Patent classifications
C07F13/00
Radiolabeled and fluorescent PARP inhibitors for imaging and radiotherapy
The present disclosure relates to compounds of Formula I and II, wherein R.sup.1-R.sup.20 and FL are defined herein. Also provided are methods of targeting alpha-radiation to poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, reducing proliferation of cancer cells, reducing proliferation of cancer cells, detecting intact and enzymatically active poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, detecting PARP-1 enzyme expression in a subjects tissue sample, monitoring cancer treatment in a subject, or detecting a PARP-1 receptive cancer in a subject. ##STR00001##
Radiolabeled and fluorescent PARP inhibitors for imaging and radiotherapy
The present disclosure relates to compounds of Formula I and II, wherein R.sup.1-R.sup.20 and FL are defined herein. Also provided are methods of targeting alpha-radiation to poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, reducing proliferation of cancer cells, reducing proliferation of cancer cells, detecting intact and enzymatically active poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, detecting PARP-1 enzyme expression in a subjects tissue sample, monitoring cancer treatment in a subject, or detecting a PARP-1 receptive cancer in a subject. ##STR00001##
PRODUCTION METHOD FOR RADIOLABELED ARYL COMPOUND
The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I, or .sup.131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH).sub.2) or an ester group thereof, with a radionuclide selected from .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I and .sup.131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.
PRODUCTION METHOD FOR RADIOLABELED ARYL COMPOUND
The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I, or .sup.131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH).sub.2) or an ester group thereof, with a radionuclide selected from .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I and .sup.131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.
High Yield Synthesis Of Metal-Organic Frameworks
Metal-organic frameworks are synthesized from either a high concentration synthesis where reaction solutions comprising increased reagent concentrations, or suspensions of reagents which exceed their solubility limit in the reaction solution in a high solids synthesis. In both approaches, the solubility of reagent is maximized by inclusion of a buffer, fixing a nominal pH of the reaction solution to allow metal-organic framework formation. These methods improve yields and scale up of metal-organic frameworks.
Hydroxycitric acid metal heterocyclic compounds with covalent characteristics
Hydroxycitric acid-metal heterocyclic compounds with covalent characteristics are provided. The subject hydroxycitric acid compounds include monomeric hydroxycitric acid (HCA) compounds having a divalent metal, lactone forms thereof, and dimeric compound forms thereof. The monomeric HCA compound includes a divalent metal (X) bonded via a 5-membered ring to both the carboxylic acid and the hydroxy group of the central C2 carbon of the HCA. In addition, a monovalent metal (Y) can also be bonded to the carboxylic acid of C3 or C1, or to both C1 and C3. The subject dimeric compounds include monomeric HCA compounds linked via a second divalent metal (X) to a carboxylic acid group of each HCA unit at C3 or C1. Also provided are compositions including a monomeric HCA compound and one or more other additional compounds. Methods of alleviating at least one symptom associated with a target disease or condition in a subject are provided.
PSMA-TARGETING COMPOUNDS AND USES THEREOF
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
Coordination Complex and Electronic Device Comprising the Same
The present invention relates to an electronic device comprising a hole injection layer and/or a hole transport layer and/or a hole generating layer, wherein at least one of the hole injection layer, the hole transport layer and the hole generating layer comprises a coordination complex comprising at least one electropositive atom M having an electro-negativity value according to Allen of less than 2.4 and at least one ligand L having the following structure:
##STR00001##
wherein R.sup.1 and R.sup.2 are independently selected from the group, consisting of C.sub.1 to C.sub.30 hydrocarbyl groups and C.sub.2 to C.sub.30 heterocyclic groups, wherein R.sup.1 and/or R.sup.2 may optionally be substituted with at least one of CN, F, Cl, Br and I.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
The present invention includes novel heteroleptic/homoleptic iridium complexes containing two tridentate ligands, where at least one of the tridentate ligands comprises of pyridinium-derived N-heterocyclic carbene. The compounds of the present invention may be useful for organic electroluminescent devices.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
The present invention includes novel heteroleptic/homoleptic iridium complexes containing two tridentate ligands, where at least one of the tridentate ligands comprises of pyridinium-derived N-heterocyclic carbene. The compounds of the present invention may be useful for organic electroluminescent devices.