New disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission

A technology of pyrrolidine and difluorophenyl, applied in the field of novel disubstituted phenylpyrrolidine and these compounds, can solve the problem of no norepinephrine and dopamine neurotransmission, etc.

Inactive Publication Date: 2010-05-19
NSAB FILIAL AF NEUROSEARCH SVERIGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0025] Therefore, in WO 01 / 46146, WO 92 / 18475, J. Med. Chem. 1994, 37, 2735 or Bioorg. Med. Chem. Lett. A guide to neurotransmission of norepinephrine and dopamine

Method used

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  • New disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission
  • New disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission
  • New disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0187] figure 1 .Example 1, 50 μmol / kg subcutaneous striatal amine

[0188] Example 1 (subcutaneous injection) was injected at time point 0. exist figure 1 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

[0189] figure 2 .Example 1, 50 μmol / kg subcutaneously p.f. cortical amine

[0190] Example 1 (subcutaneous injection) was injected at time point 0. exist figure 2 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

Embodiment 2

[0191] image 3 .Example 2, 50 μmol / kg subcutaneous striatal amine

[0192] Example 2 was injected at time point 0 (subcutaneous injection). exist image 3 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

[0193] Figure 4 .Example 2, 50 μmol / kg subcutaneously p.f. cortical amine

[0194] Example 2 was injected at time point 0 (subcutaneous injection). exist Figure 4 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

[0195] Figure 5 : Example 3, 50 μmol / kg subcutaneous striatal amine

[0196] Example 3 was injected at time point 0 (subcutaneous injection). exist Figure 5 Values ​​stated in represent percentage of control relati...

Embodiment 5

[0203] Figure 9 .Example 5, 50 μmol / kg subcutaneous striatal amine

[0204] Example 5 was injected at time point 0 (subcutaneous injection). exist Figure 9 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

[0205] Figure 10 .Example 5, 50 μmol / kg subcutaneously p.f. cortical amine

[0206] Example 3 was injected at time point 0 (subcutaneous injection). exist Figure 10 Values ​​stated in represent percentage of control relative to baseline value. Microdialysis was performed in conscious and freely moving rats. Dopamine = DA; Norepinephrine = NA; Serotonin = 5-HT; Error bars = SEM

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Abstract

The present invention provides compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-(disubstituted aryl)-pyrrolidines for the treatment of central nervous system disorders.

Description

technical field [0001] The present invention relates to novel disubstituted phenylpyrrolidines and the use of these compounds, and more particularly to the use of 3-(disubstituted aryl)-pyrrolidines for the treatment of disorders of the central nervous system, which compounds increase lactation Extracellular levels of catecholamines, dopamine, and norepinephrine in cortical regions of the animal brain. Background technique [0002] The cerebral cortex includes several major regions involved in higher functions such as thinking, feeling, memory, and planning (Principles of Neural science, 2nd Edition, Elsevier Science Publishing co., Inc. 1985, pp. 671-687 ). The biogenic amines, namely dopamine, norepinephrine and serotonin, are important for mammalian cortical function. Elevated dopamine and norepinephrine pathways innervate the cortex. Serotonergic neurons of the central nervous system map nearly all regions of the brain, including the cerebral cortex (Fundamental Neuro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/08A61K31/40A61P25/00
CPCC07D207/08A61P25/00A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28
Inventor C·索尼森L·斯万森F·彼德松N·瓦特斯S·瓦特斯
Owner NSAB FILIAL AF NEUROSEARCH SVERIGE
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