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Combinations of monoamine reuptake inhibitors and potassium channel activators

A monoamine reuptake and inhibitor technology, applied in the field of novel benzimidazole derivatives, can solve problems such as adverse effects, time-limited therapeutic use, and poor permeability of the blood-brain barrier

Inactive Publication Date: 2009-07-22
NEUROSEARCH AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Depression is treated with a variety of drugs that act on the presynaptic MA uptake system: the oldest of these compounds, the tricyclic antidepressants such as imipramine, are also the least selective, inhibiting all MA uptake systems as well as some MA receptors, and has many adverse effects clinically
Second generation compounds, the selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine and paroxetine are widely used and have much fewer classic side effects than tricyclic compounds (decreased libido is still a problem ), although the prolonged duration of action and high proportion of non-responders would limit their therapeutic use
However, due to the poor blood-brain barrier permeability of alittin, this compound is not suitable for behavioral testing

Method used

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  • Combinations of monoamine reuptake inhibitors and potassium channel activators
  • Combinations of monoamine reuptake inhibitors and potassium channel activators
  • Combinations of monoamine reuptake inhibitors and potassium channel activators

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Embodiment Construction

[0027] pharmaceutical composition

[0028] In a first aspect, the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) selected from:

[0029] A) monoamine reuptake inhibitors; and

[0030] B) SK inhibitors;

[0031] and one or more adjuvants, excipients, carriers and / or diluents.

[0032] The carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation and not deleterious to the recipient thereof.

[0033] In a preferred embodiment, the active pharmaceutical ingredient (API) exhibits biological activity at submicromolar levels (ie below 1 μM), preferably at low nanomolar levels (ie below 0.1 μM).

[0034] In another preferred embodiment, the monoamine reuptake inhibitor is a dopamine uptake inhibitor, especially bupropion, sertraline, nomifensine, or mazindol, or vanoxerine, or norepinephrine uptake inhibitors, especially amoxapine,...

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Abstract

This invention provides pharmaceutical compositions comprising therapeutically effective amounts of a monoamine reuptake inhibitor and an SK inhibitor. In another aspect the invention provides novel benzoimidazole derivatives for use according to the invention.

Description

technical field [0001] The present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a monoamine reuptake inhibitor and an SK inhibitor. In another aspect, the invention provides novel benzimidazole derivatives for use according to the invention. Background technique [0002] Monoaminergic (MA) neurons are located in a limited number of different brain regions: dopaminergic neurons in the ventral tegmental area (VTA) and substantia nigra compacta (SNc), serotonergic neurons in the spinal nucleus, Noradrenergic neurons in the locus coeruleus. All MA neurons exert a wide range of modulatory neurotransmission in the brain, with the dopaminergic system projecting to the nucleus accumbens, prefrontal cortex and limbic system (VTA) and striatum (SNc). Both spinal serotonergic and coeruleus norepinephrine neurons project throughout the forebrain. [0003] Monoaminergic neurotransmission is key to the treatment of a large number of p...

Claims

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Application Information

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IPC IPC(8): A61K31/445A61K31/495A61K45/06A61P25/00A61P25/16A61P25/30A61P43/00A61P1/00
Inventor U·S·瑟伦森B·L·埃里克森L·托伊贝尔D·彼得斯D·斯特罗贝克T·H·约翰森P·克里斯托弗森J·P·雷德罗比
Owner NEUROSEARCH AS
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