A61K2123/00

Bifunctional do2pa derivatives, chelates with metallic cations and use thereof

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. ##STR00001##

ANTIBODIES
20230391851 · 2023-12-07 ·

A method for analyzing protein(s) in a sample using an immunoassay kit includes creating protein-reducing and/or protein-denaturing conditions by contacting the sample with a reducing and/or denaturing agent provided in the immunoassay kit, to provide a partially or fully denatured protein population. One or both of a presence and an amount of one or more protein-associated analytes are determined under the created protein-reducing and/or protein-denaturing conditions by contacting the partially or fully denatured protein population with one or more specific antibodies or binding fragments thereof provided in the immunoassay kit. The one or more specific antibodies or binding fragments thereof include one or more chemically-introduced non-disulfide cross-links between at least one heavy chain or binding fragment thereof and at least one light chain or binding fragment thereof.

TRUNCATED EVANS BLUE MODIFIED FIBROBLAST ACTIVATION PROTEIN INHIBITOR, PREPARATION METHOD AND APPLICATION THEREOF

The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L.sub.1, L.sub.2, L.sub.3, L.sub.4 and X. The compound has the following structure shown in Formula (I), where R.sub.1 is a fibroblast activation protein inhibitor; L.sub.1 is lysine, glutamic acid, or a derivative structure thereof; L.sub.2 is —(CH.sub.2).sub.n—, n is an integer from 0 to 30, and each —CH.sub.2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L.sub.3 is —(CH.sub.2).sub.m—, m is an integer from 0 to 30, and each —CH.sub.2— may be individually substituted or unsubstituted with —O— or —(CO)—; L.sub.4 is —(CH.sub.2).sub.p—, p is an integer from 0 to 30, and each —CH.sub.2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or

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and R.sub.2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-life in blood circulation, improving the uptake and enrichment in tumors and prolonging the retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of FAP.

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Half-Curcuminoids as Amyloid-Beta PET Imaging Agents
20220001035 · 2022-01-06 ·

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Half-curcuminoids as amyloid-beta PET imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

ENHANCED SURGICAL VISUALIZATION OF VIABLE TISSUE AND PEPTIDES THEREFOR
20210268127 · 2021-09-02 ·

The various embodiments relate to the identification of non-viable tissue for debridement using a pH low insertion peptide conjugate. pH low insertion peptide conjugates are described having fluorescent dye for introduction to the wound area. The peptides may further be conjugated with a drug for introduction to the tissue.

.SUP.18.F-labeled compounds for PET imaging and uses thereof

The present invention relates to .sup.18F-labeled compounds suitable for positron emission tomography (PET) imaging. The invention further relates to the use of these compounds for carrying out PET scans, imaging the indoleamine 2,3-dioxygenase, pathway, predicting the responsiveness of a subject with a solid tumor to therapies including immunotherapy such as PD-1/PD-L1 inhibition, and determining whether a solid tumor in a subject contains tumor-infiltrating immune cells.

CONFORMATIONAL RESTRICTION OF CYANINE FLUOROPHORES IN FAR-RED AND NEAR-IR RANGE

Conformationally restricted cyanine fluorophores, as well as methods of making and using the compounds, are described. The conformationally restricted cyanine fluorophores have a chemical structure according to Formula I, or a stereoisomer or pharmaceutically acceptable salt thereof:

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wherein A is

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and wherein each “*” designates an attachment point of A.

Method for injectable delivery of a therapeutic agent into a fish embryo
11078460 · 2021-08-03 ·

Fish embryos may be successfully vaccinated or therapeutically treated if the therapeutic agent is injected into the yolk sac. Therapeutic agents may be directly injected or released from microspheres and enter the circulation and tissues. Injection into the yolk sac, combined with the use of carriers, allows for a continued, controlled release of therapeutic agents and processing of antigens. Fish vaccination or therapeutic treatment, selecting fish embryos post fertilization at the one-cell to eyed egg stage of development, and injecting the yolk sac with carriers associated with an antigen(s) or therapeutic agent(s), may be fully automated.

RADIOLABELLED mGluR2 PET LIGANDS

The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.