Method of improving cognition and social behavior in humans having deficits therein due to neurodegenerative disorders and compounds and compositions therefor
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsMehrdad Shamloo, Bitna Yi, Pooneh Memar Ardestani
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Abstract
A β1-ADR agonist prodrug compound, which is hydrolysable in vivo to release a β1-ADR agonist compound, and which prodrug compound contains a group which imparts greater lipophilicity and CNS bioavailability to the prodrug compound relative to the β1-ADR agonist compound.
Claims36
A β1-ADR agonist prodrug compound, which is hydrolysable in vivo to release a corresponding β1-ADR agonist compound, and which prodrug compound contains at least one group which imparts greater lipophilicity and CNS bioavailability to the prodrug compound relative to the corresponding β1-ADR agonist compound.
A method of selecting one or more β1-ADR agonist prodrugs for therapeutic use, which comprises:
- a) selecting one or more prodrug compounds having an enhanced c log P value relative to the corresponding β1-ADR agonist compound;
- b) subjecting the selected prodrug compounds from step a) to a battery of ADME tests, and determining SPR values for the prodrug compounds.
- c) selecting one or more prodrug compounds from step b) and subjecting said prodrug compounds to in vivo biodistribution and pharmacokinetic evaluation;
- d) selecting one or more prodrug compounds from step c) for pre-clinical animal model studies;
- and
- e) producing a TPP for each compound selected in all of steps a)-d), for further development and therapeutic use.
Dependencies are inferred from the claim text.