401-86-5

Upstream product

• 349-55-3 5-(trifluoromethyl)-m-anisidine 
• 349-57-5 3-nitro-5-(trifluoromethyl)phenol 
• 328-79-0 1-methoxy-3-nitro-5-trifluoromethyl-benzene 
• 401-99-0 3,5-dinitrobenzotrifluoride 

Downstream Products

• 454-68-2 5-(trifluoromethyl)phenyl-1,3-diol 
• 315-15-1 2-amino-6-hydroxy-4-trifluoromethyl-benzoic acid 
• 349-62-2 1-acetoxy-3-acetylamino-5-trifluoromethyl-benzene 
• 320-13-8 2,4-dihydroxy-6-trifluoromethyl-benzaldehyde 
• 500-57-2 1,3-bis-(4-nitro-benzoyloxy)-5-trifluoromethyl-benzene 
• 774230-93-2 N-(3-hydroxy-5-trifluoromethyl-phenyl)-guanidine 
• 1613588-75-2 tert-butyl 3-(2-(3-amino-5-(trifluoromethyl)phenoxy)-5-nitrophenyl)prop-2-ynylcarbamate 
• 1613588-76-3 C₂₈H₃₃F₃N₄O₇ 
• 1613588-77-4 C₂₈H₃₉F₃N₄O₅ 
• 1613588-78-5 C₅₀H₆₉F₆N₇O₁₀S₂ 
• 1613588-73-0 C₃₀H₃₇F₆N₇O₂S₂*C₂HF₃O₂ 

Relevant academic research and scientific papers

Second-Generation Inhibitors of the Mitochondrial Permeability Transition Pore with Improved Plasma Stability

Excessive mitochondrial matrix Ca2+ and oxidative stress leads to the opening of a high-conductance channel of the inner mitochondrial membrane referred to as the mitochondrial permeability transition pore (mtPTP). Because mtPTP opening can lead to cell death under diverse pathophysiological conditions, inhibitors of mtPTP are potential therapeutics for various human diseases. High throughput screening efforts led to the identification of a 3-carboxamide-5-phenol-isoxazole compounds as mtPTP inhibitors. While they showed nanomolar potency against mtPTP, they exhibited poor plasma stability, precluding their use in in vivo studies. Herein, we describe a series of structurally related analogues in which the core isoxazole was replaced with a triazole, which resulted in an improvement in plasma stability. These analogues were readily generated using the copper-catalyzed “click chemistry”. One analogue, N-(5-chloro-2-methylphenyl)-1-(4-fluoro-3-hydroxyphenyl)-1H-1,2,3-triazole-4-carboxamide (TR001), was efficacious in a zebrafish model of muscular dystrophy that results from mtPTP dysfunction whereas the isoxazole isostere had minimal effect.

SECOND GENERATION INHIBITORS OF MITOCHONDRIAL PERMEABILITY TRANSITION PORE WITH IMPROVED PLASMA STABILITY

The present invention provides compounds useful as mitochondrial permeability transition pore (mtPTP) inhibitors, the compounds being of Formula (I), or a pharmaceutically acceptable salt thereof wherein R11 is selected from the group of H, halogen, and C11-C33 alkyl; and R22 is selected from the group of H, CF33, and halogen; with the proviso that at least one of R11 and R22 is halogen or CF33.

Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8

Endosomal toll-like receptors (TLRs) 7 and 8 recognize viral single-stranded RNAs, a class of imidazoquinoline compounds, 8-oxo-adenosines, 8-aminobenzodiazepines, pyrimidines, and guanosine analogues. Substantial evidence is present linking chronic inflammation mediated specifically by TLR7 to the progression of autoimmunity. We identified a new TLR7/8 dual inhibitor (1) and a TLR8-specific inhibitor (2) based on our previous screen targeting TLR8. Compound 1, bearing a benzanilide scaffold, was found to inhibit TLR7 and TLR8 at low micromolar concentrations. We envisioned making modifications on the benzanilide scaffold of 1 resulting in a class of highly specific TLR7 inhibitors. Our efforts led to the discovery of a new TLR8 inhibitor (CU-115) and identification of a TLR7/8 dual inhibitor (CU-72), bearing a distinct diphenyl ether skeleton, with potential for TLR7 selectivity optimization. Given the role of TLR8 in autoimmunity, we also optimized the potency of 2 and developed a new TLR8 inhibitor bearing a 1,3,4-oxadiazole motif.

Electron-Deficient Chiral Lactic Acid-Based Hypervalent Iodine Reagents

Novel electron-deficient chiral hypervalent iodine reagents were prepared in good overall yields. The reactivity and stereoselectivity of these reagents in oxidative rearrangements of alkenes to α-aryl ketones were investigated. The results show that the new reagents have good reactivity and generate products with high enantiomeric excess.

Hybrid Compounds And Methods Of Making And Using The Same

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a

PRMT1 INHIBITORS AND USES THEREOF

Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-media

PROTEIN KINASE MODULATORS AND METHOD OF USE

The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.

THIAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES

The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.