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US 11,077,108 B2Granted
Allosteric corticotropin-releasing factor receptor 1 (CRFR1) antagonists that decrease p-tau and improve cognition
AssigneeThe Regents of the University of California
InventorsMohammad Parvez Alam, Varghese John, Barbara Jagodzinska
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Abstract
In various embodiments novel allosteric antagonists of the CRFR1 receptor are provided. It discovered that allosteric CRFR1 receptor antagonists are effective to modulate p-Tau levels in Alzheimer's disease (AD) models. In one illustrative embodiment, a compound that is a CRFR1 receptor antagonist is a compound according to the formula or a pharmaceutically acceptable salt, ester, amide, solvate, or prodrug thereof.
Claims14
A compound that is a CRFR1 receptor antagonist, wherein said compound is a compound according to the formula
- or a pharmaceutically acceptable salt, enantiomer, or solvate thereof, wherein:
- X and Y are independently selected from the group consisting of Me, H, CF3, deuterated methyl, and halogen;
- R1 is an unsubstituted aminoaryl or a substituted aminoaryl, wherein the substituted aminoaryl is substituted with a substituent selected from the group consisting of CH3, OCH3, halogen, CH2NH2, CN, and CR83, wherein R8 is halogen;
- and
- R2 is an unsubstituted branched alkoxide or a substituted branched alkoxide, wherein the substituted branched alkoxide is substituted with a substituent selected from the group consisting of OCH3, CH3, and CH2OH, and wherein at least one of R1 or R2 is substituted with —OCH3.
2 more elements
Dependencies are inferred from the claim text.