Nonracemic mixtures and uses thereof

A composition and drug technology, applied in the direction of active ingredients of heterocyclic compounds, drug combination, drug delivery, etc., can solve problems such as erectile dysfunction, pain, QT interval prolongation, etc.

Pending Publication Date: 2020-12-22
SUNOVION PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other side effects associated with racemic amisulpride include prolongation of the QT interval and inc...

Method used

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  • Nonracemic mixtures and uses thereof
  • Nonracemic mixtures and uses thereof
  • Nonracemic mixtures and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0264] Embodiment 1. A pharmaceutical composition comprising an unequal mixture of (R)-(+)-amisulpride and (S)-(-)-amisulpride or a pharmaceutically acceptable salt thereof, wherein said The amount of (R)-(+)-amisulpride is greater than the amount of said (S)-(-)-amisulpride, wherein said unequal mixture is effective to provide in a subject after administration :

[0265] about 20% to about 60% dopamine D 2 receptor occupancy; and

[0266] Suppression of time during rapid eye movement (REM) sleep, characterized by one or more of the following:

[0267] The amount of reduction in REM sleep greater than about 10 minutes,

[0268] The amount of delay to REM sleep is greater than about 20 minutes, or

[0269] The reduction in total REM sleep time relative to total sleep time is greater than about 5%.

Embodiment approach 2

[0270] Embodiment 2. The pharmaceutical composition according to embodiment 1, wherein the dopamine D 2 Receptor occupancy is about 30% to about 50%.

Embodiment approach 3

[0271] Embodiment 3. The pharmaceutical composition according to embodiment 1, wherein the reduction in REM sleep is from about 15 minutes to about 45 minutes.

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Abstract

Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.

Description

technical field [0001] The present invention relates to the pharmaceutical composition of non-racemic amisulpride and its method and use. Background technique [0002] Amisulpride is a member of the benzamide chemical class with the chemical name 4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2- Methoxy-benzamide. The chemical structure of amisulpride is as follows: [0003] [0004] There is a need for better treatment of psychiatric and mood disorders, including bipolar disorder, especially depression associated with bipolar disorder. For example, psychiatrists state that about 25% of all bipolar disorders are refractory during manic episodes and about 70% are refractory during depressive episodes. Therefore, there is a need for medications that relieve depressive symptoms in bipolar patients. [0005] Dopamine receptor antagonists are a class of drugs used to treat mental disorders, yet effective D 2 Occupancy levels were also associated with deleterio...

Claims

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Application Information

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IPC IPC(8): A61K31/40C07D207/09A61P25/00
CPCA61P25/24A61K31/40A61K9/0053A61K9/08A61P25/18
Inventor S·C·霍普金斯K·S·科比安J·R·斯努尼安H·S·威尔金森
Owner SUNOVION PHARMA INC
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