C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 233/54 (2006.01) A61K 49/04 (2006.01)
Patent
CA 2193389
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 structure (I) wherein n is an integer from 3 to 20; R1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; R2, R3 and R4 are independently H, alkyl, fluoroalkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, -COO-alkyl, -COO-aryl, -COO-aralkyl, cyano, sulfonyl, carboxamido or sulfonamido; R5 is H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido; R6 and R7 are independently alkyl, cycloalkyl, aryl or aralkyl; and R8 and R9 are independently H or -COR6. 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.
L'invention concerne des procédés d'imagerie diagnostique par rayons X du système lymphatique et/ou sanguin d'un mammifère, et consiste à administrer une quantité ayant un effet de contraste d'un agent à base d'ester aryloxy iodé particulaire ayant la structure (A) dans laquelle m est un nombre entier compris entre 3 et 20; R?1¿ représente H, alkyle, fluoroalkyle, cycloalkyle, aryle, aralkyle, alkoxyalkyle ou acétamino alkyle; R?2¿, R?3¿ et R?4¿ représentent indépendamment H, alkyl, fluoroalkyle, alkoxy, aryloxy, halogène, hydroxy, acylamino, acétamidoalkyle, -COO-alkyle, -COO-aryle, -COO-aralkyle, cyano, sulfonyl, carboxamido ou sulfonamido; R?5¿ représente H, alkyle, fluoroalkyle, halogène, hyroxy, acylamino, acétaminoalkyle, cyano, sulfonile, carboxamido ou sulfonamido; R?6¿ et R?7¿ représentent indépendament alkyle, cycloalkyle, aryle ou aralkyle; et R?8¿ et R?9¿ représentent indépendament H ou -COR?6¿. L'invention concerne en outre deux nouveaux agents de contraste à base d'esters aryloxy iodé ayant la structure ci-dessus aryloxy iodé ayant la structure ci-dessus dans laquelle n est un nombre entier compris entre 5 et 20, des compositions de contraste par rayons X comprenant de tels agents, et des procédés d'imagerie diagnostique par rayons X utilisant ces agents.
Bacon Edward R.
Caulfield Thomas S.
Illig Carl R.
Osifo Irennegbe K.
Nanosystems L.l.c.
Smart & Biggar
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