C07D257/02

BIFUNCTIONAL do2pa DERIVATIVES, CHELATES WITH METALLIC CATIONS AND USE THEREOF
20220143230 · 2022-05-12 ·

Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R.sup.1, R.sup.1′, R.sup.2, R.sup.2′, R.sup.3, R.sup.3′, L.sup.1, L.sup.1′, L.sup.2 and L.sup.2′ are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.

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DOTA-HAPTEN COMPOSITIONS FOR ANTI-DOTA/ANTI-TUMOR ANTIGEN BISPECIFIC ANTIBODY PRETARGETED RADIOIMMUNOTHERAPY

The present disclosure provides compositions and methods for the detection and treatment of cancer. Specifically, the compositions of the present technology include novel compounds that may be complexed with a radioisotope. Also disclosed herein are methods of the using the DOTA-haptens of the present technology in diagnostic imaging as well as pretargeted radioimmunotherapy.

METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T.sub.1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T.sub.1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. .sup.86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T.sub.1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T.sub.1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. .sup.86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

PROCEDURE FOR OBTAINING GADOTERATE MEGLUMINE FROM HIGH-PURITY TETRAXETAN (DOTA) AND ITS USE IN THE PREPARATION OF INJECTABLE GALENICAL FORMULATIONS

The present invention refers to a process for obtaining gadoterate meglumine from high purity tetraxetan (DOTA) which does not require the use of organic solvents and optimizes the conditions of the synthetic process. The tetraxetan from which the gadoterate meglumine is obtained by a synthetic process that includes a purification step in which at least one electrodialysis is performed. This procedure makes it possible to obtain a tetraxetan and a gadoterate meglumine with minimal amounts of impurities.

PROCEDURE FOR OBTAINING GADOTERATE MEGLUMINE FROM HIGH-PURITY TETRAXETAN (DOTA) AND ITS USE IN THE PREPARATION OF INJECTABLE GALENICAL FORMULATIONS

The present invention refers to a process for obtaining gadoterate meglumine from high purity tetraxetan (DOTA) which does not require the use of organic solvents and optimizes the conditions of the synthetic process. The tetraxetan from which the gadoterate meglumine is obtained by a synthetic process that includes a purification step in which at least one electrodialysis is performed. This procedure makes it possible to obtain a tetraxetan and a gadoterate meglumine with minimal amounts of impurities.

Method for manufacturing calteridol

It is disclosed a method for preparing calteridol used as MRI contrast agents. It provides a method for preparing calteridol comprising: obtaining teridol represented by the following Formula 2 by reacting gadoteridol represented by the following Formula 1 with decomplexing agent; and obtaining calteridol represented by the following Formula 3 by reacting calcium ion with teridol represented by following Formula 2. ##STR00001##

Method for manufacturing calteridol

It is disclosed a method for preparing calteridol used as MRI contrast agents. It provides a method for preparing calteridol comprising: obtaining teridol represented by the following Formula 2 by reacting gadoteridol represented by the following Formula 1 with decomplexing agent; and obtaining calteridol represented by the following Formula 3 by reacting calcium ion with teridol represented by following Formula 2. ##STR00001##

NOVEL AZOBENZENE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE FOR THERAPEUTIC TREATMENT ASSOCIATED WITH IONIZING RADIATIONS

The present invention relates to new ionizing radiation-activatable derivatives, their preparation process and their therapeutic uses.

NOVEL AZOBENZENE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE FOR THERAPEUTIC TREATMENT ASSOCIATED WITH IONIZING RADIATIONS

The present invention relates to new ionizing radiation-activatable derivatives, their preparation process and their therapeutic uses.