoms in the presence of alkali metal methylate and condensation of the resulting 2-formylalkanoic acids or their alkali metal enolates with compounds of the formula X--(CH.sub.2).sub.m --Z wherein X is Cl, Br, or OH, and Z is Cl, Br, I, alkyl- or arylsulfonyl, or OH.
Abstract: .alpha., .omega.-BIS-[5-(DIHYDROXYALKYL) AMINOCARBONYL-3-HYDROXYACYL-AMINO-2,4,6-TRIIODO-BENZOYL-AMINO]-OXAALKANE COMPOUNDS OF THE FORMULA ##STR1## wherein R.sub.1 is ##STR2## R and R' are hydrogen or methyl, R.sub.2 is dihydroxyalkyl having 3 or 4 carbon atoms,N is 2 or 3,M is an integer between 1 and 5, andN(m+1) is an integer between 4 and 12,Are readily soluble in water to yield injectable radiopaque contrast compositions which are well tolerated and stable. The compounds are prepared in good yields by reacting a reactive derivative of a 5-(di-hydroxyalkyl)aminocarbonyl-3-acyloxyacylamino-2,4,6-triiodo-benzoic acid with an .alpha.,.omega.-diamino-oxaalkane of the formulaR--NH--C.sub.n H.sub.2n --(O--C.sub.n H.sub.2n)--NH--R.