NEW COMBINATIONS OF H3 RECEPTOR ANTAGONISTS AND NOREPINEPHRINE REUPTAKE INHIBITORS AND THEIR THERAPEUTIC USE Russian patent published in 2023 - IPC A61K31/5375 A61K31/4545 A61K31/4453 A61P25/26 

Abstract RU 2809163 C2

FIELD: medicine.

SUBSTANCE: group of inventions relates to combinations of an antagonist or inverse agonist of H3 receptors and an antidepressant, the use of a combination and a pharmaceutical composition. The following is proposed: a combination containing, in a therapeutically effective amount, an H3 receptor antagonist or inverse agonist selected from one of the following compounds: BP1.3656B and pitolisant, and any pharmaceutically acceptable salts or solvates of these compounds, and an antidepressant selected from the group of norepinephrine reuptake inhibitors consisting of duloxetine, reboxetine and atomoxetine, for the treatment and/or prevention of a disorder selected from the following: excessive sleepiness in the daytime due to alcohol abuse and/or attention and cognitive deficits in a patient with norepinephrine release deficiency. Use of the above combination in a therapeutically effective amount for the treatment and/or prevention of a disorder selected from the following: excessive sleepiness in the daytime due to alcohol abuse and/or attention and cognitive deficits in a patient with norepinephrine release deficiency, wherein doses of pitolisant used range between 5 and 40 mg/day, BP1.3656B doses range 1–100 mcg/day, duloxetine doses range 20–120 mg/day, reboxetine doses range 2–12 mg/day and the doses of atomoxetine used are in the range 10–100 mg/day. A pharmaceutical composition for the treatment and/or prevention of a disorder selected from the following: excessive sleepiness in the daytime due to alcohol abuse and/or attention and cognitive deficits in a patient with norepinephrine release deficiency, comprising the above-described combination.

EFFECT: above group of inventions allows, by combining an antagonist or inverse agonist of H3 receptors and an antidepressant — norepinephrine reuptake inhibitor, to achieve synergistic activation of noradrenergic transmission of nerve signals in the prefrontal cortex.

10 cl, 5 dwg, 1 tbl, 2 ex

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RU 2 809 163 C2

Authors

Ligneau, Xavier

Landais, Laurent

Perrin, David

Lecomte, Jeanne Marie

Schwartz, Jean Charles

Dates

2023-12-07Published

2019-07-26Filed