Title:
COMPOUNDS FOR TAU PROTEIN DEGRADATION
Document Type and Number:
Japanese Patent JP2023106366
Kind Code:
A
Abstract:
To provide bifunctional compounds that bind to tau protein and/or promote targeted ubiquitination for the degradation of tau protein.SOLUTION: There is provided bifunctional compounds that bind to tau protein whose aggregation is related to a variety of neurodegenerative diseases (e.g., tauopathies), and can promote tau protein degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon) which can ubiquitinate tau protein, and labeling it for proteasomal degradation. There is also provided radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.SELECTED DRAWING: None
Inventors:
NATHANAEL S GRAY
STEPHEN J HAGGARTY
CAI QUAN
MARIA CATARINA TELO BAPTISTA LIMA DA SILVA
ZHANG TINGHU
FLEUR M FERGUSON
STEPHEN J HAGGARTY
CAI QUAN
MARIA CATARINA TELO BAPTISTA LIMA DA SILVA
ZHANG TINGHU
FLEUR M FERGUSON
Application Number:
JP2023062212A
Publication Date:
August 01, 2023
Filing Date:
April 06, 2023
Export Citation:
Assignee:
DANA FARBER CANCER INST INC
MASSACHUSETTS GEN HOSPITAL
MASSACHUSETTS GEN HOSPITAL
International Classes:
C07D471/04; A61K31/437; A61K31/4545; A61K38/05; A61K47/55; A61K51/04; A61P25/28; C12Q1/02; G01N33/68
Attorney, Agent or Firm:
Kiyoshi Kuzuwa