C07D273/02

AI ASSISTED CYCLIC CARBONATE MONOMER SYNTHESIS

A method for synthesizing cyclic carbonate monomers using carbon dioxide (CO.sub.2) is provided. The method also includes combining reagents to synthesize the cyclic carbonate monomer, the reagents including a substrate that is a 1,X-diol, where X is between 2 and 5, a base that is a tertiary amine, a promoter that is a multidentate, bis-tertiary amine base where nitrogens are separated by 2 to 4 carbon atoms, a solvent, and CO.sub.2.

AI ASSISTED CYCLIC CARBONATE MONOMER SYNTHESIS

A method for synthesizing cyclic carbonate monomers using carbon dioxide (CO.sub.2) is provided. The method also includes combining reagents to synthesize the cyclic carbonate monomer, the reagents including a substrate that is a 1,X-diol, where X is between 2 and 5, a base that is a tertiary amine, a promoter that is a multidentate, bis-tertiary amine base where nitrogens are separated by 2 to 4 carbon atoms, a solvent, and CO.sub.2.

Macrocyclic immunomodulators

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): ##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS

The compounds of the present invention are represented by the following compounds having Formula I and Formula (I′): where the substituents R.sup.1, R.sup.2, R.sup.2′, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein and where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

##STR00001##

PET PROBES OF RADIOFLUORINATED CARBOXIMIDAMIDES FOR IDO-TARGETED IMAGING
20170340758 · 2017-11-30 ·

.sup.18F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-amino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an .sup.18F. The .sup.18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.

PET PROBES OF RADIOFLUORINATED CARBOXIMIDAMIDES FOR IDO-TARGETED IMAGING
20170340758 · 2017-11-30 ·

.sup.18F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-amino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an .sup.18F. The .sup.18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.

AN IMPROVED PROCESS FOR THE PREPARATION OF RALTEGRAVIR

The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

##STR00001##

AN IMPROVED PROCESS FOR THE PREPARATION OF RALTEGRAVIR

The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

##STR00001##

Compounds for use as iron(III) MRI contrast agents

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macrocyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.

Synthesis of syrbactin proteasome inhibitors

The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs.