Claims for Patent: 4,364,921

Summary for Patent: 4,364,921

Title:	Novel triiodinated isophthalic acid diamides as nonionic X-ray contrast media
Abstract:	New triiodinated isophthalic acid diamides of the formula ##STR1## wherein the amide residues --CO--N.R1 R2 and --CO--N.R3 R4 are different from each other andR1 is hydrogen or C1-6 alkyl,R2 is mono- or polyhydroxyalkyl,R3 is hydrogen or C1-6 alkyl,R4 is mono- or polyhydroxylalkyl,R5 is C1-6 alkyl or mono- or polyhydroxy-C1-6 -alkyl or C1-3 -alkoxy-C1-3 -alkyl, andR6 is hydrogen, C1-6 alkyl or mono- or polyhydroxyalkyl provide superior nonionic X-ray contrast media.
Inventor(s):	Ulrich Speck, Peter Blaszkiewicz, Dieter Seidelmann, Erich Klieger
Assignee:	Bayer Pharma AG
Application Number:	US06/127,613
Patent Claims:	1. A triiodinated isophthalic acid diamide of the formula ##STR8## wherein the amide residues --CO--N.R1 R2 and --CO--N.R3 R4 are different from each other andR1 is hydrogen or C1-6 alkyl, R2 is mono- or polyhydroxyalkyl, R3 is hydrogen or C1-6 alkyl, R4 is mono- or polyhydroxyalkyl, R5 is C1-6 alkyl or monohydroxy-C1-6 -alkyl or C1-3 -alkoxy-C1-3 -alkyl, and R6 is hydrogen or C1-6 alkyl or mono-. 2. 5-Methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-dihydroxypropyl)]diamide, a compound of claim 1. 3. 5-(S-2-Hydroxypropionylamino)-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-dihydroxypropyl)]diamide, a compound of claim 1. 4. 5-Methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2-hydroxy-1-hydroxymethylethyl)]diamide, a compound of claim 1. 5. The compound of claim 1, wherein at least one of R1, R2, R3 or R4 is dihydroxyalkyl. 6. A compound of claim 5, wherein at least one of R1 or R2 is dihydroxyalkyl and at least one of R3 and R4 is dihydroxyalkyl. 7. A compound of claim 5 or 6 wherein all alkyl moieties in R1, R2, R3 and R4 have three carbon atoms. 8. A pharmaceutical composition for use as an X-ray contrast agent comprising a radiopaque amount of a compound of Claim 1 and a pharmaceutically acceptable carrier. 9. A method of conducting a radiological examination of a patient which comprises administering to the patient a radiopaque amount of a compound of claim 1. 10. 5-Acetylamino-2,4,6-triiodoisophthalic Acid [(2,3-dihydroxypropyl)-(2,3-dihydroxy-N-methyl-propyl)]diamide. 11. A compound of claim 1 wherein R5 is methoxymethyl 1-hydroxyethyl or methyl. 12. A compound of claim 1, wherein R1 and R3 each are H or CH3, and R2 and R4 each are --CH2 --CHOH--CH2 OH or ##STR9## 13. A composition of claim 8 wherein the carrier is pharmaceutically acceptable for angiography. 14. A method of claim 9, wherein the radiological examination is angiography. 15. A compound of claim 11, wherein R6 is H or C1-4 -alkyl.