MACROCYCLIC COMPOUNDS AND USES THEREOF

摘要

The present invention relates to novel macrocyclic compounds of Formula I and their use as novel therapeutic agents for example as novel compounds used in methods of preventing and/or treating a disease, condition or state in a subject associated with dysregulation of protease activity and/or dysregulation of proteosome activity

主权项

1. A compound of Formula I and/or a pharmaceutically acceptable salt, solvate, tautomer, hydrate or prodrug derivative thereof: wherein:
R1 is alkyl, aryl, heteroalkyl, or a side chain of a natural or non-natural alpha amino acid;R2 is CH(═O), CHR4OH, C(═O)R4, C(═O)C(═O)NHR4, CHR4NHR4, B(OH)2, or a heterocycle, and R4 is H, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy or optionally substituted heteroarylalkoxy;Z is a heterocycle or a heteroaryl;Y is C(═O), C(═S), C(═NR5), CH2, CHR5, and R5 is H, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy or optionally substituted heteroarylalkoxy;W is no atom, alkyl, heteroalkyl, heterocycle, aryl, or heteroaryl;R3 is alkyl, heteroalkyl, heterocycle, aryl, heteroaryl; andX is no atom, alkyl, heteroalkyl, heterocycle, aryl, or heteroaryl.