1600563-62-9

Upstream product

• 100377-32-0 N-methyl-N-methoxyisonicotinamide 
• 103-80-0 phenylacetyl chloride 
• 52727-57-8 5-bromo-2-aminobenzoic acid methyl ester 
• 2613-89-0 phenylmalonic acid 
• 106-40-1 4-bromo-aniline 
• 909365-96-4 6-bromo-4-hydroxy-3-phenylquinolin-2(1H)-one 
• 452349-62-1 methyl 5-bromo-2-(2-phenylacetamido)benzoate 
• 55-22-1 pyridine-4-carboxylic acid 
• 1600562-81-9 6-bromo-2,4-dichloro-3-phenylquinoline 
• 1600562-94-4 (1-methyl-1H-imidazol-5-yl)(pyridin-4-yl)methanone 

Downstream Products

• 1600565-07-8 (2,4-diethyl-3-phenylquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600564-41-7 {4-chloro-2-[(2-methoxyethyl)(methyl)amino]-3-phenylquinolin-6-yl}(1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600564-84-8 [2-chloro-4-(1-methylethoxy)-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600564-92-8 [4-chloro-2-(1-methylethoxy)-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600565-11-4 (4-chloro-2-(diethylamino)-3-phenylquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600563-67-4 [4-chloro-2-(4-methylpiperazin-1-yl)-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600564-58-6 1-{4-chloro-6-[hydroxy(1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethyl]-3-phenylquinolin-2-yl}piperidin-4-ol trifluoroacetate 
• 1600564-60-0 1-{2-chloro-6-[hydroxy(1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethyl]-3-phenylquinolin-4-yl}piperidin-4-ol trifluoroacetate 
• 1600564-64-4 [4-chloro-2-(4-methoxypiperidin-1-yl)-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600563-65-2 [2-chloro-4-(methylamino)-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600565-17-0 [2-(diethylamino)-4-methyl-3-phenylquinolin-6-yl](1-methyl-1H-imidazol-5-yl)pyridin-4-ylmethanol trifluoroacetate 
• 1600563-64-1 C₂₆H₂₂ClN₅O 
• 1600564-19-9 C₂₇H₂₄ClN₅O 

Relevant academic research and scientific papers

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.

6-Substituted quinolines as RORγt inverse agonists

We identified 6-substituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). The synthesis of this class of RORγt modulators is reported, and optimization of the substituents at the quinoline 6-position that

HETEROARYL 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.