416852-53-4

Upstream product

• 358780-13-9 6-(trifluoromethyl)nicotinoyl chloride 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 149806-05-3 6-bromo-N-methoxy-N-methylpyridine-3-carboxamide 
• 15226-74-1 dicobalt octacarbonyl 
• 436799-32-5 5-bromo-2(trifluoromethyl)pyridine 
• 231291-22-8 6-trifluoromethylnicotinic acid 

Downstream Products

• 386704-12-7 6-(trifluoromethyl)pyridine-3-carbaldehyde 
• 1179905-36-2 3-(4-fluoro-3-trifluoromethylphenyl)-5,5-dimethyl-1-(6-trifluoromethyl-pyridin-3-ylmethyl)imidazolidine-2,4-dione 
• 1599529-74-4 (2,4-dichloro-3-(4-(trifluoromethyl)benzyl)quinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599530-45-6 (3-(4-(1H-pyrazol-1-yl)benzyl)-4-chloro-2-methoxy-8-methylquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599530-96-7 (3-(4-(1H-pyrazol-1-yl)benzyl)-4-chloro-8-fluoro-2-methoxyquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599531-06-2 (4-chloro-2-methoxy-3-(4-(trifluoromethyl)benzyl)quinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599531-10-8 3-(4-(1H-pyrazol-1-yl)benzyl)-6-(hydroxy(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methyl)-8-methylquinolin-2,4-dicarbonitrile 
• 1599531-32-4 (3-(4-(1H-pyrazol-1-yl)benzyl)-4-chloro-2-(diethylamino)quinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599531-31-3 3-(4-(1H-pyrazol-1-yl)benzyl)-2-(diethylamino)-6-(hydroxy(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methyl)quinolin-4-carbonitrile 
• 1599531-11-9 (3-(4-(1H-pyrazol-1-yl)benzyl)-2,4-dichloro-8-methylquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599531-71-1 (2-(azetidin-1-yl)-4-chloro-3-(4-(trifluoromethyl)benzyl)quinolin-6-yl)(1-methyl-1H-imidazol-5-yl)(6-(trifluoromethyl)pyridin-3-yl)methanol 
• 1599529-25-5 C₃₂H₂₆ClF₃N₆O₂ 
• 1599529-85-7 C₃₂H₂₆ClF₃N₆O₂ 
• 1599531-82-4 C₃₁H₂₃ClF₄N₆O₂ 

Relevant academic research and scientific papers

Biocatalytic Strategy for the Highly Stereoselective Synthesis of CHF2-Containing Trisubstituted Cyclopropanes

The difluoromethyl (CHF2) group has attracted significant attention in drug discovery and development efforts, owing to its ability to serve as fluorinated bioisostere of methyl, hydroxyl, and thiol groups. Herein, we report an efficient biocat

3-Substituted Quinolines as RORγt Inverse Agonists

We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). These molecules are potent binders but are high molecular weight and they exhibited poor solubility at pH 2 and pH 7. This manuscript details our efforts at improving physical chemical properties for this series of compounds by increasing the diversity at the 3-position (i.e. introducing heteroatoms and lowering the molecular weight). These efforts have led to molecules which are potent binders with improved solubility.

Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt

A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.

HETEROARYL LINKED QUINOLINYL MODULATORS OF RORγT

The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification, The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndro

METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

PHENYL LINKED QUINOLINYL MODULATORS OF RORyt

The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also

HETEROARYL LINKED QUINOLINYL MODULATORS OF ROR?T

The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification, The invention also

METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt

The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

METHYLENE LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T

The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

PHENYL LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T

The present invention comprises compounds of Formula I. Formula I wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The inve