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US 5,190,982 AGranted
Ultrasonic contrast agents, processes for their preparation and the use thereof as diagnostic and therapeutic agents
AssigneeHoechst Aktiengesellschaft
InventorsRaimund Erbel, Rainer Zotz, Volker Krone, Michael Magerstadt, Axel Walch
Life of this patent
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Abstract
The invention relates to ultrasonic contrast agents composed of microparticles which contain a gas and polyamino-dicarboxylic acid-co-imide derivatives, to processes for their preparation and to their use as diagnostic and therapeutic agents.
Claims1
A process for the preparation of an ultrasonic contrast agent composed of microparticles which contain a gas and a polyamino-dicarboxylic acid-co-imide derivative of the formula I ##STR4## in which n is 1 or 2
- x is 1 to 500
- y is 1 to 500, where
- x+y is 2 to 1000, and
- R is O--R.sup.1 or NH--R.sup.2, in which R.sup.2 is H, (CH.sub.2)m--OR.sup.1, (CH.sub.2)m--O--C(O)--R.sup.1 or (CH.sub.2).sup.m --O--C(O)--OR.sup.1, and
- m is 2 to 6, and
- R.sup.1 is H, aryl, aralkyl, arylalkenyl, alkyl or C.sub.3 -C.sub.8 -cycloalkyl or a biologically inactive steroid alcohol or an amino acid, where aryl is unsubstituted or is substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkylcarbonyloxy, C.sub.1 -C.sub.4 -alkoxy-carbonyl, C.sub.1 -C.sub.4 -alkoxy or hydroxyl,
- where the alkyl radicals specified for R.sup.1 have 1-22 carbon atoms and the alkenyl radicals have 2-22 carbon atoms, which are not interrupted or are interrupted by a carbonyloxy or oxycarbonyl group, where the repeating units placed in square brackets are distributed randomly and/or in blocks in the polymer, and where both the repeating units labeled with x and those labeled with y are identical or different and where the amino acids are .alpha.- and/or .beta.-linked, which process comprises:
- (a) a solution of one or more polyamino-dicarboxylic acid-co-imide derivatives of the formula I or a solution of this or these derivatives which additionally contains one or more other polymers and/or physiologically acceptable auxiliaries being spray-dried, or
- (b) one or more polyamino-dicarboxylic acid-co-imide derivatives of the formula I being dissolved in a solvent or solvent mixture with high melting point, or these derivatives being mixed with one or more other polymers and/or physiologically acceptable auxiliaries and dissolved in a solvent mixture with high melting point and then added dropwise to a condensed cold gas and subsequently the solvent being removed, or
- (c) one or more polyamino-dicarboxylic acid-co-imide derivatives of the formula I being dissolved in a solvent or solvent mixture and subsequently, where appropriate after addition of another solvent and/or of one or more other polymers, being precipitated or dispersed in water, and the resulting suspension being freed of solvents.
7 more elements
Dependencies are inferred from the claim text.