Patent classifications
C07F9/6515
LONG-LIVED GADOLINIUM BASED TUMOR TARGETED IMAGING AND THERAPY AGENTS
Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula:
##STR00001##
or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
Chelated PSMA Inhibitors
Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable diluent; and (3) methods for imaging prostate cancer cells.
##STR00001##
HBED-Bisphosphonates, Radiometal Conjugates and Their Use as Theranostic Agents
The present invention relates to compounds according to Formula I or Formula II, which are potential bone imaging agents. Certain compounds labeled with .sup.68Ga displayed excellent bone uptake and retention. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula II or a pharmaceutically acceptable salt thereof.
##STR00001##
Long-lived gadolinium based tumor targeted imaging and therapy agents
Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001## or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
Long-lived gadolinium based tumor targeted imaging and therapy agents
Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001## or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.