942282-44-2

Upstream product

• 114897-92-6 2-(4-bromo-2-fluoro-phenyl)acetic acid 
• 114897-91-5 (4-bromo-2-fluorophenyl)acetonitrile 
• 76283-09-5 4-bromo-2-fluorobenzyl bromide 
• 51436-99-8 2-fluoro-4-bromotoluene 
• 557-21-1 zinc(II) cyanide 
• 193290-19-6 methyl 2-(4-bromo-2-fluoro-phenyl)acetate 
• 557-21-1 dicyanozinc 

Downstream Products

• 1428761-09-4 methyl 2-(2-fluoro-4-(N-hydroxycarbamimidoyl)phenyl)acetate 
• 1428761-10-7 methyl 2-(2-fluoro-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)acetate 
• 170572-49-3 2-fluoro-4-cyanotoluene 
• 193290-21-0 3-fluoro-4-(2-hydroxyethyl)benzonitrile 

Relevant academic research and scientific papers

PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND USE

The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof, or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatmen

Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists

GSK805 (1) is a potent RORγt inverse agonist, but a drawback of 1 is its low solubility, leading to a limited absorption in high doses. We have explored detailed structure-activity relationship on the amide linker, biaryl and arylsulfonyl moieties of 1 trying to improve solubility while maintaining RORγt activity. As a result, a novel series of carboxyl-containing biaryl urea derivatives was discovered as potent RORγt inverse agonists with improved drug-like properties. Compound 3i showed potent RORγt inhibitory activity and subtype selectivity with an IC50 of 63.8 nM in RORγ FRET assay and 85 nM in cell-based RORγ-GAL4 promotor reporter assay. Reasonable inhibitory activity of 3i was also achieved in mouse Th17 cell differentiation assay (76percent inhibition at 0.3 μM). Moreover, 3i had greatly improved aqueous solubility at pH 7.4 compared to 1, exhibited decent mouse PK profile and demonstrated some in vivo efficacy in an imiquimod-induced psoriasis mice model.

BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME

The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.

8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.

NEW OXABISPIDINE COMPOUNDS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS

There is provided compounds of formula I, [Chemical formula should be inserted here. Please see paper copy] wherein R1 to R4 , R41 to R46 and Z have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias