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Novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their medical use

A technology of nonylpyrimidine and diaza, which is applied in the field of preparation of pharmaceutical compositions, and can solve the problems of not disclosing diazabicycles, etc.

Inactive Publication Date: 2011-02-09
NEUROSEARCH AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the diazabicyclo of the present invention has never been disclosed

Method used

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  • Novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their medical use
  • Novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their medical use
  • Novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their medical use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Preparation Example

[0126] All reactions involving air-sensitive reagents or intermediates were performed under nitrogen in 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] The title compound was prepared according to J. Med. Chem. 1993362311-2320 (and according to a slightly modified method described below).

[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 anhydrous dioxane (130 ml) was added LiAlH under argon 4 (4.9 g; 130 mmol). The mixture was refluxed for 6 hours and then allowed to reach room temperature. Water (5ml in 10ml of dioxane) was added dropwise to the reaction mixture, the mixture was stirred for 0.5 hours and then filtered through a glass filter. The solvent was evaporated and the res...

Embodiment 2

[0166] in the rat brain 3 Inhibition of H-alpha-Craitus Venom Binding in Vitro

[0167] The alpha of a compound binding to a nicotinic receptor can be determined essentially according to standard assays such as described in WO 2006 / 087306. 7 - Subtype affinity. In this analysis, the measured values ​​are expressed as IC 50 (Test substance inhibits 3 Concentration at which 50% of H-α-bungarovenom specifically binds).

[0168] Compounds of the invention determined in assays exhibit activity in the lower micromolar range, preferred compounds of the invention exhibit activity in the submicromolar range (i.e., IC 50 less than 1 μM).

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Abstract

This invention relates to novel 1,4-diaza-bicyclo [3.2.2]nonyl pyrimidine derivatives of formula (I) and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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 1,4-diaza-bicyclo[3.2.2]nonylpyrimidine 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 various diseases or disorders related to the cholinergic system of the central nervous system (CNS), peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, Endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms resulting from cessation of chemical substance abuse. Background technique [0003] The endogenous cholinergic neurotransmitter, acetylcholine, exerts its biologic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551C07D471/08A61P25/00
CPCC07D471/08A61P1/04A61P1/12A61P1/14A61P11/00A61P11/06A61P15/00A61P15/04A61P15/06A61P15/10A61P17/02A61P17/10A61P21/02A61P21/04A61P25/00A61P25/02A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/32A61P25/34A61P25/36A61P29/00A61P3/04A61P31/18A61P43/00A61P9/06A61P9/10A61P9/12A61P3/10
Inventor D·佩特斯D·B·蒂默曼E·O·尼尔森G·M·欧尔森T·戴赫林J·K·克里斯坦森J·P·雷德罗伯J·D·米克尔森
Owner NEUROSEARCH AS
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