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EP0614668A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Composition of iodobenzoic acid derivatives for visualization of the gastrointestinal tract

Assignee: GE Healthcare AS
•
Filing: 1994-03-10
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Granted: —
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Expires: 2014-03-10
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Abstract

Abstract Disclosed are contrast agents of the formula or a pharmaceutically acceptable salt thereof, contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein Z = H, halo, C 1 -C 20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R = C 1 -C 25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CRi R 2 )p - (CR 3 = CR 4 ) mQ , or (CR 1 R 2 )p - C ≡ C - Q ; Ri, R 2 , R 3 and R 4 are independently lower-alkyl, optionally substituted with halo; x is 1-3 y is 1-4; n is 1-5; m is 1-15; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl in an aqueous, pharmaceutically acceptable carrier.

Inventors

  • 👤 Carl R. C/O Sterling Winthrop Inc. Illig
  • 👤 Brent D. C/O Sterling Winthrop Inc. Douty

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 11:22
CPC Classifications
A; A61; A61K; A61K49/00; A61K49/04; A61K49/0433; C; C07; C07C; C07C69/00; C07C69/76; C07C69/84; C07C69/92

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 123 words
A compound of the formula : or a pharmaceutically acceptable salt thereof wherein Z = H, halo, C 1 -C 20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R = C l -C 25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CRi R 2 )p-(CR 3 =CR 4 ) m Q, or (CR, R 2 ) p C≡C-Q; Ri, R 2 , R 3 and R 4 are independently lower-alkyl, optionally substituted with halo; x is 1-3 y is 1-4; n is 1-5; m is 1-15; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
Claim 2
Dependent Claim 123 words
A compound of the formula : or a pharmaceutically acceptable salt thereof wherein Z = H, halo, C 1 -C 20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R = C l -C 25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CRi R 2 )p-(CR 3 =CR 4 ) m Q, or (CR, R 2 ) p C≡C-Q; Ri, R 2 , R 3 and R 4 are independently lower-alkyl, optionally substituted with halo; x is 1-3 y is 1-4; n is 1-5; m is 1-15; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
Claim 3
Dependent Claim 25 words
A compound as claimed in claim 1, selected from the group consisting of: 2-octyl 2,3,5-triiodobenzoate, 3,3,4,4,5,5,6,6,7,7,8,8-dodecafluoro-2-octyl 2,3,5-triiodobenzoate, bis (2-hexyl) 2,3,5,6-tetraiodoterephthalate, ethyl 3-(2-octyloxy)-2,4,6-triiodobenzoate and bis(2-octyl) 5-(2-octyloxy)-2,4,6-triiodoisophthalate.
Claim 4
Dependent Claim 38 words
An orally or rectally administerable x-ray contrast composition for visualization of the gastrointestinal tract comprising a contrast agent as defined in either of the preceding claims, or a pharmaceutically acceptable salt thereof, in an aqueous, pharmaceutically acceptable carrier.
Claim 5
Dependent Claim 14 words
An x-ray contrast composition as claimed in claim 3 containing at least one surfactant.
Claim 6
Dependent Claim 14 words
An x-ray contrast composition as claimed in claim 4 wherein said surfactant is cationic.
Claim 7
Dependent Claim 14 words
An x-ray contrast composition as claimed in claim 4 wherein said surfactant is anionic.
Claim 8
Dependent Claim 14 words
An x-ray contrast composition as claimed in claim 4 wherein said surfactant is zwitterionic.
Claim 9
Dependent Claim 14 words
An x-ray contrast composition as claimed in claim 4 wherein said surfactant is nonionic.
Claim 10
Dependent Claim 27 words
An x-ray contrast composition as claimed in claim 4 wherein said surfactant is present from about 0.01 % w/v to about 15% w/v in said aqueous formulation.
Claim 11
Independent Claim 62 words
A method of carrying out x-ray examination of the gastrointestinal tract of a patent in need of such examination which comprises orally or rectally administering to the patient an x-ray contrast composition as defined in any one of claims 3 to 9 comprising an x-ray contrast agent, or a pharmaceutically acceptable salt thereof, as defined in either of claims 1 and 2.
Claim 12
Dependent Claim 36 words
A method as claimed in claim 10 wherein the amount of contrast agent administered to said patient contains from about 0.1 to about 16 g iodine/kg body weight for regular x-ray visualization of the gastrointestinal tract.
Claim 13
Dependent Claim 36 words
A method as claimed in claim 10 wherein the amount of contrast agent administered to said patient contains from about 1 to about 600 mg iodine/kg body weight for CT scan visualization of the gastrointestinal tract.

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