公开(公告)号：EP0617970A2

公开(公告)日：1994-10-05

申请号：EP94200842.6

申请日：1994-03-29

申请人： NYCOMED IMAGING AS

发明人： Bacon, Edward R., c/o STERLING WINTHROP INC. ,  Daum, Sol J., c/o STERLING WINTHROP INC. ,  Estep, Kimberley G. c/o STERLING WINTHROP INC. ,  Josef, Kurt A., c/o STERLING WINTHROP INC. ,  Douty, Brent D., c/o STERLING WINTHROP INC. ,  Illig, Carl R., c/o STERLING WINTHROP INC.

IPC分类号： A61K49/04

CPC分类号： A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

摘要： 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, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation; and an x-ray contrast producing agent of the formula

or a pharmaceutically accetable salt thereof,
wherein

X =
or

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, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy,
n is 1-5;
y is 0-4; and
w is 1-4,

in a pharmaceutically acceptable carrier and a method of its use in diagnostic radiology of the GI tract.

摘要翻译： 一种X射线对比组合物，其设计用于将薄的柔性膜沉积在吸收患者肠内表面的营养物的粘膜上，以在营养吸收内表面和肠内容物之间形成屏障，该柔性膜 保留与粘膜衬里结合的膜直到通过正常细胞周转消除为止包括基于w / v：（a）在pH 5-8范围内能够在胃肠道上形成膜膜的0.1-15％的聚合物材料， 该聚合物材料选自：（i）以电离形式携带负电荷的阴离子聚合物; （ii）以电离形式携带正电荷的阳离子聚合物; （iii）在O，N，S，F，Cl，Br和I上具有极化电子的中性聚合物; 与（b）0.1-15％的二价阳离子结合，以增强柔性膜膜与粘膜衬里的结合，阳离子选自Ca2 +，Mg2 +，Zn2 +或Ba2 +; 和（c）0.001-75％的式（I）的X射线造影剂或其盐之一。 在（I）中，X = CO; Z = H，卤素，5-20C烷基，环烷基等; R = 1-25C烷基，环烷基或芳基等; n = 1-5; y = 0-4; w = 1-4。

公开(公告)号：EP0617969A3

公开(公告)日：1995-09-06

申请号：EP94200841.8

申请日：1994-03-29

申请人： NYCOMED IMAGING AS

发明人： Bacon, Edward R., c/o STERLING WINTHROP INC. ,  Daum, Sol J., c/o STERLING WINTHROP INC. ,  Estep, Kimberley G., c/o STERLING WINTHROP INC. ,  Josef, Kurt A., c/o STERLING WINTHROP INC. ,  Douty, Brent D., c/o STERLING WINTHROP INC. ,  Illig, Carl R., c/o STERLING WINTHROP INC.

IPC分类号： A61K49/04 ,  C07C69/017 ,  C07C69/63 ,  C07C69/74 ,  C07C309/65

CPC分类号： B82Y5/00 ,  A61K49/04 ,  A61K49/0404 ,  A61K49/0409 ,  A61K49/0433 ,  C07C69/017 ,  C07C69/63 ,  C07C69/74 ,  C07C309/65

摘要： 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
X=
  or ―SO₂―;
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, aryl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene, lower-alkoxy-carbonyloxy;
n =  1-5;
y =  0-4; and
w =  1-4.

摘要翻译： 本发明公开了含水组合物中含有的式“IMAGE”的造影剂及其用于胃肠道诊断放射学的方法，其中X = 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被卤素或卤代低级烷基取代; R = C 1 -C 25烷基，环烷基，芳基或卤代低级烷基，任选被卤素，氟代低级烷基，低级烷氧基，羟基，羧基或低级烷氧基羰基，低级烯基，低级 - 炔基， 低级亚烷基，低级烷氧基 - 羰氧基; N = 1-5; Y = 0-4; 并且在药学上可接受的载体中w = 1-4。

公开(公告)号：EP0617970A3

公开(公告)日：1995-09-06

申请号：EP94200842.6

申请日：1994-03-29

申请人： NYCOMED IMAGING AS

发明人： Bacon, Edward R., c/o STERLING WINTHROP INC. ,  Daum, Sol J., c/o STERLING WINTHROP INC. ,  Estep, Kimberley G. c/o STERLING WINTHROP INC. ,  Josef, Kurt A., c/o STERLING WINTHROP INC. ,  Douty, Brent D., c/o STERLING WINTHROP INC. ,  Illig, Carl R., c/o STERLING WINTHROP INC.

IPC分类号： A61K49/04

CPC分类号： A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

摘要： 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, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation; and an x-ray contrast producing agent of the formula

or a pharmaceutically accetable salt thereof,
wherein
X = or
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, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy, n is 1-5; y is 0-4; and w is 1-4,
in a pharmaceutically acceptable carrier and a method of its use in diagnostic radiology of the GI tract.

公开(公告)号：EP0617969A2

公开(公告)日：1994-10-05

申请号：EP94200841.8

申请日：1994-03-29

申请人： NYCOMED IMAGING AS

发明人： Bacon, Edward R., c/o STERLING WINTHROP INC. ,  Daum, Sol J., c/o STERLING WINTHROP INC. ,  Estep, Kimberley G., c/o STERLING WINTHROP INC. ,  Josef, Kurt A., c/o STERLING WINTHROP INC. ,  Douty, Brent D., c/o STERLING WINTHROP INC. ,  Illig, Carl R., c/o STERLING WINTHROP INC.

IPC分类号： A61K49/04 ,  C07C69/017 ,  C07C69/63 ,  C07C69/74 ,  C07C309/65

CPC分类号： B82Y5/00 ,  A61K49/04 ,  A61K49/0404 ,  A61K49/0409 ,  A61K49/0433 ,  C07C69/017 ,  C07C69/63 ,  C07C69/74 ,  C07C309/65

摘要： 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
X=
  or ―SO₂―;
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, aryl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene, lower-alkoxy-carbonyloxy;
n =  1-5;
y =  0-4; and
w =  1-4.