C07D515/04

Ataxia Telengiectasia And RAD3-Related (ATR) Inhibitors And Methods Of Their Use

The disclosure is directed to compounds and compositions that inhibit Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase and methods of their use.

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Bicyclic methylene aziridines and reactions thereof

The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.

Bicyclic methylene aziridines and reactions thereof

The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.

Inhibitors of KEAP1-Nrf2 protein-protein interaction

Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.

Inhibitors of KEAP1-Nrf2 protein-protein interaction

Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.

Polyester resin, method for producing polyester resin, and toner using said polyester resin

A polyester resin having low-temperature (80-240° C.) fluidity, storage stability, and achieving both dispersibility and grindability, where the polyester resin includes, in reacted form: a polyhydric alcohol; a polycarboxylic acid; a sulfonate component, which is a bis(2-hydroxyethyl)isophthalate sulfonic acid salt; and a hetero alicyclic skeleton, which can be a monomer of formula (1) and/or formula (2): ##STR00001## where X is O, S, or NH and R.sub.1 to R.sub.4 are functional groups. Also, a method for producing the polyester resin by polymerizing a mixture containing the polyhydric alcohol, the polycarboxylic acid, the sulfonate component and the hetero alicyclic skeleton component having formula (1) and/or (2).

Polyester resin, method for producing polyester resin, and toner using said polyester resin

A polyester resin having low-temperature (80-240° C.) fluidity, storage stability, and achieving both dispersibility and grindability, where the polyester resin includes, in reacted form: a polyhydric alcohol; a polycarboxylic acid; a sulfonate component, which is a bis(2-hydroxyethyl)isophthalate sulfonic acid salt; and a hetero alicyclic skeleton, which can be a monomer of formula (1) and/or formula (2): ##STR00001## where X is O, S, or NH and R.sub.1 to R.sub.4 are functional groups. Also, a method for producing the polyester resin by polymerizing a mixture containing the polyhydric alcohol, the polycarboxylic acid, the sulfonate component and the hetero alicyclic skeleton component having formula (1) and/or (2).

SPIRO-SULFONAMIDE DERIVATIVES AS INHIBITORS OF MYELOID CELL LEUKEMIA-1 (MCL-1) PROTEIN

The disclosure is directed to crystalline forms of the compound of Formula I: Formula (I), and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of Formula I as well as methods of their use and preparation, are also described.

##STR00001##