4765-22-4

Upstream product

• 20862-85-5 2-(1H-indol-3-yl)propanenitrile 
• 783349-72-4 3-(2-amino-1-methyl-methyl)-indole-1-carboxylic acid tert-butyl ester 
• 3156-51-2 3-(2-nitroethenyl)-1H-indole 
• 143703-45-1 2-[1-(benzenesulfonyl)indol-3-yl]acetonitrile 
• 143703-49-5 2-[1-(benzenesulfonyl)indol-3-yl]propanenitrile 
• 58550-78-0 N-benzenesulfonyl-3-(bromomethyl)indole 

Downstream Products

• 174727-73-2 2-<1-(2,5-dimethylbenzyl)indol-3-yl>propylamine 
• 1053697-16-7 (3aS,4S,6R,6aR)-6-(6-{2-[1-(2,5-Dimethyl-benzyl)-1H-indol-3-yl]-propylamino}-purin-9-yl)-2,2-dimethyl-tetrahydro-furo[3,4-d][1,3]dioxole-4-carboxylic acid cyclopropylamide 
• 944318-99-4 N-(1-(1H-indol-3-yl)propan-2-yl)-4-((dimethylamino)(phenyl)methyl)-cyclohexanamine hydrochloride 

Relevant academic research and scientific papers

Synthesis of β-substituted tryptamines by regioselective ring opening of aziridines

Functionalized tryptamines are targets of interest for development as small molecule therapeutics. The ring opening of aziridines with indoles is a powerful method for tryptamine synthesis if site selectivity can be controlled. 4-Nitrobenzyl carbamate (PN

INDOLE AHR INHIBITORS AND USES THEREOF

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

New insights into the catalytic reduction of aliphatic nitro compounds with hypophosphites under ultrasonic irradiation

This work describes an efficient process for the reduction of nitro compounds to the corresponding amines with a catalytic amount of Pd/C (0.6 mol%), and a mixture of sodium hypophosphite and hypophosphorous acid as a reducing agent in H2O/2-MeTHF at 60 °C. The reaction was optimized under silent conditions. The conditions for the in situ production of H2 using the mixture NaH2PO2/H3PO2 were studied. The influence of ultrasonic activation was investigated both in terms of efficiency and kinetics. The reaction was shown to be efficient in water, at 70 °C with a quantitative conversion and a maximal yield in only 15 min thanks to the ultrasonic activation. Finally, ultrasound was proved to act as a physical agent of phase transfer.

Reduction of aromatic and aliphatic nitro groups to anilines and amines with hypophosphites associated with Pd/C

The reduction of aromatic and aliphatic nitro groups to anilines and amines is performed with good yield and selectivity in short reaction times. A mixture of sodium hypophosphite and phosphinic acid is used in the presence of a heterogeneous catalyst 2.5 mol% of Pd/C (5%) in a biphasic water/2-MeTHF system.

Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)

Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC50 = 4 nM, Eff = 149%). Oral administration of 6m to LDLR-/- mice results in lowering of cholesterol and triglycerides. Chronic administration in an atherosclerosis model results in significant reduction in aortic arch lesions.

Beta-carbolines useful for treating inflammatory disease

This invention provides beta-carboline compounds of formula III-A-aa: wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.

Azepinoindole derivatives as pharmaceutical agents

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS

The present invention is directed to compounds of formula (I) and formula (II): formula (I) and (II), wherein R1-R8, A and n are as described in the description. These compounds are used in pharmaceutical compositions and methods for modulating the activity of orphan nuclear receptors.