Amplifier molecules for enhancement of diagnosis and therapy

DETAILED DESCRIPTION As used herein, an "amplifier" or "amplifier molecule" is a chemical compound having a multiplicity of terminal amine moieties, each serving as a locus to which one or two of any of several desired functional groups can be chemically attached, thereby allowing the synthesis of branched molecules having a multiplicity of functional groups per molecule.
As described herein, chemical groups having pharmacologic utility can be attached to the terminal amines of amplifier molecules, yielding molecules having an enhanced effect over molecules having only one such group.
An "amplification factor" refers to the number of terminal amines present in each amplifier molecule.
For example, a molecule with an amplification factor of six has six terminal amines.
Each terminal amine, in turn, can accept either one or two functional groups, depending on the particular group added thereto, in place of the hydrogen atoms.
Any of the amplified pharmacological compounds of the present invention may be introduced into the body of a human or other warm-blooded animal by any pharmacologically suitable carrier.
Generally, buffered isotonic saline solution is the carrier of choice.
Compounds intended for diagnostic use are generally administered intravenously such as presently done, for example, with gadolinium-DTPA for MRI contrast enhancement.
The following basic methods and equipment were used during the work resulting in the present invention: Melting points were obtained on a Thomas Hoover apparatus and were uncorrected.
NMR spectra were recorded on a Nicolet QE 300 spectrometer in CDCl.
sub.
3 unless otherwise stated.
Chemical shifts are expressed in d units relative to tetramethylsilane (Me.
sub.
4 Si).
IR spectra were recorded on a Nicolet DX-FT IR spectrometer in CDCl.
sub.
3 solvent unless otherwise stated.
Elemental analyses were determined by Desert Analytics, Tucson, Ariz.
All reactions were routinely run under N.
sub.
2 atmosphere.
For flash chromatography, Grade 633, 200-425 mesh 60