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 therof. 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.

A process is provided in which the resulting Fe-tCDTA contrast agent has a reduced osmolality. The process according to the invention comprises the following steps: a) preparing an aqueous solution of tCDTA and FeO(OH), tCDTA and FeO(OH) being present in a molar ratio of from 1:1 to 1:1.4; b) b.1) adjusting a pH of the aqueous solution to between pH 2.5 and pH 4.5 by adding a base, preferably meglumine, and separating the precipitate; or b.2) precipitating the Fe-tCDTA contrast agent from the aqueous solution by adding acetone, separating the precipitate, and preparing an aqueous solution from the precipitate; and c) adjusting a pH of the aqueous solution to between pH 6.5 and pH 8.0 by adding a base, preferably meglumine, and separating the precipitated FeO(OH).

The present invention relates to a complex of formula (II) constituted of at least 90% of a diastereoisomeric excess comprising a mixture of isomers II-RRR and II-SSS of formulae:

##STR00001##

The present invention also relates to a process for preparing and purifying said complex of formula (II), and also to a composition comprising said complex.

Disclosed herein are a dual-targeted carbonic anhydrase IX complex, a contrast agent comprising the same, and a synthesizing method thereof. The dual-targeted carbonic anhydrase IX complex includes a carbonic anhydrase IX (CA9) binding peptide, a sulfonamide derivative, and a metal chelating agent. The dual-targeted carbonic anhydrase IX complex has potential for use as a molecular nuclear drug.

The present invention relates to a new class of high relaxivity extracellular gadolinium chelate complexes, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents.

In some aspects, the present disclosure provides gadolinium based sensors which may be used to image zinc ions in vivo. In some embodiments, the compounds show appropriate reactivity with zinc ions while maintaining high relaxivity to achieve improved background relative to other sensors.

The present invention relates to compounds (reactive conjugates) for the chemical modification of therapeutic antibodies or proteins. The compounds enable the regioselective attachment of payloads to an antibody or antibody fragment in one single step, thereby producing a modified antibody or modified antibody fragment, which can be used for diagnosing, monitoring, imaging or treating disease.

Gadolinium based contrast agents (GCA) incorporating linear ligand chelation are fundamentally different from GCAs incorporating macrocyclic ligands. The macrocyclic GCAs are synthesized by pathways characterized by the formation of a sequence of metastable complexes before obtaining the final stable complex. The synthesis of linear GCAs do not form metastable complexes. Commercial macrocyclic GCAs contain unstable metastable complexes. These metastable species are not regulated and quickly release free Gd3+ ions upon administration into the body. Gadolinium based contrast agents with near zero metastable species content and methods of synthesizing the same are disclosed. Gadolinium based contrast agents with long dissociation time in the body, and low free Gd3+ ion formation are obtained using a synthesis method which departs in novel ways from the traditional free Gd3+-based synthesis methods.

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macrocyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.

The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof.