934601-20-4

Upstream product

• 1021537-03-0 1-(4-fluorophenyl)-5-nitro-1H-indazole 
• 352-34-1 4-fluoro-1-iodobenzene 
• 19335-11-6 1H-indazol-5-ylamine 
• 27996-87-8 2-fluoro-5-nitrobenzaldehye 
• 371-14-2 4-fluorophenylhydrazine 
• 1765-93-1 4-fluoroboronic acid 
• 5401-94-5 5-nitroindazole 

Downstream Products

• 1025762-98-4 1-(4-fluorophenyl)-5-iodo-1H-indazole 
• 1032650-17-1 [1-(4-fluorophenyl)-1H-indazol-5-yl]-((E)-2-phenyl-1-trifluoromethylvinyl)amine 
• 1034156-20-1 1-(4-fluorophenyl)-1H-indazol-5-ol 
• 1070341-77-3 N-((S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-ylamino]methyl}propyl)-2-nitrobenzenesulfonamide 

Relevant academic research and scientific papers

Novel Indazole-based MKK7–TIPRL Interaction Inhibitors as TRAIL Sensitizers

This work describes the process by which a metabolically unstable TRT-0002 compound exhibiting Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-sensitizing activity for Huh7 cells at a high working concentration (40 μM) is converted to more potent and metabolically improved analogues by modifying the 5-amino group and the 1-aryl moiety in the 1H-indazole skeleton. The efforts enabled us to identify 5-sulfonamido derivatives, TRT-0029 and TRT-0173 compounds, working at lower concentrations (10 and 20 μM, respectively) and with improved metabolic stabilities. As reported previously by us, co-treating cultured Huh7 cells with either TRT-0029 or TRT-0173 and TRAIL resulted in TRAIL-induced apoptosis due to the inhibition of the MKK7–TOR signaling pathway regulator-like (TIPRL) interaction and subsequent phosphorylation of MKK7 and JNK. In addition, the injection of TRT-0029 or TRT-0173 compound suppressed tumor growth in combination with TRAIL in an in vivo hepatocellular carcinoma (HCC) mouse xenograft model. TRT-0029 and TRT-0173 compounds and the relevant structure–activity relationship can provide an insight into further study on optimization of potency and metabolic stability.

Novel indazole derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer containing the same as an active ingredient

The present invention relates to a novel indazole derivative, a production method thereof, and a pharmaceutical composition for preventing or treating cancer containing the same as an active ingredient. According to the present invention, the compound, an optical isomer thereof, or a pharmaceutically acceptable salt thereof shows outstanding inhibitory activities on TRAIL-resistance regarding cancer which is resistant to tumor necrosis factor related apoptosis (TRAIL), and thus can be useful for preventing and treating cancer when used as a pharmaceutical composition containing the same as the active ingredient in conjunction with TRAIL.(AA) Cancer cell survival rate(BB) Compound alone(CC) Compound + TRAIL(DD) Example 10COPYRIGHT KIPO 2017

4-(PIPERRAZIN-1-YL)-PYRROLIDIN-2-ONE COMPOUNDS AS MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS

The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative diseases (e.g., Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis and the like), anxiety disorder, pain (e.g., inflammatory pain, carcinomatous pain, nervous pain and the like), epilepsy and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Enantioselective synthesis of chiral β-aryloxy alcohols by ruthenium-catalyzed ketone hydrogenation via dynamic kinetic resolution (DKR)

A highly efficient enantioselective synthesis of chiral β-aryloxy alcohols by the [RuCl2[(S)-SDP][(R, R)-DPEN]} [(Sa,R, R)-1a; SDP = 7, 7′-bis-(diarylphosphino)-1,1′-spirobiindane; DPEN = trans-1,2-diphenylethylenediamine] complex-ca

Cyclic phenyl-substituted indazols, a process for their production and their use as anti-inflammatory agents

The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is -N-, -NR1-, -O-, -S-, -SO2- or -CR2-; F is -N-, -NR1a-, -O-, -S-, SO2- or -CR2a-; G is N, -NR1b-, -O-, -S-, SO2- or -CR2b-, provided that the E-F-G containing heterocyclic ring formed does not contain a S-S or S-O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.