KAPPA OPIOID AGONISTS AND USES THEREOF

摘要

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

主权项

1. A compound selected from Formula I: wherein:
R1 is selected from optionally substituted aryl, optionally substituted amino, and optionally substituted aryloxy;R2 is selected from hydrogen, optionally substituted aryl, and X-POLY;R3 is selected from hydrogen and an optionally substituted alkyl;R4 is selected from an optionally substituted aryl;R5 is selected from hydrogen, optionally substituted alkyl, and X-POLY;R6 is selected from hydrogen and an optionally substituted alkyl; orR5 and R6 may be taken together to form an optionally substituted heterocyclyl; provided at least one of R1, R2, R4, R5, and R6 are an X-POLY group or are substituted with an ˜X-POLY group, wherein X is an optional linker and POLY is a water soluble, non-peptidic oligomer; andprovided that when R1 is phenyl, R2 is phenyl, R3 is methyl, R4 is phenyl, and R5 and R6 are taken together to form a pyrrolidinyl group, the pyrrolidinyl group is not substituted with ˜X-POLY;and pharmaceutically acceptable salts and solvates thereof.