The present invention has an object to provide a phosphoramidite activator that improves a solubility of 5-benzylthio-1H-tetrazole in acetonitrile and does not reduce the yield and a purity of a target product.

The present invention relates to a phosphoramidite activator containing (i) at least one compound that is selected from the group consisting of piperidine, pyrrolidine, N-alkylpiperidine, and N-alkylpyrrolidine, (ii) 5-benzylthio-1H-tetrazole, and (iii) acetonitrile; and a method for activating a phosphoramidite and a method for synthesizing a phosphate ester or a thiophosphate ester, both methods using the activator.

Compounds and compositions that have a Protein Recognition Moiety bound to an electrophile for the selective covalent modification of targeted proteins to treat disorders mediated by the targeted protein are described.

Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes click chemistry to covalently bind reporter molecules to tissue.

Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes click chemistry to covalently bind reporter molecules to tissue.

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.

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.

Dual-modality contrast agents are disclosed herein, having the general formula:

##STR00001## R.sub.1 includes a chelating moiety that is chelated to a Mn.sup.2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

The present invention relates to new class of functionalized polyazamacrocycles including at least one phosphonic or phosphinic group linked to a nitrogen atom of the macrocyclic cage, and capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.