Patent classifications
C07B59/008
Methods and systems for measuring plasma renin activity
Disclosed are methods and systems for the quantification of AngI and/or determination of plasma renin activity in a sample. The methods and systems disclosed herein can be useful for diagnosis of hypertension, aldosteronism and other abnormalities of the renin angiotensin aldosterone system (RAAS).
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.
DEUTERATED FORMS OF CARBETOCIN AND ANALOGS THEREOF
The present disclosure relates to deuterated forms of oxytocin, carbetocin and analogs thereof. The disclosed deuterated compounds may have similar biochemical potency and selectivity as the parent compound, and, in select instances, the selective deuteration may enable substantial benefits to their overall therapeutic profile, such as reduced adverse side effects with a decreased metabolic liability, extended pharmacological effective life, enhanced subject compliance, and/or may also decrease population pharmacokinetic variability. The present disclosure also includes pharmaceutical compositions of deuterated compounds, which may be used to treat various diseases and conditions.
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.
Automatic process platform for the production of astatine-211 [At-211]-radiopharmaceuticals
A system and method for automatic production of astatine-211 labeled molecules is described. The invention represents a significant advantage in the preparation of At-211 radiopharmaceuticals including better reproducibility, reduced production time and increased radiation safety. The invention also enables routine automatic synthesis of radiopharmaceuticals in a clinical setting, in conjunction or at short distance from a cyclotron unit capable of producing the radionuclide.
RADIOLABELING OF POLYPEPTIDES
Improved methods of radiolabeling antibodies using click chemistry are described. Also described are pharmaceutical compositions and uses related to the radiolabeled antibodies produced by the methods.
METHOD FOR LABELING RADIOISOTOPE, RADIOLABELING COMPOUNDS USING QUINONE COMPOUND AND KIT COMPRISING THE SAME FOR LABELING RADIOISOTOPE
The present disclosure relates to a method for labeling a radioisotope includes providing a cyclooctyne compound represented by the following formula (I), and to which a biomolecule, a fluorescent dye, or a nanoparticle compound is bound, and reacting the cyclooctyne compound with a quinone compound represented by the following formula (II) and labeled with the radioisotope in room temperature; a radiolabeling compound represented by the following formula (II), for labeling a molecule having a cyclooctyne moiety; and a composition for medical diagnosis or for treating cancer comprising a quinone compound represented by the following formula (II) and labeled with the radioisotope:
##STR00001##
in formula (I), Z is the biomolecule, the fluorescent dye, or the nanoparticle compound,
##STR00002##
in formula (II), b is 0 or an integer from 1 to 10; L is CH.sub.2, COO, or CONH; M is the radioisotope.
Method for synthesizing iodo- or astatoarenes using diaryliodonium salts
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
18F-LABELED PEPTIDE LIGANDS USEFUL IN PET AND CERENKOV LUMINESCENE IMAGING
The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via .sup.18F-labeled peptide ligands disclosed herein.
METHOD FOR SYNTHESIZING IODO- OR ASTATOARENES USING DIARYLIODONIUM SALTS
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.