Patent classifications
C07B59/008
MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT
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
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
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
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
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.