953885-64-8

Upstream product

• 5345-27-7 3-(methylsulfonyl)benzoic acid 
• 54857-54-4 3-(methylsulfonyl)benzoyl chloride 
• 1370447-75-8 tert-butyl 2-[3-(methylsulfonyl)benzoyl]hydrazinecarboxylate 
• 22821-69-8 methyl 3-(methanesulfonyl)benzoate 

Downstream Products

• 1423715-22-3 (E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(methylsulfonyl)benzohydrazide 
• 1370447-77-0 {3-[3-(methylsulfonyl)phenyl]-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl}acetic acid 
• 1370447-78-1 2-{3-[3-(methylsulfonyl)phenyl]-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl}-N-(propan-2-yl)acetamide 
• 1370447-76-9 ethyl N-({2-[3-(methylsulfonyl)benzoyl]hydrazinyl}carbonyl)glycinate 
• 1454288-72-2 1-(2-chlorophenyl)-5-(5-(3-(methylsulfonyl)phenyl)-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3-carboxylic acid 
• 1454288-71-1 methyl 1-(2-chlorophenyl)-5-(5-(3-(methylsulfonyl)phenyl)-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3-carboxylate 
• 1454288-73-3 methyl 1-(2-chlorophenyl)-5-(5-(3-(methylsulfonyl)phenyl)-1,3,4-oxadiazol-2-yl)-1H-pyrazole-3-carboxylate 
• 1454290-84-6 methyl 1-(2-chlorophenyl)-5-(2-(3-(methylsulfonyl)benzoyl)hydrazinecarbonyl)-1H-pyrazole-3-carboxylate 

Relevant academic research and scientific papers

Structure based discovery of novel hexokinase 2 inhibitors

Hexokinase 2 (HK2) is over-expressed in most of human cancers and has been proved to be a promising target for cancer therapy. In this study, based on the structure of HK2, we screened over 6 millions of compounds to obtain the lead. A total of 26 (E)-N′-(2,3,4-trihydroxybenzylidene) arylhydrazide derivatives were then designed, synthesized, and evaluated for their HK2 enzyme activity and IC50 values against two cancer cell lines. Most of the 26 target compounds showed excellently in vitro activity. Among them, compound 3j showed the strongest inhibitory effects on HK2 enzyme activity with an IC50 of 0.53 ± 0.13 μM and exhibited the most potent growth inhibition against SW480 cells with an IC50 of 7.13 ± 1.12 μM, which deserves further studies.

[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES

The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

1, 2, 4-TRIAZOLONE DERIVATIVE

The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.

LIVER X RECEPTOR (LXR) MODULATORS FOR THE TREATMENT OF DERMAL DISEASES, DISORDERS AND CONDITIONS

Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containg such compounds.

SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS

In one aspect, the invention relates to substituted (E)-N'-(1- phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods fo