Fluorinated mu-opioid receptor agonists
AssigneeThe United State of America, as represented by the Secretary, Department of Health and Human
InventorsMichael Michaelides, Juan L. Gomez, Kenner C. Rice, Agnieszka Sulima, Michael H. Baumann
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Abstract
The invention provides a fluorinated compound of Formula (I): a deuterated or tritiated variant thereof, or a pharmaceutically acceptable salt thereof, wherein at least one C—H bond on the compound of Formula (I) is replaced with a C—F bond or a C—18F bond. The invention further provides compositions comprising the fluorinated compound, a deuterated or tritiated variant thereof, or a pharmaceutically acceptable salt thereof, and methods of using the fluorinated compound, a deuterated or tritiated variant thereof, or a pharmaceutically acceptable salt thereof.
Claims29
A fluorinated compound of Formula (I):
- a deuterated or tritiated variant thereof, or a pharmaceutically acceptable salt thereof,
- wherein X is optionally present and, when present, is —O—, —S—, or —NR4—,
- wherein each of R1, R2, R3, and R4 is independently selected from hydrogen, a substituted or unsubstituted C1-6 alkyl group, a substituted or unsubstituted C2-6 alkenyl group, a substituted or unsubstituted C2-6 alkynyl group, a substituted or unsubstituted C1-6 heteroalkyl group, a substituted or unsubstituted C3-6 cycloalkyl group, a substituted or unsubstituted C3-6 heterocycloalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted alkaryl group, a substituted or unsubstituted arylalkyl group, and a combination thereof, and
- wherein at least one C—H bond on the compound of Formula (I) is replaced with a C—F bond or a C—18F bond.
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32-36. (canceled)
A compound of formula
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.