公开(公告)号：EP0609586A2

公开(公告)日：1994-08-10

申请号：EP93203674.2

申请日：1993-12-24

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl, c/o Sterling Winthrop Inc. ,  Cooper, Eugene R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc. ,  Upson, Donald, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc. ,  Caulfield, Thomas J., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Robinson, Shaughnessy, c/o Sterling Winthrop Inc. ,  Spara, Paul P., c/o Sterling Winthrop Inc.

IPC: A61K49/04 ,  C07C22/04

CPC classification number: A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

Abstract: Disclosed are contrast agents of the formula

or pharmaceuticaoly acceptable salts thereof,
contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein

Z = H, halo, C₁-C₂₀ alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;
R = C₁-C₂₅ 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, (CR₁R₂) p - (CR₃ = CR₄) m Q, or (CR₁R₂) p - C ≡ C - Q;
R₁, R₂, R₃ and R₄ are independently lower-alkyl, optionally substituted with halo;
x 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.

Abstract translation: 口服或直肠给药 X射线对比组合 用于胃肠道的可视化包括0.001-75w / v％的式（I）的造影剂（或（I）的盐），其形式为水溶液。 分散体含有0.01-15w / v％的选自三甲基溴化铵，月桂基硫酸钠，十七烷基硫酸钠，烷基苯磺酸，丁基萘磺酸钠和磺基琥珀酸钠和两性离子表面活性剂中的至少一种表面活性剂。 在（I）中，Z = H，卤素，1-20C烷基，环烷基，低级烷氧基或CN，其中烷基和环烷基gps。 是选择。 substd。 卤代或卤代低级烷基; R = Me，Et，Pr，9-25C烷基，卤代低级烷基， substd。 （CR 1 R 2）p（CR 3 = CR 4）m Q或（CR 1 R 2）p C = C 1 -C 6烷基，C 1 -C 6烷基羰基或低级烷氧基羰氧基 ; （原文如此）; R1-R4 =低级烷基选择。 substd。 被晕 x = 1-4; n = 1-5; m = 1-15; p = 1-10; Q = H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基。

公开(公告)号：EP0609587A2

公开(公告)日：1994-08-10

申请号：EP93203675.9

申请日：1993-12-24

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl R., c/o Sterling Winthrop Inc. ,  Cooper, Eugene R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc. ,  Upson, Donald, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc. ,  Caulfield, Thomas J., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Robinson, Shaughnessey, c/o Sterling Winthrop Inc. ,  Spara, Paul P., c/o Sterling Winthrop Inc.

IPC: A61K49/04

CPC classification number: A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing
agent of the formula

or a pharmaceutically acceptable salt thereof,
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-alkoxycarbonyl or lower-alkoxy-carbonyloxy, (CR 1 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 1-4;
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 a pharmaceutically acceptable carrier.

Abstract translation: 公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物，其包含能够在胃肠道上形成涂层的聚合物材料和式CHEM的x射线产生剂或其药学上可接受的盐，以及 其用于诊断胃肠道放射学的方法，其中Z = H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，氰基，其中烷基和环烷基可以被卤素或卤代低级烷基取代; R = C 1 -C 25烷基，环烷基或卤代低级烷基，任选被卤素，氟 - 低级 - 烷基，芳基，低级 - 烷氧基，羟基，羧基低级 - 烷氧基羰基或低级烷氧基 - 羰氧基取代，（CR 1 R 2） -CR3 = CR4）mQ，或（CR1R2）pC IDENTICAL CQ; R 1，R 2，R 3和R 4独立地为低级烷基，任选被卤素取代; x为1-4; n为1-5; m为1-15; p为1-10; Q为药学上可接受的载体中的H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基。

公开(公告)号：EP0609586A3

公开(公告)日：1995-09-06

申请号：EP93203674.2

申请日：1993-12-24

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl, c/o Sterling Winthrop Inc. ,  Cooper, Eugene R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc. ,  Upson, Donald, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc. ,  Caulfield, Thomas J., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Robinson, Shaughnessy, c/o Sterling Winthrop Inc. ,  Spara, Paul P., c/o Sterling Winthrop Inc.

IPC: A61K49/04 ,  C07C22/04

CPC classification number: A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

Abstract: Disclosed are contrast agents of the formula

or pharmaceuticaoly acceptable salts thereof,
contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein
Z = H, halo, C₁-C₂₀ alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R = C₁-C₂₅ 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, (CR₁R₂) p - (CR₃ = CR₄) m Q, or (CR₁R₂) p - C ≡ C - Q; R₁, R₂, R₃ and R₄ are independently lower-alkyl, optionally substituted with halo; x 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.

公开(公告)号：EP0568156A1

公开(公告)日：1993-11-03

申请号：EP93201202.4

申请日：1993-04-27

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc.

IPC: A61K49/04

CPC classification number: A61K49/0461 ,  Y10S514/941 ,  Y10S514/942

Abstract: An orally or rectally administrable X-ray contrast formulation for X-ray examination of the gastrointestinal tract comprising: an X-ray contrast agent having the formula

wherein
   R is a substituted or unsubstituted alkyl group containing from 2 to 8 carbon atoms; and
   n is 1 to 5;
   the X-ray contrast agent being in the form of an aqueous dispersion in the formulation and a method for its use in diagnostic radiology of the gastrointestinal tract. The preferred contrast agent is the sec-octyl ether of 2,4,6-triiodophenol.

Abstract translation: 一种用于胃肠道X线检查的口服或直肠给药的X射线造影剂，包括：具有式CHEM的X射线造影剂，其中R是含有2至8个碳原子的取代或未取代的烷基; n为1〜5; 制剂中水分散体形式的X射线造影剂及其用于胃肠道诊断放射学的方法。 优选的造影剂是2,4,6-三碘苯酚的仲辛基醚。

公开(公告)号：EP0609587A3

公开(公告)日：1995-09-06

申请号：EP93203675.9

申请日：1993-12-24

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl R., c/o Sterling Winthrop Inc. ,  Cooper, Eugene R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc. ,  Upson, Donald, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc. ,  Caulfield, Thomas J., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Robinson, Shaughnessey, c/o Sterling Winthrop Inc. ,  Spara, Paul P., c/o Sterling Winthrop Inc.

IPC: A61K49/04

CPC classification number: A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula

or a pharmaceutically acceptable salt thereof,
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-alkoxycarbonyl or lower-alkoxy-carbonyloxy, (CR 1 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 1-4; 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 a pharmaceutically acceptable carrier.

公开(公告)号：EP0568155A1

公开(公告)日：1993-11-03

申请号：EP93201201.6

申请日：1993-04-27

Applicant: NYCOMED IMAGING AS

Inventor： Illig, Carl R., c/o Sterling Winthrop Inc. ,  Toner, John L., c/o Sterling Winthrop Inc.

IPC: A61K49/04

CPC classification number: B82Y5/00 ,  A61K49/0442 ,  A61K49/0461

Abstract: An X-ray contrast formulation for oral or retrograde examination comprising:
   a polymeric material capable of forming a coating on the gastrointestinal tract, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation; and
   a nonionic X-ray contrast producing agent having the formula:

   wherein R is a substituted or unsubstituted alkyl group containing from 2 to 8 carbon atoms wherein said substituents are selected from the group consisting of C₁-C₆ alkyl, hydroxy and alkoxy; and n is 1 to 5;
   in a pharmaceutically acceptable carrier and a method for its use in diagnostic radiology of the gastrointestinal tract. The preferred contrast agent is the sec-octyl ether of 2,4,6-triodophenol.

Abstract translation: 一种用于口服或逆行检查的X射线造影剂，其包括：能够在胃肠道上形成涂层的聚合物材料，所述聚合物材料与二价阳离子结合，其上含有可极化电子的原子; 和具有下式的非离子X射线造影剂：其中R是取代或未取代的含有2至8个碳原子的烷基，其中所述取代基选自C1-C6烷基，羟基和烷氧基 ; n为1〜5; 在药学上可接受的载体中，以及其用于胃肠道诊断放射学的方法。 优选的造影剂是2,4,6-三苯酚的仲辛基醚。