77333-45-0

Upstream product

• 16554-45-3 2-methoxy-6-nitroaniline 
• 603-85-0 2-Amino-3-nitrophenol 

Downstream Products

• 77333-46-1 4-amino-3-methoxy-5-nitrobenzonitrile 
• 1372539-81-5 N-(2-methoxy-4-morpholino-6-nitrophenyl)acetamide 
• 1426821-99-9 7-bromo-1-(2-chlorophenyl)-9-methoxy-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline 
• 1426822-00-5 7-bromo-9-methoxy-4-methyl-1-o-tolyl-[1,2,4]triazolo[4,3-a]quinoxaline 
• 1351780-67-0 N-(4-bromo-2-methoxy-6-nitrophenyl)acetamide 

Relevant academic research and scientific papers

SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS

The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.

DEGRADERS OF KELCH-LIKE ECH-ASSOCIATED PROTEIN 1 (KEAP1)

The present invention relates to bifunctional compounds, compositions, and methods for treating diseases or conditions mediated by Kelch-like ECH-associated protein 1 (KEAP1). In some aspects, the present invention is directed to methods of treating disea

A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity

Inhibiting the protein-protein interaction (PPI) between the transcription factor Nrf2 and its repressor protein Keap1 has emerged as a promising strategy to target oxidative stress in diseases, including central nervous system (CNS) disorders. Numerous non-covalent small-molecule Keap1-Nrf2 PPI inhibitors have been reported to date, but many feature suboptimal physicochemical properties for permeating the blood-brain barrier, while others contain problematic structural moieties. Here, we present the first side-by-side assessment of all reported Keap1-Nrf2 PPI inhibitor classes using fluorescence polarization, thermal shift assay, and surface plasmon resonance - and further evaluate the compounds in an NQO1 induction cell assay and in counter tests for nonspecific activities. Surprisingly, half of the compounds were inactive or deviated substantially from reported activities, while we confirm the cross-assay activities for others. Through this study, we have identified the most promising Keap1-Nrf2 inhibitors that can serve as pharmacological probes or starting points for developing CNS-active Keap1 inhibitors.

HETEROCYCLIC COMPOUND

The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).

3-(2,3-DIHYDRO-1H-INDEN-5-YL)PROPANOIC ACID DERIVATIVES AND THEIR USE AS NRF2 REGULATORS

The present invention relates to compounds of Formula (I), and Formula (II), wherein B is benzotriazolyl, phenyl, triazolopyridinyl, or -(CH2)2-triazolyl each of which may be unsubstituted or substituted by 1, 2, or 3 substituents independently chosen from -C1-3 alkyl, -O-C1-3 alkyl, CN, - (CH2)2-O-(CH2)2-OR4 and halo; and D is -C(O)OH, -C(O)NHSO2CH3, -SO2NHC(O)CH3, 5-(trifluoromethyl)-4H-1,2,4-triazol-2-yl, or tetrazolyl; and their use as NRF2 regulators.

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery

KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress. Pharmacological intervention has focused on molecules that decrease NRF2-ubiquitination through covalent modification of KEAP1 cysteine residues, but such electrophilic compounds lack selectivity and may be associated with off-target toxicity. We report here the first use of a fragment-based approach to directly target the KEAP1 Kelch-NRF2 interaction. X-ray crystallographic screening identified three distinct "hot-spots" for fragment binding within the NRF2 binding pocket of KEAP1, allowing progression of a weak fragment hit to molecules with nanomolar affinity for KEAP1 while maintaining drug-like properties. This work resulted in a promising lead compound which exhibits tight and selective binding to KEAP1, and activates the NRF2 antioxidant response in cellular and in vivo models, thereby providing a high quality chemical probe to explore the therapeutic potential of disrupting the KEAP1-NRF2 interaction.

NRF2 REGULATORS

The present invention relates to aryl analogs Formula (I), pharmaceutical compositions containing them and their use as Nrf2 regulators.

NRF2 REGULATORS

The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

NRF2 REGULATORS

Provided are aryl analogs，pharmaceutical compositions containing them and their use as NRF2 regulators.

HETEROCYCLIC KINASE INHIBITORS

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.