AMINOPYRIMIDINYL DERIVATIVES FOR THE TREATMENT OF PARKINSON'S DISEASE
개요
발명자
Alessio CIULLI; Xingui LIU; Nikolai MAKUKHIN; Dario ALESSI; Alexia KALOGEROPULOU
IPC 분류
CPC 분류
Disclosed are heterobifunctional compounds that can induce the degradation of leucine-rich repeat kinase 2 (LRRK2) and PDE6D. These compounds can engage LRRK2 on one end and bind to an ubiquitin E3 ligase (e.g. cereblon, Von Hippel-Lindau, or Cellular Inhibitor of Apoptosis (cIAP)) on the other end and therefore bring LRRK2 in close proximity to the E3 ligase and induce the ubiquitination and degradation of the LRRK2 protein. Also disclosed are pharmaceutical composition comprising the heterobifunctional compounds and methods of using the compounds to treat LRRK2 and PDE6D-related diseases and disorders.
원문 (중국어)
Disclosed are heterobifunctional compounds that can induce the degradation of leucine-rich repeat kinase 2 (LRRK2) and PDE6D. These compounds can engage LRRK2 on one end and bind to an ubiquitin E3 ligase (e.g. cereblon, Von Hippel-Lindau, or Cellular Inhibitor of Apoptosis (cIAP)) on the other end and therefore bring LRRK2 in close proximity to the E3 ligase and induce the ubiquitination and degradation of the LRRK2 protein. Also disclosed are pharmaceutical composition comprising the heterobifunctional compounds and methods of using the compounds to treat LRRK2 and PDE6D-related diseases and disorders.