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

申请人： NYCOMED IMAGING AS

发明人： 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 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：EP0609586A2

公开(公告)日：1994-08-10

申请号：EP93203674.2

申请日：1993-12-24

申请人： NYCOMED IMAGING AS

发明人： 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分类号： A61K49/04 ,  C07C22/04

CPC分类号： A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

摘要： 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.

摘要翻译： 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：EP0609588A3

公开(公告)日：1995-09-06

申请号：EP93203676.7

申请日：1993-12-24

申请人： NYCOMED IMAGING AS

发明人： Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Illig, Carl, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc.

IPC分类号： A61K49/04 ,  C07C22/04 ,  C07C25/02

CPC分类号： C07C17/354 ,  A61K49/0438 ,  A61K49/0461 ,  C07C17/12 ,  C07C17/2635 ,  C07C25/02 ,  C07C25/24 ,  C07C69/65

摘要： Disclosed are contrast agents of the formula

or pharmaceutically acceptable salts thereof,
contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein
R = C 1 -C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxycarbonyloxy, (CR i R 2 )p-(CR 3 =CR 4 ) m Q, or (CR 1 R 2 )p-C=C-Q; Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.

摘要翻译： 口服或直肠给药的X线对照组合物。 包括具有式（I）的造影剂或（I）的盐。 药学上可接受的载体 选自两性离子表面活性剂，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，琥珀酸丁磺酸盐，羧酸酯，羧酸酰胺，乙氧基化烷基酚和乙氧基化脂族醇的至少一种表面活性剂，脱水山梨醇酯，聚氧乙烯 烷基醚和聚氧乙烯山梨糖醇酐脂肪酸酯。 R = CH 3，C 2 H 5，n-C 3 H 7，4-25 C烷基，环烷基，不饱和的。 烯丙基（sic）或卤代低级烷基，其各自可以选择。 被删除 （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C CC-Q; R1，R2，R3和R4各自独立地为H或opt。 晕子 低级烷基，n为2-5，m为2-5，p为1-10，Q为H，低级烷基，烯基，低级炔基，低级亚烷基（sic），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

申请人： NYCOMED IMAGING AS

发明人： 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分类号： A61K49/04 ,  C07C22/04

CPC分类号： A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

摘要： 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：EP0609588A2

公开(公告)日：1994-08-10

申请号：EP93203676.7

申请日：1993-12-24

申请人： NYCOMED IMAGING AS

发明人： Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Illig, Carl, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc.

IPC分类号： A61K49/04 ,  C07C22/04 ,  C07C25/02

CPC分类号： C07C17/354 ,  A61K49/0438 ,  A61K49/0461 ,  C07C17/12 ,  C07C17/2635 ,  C07C25/02 ,  C07C25/24 ,  C07C69/65

摘要： Disclosed are contrast agents of the formula

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

R = C 1 -C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxycarbonyloxy, (CR i R 2 )p-(CR 3 =CR 4 ) m Q, or (CR 1 R 2 )p-C=C-Q;
Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo;
n is 1-5;
m is 1-5;
p is 1-10; and
Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.

摘要翻译： 口服或直肠给药的X线对照组合物。 包括具有式（I）的造影剂或（I）的盐。 药学上可接受的载体 选自两性离子表面活性剂，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，琥珀酸丁磺酸盐，羧酸酯，羧酸酰胺，乙氧基化烷基酚和乙氧基化脂族醇的至少一种表面活性剂，脱水山梨醇酯，聚氧乙烯 烷基醚和聚氧乙烯山梨糖醇酐脂肪酸酯。 R = CH 3，C 2 H 5，n-C 3 H 7，4-25 C烷基，环烷基，不饱和的。 烯丙基（sic）或卤代低级烷基，其各自可以选择。 被删除 （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C CC-Q; R1，R2，R3和R4各自独立地为H或opt。 晕子 低级烷基，n为2-5，m为2-5，p为1-10，Q为H，低级烷基，烯基，低级炔基，低级亚烷基（sic），芳基或芳基 - 低级烷基。

公开(公告)号：EP0609589A3

公开(公告)日：1995-09-06

申请号：EP93203677.5

申请日：1993-12-24

申请人： NYCOMED IMAGING AS

发明人： Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Illig, Carl, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc.

IPC分类号： A61K49/04

CPC分类号： C07C17/12 ,  A61K49/0461 ,  C07C17/2635 ,  C07C17/354 ,  C07C25/02 ,  C07C69/65 ,  C07C25/24

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 producing agent of the formula

or a pharmaceutically acceptable salt thereof,
and methods for their use in diagnostic radiology of the gastrointestinal tract wherein
R= C 1 -C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxycarbonyloxy, (CRi R 2 )p-(CR 3 =CR 4 ) m Q, or (CR 1 R 2 )p-C=C-Q; Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; 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：EP0609589A2

公开(公告)日：1994-08-10

申请号：EP93203677.5

申请日：1993-12-24

申请人： NYCOMED IMAGING AS

发明人： Josef, Kurt A., c/o Sterling Winthrop Inc. ,  Bacon, Edward R., c/o Sterling Winthrop Inc. ,  Estep, Kimberley G., c/o Sterling Winthrop Inc. ,  Illig, Carl, c/o Sterling Winthrop Inc. ,  Douty, Brent D., c/o Sterling Winthrop Inc.

IPC分类号： A61K49/04

CPC分类号： C07C17/12 ,  A61K49/0461 ,  C07C17/2635 ,  C07C17/354 ,  C07C25/02 ,  C07C69/65 ,  C07C25/24

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 producing agent of the formula

or a pharmaceutically acceptable salt thereof,
and methods for their use in diagnostic radiology of the gastrointestinal tract wherein

R= C 1 -C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxycarbonyloxy,
(CRi R 2 )p-(CR 3 =CR 4 ) m Q, or (CR 1 R 2 )p-C=C-Q;
Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo;
n is 1-5;
m is 1-5;
p is 1-10; and
Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.

摘要翻译： 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，所述聚合物材料具有与二价阳离子结合的含有可极化电子的原子，以及x 式的片剂生产剂或其药学上可接受的盐，以及其用于胃肠道诊断放射学的方法，其中R = C 1 -C 25烷基，环烷基，不饱和烯丙基或卤代低级烷基，任选取代 （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p C标识CQ;（C 1 -C 6）烷基， R 1，R 2，R 3和R 4独立地为H，低级烷基，任选被卤素取代; n为1-5; m为1-5; p为1-10; Q为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

申请人： NYCOMED IMAGING AS

发明人： 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 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.

摘要翻译： 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。