n-oxides of diazabicyclononylpyrimidine derivatives and their medicinal uses

A nonylpyrimidine and oxide technology, applied in the field of N-oxides, can solve the problems of undisclosed diazabicyclic nonylpyrimidine derivatives, etc.

Inactive Publication Date: 2011-12-21
NEUROSEARCH AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the diazabicyclonylpyrimidine derivatives of the present invention are not disclosed

Method used

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  • n-oxides of diazabicyclononylpyrimidine derivatives and their medicinal uses
  • n-oxides of diazabicyclononylpyrimidine derivatives and their medicinal uses
  • n-oxides of diazabicyclononylpyrimidine derivatives and their medicinal uses

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0126] All reactions involving air-sensitive reagents or intermediates were performed under nitrogen and anhydrous solvents. Magnesium sulfate was used as a drying agent during the operation, and the solvent was evaporated under reduced pressure.

[0127] 1,4-Diazabicyclo[3.2.2]nonane (intermediate compound)

[0128] according to J. Med. Chem. 1993362311-2320 (and according to a slightly modified procedure described below) to prepare the title compound.

[0129] 1,4-Diazabicyclo[3.2.2]nonane (intermediate compound)

[0130] To a solution of 1,4-diazabicyclo[3.2.2]nonan-3-one (15.8 g; 113 mmol) in dry dioxane (130 ml) was added LiAlH4 (4.9 g; 130mmol). The mixture was refluxed for 6 hours and then allowed to reach room temperature. Water (5 ml in 10 ml of dioxane) was added dropwise to the reaction mixture, the mixture was stirred for 0.5 hours and then filtered off through a glass filter. The solvent was evaporated and the residue was distilled with a Kugelrohr appa...

Embodiment 2

[0148] in the hippocampus 3 Inhibition of H-α-bungarotoxin binding in vitro

[0149] In this example, it was determined that compounds of the invention bind to the nicotinic receptor alpha 7 - Subtype affinity.

[0150] α-bungarotoxin is a peptide isolated from the venom of the cobra snake (Bungarus multicinctus). It has a high affinity for the nicotinic receptors of nerves and neuromuscular where it is a potent antagonist.

[0151] 3 H-α-bungarotoxin is labeled by α in the brain 7 Subtype isoforms and alpha in the neuromuscular junction 1 Isoforms of nicotinic acetylcholine receptors.

[0152] tissue preparation

[0153]At predetermined time points after injection, mice were sacrificed by decapitation, hippocampi were rapidly excised on ice, and the tissue from each animal was weighed. Preparations were carried out at 0-4°C unless otherwise stated. Using an Ultra-Turrax homogenizer, homogenize individual hippocampi (2 per animal) for 10 seconds in 75 volumes of ice...

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Abstract

The present invention relates to novel N-oxides of certain diazabicyclononylpyrimidine derivatives and their use in the preparation of pharmaceutical compositions. The compounds of the present invention were found to be cholinergic ligands of nicotinic acetylcholine receptors and modulators of monoamine receptors and transporters. Due to their pharmacological properties, the compounds of the present invention can be used in the treatment of different diseases or disorders, for example diseases or disorders involving the cholinergic system of the central nervous system (CNS), peripheral nervous system (PNS), diseases involving smooth muscle contraction or disorder, endocrine disease or disorder, disease or disorder involving neurodegeneration, disease or disorder involving inflammation, pain, and withdrawal symptoms resulting from cessation of chemical substance abuse.

Description

technical field [0001] The present invention relates to novel N-oxides of certain diazabicyclononylpyrimidine derivatives and their use in the preparation of pharmaceutical compositions. The compounds of the present invention were found to be cholinergic ligands of nicotinic acetylcholine receptors and modulators of monoamine receptors and transporters. [0002] Due to their pharmacological properties, the compounds of the present invention can be used in the treatment of different diseases or disorders, for example diseases or disorders involving the cholinergic system of the central nervous system (CNS), peripheral nervous system (PNS), diseases involving smooth muscle contraction or disorder, endocrine disease or disorder, disease or disorder involving neurodegeneration, disease or disorder involving inflammation, pain, and withdrawal symptoms resulting from cessation of chemical substance abuse. Background technique [0003] The endogenous cholinergic neurotransmitter a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/08A61K31/53A61P25/28
CPCC07D471/08A61P1/00A61P1/12A61P1/16A61P15/00A61P15/06A61P17/00A61P21/00A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/32A61P25/34A61P25/36A61P29/00A61P3/00A61P3/04A61P43/00A61P9/06
Inventor D·彼特斯D·B·逖米尔曼E·D·克里斯托福森E·O·尼尔森
Owner NEUROSEARCH AS
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