Dendritic amplifier molecules having multiple terminal active gr

Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing

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436173, 436803, 436806, 1286534, 128654, 5303913, 534 16, 514241, 514408, 514645, 556 50, 556 61, 556148, 544181, 544211, 560 35, 560171, 562561, 562565, 564 26, 564 27, 564 29, 424 934, 424 935, 424 933, 424 9361, C07F 1100, A61K 4900, A61K 4902, C12N 996, C07D20948, C07D20738, C07C 6980

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active

055674119

ABSTRACT:
Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject. Also disclosed are methods for using the compounds in diagnosis and therapy, such as obtaining a magnetic resonance image of a subject.

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