Methods and compositons for stimulating neurogenesis and inhibiting neuronal degeneration
Inventors
Assignees
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Publication Number
US-8039462-B2
Publication Date
2011-10-18
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, and depression. This invention could also be used 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 patent discloses pharmaceutical compositions and methods for stimulating neurogenesis and inhibiting neuronal degeneration in mammals, including humans, for neuronal-loss disorders, neurodegenerative diseases, psychiatric disorders, and aging. The therapeutic approach is associated with administering effective amounts of compounds defined by formulas with multiple substituent variables and selected structures, together with a pharmaceutically acceptable carrier.
The compound definitions are expressed through Markush-style R-group selection rules, including R1, R2, R3, R4, R5, R6, R8, R9, R10, and R11, with further substituent definitions for related groups and provisos. The disclosure also references physiologically acceptable salts, solvates, and hydrates, and chemical structures labeled as Formulas I–XV, including specific structures such as Formula I and Formula XII–XIV.
The patent also describes formulation and delivery concepts for administering the compounds, including parenteral or injection routes and sustained/controlled release and implantable delivery concepts. Sterile injection solutions, aqueous and non-aqueous sterile suspensions, isotonic preparations, lyophilized preparations, optional additional therapeutic agents, and kit formats using unit-dose or multi-dose containers and compartments are described.
Claims Coverage
The independent claims cover pharmaceutical compositions and compounds defined by Markush-type structural formula constraints, with physiologically acceptable salts, solvates, hydrates, and pharmaceutically acceptable carriers. Across the claim families, the inventive coverage centers on formula-based substituent selections and selected structures, with dependent refinements including at least one R1 substituent being not hydrogen.
Pharmaceutical composition with formula-defined substituents and pharmaceutically acceptable carrier
A pharmaceutical composition comprising a compound of a formula with substituent definitions for R1, R2, R3, R4, R5, and R6, together with a pharmaceutically acceptable carrier.
Compound selected from an enumerated structure set with physiologically acceptable derivatives
A compound having a structure selected from an enumerated group, together with physiologically acceptable salts, solvates, and hydrates thereof.
Pharmaceutical composition with additional substituent options and pharmaceutically acceptable carrier
A pharmaceutical composition comprising a compound of a formula with substituent definitions for R1, R2, R3, R4, R6, and additional substituent sets including R8 and R9, together with a pharmaceutically acceptable carrier.
Pharmaceutical composition with extended substituent set including R10 and R8/R9 options
A pharmaceutical composition comprising a compound of a formula with substituent definitions for R1, R2, R3, R4, R6, R10, and R8, together with a pharmaceutically acceptable carrier.
Pharmaceutical composition with formula-defined substituents including R11
A pharmaceutical composition comprising a compound of a formula with substituent definitions for R1, R2, R3, R4, R6, R11, and R8, together with a pharmaceutically acceptable carrier.
Overall, the independent claims define pharmaceutical compositions and compounds via enumerated structural formula constraints, including multiple R-group selections and selected structures. Compound-only claim types require physiologically acceptable derivatives, while composition claims include a pharmaceutically acceptable carrier.
Stated Advantages
Stimulating neurogenesis and/or inhibiting neuronal degeneration in mammals.
Treatment of neurodegenerative diseases, psychiatric disorders, aging, and neuronal-loss disorders including Alzheimer’s disease, stroke, traumatic brain injury, and depression.
Formulation and delivery concepts include parenteral or injection administration, sustained/controlled release, implantable delivery concepts, sterile injection solutions, aqueous and non-aqueous sterile suspensions, isotonic preparations, lyophilized preparations, and kit formats.
In vitro neurogenesis and neurodegeneration inhibition results are provided.
Drug-like properties/toxicity screening and BBB penetration criteria are described.
Documented Applications
Stimulation of neurogenesis and/or inhibition of neuronal degeneration in mammals for neurodegenerative diseases.
Stimulation of neurogenesis and/or inhibition of neuronal degeneration in mammals for psychiatric disorders.
Stimulation of neurogenesis and/or inhibition of neuronal degeneration in mammals for aging.
Treatment of neuronal-loss disorders, including Alzheimer’s disease, stroke, traumatic brain injury, and depression.
Parenteral/injection administration and formulation/delivery use cases including sterile injection solutions, sterile suspensions, isotonic preparations, lyophilized preparations, and related kit/unit-dose or multi-dose container formats.
Sustained/controlled release and implantable delivery concepts for delivering the compounds.
Research products and kits are referenced as part of the disclosure context.
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