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Claims for Patent: 4,094,966

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Claims for Patent: 4,094,966

Title: Iodobenzene derivatives and X-ray contrast media containing the same
Abstract:The present invention provides new iodobenzene derivatives which have at least two benzene nuclei and one carboxylic group. These derivatives possess a low toxicity and may be used as X-ray contrast media.
Inventor(s): Tilly; Guy (Aulnay-sous-Bois, FR), Hardouin; Michel Jean Charles (Aulnay-sous-Bois, FR), Lautrou; Jean (Aulnay-sous-Bois, FR)
Assignee: Laboratoires Andre Guerbet (Aulnay-sous-Bois, FR)
Application Number:05/748,323
Patent Claims: 1. An iodobenzene derivative selected from the group consisting of a compound of formula ##STR113## in which: R.sub.1 is selected from the group consisting of hydrogen, a radical having the formula ##STR114## R.sub.5 and R.sub.6 being selected from the group consisting of hydrogen, lower alkyl and lower hydroxy alkyl, and a radical of the formula ##STR115## R.sub.7 being a lower alkanoyl radical and R.sub.8 being selected from the group consisting of hydrogen, lower alkyl and lower hydroxylakyl,

R.sub.2 is selected from the group consisting of hydrogen, a radical having the formula ##STR116## in which R.sub.9 and R.sub.10 have the meanings given for R.sub.5 and R.sub.6, and a radical of the formula ##STR117## in which 11 has the meaning given for R.sub.7 or represents a hydrogen atom and R.sub.12 has the meaning given for R.sub.8,

R.sub.3 is selected from the group consisting of hydrogen, a radical having the formula ##STR118## in which R.sub.13 and R.sub.14 have the meanings given for R.sub.5 and R.sub.6, and a radical of the formula ##STR119## in which R.sub.15 has the meaning given for R.sub.7 or represents hydrogen and R.sub.16 has the meaning given for R.sub.8,

R.sub.4 is selected from the group consisting of hydrogen, lower alkyl and lower hydroxylakyl, a lower alkyl ester thereof and a salt with a pharmaceutically acceptable base.

2. An iodobenzene derivative selected from 2,4,6-tri-iodo-3-N-methylcarbamyl-5-bis {[2,4,6-triiodo-3,5-bis (N-hydroxyethylcarbamyl-phenyl]carbamyl-methyl} aminoacetamidobenzoic acid and a salt thereof with a pharmaceutically acceptable base.

3. An iodobenzene derivative selected from 2,4,6-triiodo-3-N-methylacetamido-5-bis {[2,4,6-triiodo-3,5-bis (N-hydroxyethyl-carbamyl)-phenyl] carbamyl-methyl} aminoacetamidobenzoic acid and a salt thereof with a pharmaceutically acceptable base.

4. An iodobenzene derivative selected from 2,4,6-triiodo-3-N-methylcarbamyl-5-bis {[2,4,6-triiodo-3,5-bis (N-hydroxyethyl-carbamyl)-phenyl]carbamyl-methyl} amino-N-methylacetamido-benzoic acid and a salt thereof with a pharmaceutically acceptable base.

5. An X-ray contrast mdium comprising an aqueous solution of an effective amount of a compound as claimed in claim 1.

6. An X-ray contrast medium comprising an aqueous solution of an effective amount of a pharmacologically acceptable salt of a compound as claimed in claim 1.

7. An X-ray contrast medium as claimed in claim 6 in which 100 ml of said solution contains 5-100 g of said salt.
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