1045335-20-3

Upstream product

• 5418-51-9 5-nitro-2-hydroxypyridine 
• 4548-45-2 2-chloro-5-nitropyridine 
• 939377-43-2 1-(5-nitropyridin-2-yl)azetidin-3-ol 

Downstream Products

• 1419600-30-8 1-((1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methyl)-3-(6-(3-hydroxyazetidin-1-yl)pyridin-3-yl)urea 
• 1173705-84-4 N-[6-(3-hydroxyazetidin-1-yl)pyridin-3-yl]-6-trimethylsilyl-1-[(3-fluorophenyl)methyl]-1H-indole-2-carboxamide 
• 1186429-10-6 N-[6-(3-hydroxyazetidin-1-yl)pyridin-3-yl]-5-trimethylsilyl-1-[(3-fluorophenyl)methyl]-1H-indole-2-carboxamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation N2-(2-alkyoxy-6-aliphatic aminopyridin-3-yl)-2,4-diaminepyrimidine derivatives bearing acylamino or DBTD ‘head’ as potential ALK inhibitors

Aiming to develop promising ALK inhibitors, two series of N2-(2-alkyoxy-6-aliphatic aminopyridin-3-yl)-2,4-diaminepyrimidine derivatives (22a-x and 23a-d) were designed according to scaffold hopping and bioisosterism principles. All compounds were efficiently synthesized by concise reactions and anti-proliferative activities on ALK-addicted H2228, Karpas299 cells and EGFR-expressive A549 cell were evaluated by MTT assay. Several compounds exhibited potential cytotoxic activities with IC50 values below 0.10 μM. Five compounds (22g, 22h, 22l, 22s and 23a) were selected for further enzymatic determination, resulting in the discovery of 22l against ALK and ALKL1196M with IC50 values of 2.1 nM and 3.8 nM. Particularly, western blot and cell apoptosis assays identified 22l as a promising ALK inhibitor, which was capable of obviously inhibiting cellular ALK activity and inducing cell apoptosis. Eventually, molecular docking modes of 22l with ALK confirmed structural basis in accordance with the SARs analysis.

TANK-BINDING KINASE INHIBITOR COMPOUNDS

Compounds having the following formula (I) and methods of their use and preparation are disclosed:

SUBSTITUTED HETEROAROMATIC PYRAZOLE-CONTAINING CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS

The invention relates to substituted heteroaromatic pyrazole-containing carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Substituted Heteroaromatic Pyrazole-Containing Carboxamide and Urea Compounds as Vanilloid Receptor Ligands

Substituted heteroaromatic pyrazole-containing carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also to a method of using these compounds for treating and/or inhibiting pain and further diseases and/or disorders.

COMPOSITIONS AND THERAPEUTIC USES OF IKK-RELATED KINASE EPSILON AND TANKBINDING KINASE 1 INHIBITORS

The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.

DERIVATIVES OF INDOLE-2-CARBOXAMIDES AND OF AZAINDOLE-2-CARBOXAMIDES SUBSTITUTED WITH A SILANYL GROUP, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

This disclosure relates to compounds of formula (I): wherein G1, G2, G3, G4, n, Y, Z, Z1, Z2, Z3, and Z4 are as defined in the disclosure, or a salt thereof, or a hydr

N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy

The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in th

N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof

The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a proces

Diacylglycerol acyltransferase inhibitors

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.