Schering Aktiengesellschaft

Heinrich Pfeiffer

Ulrich Speck

Heinz Gries

Wolfgang Mutzel

Hanns-Joachim Weinmann

Douwe Rosenberg

Wolfgang Muetzel

Paul-Eberhard Schulze

Franz-Josef Renneke

Georg-Alexander Hoyer

Georg-Alexander Hayden

Hans-Martin Siefert

Bernhard Acksteiner

A diagnostic medium contains at least one physiologically well tolerated complex salt comprising an anion of a complexing acid and one or more central ion or ions of an element with an atomic number of 21 to 29, 42, 44 or 57 to 83 and, optionally, one or more physiologically biocompatible cation or cations of an inorganic and/or organic base or amino acid, optionally, with additives customary in galenic formulations, dissolved or suspended in an aqueous medium.

Method of enhancing paramagnetism in chelates for MRI

Nonionic compounds of the formula ##STR1## wherein X is --CONR.sub.1 R.sub.2, --COOR.sub.3, --CH.sub.2 NHR.sub.7 or --CH.sub.2 OH; Y is --1R.sub.1 R.sub.2 or --OR.sub.3 ; and Z is --NR.sub.1 R.sub.2, --NHR.sub.7 or --OR.sub.3 ; and wherein R.sub.1 R.sub.2 and R.sub.3 in X, Y or Z, and R.sub.7 in X and Z, are identical or different, R.sub.1 and R.sub.2, and each is hydrogen, C.sub.1-6 -alkyl or C.sub.2-8 - alkyl substituted by 1-5 OH groups and/or by a C.sub.1-3 -alkoxy group; R.sub.3 is C.sub.1-4 -alkyl or C.sub.2-4 -alkyl substituted by 1-2 OH groups and/or by a C.sub.1-3 -alkoxy group; and R.sub.7 is an acyl group of a C.sub.2-5 OH group and/or by a C.sub.1-3 -alkoxy group are highly advantageous X-ray contrast agents.

Nonionic 5-C-substituted 2,4,6-triiodoisophthalic acid derivatives

Agents useful for influencing the relaxation times in NMR diagnostics, contain at least one paramagnetic, physiologically compatible complex salt comprising a chelate from an open-chain or cyclic complex-forming compound containing organic nitrogen, phosphorus, oxygen and/or sulfur, and a complexed ion of the lanthanide elements of atomic number 57-70 or of the transition metals of atomic numbers 21-29, 42 and 44, and, optionally, an inorganic or organic base or acid.

Method to enhance NMR imaging using chelated paramagnetic ions

Novel N-hydroxyethylated 2,4,6-triiodoaminoisophthalic acid bistrihydroxybutylamides of Formula (I) ##STR1## wherein R is a trihydroxybutyl residue, are excellently suitable, due inter alia, to their outstanding compatibility and high water solubility, as opacifying compounds in X-ray contrast media for use in X-ray diagnostic examination methods.

N-Hydroxyethylated 2,4,6-triiodoaminoisophthalic acid

Novel N-hydroxyalkylated dicarboxylic acid bis(3,5-dicarbamoyl-2,4,6-triiodoanilides) have Formula I ##STR1## wherein R.sup.1 is a lower, linear or branched mono- or polyhydroxyalkyl residue,

Novel N-hydroxyalkylated dicarboxylic acid

Unsymmetrically substituted dicarboxylic-acid-bis-(2,4,6-triiodo-anilides) of formula I ##STR1## wherein X is straight-chain or branched alkylene interrupted by one or more oxygen atoms,

Unsymmetrically substituted

Compounds of the formula ##STR1## wherein R.sup.1 is hydroxy-C.sub.2-8 -alkyl containing 1-5 OH-groups;

Triiodinated 5-aminoisophthalic acid derivatives

Ionic compounds of the formula ##STR1## wherein X is --CONR.sub.1 R.sub.2, --CH.sub.2 NH.multidot.Acyl or --CH.sub.2 OH; Y is --NR.sub.3 R.sub.4, --NH.multidot.Acyl or OR.sub.5 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 can be identical or different, and each is hydrogen, C.sub.1-6 - alkyl or C.sub.2-8 -alkyl substituted by 1-5 OH groups and/or by one C.sub.1-3 -alkoxy group, R.sub.5 is C.sub.1-6 alkyl or C.sub.2-8 -alkyl substituted by 1-5 OH groups and/or by one C.sub.1-3 -alkoxy group, and Acyl, which can be the same or different in X and Y, is C.sub.2-6 -alkanoyl or C.sub.2-6 -alkanoyl substituted by 1-4 OH groups and/or by one C.sub.1-3 -alkoxy group, or a physiologically compatible salt thereof with an inorganic or organic base, have valuable properties as X-ray contrast agents.

Ionic 5-C-substituted 2,4,6-triiodoisophthalic acid derivatives

Dicarboxylic acid bis(3,5-dicarbamoyl-2,4,6-triiodoanilides) of the formula ##STR1## wherein R.sub.1 is lower straight-chain or branched-chain mono- or polyhydroxyalkyl;

Dicarboxylic acid bis(3,5-dicarbamoyl-2,4,6-triiodoanilides) useful as

The sodium salt of 1,3-dihydroxy-2-nitropropane is catalytically hydrogenated in an inert solvent to produce 1,3-dihydroxy-2-aminopropane, which can be isolated in crystalline form.

Process for the preparation of serinol (1,3-dihydroxy-2-aminopropane)

Triiodized N-methyldicarboxylic acid anilides of the Formula ##STR1## wherein R.sub.1 is hydrogen, halogen, carboxyl, N-monoacylamino, N-monoalkoxyacylamino, N-alkyl-N-acylamino, N-alkyl-N-alkoxyacylamino, N,N-diacylamino, N-acylaminomethyl, ##STR2## wherein A is alkylene of 2 or 3 carbon atoms which can be interrupted by an oxygen atom, and R.sub.3 and R.sub.4 are each hydrogen, lower alkyl or hydroxyalkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 to 7 member heterocyclic ring which can contain a further oxygen, nitrogen, or sulfur hetero atom; R.sub.2 is halogen, hydroxy, lower alkoxy, hydroxyalkoxy or alkoxyalkoxy; and X is straight or branched alkylene of 2-14 carbon atoms interrupted by one or more oxygen or sulfur atoms, and the salts of these compounds with physiologically compatible bases are valuable radiopaque agents.

Growing community of inventors

Berlin, Germany

Heinrich Pfeiffer