Use of fluoroethylnormemantine for the prevention and treatment of anxiety
Inventors
Assignees
Melchior Investissements Et Industries • Rest Therapeutics SAS
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Publication Number
US-11464751-B2
Publication Date
2022-10-11
Expiration Date
Abstract
The present invention relates to fluoroethylnormemantine or one of the salts thereof for the treatment of anxiety and, more particularly, post-traumatic stress conditions, either alone or in combination with chemical antidepressant treatments or cognitive and behavioral techniques.
Core Innovation
The invention relates to a method of treating an anxiety disorder in a patient in need thereof by administration of a compound of formula (I) and/or a pharmaceutically acceptable salt thereof. The disclosure emphasizes fluoroethylnormemantine (FENM), identified as compound (I), and pharmaceutically acceptable salt forms (compound (II)) with defined counter-ions. The background and summary context frame the goal as addressing anxiety disorders, with a focus on post-traumatic stress disorder (PTSD) and anxiety disorders related to post-traumatic stress.
The disclosure states that FENM lacks a schizophrenia-inducing effect while providing anxiolytic activity. It characterizes effects in anxiety-related experimental contexts such as light-dark box and light gradient field paradigms, and reports rapid onset versus memantine in the disclosed comparisons. It also reports PTSD-related outcomes in fear conditioning, fear extinction, and fear stabilization contexts, including protective and delayed treatment effects.
The disclosed summary positions the compound relative to other agents by reporting non-clinical comparative findings versus memantine, propranolol, and ketamine, and indicates antidepressant-like effects in a forced swimming test context. It further references reduced drowsiness and a lack of sensory-filtering disturbance in a pre-pulse inhibition (PPI) context. The embodiment-style coverage includes treatment and prophylaxis of anxiety disorders, including PTSD, and combination contexts with named agents and/or cognitive-behavioral therapy (CBT).
Claims Coverage
The independent claims cover treatment of anxiety disorders using a compound of formula (I) or pharmaceutically acceptable salts, and prophylactic prevention of anxiety disorders related to post-traumatic stress. Across the claim coverage, the inventive features include specific salt structures, selected anxiety disorder types, and combination-product formulations including propranolol or an antidepressant, with an additional patient-history qualifier in at least one dependent claim.
Treating an anxiety disorder using a compound of formula (I)
A method comprising treating an anxiety disorder in a patient in need thereof via administration of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Salt defined by formula (II) with enumerated counter-anions
The method is characterized in that the pharmaceutically acceptable salt corresponds to formula (II), where NH3+ is paired with a counter-anion X− selected from the listed halide and salt anions.
Targeting selected anxiety disorders
The anxiety disorder is selected from PTSD, specific phobia, social phobia, generalized anxiety disorder, panic disorder with or without agoraphobia, or obsessive compulsive disorder.
Combination product with propranolol and formulation with pharmaceutically acceptable excipients
A method in which a patient is administered a combination product containing component (A) with a compound of formula (I) or a pharmaceutically acceptable salt and component (B) of propranolol, with both components formulated using at least one pharmaceutically acceptable excipient.
Combination product with an antidepressant component and formulation with pharmaceutically acceptable excipients
A method in which a patient is administered a combination product containing component (A) with a compound of formula (I) or a pharmaceutically acceptable salt and component (C) as an antidepressant, where both components are formulated with at least one pharmaceutically acceptable excipient.
Prophylactically preventing anxiety disorders related to post-traumatic stress
A method comprising prophylactically treating a patient in need thereof via administration to the patient of a compound of formula (I) or a pharmaceutically acceptable salt thereof, to thereby prevent the appearance in the patient of anxiety disorders related to post-traumatic stress.
Treating a patient with repeated childhood abuse
The method is applied to a patient who has experienced repeated childhood abuse.
Overall, the claim set centers on administering a compound of formula (I) or pharmaceutically acceptable salts to treat anxiety disorders, with coverage for particular salt counter-ions, a defined set of anxiety disorder types including PTSD, and prophylaxis aimed at preventing anxiety disorders related to post-traumatic stress. Additional dependent features include combination products with propranolol or an antidepressant, both formulated with pharmaceutically acceptable excipients, and an added patient-history qualifier for repeated childhood abuse.
Stated Advantages
FENM lacks a schizophrenia-inducing effect.
FENM provides anxiolytic activity.
Reported rapid onset versus memantine.
Reported protective and delayed treatment effects in PTSD-related contexts, including fear conditioning, fear extinction, and fear stabilization.
Reported antidepressant-like effects in a forced swimming test context.
Reduced drowsiness.
No sensory-filtering disturbance in a pre-pulse inhibition (PPI) context.
Documented Applications
Treating an anxiety disorder in a patient, including PTSD, specific phobia, social phobia, generalized anxiety disorder, panic disorder with or without agoraphobia, and obsessive-compulsive disorder.
Prophylactically preventing the appearance in a patient of anxiety disorders related to post-traumatic stress.
Combination-product treatment contexts pairing the compound of formula (I) with propranolol.
Combination-product treatment contexts pairing the compound of formula (I) with an antidepressant.
Treatment targeted to a patient who has experienced repeated childhood abuse.
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