767342-42-7

Upstream product

• 59489-71-3 5-amino-2-bromopyrazine 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 767342-44-9 N-(5-bromo-pyrazin-2-yl)-N-cyanomethyl-4-methyl-benzenesulfonamide 
• 1447913-61-2 N-(5-bromo-1-(1-cyclopropyl-1-oxopropan-2-yl)pyrazin-2(1H)-ylidene)-4-methylbenzenesulfonamide 
• 1162681-03-9 2-(5-bromo-2-(tosylimino)pyrazin-1(2H)-yl)acetamide 

Relevant academic research and scientific papers

IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF

The present disclosure provides compounds of Formula (I′) (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, cocrystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof

IMIDAZO-FUSED HETEROCYCLES AND USES THEREOF

Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using imidazole-fused heterocycle amines. Some of the disclosed embodiments include imizazo-fused

Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition

Melanin-concentrating hormone (MCH) is an attractive target for antiobesity agents, and numerous drug discovery programs are dedicated to finding small-molecule MCH receptor 1 (MCHR1) antagonists. We recently reported novel pyridine-2(1H)-ones as aliphatic amine-free MCHR1 antagonists that structurally featured an imidazo[1,2-a]pyridine-based bicyclic motif. To investigate imidazopyridine variants with lower basicity and less potential to inhibit cytochrome P450 3A4 (CYP3A4), we designed pyridine-2(1H)-ones bearing various less basic bicyclic motifs. Among these, a lead compound 6a bearing a 1H-benzimidazole motif showed comparable binding affinity to MCHR1 to the corresponding imidazopyridine derivative 1. Optimization of 6a afforded a series of potent thiophene derivatives (6q-u); however, most of these were found to cause time-dependent inhibition (TDI) of CYP3A4. As bioactivation of thiophenes to form sulfoxide or epoxide species was considered to be a major cause of CYP3A4 TDI, we introduced electron withdrawing groups on the thiophene and found that a CF3 group on the ring or a Cl adjacent to the sulfur atom helped prevent CYP3A4 TDI. Consequently, 4-[(5-chlorothiophen-2-yl)methoxy]-1-(2-cyclopropyl-1-methyl-1H-benzimidazol-6-yl)pyridin-2(1H)-one (6s) was identified as a potent MCHR1 antagonist without the risk of CYP3A4 TDI, which exhibited a promising safety profile including low CYP3A4 inhibition and exerted significant antiobesity effects in diet-induced obese F344 rats.

Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5

The present invention relates to compounds assumed to be capable of modulating the activity of the proteins ScyI1 and Grk5, thereby regulating the expression and/or release of insulin as well as to pharmaceutical compositions containing such compounds and the use thereof especially for the treatment of a metabolic disease such as diabetes, obesity and impaired adipogenesis.

FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE

The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.

COMPOUND LIBRARIES

The present invention relates to compounds capable of binding to the active site of protein kinase enzymes. The invention further relates to libraries of compounds and a family of libraries of compounds for use in screening programmes against protein kinases as well as the individual compounds for use in hit to lead and lead optimisation projects, and similar stages in the drug discovery process. The invention also provides methods for making compounds and libraries.