C07B59/008

MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT
20190240360 · 2019-08-08 · ·

A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH.sub.2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.

COMPOSITIONS AND METHODS FOR DETECTION OF BETA N METHYLAMINO L ALANINE IN CU ZN SUPEROXIDE DISMUTASE 1
20190241607 · 2019-08-08 ·

Provided herein are isotopically labeled reagents, including isotopically labeled small molecules and peptides, that can be used to detect and/or quantify -N-methylamino-L-alanine (BMAA) in the Cu/Zn Superoxide Dismutase 1 (SOD1) protein. Further provided are methods for detecting, preventing, or treating amyotrophic lateral sclerosis in a subject using isotopically labeled reagents to detect and/or quantify -N-methylamino-L-alanine (BMAA) in the Cu/Zn Superoxide Dismutase 1 (50D1) protein. Further provided are isotopically labeled reagents and methods for detecting BMAA in additional proteins from patient samples.

PREPARATION OF 212PB LABELED MONOCLONAL ANTIBODIES
20190194087 · 2019-06-27 ·

The present invention relates to the generation of lead-212 for therapeutic use. Specifically, are methods related to the generation of lead-212 based radio labelled proteins, such as radioimmunoconjugates, embodiments of the present invention.

MATERIALS AND METHODS FOR DETECTION AND QUANTIFICATION OF BETA-N-METHYLAMINO-L-ALANINE

Provided herein are isotopically labeled reagents, including isotopically labeled small molecules and peptides, that can be used to detect and/or quantify -N-methylamino-L-alanine (BMAA) in a sample. The reagents can be used as stable isotope labeled standards in analytical methods, including in conjunction with mass spectrometry, to detect and/or quantify BMAA in a sample, such as a protein sample from a subject.

Methods and compositions for imaging amyloid deposits

Methods and diagnostic compositions for detection of amyloid deposits using a chimeric (e.g., mouse-human) antibody or antigen-binding fragment thereof linked to a detectable label are disclosed.

COMPOUND AND LABELED BIOLOGICAL SUBSTANCE USING THE SAME

There are provided a compound having at least two phosphor moieties and a structure represented by General Formula (I), and a labeled biological substance.

##STR00001##

In the formula, X.sup.1 to X.sup.3 represent O, S, >NR.sup.1, or >CR.sup.2R.sup.3. R.sup.1 to R.sup.3 represent a hydrogen atom or a substituent. L.sup.a and L.sup.b represents a single bond or a divalent linking group. n is an integer of 2 or more.

However, at least one among R.sup.1 to R.sup.3, which are contained in a structure parenthesized in ( ).sub.n, L.sup.a, and L.sup.b includes -(L-O).sub.gR.sup.E, where -(L-O).sub.gR.sup.E in each of these groups is not bonded to at least any one of a phosphor or a biological substance.

L represents an alkylene group, R.sup.E represents a hydrogen atom or an alkyl group, and g is 1 to 24.

* represents a bonding site.

PSMA targeted compounds and uses thereof

PSMA targeted compounds, pharmaceutical compositions comprising these compounds, and methods for treating and detecting cancers in a subject are described herein.

Radiotracer compositions and methods

The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to radiotracer compositions which comprises .sup.18F-labelled c-Met binding peptides. The invention provides said compositions, as well as associated automated methods of preparation and cassettes.

METHODS OF MAKING 18F-LABELED PRECURSORS AND PEPTIDES, LABELED C-MET BINDING PEPTIDES, AND METHODS OF USE THEREOF
20190151483 · 2019-05-23 ·

Described herein are novel methods for the synthesis of radiolabeling synthons such as [.sup.18F]fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester, and also methods of labeling a protein or peptide comprising a free amine group. A novel c-Met binding peptide, and imaging methods, are also described.

ISOTOPICALLY MODIFIED COMPOSITION AND THERAPEUTIC USES THEREOF
20190084900 · 2019-03-21 ·

This disclosure relates to isotopically modified amino acids and their pharmaceutical or nutritional uses in stabilizing pharmaceutical protein-based formulations, proteins with long life span, and preventing or treating disease such as Alzheimer's disease. Specifically, the disclosure provides protein drugs having increased stability comprising an L-aspartate (L-Asp) residue or an L-asparagine (L-Asn) residue, wherein the L-Asp residue or the L-Asn residue comprises a deuterium atom.