NOVEL CASCADE POLYMER COMPLEXES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
    2.
    发明申请
    NOVEL CASCADE POLYMER COMPLEXES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
    新型聚合物复合物,其制备方法和包含它们的药物组合物

    公开(公告)号:US20080213187A1

    公开(公告)日:2008-09-04

    申请号:US12015769

    申请日:2008-01-17

    IPC分类号: A61K49/06 C07C69/76 C07C39/04

    CPC分类号: A61K49/085 A61K49/124

    摘要: 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.

    摘要翻译: 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。

    Cascade polymer complexes, process for their production and
pharmaceutical agents containing said complexes
    9.
    发明授权
    Cascade polymer complexes, process for their production and pharmaceutical agents containing said complexes 失效
    级联聚合物复合物,其制备方法和含有所述复合物的药剂

    公开(公告)号:US5874061A

    公开(公告)日:1999-02-23

    申请号:US777666

    申请日:1996-12-20

    摘要: Cascade polymer complexes that containa) complexing ligands of general formula IA--{X--�Y--(Z--(W--K.sub.w).sub.z).sub.y!.sub.x }.sub.a, (I) in whichA stands for a nitrogen-containing cascade nucleus of base multiplicity a,X and Y, independently of one another, stand for a direct bond or a cascade reproduction unit of reproduction multiplicity x or y,Z and W, independently of one another, stand for a cascade reproduction unit of reproduction multiplicity z or w,K stands for the radical of a complexing agent, a stands for numbers 2 to 12, x, y, z and w, independently of one another, stand for numbers 1 to 4, provided that at least two reproduction units are different, that 16.ltoreq.a.multidot.x.multidot.y.multidot.z.multidot.w.ltoreq.64 holds true for the product of the multiplicities, and that at least one of cascade reproduction units X, Y, Z, W stands for a 1,4,7,10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane reproduction unit,b) at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83,c) optionally cations of inorganic and/or organic bases, amino acids or amino acid amides as well asd) optionally acylated terminal amino groups are valuable compounds for diagnosis and therapy.

    摘要翻译: 含有a)通式IA- {X- [Y-(Z-(W-Kw)z)y] x} a,(I)的络合配体的级联聚合物络合物,其中A代表含氮级联核 基本多重性a,X和Y彼此独立地代表再现多重性x或y,Z和W的直接键合或级联再现单元,彼此独立地代表再现倍数z的级联再现单位 或w,K表示络合剂的基团,代表数字2至12,x,y,z和w彼此独立地代表数字1至4,条件是至少两个再现单位不同 ,多重性的乘积为16,并且级联再现单位X,Y,Z,W中的至少一个代表1,4,7,10-四氮杂环十二烷或1 ,4,8,11-四氮杂环十四烷再生单元,b)原子序数为20至29,39,42,44或57-83的元素的至少16个离子,c)任选的Inor阳离子 甘氨酸和/或有机碱,氨基酸或氨基酸酰胺以及d)任选地酰化的末端氨基是用于诊断和治疗的有价值的化合物。