114604-68-1

Upstream product

• 91427-23-5 1-[4-(3-chloropropoxy)phenyl]ethanone 
• 99-93-4 4-Hydroxyacetophenone 

Downstream Products

• 115407-44-8 6-<4-(chloropropoxy)phenyl>imidazo<2,1-b>thiazole 
• 114604-69-2 2-<4-(chloropropoxy)phenyl>imidazo<1,2-a>pyridine 
• 115407-31-3 2-<4-(chloropropoxy)phenyl>imidazo<1,2-a>pyrimidine 
• 114604-72-7 2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyridine 
• 114604-70-5 2-<4-(chloropropoxy)phenyl>-8-methylimidazo<1,2-a>pyridine 
• 115407-30-2 6-<4-(chloropropoxy)phenyl>imidazo<1,2-b>triazine 
• 115407-32-4 2-<4-(chloropropoxy)phenyl>-7-methylimidazo<1,2-a>pyrimidine 
• 114604-71-6 6-bromo-2-<4-(chloropropoxy)phenyl>imidazo<1,2-a>pyridine 
• 114604-74-9 8-Benzyloxy-2-[4-(3-chloro-propoxy)-phenyl]-imidazo[1,2-a]pyridine 
• 114979-73-6 4-[4-(3-Chloro-propoxy)-phenyl]-2-phenyl-thiazole 
• 1391636-58-0 C₂₁H₂₆ClN₃O₃ 
• 115407-45-9 6-<4-(chloropropoxy)phenyl>-2-methylimidazo<2,1-b>-1,3,4-thiadiazole 
• 114979-93-0 4-[4-(3-Imidazol-1-yl-propoxy)-phenyl]-2-(4-trifluoromethyl-phenyl)-thiazole 
• 114979-80-5 Dibutyl-(3-{4-[2-(4-trifluoromethyl-phenyl)-thiazol-4-yl]-phenoxy}-propyl)-amine 

Relevant academic research and scientific papers

Preparation and applications of phenylquinolinone-based and flavone-based derivative

The present invention relates to a phenylquinolinone-based and flavone-based derivative and a preparation method thereof, wherein the derivative is a histamine H3 receptor antagonist, can protect andrestore the normal function of central nervous system, e

Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists

Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinity for human H3R and demonstrated in vivo H3R functional activity in the rat dipsogenia model. Compound 9 displayed modest wake-promoting activity in the rat EEG/EMG model.

Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity

Structure-activity relationship on a novel ketone class of H3R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency, selectivity and brain penetration. Evaluation of antagonist 4 in the rat EEG/EMG model demonstrated robust wake activity thereby establishing preclinical proof of concept.

Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity

H3R structure-activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules wi

SUBSTITUTED PHENOXYPROPYLCYCLOAMINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS

The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.

Novel human histamine H(3) receptor antagonists.

High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H(3) receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with fav

2- Or 3- aryl substituted imidazo [1,2-a]pyridines

Novel 2- or 3- aryl substituted imidazo[1,2-a]pyridines and their synthesis are described. The compounds have local anesthetic properties and are useful as local anesthetic agents.

Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity

A series of heterocyclic (aryloxy)alkylamines of structures II and III were prepared and found to possess gastric antisecretory activity. Of the variety of substituted thiazoles, benzoxazoles, and benzothiazoles prepared, thiazole 18, benzoxazole 32, and benzothiazole 47 exhibited gastric antisecretory potency comparable to that of ranitidine in vivo in the pylorous ligated rat model. In an isolated rabbit parietal system, the series of thiazoles, benzoxazoles, and benzothiazoles also demonstrated similar potency to that of ranitidine toward the inhibition of both histamine-stimulated and dcAMP-stimulated uptake of amino[14C]pyrine. These compounds inhibited the H+K+-sensitive ATPase enzyme in isolated gastric microsomes. A direct correlation existed between inhibition of 14C uptake, in vivo antisecretory activity, and inhibition of the H+K+-ATPase enzyme. The more potent antisecretory compounds 18, 32 and 47 were also the more potent enzyme inhibitors. These data suggest that the mechanism responsible for the observed in vitro and in vivo gastric antisecretory activity, in these series of compounds, is a consequence of the inhibition of the H+K+-sensitive ATPase enzyme.