C07B59/00

METHOD FOR PRODUCING AROMATIC ASTATINE COMPOUND

This method for producing an aromatic astatine compound comprises reacting an aromatic iodonium ylide with astatine to produce an aromatic astatine compound.

Isotopologues of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

Method and apparatus for hydrogenation and hyperpolarization of tracer molecules for magnetic resonance imaging

In a method (100 to 208) in which hyperpolarizable tracer molecules (20, 88 to 98) are hydrogenated and then optionally also hyperpolarized for magnetic resonance imaging, it is provided that, in a first method step (104, 202), a hydrogen solution (10, 12, 4) having a saturation factor of at least 50% be prepared and that the hydrogenation reaction (186 to 190, 206) not be triggered until a subsequent, second method step (106, 204). An apparatus (1) with which the method of the invention (100 to 208) is executable is also provided.

Heterodimers of Glutamic Acid
20230095637 · 2023-03-30 ·

Compounds of Formula (Ia)

##STR00001##

wherein R is a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl, a C.sub.1-C.sub.6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p Y is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2, (CH2)p Z is H or C.sub.1-C.sub.4 alkyl, R′ is H, C(O), S(O).sub.2, C(O).sub.2, a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl or a C.sub.1-C.sub.6 substituted of unsubstituted when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C.sub.6-C.sub.12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic, groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Isobaric Multiplex Reagents for Carbonyl Containing Compound High-Throughput Quantitative Analysis

The present invention provides a set of novel isobaric chemical tags, also referred herein as SUGAR (Isobaric Multiplex Reagents for Carbonyl Containing Compound). These labeling tags are compact and easy to synthesize at high yield and purity in just a few steps using commercially available starting materials. The tagging reagents of the present invention comprise: a) a reporter group, having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an aldehyde, ketone, or carboxylic acid reactive group. The multiplex SUGAR tags are able to react with an aldehyde, ketone, or carboxylic acid group of the molecule to be tagged, which offers the capability for labeling and quantitation of glycans, proteins/peptides, and fatty acids.

CGRP ANTIGONISTS USEFUL AS TRACER COMPOUNDS FOR POSITRON EMISSION TOMOGRAPHY
20230096051 · 2023-03-30 ·

The present invention provides a compound of Formula I: wherein R.sup.1 is hydrogen, F, or .sup.18F; and R.sup.2 is hydrogen, F, or .sup.18F; or a pharmaceutically acceptable salt thereof, provided that when R.sup.1 is .sup.18F then R.sup.2 is not .sup.18F, useful as a CGRP receptor antagonist for PET imaging.

##STR00001##

DEUTERATED NICLOSAMIDE
20230102999 · 2023-03-30 ·

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that exhibit activity as mitochondrial uncoupling agents. Said chemical entities are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

A NEW METHOD OF 18F LABELLING AND INTERMEDIATE SALTS

##STR00001##

Disclosed herein is a salt of formula I: where R.sup.1, X, n, R, R.sup.1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.

A NEW METHOD OF 18F LABELLING AND INTERMEDIATE SALTS

##STR00001##

Disclosed herein is a salt of formula I: where R.sup.1, X, n, R, R.sup.1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.

Compounds useful as inhibitors of ATR kinase

The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I-A or I-B: ##STR00001##
wherein the variables are as defined herein.