159819-83-7

Upstream product

• 33184-58-6 2-benzoyl-4,5-dichloro-benzoic acid 
• 685-87-0 Diethyl 2-bromomalonate 
• 71-43-2 benzene 
• 942-06-3 4,5-dichlorophthalic anhydride 

Downstream Products

• 159819-82-6 6,7-Dichloro-2-methyl-4-phenyl-1(2H)-isoquinolinone-3-carboxylic acid 

Relevant academic research and scientific papers

2-Hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic Acid with Inbuilt β-NHydroxy-γ-keto-Acid pharmacophore as HCV NS5B polymerase inhibitors

The inbuilt 2-N-hydroxy-1-oxo-3-carboxylic acid of isoquinolone was designed as pyrophosphate mimic for hepatitis C NS5B polymerase. Various 2-hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic acid derivatives 11a-p were synthesized and evaluated as HCV NS5B polymerase inhibitors. Compound 11c exhibited moderate inhibitory potency based on the inorganic pyrophosphate generation (IC50 = 9.5 μM) and based on NTP incorporation by NS5B enzyme (IC50 = 5.9 μM). Compound 11c demonstrated antiviral activity (EC50 = 15.7 μM) and good selectivity in HCV genotype 1b replicon Ava.5 cells. Compound 11c reduced the interaction of NTP to NS5B polymerase. Docking model showed that 11c situated in similar orientation to the bound uridine triphosphate in the active site of NS5B polymerase. As a result, 2-hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic acid was disclosed as a novel inbuilt β-Nhydroxy-γ-keto-acid pharmacophore for HCV NS5B polymerase inhibitors.

Tachykinin receptor antagonists, isoquinolones and their production

Novel composition represented by the formula: STR1 wherein ring A and ring B each means a benzene ring which may be substituted; R means a hydrogen atom or an alkyl group which may be substituted; R1 means a hydrogen atom or an alkyl group which may be substituted; R2 means a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted, or R1 and R2, taken together with the adjacent nitrogen atom, jointly form a ring which may be substituted, or a pharmaceutically acceptable salt thereof which is a useful tachykinin receptor antagonist.

Condensed heterocyclic compounds, their production and use

Novel compound represented by the formula: STR1 such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3-acetamide: STR2 or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.