The invention relates to novel luminescent compositions of matter containing a fluorophore, synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.

Energetic nitrogen-rich monomers represented by the general Formula I:

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wherein each of X1 and X2 is independently NR or a covalent bond. R is H or C1-4 alkyl, each of T1 and T2 is independently a moiety selected from the group consisting of a triazole moiety, a tetrazole moiety and a guanidine moiety, at least one of T1 and T2 being substituted by at least one polymerizable group, are disclosed herein, as well as polymers based thereon, and uses of such polymers.

Energetic nitrogen-rich monomers represented by the general Formula I:

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wherein each of X1 and X2 is independently NR or a covalent bond. R is H or C1-4 alkyl, each of T1 and T2 is independently a moiety selected from the group consisting of a triazole moiety, a tetrazole moiety and a guanidine moiety, at least one of T1 and T2 being substituted by at least one polymerizable group, are disclosed herein, as well as polymers based thereon, and uses of such polymers.

The present invention relates to a method of preparation of formulations of lanthanide metal complexes of macrocyclic chelators which further comprise a small excess of free chelator. The method uses a solid phase-bound scavenger chelator to remove excess lanthanide metal ions, prior to the addition of a defined excess chelator. Also provided is a method of preparation of MRI contrast agents, together with solid-phase bound chelator meglumine salts useful in the methods.

The present invention relates to a method of preparation of formulations of lanthanide metal complexes of macrocyclic chelators which further comprise a small excess of free chelator. The method uses a solid phase-bound scavenger chelator to remove excess lanthanide metal ions, prior to the addition of a defined excess chelator. Also provided is a method of preparation of MRI contrast agents, together with solid-phase bound chelator meglumine salts useful in the methods.

Disclosed is a novel method of preparing highly pure calcobutrol using an intermediate (butrol) of gadobutrol without using highly pure gadobutrol. This method is capable of obtaining calcobutrol at high purity and high yield through a simple and environmentally friendly process, and thus can be easily applied to mass production.

Disclosed is a novel method of preparing highly pure calcobutrol using an intermediate (butrol) of gadobutrol without using highly pure gadobutrol. This method is capable of obtaining calcobutrol at high purity and high yield through a simple and environmentally friendly process, and thus can be easily applied to mass production.

This application relates to compounds of Formula I. R.sup.1a, R.sup.1b and R.sup.1c is —CO.sub.2H, —SO.sub.2H, —SO.sub.3H, —SO.sub.4H, —PO.sub.2H, —PO.sub.3H or —PO.sub.4H. R.sup.2 is a linker, e.g. butylene. R.sup.3 is a linkage, e.g. —O—, —S—, —S(O)—, S(O).sub.2—, —NHC(O)—, —C(O)NH—, or 1,2,3-triazole. R4 is —(CH.sub.2).sub.0-3CH(R.sup.7)(CH.sub.2).sub.0-3— wherein R.sup.7 is —(CH.sub.2).sub.5CH.sub.3 or certain aromatic fused-ring systems. R.sup.5 and R.sup.6 are hydrogen or methyl. Each Xaa.sup.1 (if present) is an amino acid. R.sup.X is a radiolabeling group, e.g.: a radiometal chelator optionally bound by a radiometal; an aryl substituted with a radioisotope; a prosthetic group containing a trifluoroborate; or a prosthetic group containing a silicon-fluorine-acceptor moiety. The compounds may be useful for imaging prostate-specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

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The present invention relates to metallo-β-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, R.sup.A, X.sub.1, X.sub.2 and R.sup.1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance. ##STR00001##

The present invention relates to an improved process for the preparation of macrocyclic chelant 2,2′,2″-(10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid of formula (1). The present invention further relates to the process for the preparation of metal complexes of macrocyclic chelant 2,2′,2″-(10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid of formula (1) with purity greater than 99.0% by HPLC. The present invention also relates to an improved process for the preparation of gadolinium complex of formula (1a) with macrocyclic chelant 2,2′,2″-(10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid of formula (1). The present invention further relates to a novel process for the preparation of calcium complex of formula (1b) with macrocyclic chelant 2,2′,2″-(10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl) triacetic acid of formula (1).

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