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Piperidine derivatives as histamine h3 receptor ligands

A technology of compounds and mixtures, applied in the field of histamine H3 receptor ligands

Inactive Publication Date: 2007-07-04
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still a need for other histamine H3 ligands

Method used

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  • Piperidine derivatives as histamine h3 receptor ligands
  • Piperidine derivatives as histamine h3 receptor ligands
  • Piperidine derivatives as histamine h3 receptor ligands

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0169] Example 1: 1-(3,4-dichloro-benzyl)-3-(1-methyl-piperidin-4-yl)-urea

[0170] To a solution of 3,4-dichlorobenzylamine (0.195 g, 1.11 mmol) and diisopropylethylamine (0.193 mL, 1.11 mmol) in 4 mL of THF was added chloroformic acid (4-nitrophenyl ) ester (0.223 g, 1.11 mmol) in 4 mL THF pre-made solution. The reaction mixture was stirred at room temperature for 3.5 h. 4-Amino-1-methylpiperidine (0.500 g, 4.38 mmol) was added to the above solution, and the resulting solution was stirred at room temperature for 16 h. The reaction mixture was concentrated under reduced pressure, diluted with EtOAc (50 mL), and the solution was washed with saturated aqueous sodium bicarbonate (2×50 mL) and brine (50 mL). The solvent was removed under reduced pressure, and the residue was analyzed by supercritical liquid chromatography (21 mm × 150 mm diol-bonded SiO 2 (6 μm particle size), isocratic method, 25% MeOH (with 0.5% isopropylamine) / CO 2 ) to afford the title compound (0.0744 g,...

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Abstract

The invention prepares a compound of following formula and salts, enantiomorphy isomer thereof, wherein Ar<1> and Q is defined as the description, and medicine compound with the said compound. They are effective in treament especially for despondent treamnet.

Description

technical field [0001] The present invention relates to histamine receptor ligands. More specifically, the present invention relates to histamine H3 receptor ligands, their preparation and their use. Background technique [0002] For the development of new drugs, attention is currently being paid to the histamine H3 receptor. The receptors are presynaptic autoreceptors located in the central and peripheral nervous systems, in the skin, and in organs such as the lungs, intestines, most likely the spleen and the gastrointestinal tract. Recent evidence suggests that H3 receptors display intrinsic, constitutive activity (ie, activity in the absence of agonists) both in vivo and in vitro. Compounds that act as inverse agonists are able to inhibit this activity. Histamine H3 receptors have been shown to regulate the release of histamine, as well as the release of neurotransmitters such as serotonin and acetylcholine. Some histamine H3 ligands, such as histamine H3 receptor ago...

Claims

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Application Information

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IPC IPC(8): C07D211/58C07D405/12A61K31/4468A61K31/497A61K31/4523A61P25/24C07DC07D401/12C07D401/14C07D417/12C07D471/04C07D471/10
CPCC07D401/12C07D211/58C07D471/04C07D405/12C07D417/12C07D401/14C07D471/10A61P25/24C07D413/12
Inventor 詹姆斯·福尔默西蒙·F·亨特彼得·汉利史蒂文·韦索洛斯基
Owner ASTRAZENECA AB
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