Methods and compositions for stimulating neurogenesis and inhibiting neuronal degeneration using isothiazolopyrimidinones
Inventors
Assignees
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Publication Number
US-8609840-B2
Publication Date
2013-12-17
Expiration Date
Abstract
The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
Core Innovation
The invention relates to isothiazolopyrimidinone compounds for stimulating neurogenesis and inhibiting neuronal degeneration. The disclosure presents a broad chemical scaffold defined by Formula I, in which substituents include R1, L, X, Y, Z, T (O/S/NR1), and n (2 or 3), together with optional substitution patterns.
The disclosure further describes pharmaceutical salts, solvates, and hydrates and scope for pharmaceutical compositions using pharmaceutically acceptable carriers and/or excipients, together with administration routes. Treatment is directed to mammals and humans afflicted with neurodegenerative diseases and neuropsychiatric disorders, based on the stated functions of stimulating neurogenesis and inhibiting neuronal degeneration.
The stated target conditions include neuronal-loss conditions such as Alzheimer’s disease, stroke, traumatic brain/nerve injury, and depression. Alongside therapeutic use, the disclosure also mentions research-grade neuron-promoting agents associated with the same isothiazolopyrimidinone compounds.
Claims Coverage
The provided independent claims cover two core areas: (1) a compound selected from a specified group, and (2) a pharmaceutical composition comprising such a selected compound, including pharmaceutically acceptable salts, hydrates, or solvates. Overall, the inventive features are centered on selecting from the compound group and optionally using acceptable-form variants, with composition coverage adding a pharmaceutical composition context.
Selected isothiazolopyrimidinone compound group with acceptable-form variants
A compound selected from the group consisting of the disclosed compounds, together with pharmaceutically acceptable salts, hydrates, or solvates thereof.
Pharmaceutical composition comprising selected compound with acceptable-form variants
A pharmaceutical composition comprising a compound selected from the group consisting of the disclosed compounds, together with pharmaceutically acceptable salts, hydrates, or solvates thereof.
Across the independent claim set provided, the inventive coverage is limited to selection from the disclosed compound group and inclusion of pharmaceutically acceptable salts, hydrates, or solvates, with a second independent claim extending this selection to a pharmaceutical composition.
Stated Advantages
Stimulation of neurogenesis.
Inhibition of neuronal degeneration.
Higher neurogenesis activity than LIF.
Inhibition of neuronal degeneration in the tested in vitro assays.
Documented Applications
Treatment of neuronal-loss conditions including Alzheimer’s disease, stroke, traumatic brain/nerve injury, and depression.
Use as research-grade neuron-promoting agents.
Therapeutic use for stimulating neurogenesis and/or inhibiting neuronal degeneration in mammals for neurodegenerative diseases and psychiatric disorders.
Use in the context of traumatic brain/nerve injury as referenced in the overall discussion.
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