Compositions of iodoaniline derivatives for visualization of the gastrointestinal tract
AssigneeSterling Winthrop Inc.
InventorsCarl R. Illig, Thomas J. Caulfield
Life of this patent
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Abstract
Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, n is 1-4; y is 1-4; and x is 1 or 2.
Claims28
An orally or rectally administerable x-ray contrast composition in a dispersion form for visualization of the gastrointestinal tract comprising a contrast agent having the formula, or a pharmaceutically acceptable salt thereof:
- ##STR6## wherein Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;
- R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, and halo-lower-alkyl are optionally substituted with, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy and said acetyl is optionally substituted with fluoro-lower-alkyl, aryl, lower alkoxy, hydroxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;
- n is 1-4;
- y is 1-4;
- and
- x is 1 or 2;
- and a physiologically acceptable carrier comprising a surfactant selected from the group consisting of cationic, anionic, nonionic, and zwitterionic surfactants.
A method of carrying out x-ray examination of the gastrointestinal tract of a patient in need of such examination which comprises orally or rectally administering to the patient an x-ray contrast composition in a dispersion form comprising:
- an x-ray contrast agent, or a pharmaceutically acceptable salt thereof, having the formula:
- ##STR7## wherein Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;
- R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 5 alkyl, cycloalkyl, and halo-lower-alkyl are optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy and said acetyl is optionally substituted with fluoro-lower-alkyl, aryl, lower alkoxy, hydroxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy
- n is 1-4;
- y is 1-4;
- and
- x is 1 or 2;
- and a physiologically acceptable carrier comprising a surfactant selected from the group consisting of cationic, anionic, nomonic, and zwitterionic surfactants.
Dependencies are inferred from the claim text.