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A technology for diazabicyclic and derivatives, which is applied in the field of diazabicyclic biaryl derivatives, and can solve problems such as not being disclosed
Inactive Publication Date: 2005-08-10
NEUROSEARCH AS
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Abstract
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Problems solved by technology
However, the 2,5-diazabicyclo[2.2.1]heptane of the present invention is not disclosed
Method used
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Embodiment 1
[0198] Preparation Example
[0199] All reactions involving air-sensitive reagents or intermediates were performed under nitrogen and anhydrous reagents. Magnesium sulfate was used as drying agent in the work-up procedure and the solvent was evaporated under reduced pressure.
[0201] Tert-butyl-(1S, 4S)-(+)-2,5-diazabicyclo-[2.2.1]-heptane-2-carboxylate (3.0g, 15.1mmol), 3,6 - A mixture of dibromopyridazine (3.6 g, 15.1 mmol) and dioxane (15 ml) was stirred at 90° C. for 3 days. The crude salt was filtered. Aqueous sodium hydroxide solution (50ml, 1M) was added to the solid material, and the mixture was extracted with dichloromethane. Chromatography on silica gel with dichloromethane, methanol and concentrated aqueous ammonia (89:10:1) gave the title compound as the free base. Yield 1.71 g (32%).
[0202] 2-[6-(3-Thienyl)-3-pyridazinyl]-(1S,4S...
Embodiment 2
[0234] rat brain 3 Inhibition of H-α-bungarotoxin binding in vitro
[0235] In this example, the alpha of the compounds of the invention on the nicotinic receptor 7 -Affinity for isoform binding.
[0236] α-Bungarotoxin is a peptide isolated from the venom of the Cobra snake Bungara. It has high affinity for neuronal and neuromuscular nicotinic receptors, where it acts as a potent antagonist.
[0237] alpha found in the brain 7 Subunit isoforms and alpha in the neuromuscular junction 1 isotype formation 3 H-α-bungarotoxin labels nicotinic acetylcholine receptors.
[0238] tissue preparation
[0239] Prepare at 0-4°C. Use an Ultra-Turrax homogenizer in 15 ml of 118 mM NaCl, 4.8 mM KC1, 1.2 mM MgSO 4 and 2.5mM CaCl 2 Cerebral cortices from male Wistar rats (150-250 g) were homogenized in 20 mM Hepes buffer (pH 7.5) for 10 seconds. The tissue suspension was centrifuged at 27,000 xg for 10 minutes. The supernatant was discarded and the pellet was washed twice by cent...
Embodiment 3
[0248] in cortical synaptosomes 3 Inhibition of H-5-Hydroxytryptamine Uptake in Vitro
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Abstract
This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Description
technical field [0001] The present invention relates to novel diazabicyclic biaryl derivatives which have been found to be cholinergic ligands of nicotinic acetylcholine receptors and modulators of monoamine receptors and transporters. [0002] Due to their pharmacological profile, the compounds of the present invention can be used to treat numerous diseases or conditions related to the cholinergic system of the central nervous system (CNS), peripheral nervous system (PNS), diseases or conditions related to smooth muscle contraction , endocrine diseases or conditions, diseases or conditions associated with neurodegeneration, diseases or conditions associated with inflammation, pain, and withdrawal syndromes induced by cessation of chemical substances. Background of the invention [0003] The endogenous cholinergic neurotransmitter acetylcholine exerts its biological effects through two types of cholinergic receptors, muscarinic acetylcholine receptors (mAChR) and nicotinic a...
Claims
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