US 5,412,148 A · Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy

Abstract

Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.

Claims13

Dependent claims

A compound of the formula:

##STR76## wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen, an unshared pair of elections, and C.sub.1 -C.sub.12 alkyls,
R4 is selected from the group consisting of
(a) ##STR77## wherein R6 is selected from the group consisting of hydrogen, an unshared pair of electrons, and C.sub.1 -C.sub.12 alkyls,
(b) ##STR78## wherein R7 is selected from the group consisting of hydrogen, a nitro radical, an amino radical, and
R5 is selected from the group consisting of
(a) ##STR79## wherein R8 is selected from the group consisting of hydrogen, an unshared pair of electrons, and C.sub.1 -C.sub.12 alkyls,
(b) ##STR80## wherein R9 is selected from the group consisting of hydrogen, a nitro radical, an amino radical, and an isothiocyanate radical, and wherein R10 is selected from the group consisting of hydrogen, an unshared pair of electrons, and C.sub.1 -C.sub.12 alkyls, and
(c) ##STR81## wherein R11 is selected from the group consisting of hydrogen, an unshared pair of electrons, and C.sub.1 -C.sub.12 alkyls, and wherein R12 is selected from the group consisting of hydrogen, a nitro radical, an amino radical, and an isothiocyanate radical.

5 more elements

Dependencies are inferred from the claim text.

Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy

Life of this patent

Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy

Life of this patent

Abstract

Claims13