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    • 2. 发明授权
    • Copolymers and their use as contrast agents in magnetic resonance
imaging and in other applications
    • 共聚物及其作为造影剂在磁共振成像和其他应用中的用途
    • US5458127A
    • 1995-10-17
    • US305257
    • 1994-09-13
    • Evan C. UngerGuanli Wu
    • Evan C. UngerGuanli Wu
    • A61B5/055A61B19/00A61K49/00A61K49/12A61K51/06C08G63/12C08G63/16C08G63/66C08G63/68C08G63/682C08G63/685C08G63/688C08G63/91C08G69/26C08G69/40C08G69/48C08G73/00C08G73/02C08G75/02C08G75/04C08G75/26C08G79/00G01R33/28A61B5/05
    • G01R33/5601A61B90/39A61K49/0002A61K49/103A61K49/126A61K49/128A61K51/06A61K51/065C08G63/68C08G69/40C08G69/48C08G79/00A61B2090/3954A61K2123/00Y10S436/808Y10T436/24
    • Novel compounds having use as contrast agents in magnetic resonance imaging, as well as other uses, are described. The compounds are comprised of a copolymer which comprises at least two of a first monomer of the formula X.sub.1 --(CHR.sub.2 CHR.sub.2 -Y).sub.n -(CHR.sub.2).sub.m --CHR.sub.2 CHR.sub.2 13 X.sub.2, wherein X.sub.1 and X.sub.2 are, independently, OH, NH.sub.2, NHR.sub.1, COOH, COOR.sub.1, SH, or Z, Y is O, NH, NR.sub.1, S, or CO, n is 0-10,000, m is 0 or 1, each Z is, independently, Cl, Br, or I, each R.sub.1 is, independently, a C.sub.1 -C.sub.20 substituted alkyl or cycloalkyl, and each R.sub.2 is, independently, H or OH, and at least one of a second monomer which is a polynitrilo chelating agent having at least two COOH, COOR.sub.1, or COZ groups, the first and second monomers being bound to one another to form a copolymer through an ester, amide, or carboxylic thioester linkage of at least one of the OH, NH.sub.2, NHR.sub.1, COOH, COOR.sub. 1, SH or Z groups of the first monomer, and at least one of the COOH, COOR.sub.1, or COZ groups of the second monomer. Optionally, the copolymer may also include at least one of a third monomer which is a targeting agent or a targeting agent ligand having an OH, NH.sub.2, NHR.sub.1, COOH, COOR.sub.1, SH, or COZ group, wherein R.sub.1 is described as above, and wherein the third monomer is also bound with the first and second monomers to form a copolymer through an ester, amide, or carboxylic thioester linkage. For magnetic resonance imaging, for example, the copolymer may further comprise a paramagnetic ion chelated to the chelating agent.
    • 描述了在磁共振成像中用作造影剂的新型化合物以及其它用途。 所述化合物由包含式X1-(CHR2CHR2-Y)n-(CHR2)m-CHR2CHR2X2的第一单体中的至少两种的共聚物组成,其中X 1和X 2独立地是OH,NH 2,NHR 1, COOH,COOR1,SH或Z,Y是O,NH,NR1,S或CO,n是0-10,000,m是0或1,每个Z独立地是Cl,Br或I,每个R1是 独立地是C 1 -C 20取代的烷基或环烷基,并且每个R 2独立地是H或OH,以及作为具有至少两个COOH,COOR1或COZ基团的多元三叉螯合剂的第二单体中的至少一种, 第一和第二单体彼此结合以通过第一单体的OH,NH 2,NHR 1,COOH,COOR 1,SH或Z基团中的至少一个的酯,酰胺或羧酸硫键连接形成共聚物,以及 第二单体的COOH,COOR1或COZ基团中的至少一个。 任选地,共聚物还可以包括作为靶向剂的第三单体或具有OH,NH 2,NHR 1,COOH,COOR 1,SH或COZ基团的靶向剂配体中的至少一种,其中R 1如上所述,以及 其中第三单体也与第一和第二单体结合以通过酯,酰胺或羧酸硫酯键形成共聚物。 对于磁共振成像,例如,共聚物可以进一步包含与螯合剂螯合的顺磁离子。