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    • 2. 发明申请
    • NOVEL CASCADE POLYMER COMPLEXES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
    • 新型聚合物复合物,其制备方法和包含它们的药物组合物
    • US20080213187A1
    • 2008-09-04
    • US12015769
    • 2008-01-17
    • Heribert SCHMITT-WILLICHHeiko SchirmerBernd MisselwitzHanns-Joachim WeinmannPeter Caravan
    • Heribert SCHMITT-WILLICHHeiko SchirmerBernd MisselwitzHanns-Joachim WeinmannPeter Caravan
    • A61K49/06C07C69/76C07C39/04
    • A61K49/085A61K49/124
    • The invention relates to novel cascade polymer complexes, to compositions comprising these compounds, to the use of the complexes in NMR diagnosis, and to processes for preparing these compounds and compositions. The complex-forming cascade polymer complexes according to the invention can be described by general formula I: R-L-A-{X—[Y-(Z-{W—Kw}z)y]x}a−1   (I) where R=is an HSA-binding unit, L=is a linker or a bond, A=is a nitrogen-containing cascade core of base multiplicity a, X and Y are independently of one another a direct linkage or a cascade reproduction unit of reproduction multiplicity x and y, respectively, Z and W=are independently of one another a direct linkage or a cascade reproduction unit of reproduction multiplicity z and w, respectively, K is the residue of a complexing agent, a=is numbers 2 to 12, and x, y, z and w are independently of one another the numbers 1 to 4, with the proviso that exactly one multiplicity of the base multiplicity a of the cascade core A represents exactly one point of linkage to L, and with the proviso that the cascade polymer complexes comprise in the complexing agent residue K in total at least 4 ions of an element of atomic number 20 to 29, 39, 42 to 44 or 57 to 83 and comprise where appropriate cations of inorganic and/or organic bases, amino acids or amino amides.
    • 本发明涉及新颖的级联聚合物复合物,包含这些化合物的组合物,在NMR诊断中使用复合物,以及制备这些化合物和组合物的方法。 根据本发明的络合物形成级联聚合物复合物可以由通式I描述:<?in-line-formula description =“In-line Formulas”end =“lead”?> RLA- {X- [Y-( a-1 (I)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中R =是HSA结合单元,L =是接头或键,A = 包含碱基多重性a的级联核心,X和Y彼此独立地是再现倍数x和y的直接联动或级联再现单元,Z和W =彼此独立地是直接联动或级联再现单元 分别是繁殖多重度z和w,K是络合剂的残基,a =数字2至12,x,y,z和w彼此独立地为数字1至4,条件是准确地 级联核心A的碱基多重性a的一个多重性恰好代表连接点t的一个点 o L,条件是级联聚合物络合物在配位剂中含有总共至少4个原子序数为20至29,39,42至44或57至83的元素的残基K,并且包含适当的阳离子 无机和/或有机碱,氨基酸或氨基酰胺。