77474-23-8

Usage

InChI:InChI=1/C12H11NO4/c1-16-7-3-4-8-9(5-7)13-10(6-11(8)14)12(15)17-2/h3-6H,1-2H3,(H,13,14)

Upstream product

• 536-90-3 m-Anisidine 
• 77474-14-7 methyl 3-carbomethoxy-3-(3'-methoxyphenyl)amino-2-propenoate 
• 762-42-5 dimethyl acetylenedicarboxylate 

Downstream Products

• 259214-74-9 C₂₉H₃₂N₂O₈ 
• 300832-84-2 ciluprevir 
• 77474-33-0 7-methoxy-4-oxo-1,4-dihydroquinoline-2-carboxylic acid 

Relevant academic research and scientific papers

Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease

In this work we describe neurogenic and neuroprotective donepezil-flavonoid hybrids (DFHs), exhibiting nanomolar affinities for the sigma-1 receptor (σ1R) and inhibition of key enzymes in Alzheimer's disease (AD), such as acetylcholinesterase (AChE), 5-lipoxygenase (5-LOX), and monoamine oxidases (MAOs). In general, new compounds scavenge free radical species, are predicted to be brain-permeable, and protect neuronal cells against mitochondrial oxidative stress. N-(2-(1-Benzylpiperidin-4-yl)ethyl)-6,7-dimethoxy-4-oxo-4H-chromene-2-carboxamide (18) is highlighted due to its interesting biological profile in σ1R, AChE, 5-LOX, MAO-A and MAO-B. In phenotypic assays, it protects a neuronal cell line against mitochondrial oxidative stress and promotes maturation of neural stem cells into a neuronal phenotype, which could contribute to the reparation of neuronal tissues. Molecular modelling studies of 18 in AChE, 5-LOX and σ1R revealed the main interactions with these proteins, which will be further exploited in the optimization of new, more efficient DFHs.

Synthesis of 2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-ol; A quinoline building block for simeprevir synthesis

Two synthetic approaches to the achiral quinoline fragment of simeprevir are described. Both approaches are based on the synthesis of methyl 4-hydroxy-7-methoxy-8-methylquinoline-2-carboxylate, protection of its 4-hydroxyl group, and construction of the thiazole ring from the ester group at the 2-position. The last step is acid deprotection of the 4-hydroxyl protecting group. Georg Thieme Verlag Stuttgart. New York.

Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)

C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel series of linear tripeptide inhibitors that are very potent and selective against the NS3 protease are described. A substantial contribution to the potency of these

Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor

The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

2-AMINOCARBONYL-QUINOLINE COMPOUNDS AS PLATELET ADENOSINE DIPHOSPHATE RECEPTOR ANTAGONISTS

Compounds of formula (I), where m, n, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Hepatitis C inhibitor tri-peptides

Disclosed herein are compounds of formula (1): wherein Ris hydroxy or NHSO2Rwherein Ris (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or Ris C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1-6) alkyl, amido, amino or phenyl; Ris (C4-6)cycloalkyl; Ris t-btuyl or (C5-6) cycloalkyl and Ris (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease.

Platelet adenosine diphosphate receptor antagonists

Compounds of the following formula (I): where a, b, R1, R2, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, met

Synthesis and evaluation of quinoline carboxyguanidines as antidiabetic agents

The synthesis and in vivo activities of a series of substituted quinoline carboxyguanidines as a possible novel class of antidiabetic agents is described. (C) 2000 Elsevier Science Ltd. All rights reserved.