A61K51/0455

Precursors for radiofluorination

A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [.sup.18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A.sup.1 to the bonding unit and via bond A.sup.2 to the ring, wherein the bonding unit has second substituent(s) OH, CONH, and/or COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is N.sup.+(R.sup.1R.sup.2R.sup.3), NO.sub.2, Cl, Br, F, or I, and R.sup.1, R.sup.2, and R.sup.3 are independently C.sub.1-C.sub.6 alkyl; and (b) reacting the precursor with a [.sup.18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N.sup.+(R.sup.4R.sup.5R.sup.6R.sup.7) with R.sup.4, R.sup.5, R.sup.6, and R.sup.7 being independently C.sub.1-C.sub.6 alkyl, wherein the substituent Y is replaced by [.sup.18F] fluoride.

SYSTEMS AND METHODS FOR PLATFORM AGNOSTIC WHOLE BODY IMAGE SEGMENTATION

Presented herein are systems and methods that provide for automated analysis of three-dimensional (3D) medical images of a subject in order to automatically identify specific 3D volumes within the 3D images that correspond to specific anatomical regions (e.g., organs and/or tissue). Notably, the image analysis approaches described herein are not limited to a single particular organ or portion of the body. Instead, they are robust and widely applicable, providing for consistent, efficient, and accurate detection of anatomical regions, including soft tissue organs, in the entire body. In certain embodiments, the accurate identification of one or more such volumes is used to automatically determine quantitative metrics that represent uptake of radiopharmaceuticals in particular organs and/or tissue regions. These uptake metrics can be used to assess disease state in a subject, determine a prognosis for a subject, and/or determine efficacy of a treatment modality.

NOVEL DEUTERIUM SUBSTITUTED POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENTS AND THEIR PHARMACOLOGICAL APPLICATION

The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

STABILIZATION OF RADIOPHARMACEUTICAL COMPOSITIONS USING ASCORBIC ACID

Radiopharmaceutical compositions, and related methods, useful for medical imaging are provided. The radiopharmaceutical compositions include one or more radiopharmaceutical compounds, together with a stabilizer comprising ascorbic acid, wherein the pH of said composition is within the range of about 3.5-5.5.

SUBSTITUTED ORGANOFLUOROBORATES AS IMAGING AGENTS
20200222563 · 2020-07-16 ·

Fluoridated organofluoroborates comprising at least one .sup.18F atom and precursors thereto, for use in PET scanning.

N-[(Pyrimidinylamino)propanyl]-and N-[(Pyridinylamino)-propanyl]arylcarboxamides

The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.

Fluorinated imidazo[4,5-C]quinoline derivatives as inhibitors of bromodomain containing proteins

A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins. ##STR00001##

PRECURSORS FOR RADIOFLUORINATION

A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [.sup.18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A.sup.1 to the bonding unit and via bond A.sup.2 to the ring, wherein the bonding unit has second substituent(s) OH, CONH, and/or COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is N.sup.+(R.sup.1R.sup.2R.sup.3), NO.sub.2, Cl, Br, F, or I, and R.sup.1, R.sup.2, and R.sup.3 are independently C.sub.1-C.sub.6 alkyl; and (b) reacting the precursor with a [.sup.18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N.sup.+(R.sup.4R.sup.5R.sup.6R.sup.7) with R.sup.4, R.sup.5, R.sup.6, and R.sup.7 being independently C.sub.1-C.sub.6 alkyl, wherein the substituent Y is replaced by [.sup.18F] fluoride.

Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins

The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.

Compositions and methods for AL amyloid detection and uses thereof
10660976 · 2020-05-26 · ·

Among the various aspects of the present disclosure is the provision of compositions and methods for imaging and treating subjects with amyloidosis or multiple myeloma with or without amyloidosis.