Dendritic cascade polymers with hydrophilic iodineDendritic cascade polymers with hydrophilic iodine containing aromatics useful for preparation of X- containing aromatics useful for preparation of X-ray diagnostic agents for vascular diseases and foray diagnostic agents for vascular diseases and for cancer diagnosis r cancer diagnosis

摘要

Cascade polymers with hydrophilic iodine containing aromatics, i.e. polypropyleneamine-dendrimer (POPAM) as polymer with terminal amine groups and vinyl cyanide branch units, a triiodiaromatic signal group, a 1-15C carbon chain, and 1-20C alkyl groups are new. Cascade polymers of formula P-(K)m (I) are new. P = dendritic POPAM containing m terminal primary amine groups, with vinyl cyanide branch units; m = 4-128; K = a triiodoaromatic signal group, where the signal giving group K is a triiodoaromatic of formula (II) (denotes binding site of dendrimer amine group); L = straight chain, branched, optionally unsaturated 1-15C carbon chain, which can be interrupted by 1-3 S atoms, 1-5 sulfonyl groups, and can be substituted by 1-6 OH groups or 1-3 (CH2)p-COO2OH groups; p = 0-10; R1 = H or (CH2)q-COO2OH group; q = 1-10; X = OH, O-Na+, O-Meglumin+,or NR2R3; Y = OH, -O-Na+, -O-Meglumin+ or NR4R5; R2-R5 = H, straight chain or branched 1-20C alkyl, where alkyl group can be interrupted by 1-6 O atoms and/or can be substituted by 1-6 OH groups; R2-R5+N = form a heterocyclic ring, which optionally can be substituted by 1-3 OH; L = -CH2CH2-, -CH2CH2CH2-, -CH2OCH2-, CH2CH(OH)CH2-, CH2OCH2CH2OCH2-; R1 = H, CH2COOH, CH2CH2COOH, X, Y when identical = -N(CH3)CH2CH(OH)CH2OH, -N(CH2CH(OH)CH2OH)2, -NHCH2CH(OH)CH2OH, NHCH(CH2OH)2, -N(CH3)CH2CH(OH)CH(OH)CH(OH)CH(OH)CH2OH; -NHCH2CH(OH)CH(OH)CH(OH)CH(OH)CH2OH; X, Y when not identical = -N(CH2CH(OH)CH2OH)2, -NHCH2CH(OH)CH2OH, -NHCH(CH2OH)2; and Y = -N(CH3)-CH2-CH(OH)-CH2OH. Independent claims are also included for: (1) a process for preparation of the dendritic polymers by reaction of a polymer of formula I with an activated acid derivative of formula (III); (2) a method for preparation of a pharmaceutical agent by dissolution or suspension of an iodine containing dendritic polymer containing conventional additives in a form suitable for parenteral or enteral administration; (3) a pharmaceutical agent containing at least one dendritic polymer for preparation of an X-ray diagnostic agent. W' = Cl, Br or I, or together with adjacent carbonyl group forms a mixed anhydride; m = 4-128. All other definitions are as above.