A2-73 as a therapeutic for insomnia, anxiety, and agitation
Inventors
Assignees
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Publication Number
US-11813242-B2
Publication Date
2023-11-14
Expiration Date
Abstract
A2-73 is a useful therapeutic in the treatment of humans suffering from insomnia, anxiety or agitation. Particular attention is made to oral daily doses of from about 10 mg to about 50 mg, with particular reference to about 20 to 30 mg.
Core Innovation
The patent describes A2-73 (ANAVEX 2-73, AV2-73) as a human therapeutic intended for the treatment of insomnia, anxiety, and agitation. It also describes related therapeutics including A1-41 and A19-144, which are presented as tetrahydro-N,N-dimethyl-diphenyl furanmethanamine hydrochloride compounds and a diphenyltetrahydrofuran methanamine hydrochloride compound. The disclosure ties the therapeutic use to treating insomnia and anxiety, including a combination use among these named compounds.
The document characterizes a Phase 2a study in mild-to-moderate Alzheimer’s disease patients, reporting improvements or stability over a reported duration in insomnia, anxiety, and agitation measures. It describes outcomes using Hamilton Depression Rating Scale (HAM-D) measures and cognitive and functional endpoints including MMSE, ADCS-ADL, and Cogstate tasks. The disclosure further reports EEG/ERP P300 metrics and reports tolerability outcomes including adverse events such as dizziness and headache.
The disclosure additionally reports potential benefit in systolic blood pressure control in subjects with hypertension, including larger reductions in more severely hypertensive strata. It also describes conceptual associations for improvement in sleep and cognition through receptor activity, including sigma 1 (σ1) receptor agonism and muscarinic (M1/M1-2) agonism. Example dosing regimens and conventional pharmaceutical carrier formulation concepts are also discussed.
Claims Coverage
The partial content includes two independent claims that collectively cover a dosage form and a method of treating insomnia and/or anxiety using therapeutically effective combinations of the specified hydrochloride compounds. Across these independent claims, the core inventive features include the combination composition of A2-73, A1-41, and A19-144 and therapeutic use for insomnia and/or anxiety.
Therapeutically effective combination dosage form for insomnia or anxiety
A dosage form comprising a therapeutically effective amount of any combination of two or more of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (A2-73), tetrahydro-N,N-dimethyl-5,5-diphenyl-3-furanmethanamine hydrochloride (A1-41), and 1-(2,2-diphenyltetrahydrofuran-3-yl)-N-methylmethanamine hydrochloride (A19-144), wherein the therapeutically effective amount is effective for the treatment of insomnia, anxiety, or a combination thereof in a subject in need thereof.
Administering a therapeutically effective combination for treating insomnia or anxiety
A method of treating insomnia, anxiety or a combination thereof in a subject in need thereof, comprising administering to the subject a dosage form comprising a therapeutically effective amount of any combination of two or more of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (A2-73), tetrahydro-N,N-dimethyl-5,5-diphenyl-3-furanmethanamine hydrochloride (A1-41), and 1-(2,2-diphenyltetrahydrofuran-3-yl)-N-methylmethanamine hydrochloride (A19-144), wherein the therapeutically effective amount is an amount effective to treat insomnia, anxiety, or a combination therefore in the subject.
Together, the independent claims are directed to a dosage form containing a therapeutically effective amount of a combination of two or more of A2-73, A1-41, and A19-144 for treating insomnia and/or anxiety, and administering that dosage form to treat insomnia and/or anxiety in a subject in need thereof.
Stated Advantages
Treating insomnia, anxiety, or a combination thereof in a subject in need thereof.
Provides reported improvements or stability in insomnia/anxiety/agitation measures in a Phase 2a study in mild-to-moderate Alzheimer’s disease patients.
Reports tolerability outcomes including adverse events such as dizziness and headache.
Reports potential benefit in systolic blood pressure control in subjects with hypertension.
Documented Applications
Therapeutic treatment of insomnia, anxiety, and agitation, including in a subject in need thereof.
Phase 2a clinical study in mild-to-moderate Alzheimer’s disease patients, with outcomes reported for insomnia, anxiety, agitation, cognitive/functional endpoints, and EEG/ERP P300 metrics.
Potential benefit for systolic blood pressure control in subjects with hypertension.
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