740842-87-9

Upstream product

• 4133-35-1 6-bromo-2-tetralone 
• 75-75-2 methanesulfonic acid 

Downstream Products

• 740842-89-1 tert-butyl 7-bromo-2,3,4,5-tetrahydro-2H-benzo[c]azepine-2-carboxylate 
• 740842-88-0 tert-butyl 7-bromo-1,2,4,5-tetrahydro-3H-benzo[d]azepine-3-carboxylate 
• 1608496-72-5 C₂₀H₂₂N₂O 

Relevant academic research and scientific papers

Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases

Targeting the nuclear receptor RORγt is thought to be effective in autoimmune disorders. Tertiary sulfonamide 1 was found to be a potent RORγt inverse agonist previously. However, the high hepatic clearance value limits its druggability. In this study, we designed and synthesized a series of N-sulfonamide-tetrahydroquinolines by molecular modeling and scaffold hopping strategy, aiming at improving the metabolic stabilities. Detailed SAR exploration led to identification of potent RORγt inverse agonists such as 13 with moderate binding affinity and inhibitory activity of Th17 cell differentiation. Binding mode of 13 with RORγt-LBD was revealed by molecular docking. Moreover, 13 showed lower intrinsic clearance in mouse liver microsomes compared with 1 and potent in vivo efficacy and safety in psoriasis models, which can be used as a good starting point for the further optimization.

TETRAHYDRO-BENZOAZEPINE GLYCOSIDASE INHIBITORS

Compounds of formula (I') wherein A, R1, R2, T1, T2, T3, T4, L, W, Z, R''', m and n have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

TETRAHYDRO-BENZO[D]AZEPINE DERIVATIVES AS GPR120 MODULATORS

Novel tetrahydroisoquinoline and tetrahydrobenzazepine compounds of formula (I) capable of modulating the G-protein-coupled receptor GPR120, compositions comprising the compounds, and methods for their use for controlling insulin levelsin vivoand for the treatment of conditions such as of diabetes, inflammation, obesity and metabolic diseases. (I)

SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF

This invention provides compounds of formula (/): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the c

OXAZOLIDINONE DERIVATIVES N-SUBSTITUTED BY A BICYCLIC RING, FOR USE AS ANTIBACTERIAL AGENTS

Compounds of formula (I) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compoun