1006380-18-2

Upstream product

• 149105-00-0 N-(4-bromo-3-methylphenyl)methanesulfonamide 
• 73183-34-3 bis(pinacol)diborane 
• 631911-01-8 3-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenylamine 
• 124-63-0 methanesulfonyl chloride 
• 883715-40-0 2-(2-methyl-4-nitrophenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane 
• 7149-70-4 2-bromo-5-nitrotoluene 

Downstream Products

• 1357093-77-6 N-(4-(5-bromo-4-methoxypyridin-3-yl)-3-methylphenyl)methanesulfonamide 
• 1312099-10-7 N-(4-(4-bromo-2-formylthiophen-3-yl)-3-methylphenyl)methanesulfonamide 

Relevant academic research and scientific papers

Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3)

T-cell immunoglobulin and mucin domain-containing molecule 3 (TIM-3; HAVCR2) has emerged as an attractive immune checkpoint target for cancer immunotherapy. TIM-3 is a negative regulator of the systemic immune response to cancer and is expressed on several dysfunctional, or exhausted, immune cell subsets. Upregulation of TIM-3 is associated with tumor progression, poor survival rates, and acquired resistance to antibody-based immunotherapies in the clinic. Despite the potential advantages of small-molecule inhibitors over antibodies, the discovery of small-molecule inhibitors has lagged behind that of antibody therapeutics. Here, we describe the discovery of high-affinity small-molecule ligands for TIM-3 through an NMR-based fragment screen and structure-based lead optimization. These compounds represent useful tools to further study the biology of TIM-3 immune modulation in cancer and serve as a potentially useful starting point toward the discovery of TIM-3-targeted therapeutics.

SULFONAMIDE COMPOUNDS USEFUL AS CYP17 INHIBITORS

Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.

NOVEL THIOPHENE INHIBITORS OF S-NITROSOGLUTATHIONE REDUCTASE

The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

1, 7-NAPHTHYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS

This invention is directed to new inhibitors of the p38 mitogen-activated protein kinas having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.