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1. WO2020006157 - DOT1L DEGRADER AND USES THEREOF

Publication Number WO/2020/006157
Publication Date 02.01.2020
International Application No. PCT/US2019/039368
International Filing Date 27.06.2019
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
16
Purine radicals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07H 19/16 (2006.01)
A61P 35/00 (2006.01)
CPC
A61P 35/00
C07H 19/16
Applicants
  • DANA-FARBER CANCER INSTITUTE, INC. [US/US]; 450 Brookline Avenue Boston, MA 02215, US
Inventors
  • QI, Jun; US
  • ARMSTRONG, Scott; US
  • PARK, Paul M.; US
Agents
  • CHAO, Jessica, J.; US
  • AMUNDSEN, Eric, L.; US
  • ATTISHA, Michael, J.; US
  • ACHILLES, Daryl, L.; US
  • ALAM, Saad; US
Priority Data
62/690,79127.06.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DOT1L DEGRADER AND USES THEREOF
(FR) AGENTS DE DÉGRADATION DE DOT1L ET UTILISATIONS ASSOCIÉES
Abstract
(EN)
Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety that is a binder of a target protein DOT1L to induce degradation of DOT1L. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, such as cancers). Provided also are methods of inducing the degradation of DOT1L by administering a bifunctional compound or composition described herein, wherein one component of the bifunctional compound is a binder of an E3 ubiquitin ligase (e.g., lenalidomide, thalidomide) and another component of the compound is a binder of the target protein DOT1L in a subject.
(FR)
La présente invention concerne des composés bifonctionnels comprenant une fraction (par exemple, lénalidomide, thalidomide) qui est un liant d'une ubiquitine ligase E3 (par exemple, céréblon) et une autre fraction qui est un liant d'une protéine cible DOT1L pour induire la dégradation de DOT1L. L'invention concerne également des compositions pharmaceutiques comprenant les composés bifonctionnels, et des méthodes de traitement et/ou de prévention de maladies (par exemple, des maladies prolifératives, comme les cancers). L'invention concerne en outre des méthodes d'induction de la dégradation de DOT1L par administration d'un composé bifonctionnel ou d'une composition selon l'invention, un constituant du composé bifonctionnel étant un liant d'une ubiquitine ligase E3 (par exemple, lénalidomide, thalidomide) et un autre constituant du composé étant un liant de la protéine cible DOT1L chez un sujet.
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