摘要:
Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 6;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino;Q represents the atoms necessary to complete a carbocyclic or heterocyclic unsaturated mono- or bicyclic aromatic ring; andR.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, amino, acylamino, alkoxyalkyl, fluoroalkyl, acetamidoalkyl, COO-alkyl, cyano, carboxamido, sulfonate, sulfonamido, ureido, or carbamyl are useful as contrast agents in x-ray imaging compositions and methods.
摘要翻译:具有结构的化合物,其中(Z-COO是碘化芳族酸的残基; n是0至6的整数; R 1和R 2独立地是H,烷基,氟代烷基,环烷基,芳基,芳烷基,烷氧基或芳氧基 R 3和R 4独立地为H,烷基,氟代烷基,环烷基,芳基,芳烷基,烷氧基,芳氧基,卤素,羟基或酰基氨基; Q表示完成碳环或杂环不饱和单环或双环芳环所必需的原子; H,烷基,环烷基,芳基,芳烷基,烷氧基,芳氧基,卤素,羟基,氨基,酰氨基,烷氧基烷基,氟代烷基,乙酰氨基烷基,COO-烷基,氰基,甲酰氨基,磺酸酯,亚磺酰氨基,脲基或氨基甲酰基可用作对比剂 x射线成像组合物和方法。
摘要:
Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=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=C.sub.1 -C.sub.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, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.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; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
摘要:
Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein R is methyl, ethyl, n-propyl, C.sub.4 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 2-5;m is 2-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要:
A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p -(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.
摘要:
Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## 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=C.sub.1 -C.sub.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, lower-alkoxy-carbonyloxy;n=1-5;y=0-4; andw=1-4in an aqueous pharmaceutically acceptable carrier.
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 = C1-C25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取代,低级烯基,低级炔基, 低级亚烷基,低级烷氧基 - 羰基氧基; n = 1-5; y = 0-4; 并且在药学上可接受的载体中w = 1-4。
摘要:
Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 0 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently a substituent as defined for R.sup.1 and R.sup.2 above, halogen, hydroxy or acylamino;and R.sup.5 and R.sup.6 are independently H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, alkoxyalkyl, or acetamidoalkyl;or R.sup.5 and R.sup.6, taken together with the nitrogen atom to which they are attached, represent a 4 to 7-membered nitrogen containing ring, are useful as contrast agents in x-ray imaging compositions and methods.
摘要:
This invention relates to methods of x-ray diagnostic imaging the blood pool and/or lymph system of a mammal comprising administering a contrast effective amount of a particulate iodinated aroyloxy ester contrast agent having the structure: ##STR1## wherein n is an integer from 3 to 20; R.sup.1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, --COO-alkyl, --COO-aryl, --COO-aralkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.5 is H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.6 and R.sup.7 are independently alkyl, cycloalkyl, aryl or aralkyl; andR.sup.8 and R.sup.9 are independently H or --COR.sup.6.This invention further relates to novel iodinated aroyloxy ester contrast agents having the above structure wherein n is an integer from 5 to 20, to x-ray contrast compositions comprising such agents, and to methods of x-ray diagnostic imaging utilizing such agents.
摘要:
Disclosed are contrast agents of the formula ##STR1## wherein ##STR2## Z is H, halo, C.sub.5 -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 is C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, each of which may be optionally substituted with 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; andw is 1-4;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
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 ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## 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=C.sub.1 -C.sub.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; andw is 1-4.
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 ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinR=C.sub.1 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 1-5;m is 1-5;p is 1-10; andQ 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和具有式“IMAGE”的X射线产生剂及其用于诊断放射学的方法 的胃肠道,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 (CR 1 R 2)p - (CR 3 = CR 4)m Q或(CR 1 R 2)p C 3 B 3 CQ; 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; 并且Q是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。