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1. WO2020223456 - DEGRADATION OF AURORA KINASE (AURK) BY CONJUGATION OF AURK INHIBITORS WITH E3 LIGASE LIGAND

Publication Number WO/2020/223456
Publication Date 05.11.2020
International Application No. PCT/US2020/030663
International Filing Date 30.04.2020
IPC
A61K 31/422 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
A61K 31/427 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61K 31/437 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
CPC
A61K 47/545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
545Heterocyclic compounds
A61K 47/556
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
555pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
556enzyme catalyzed therapeutic agent [ECTA]
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • NEMUCORE MEDICAL INNOVATIONS, INC. [US]/[US]
Inventors
  • COLEMAN, Timothy, Patrick
Agents
  • TRINQUE, Brian, C.
  • AREZINA, Vladimir, I.
  • BARTON, Steven, K.
  • ANIS, Hissan
  • CHEN, Xiaoyue (peter)
Priority Data
62/841,36501.05.2019US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) DEGRADATION OF AURORA KINASE (AURK) BY CONJUGATION OF AURK INHIBITORS WITH E3 LIGASE LIGAND
(FR) DÉGRADATION DE L'AURORA KINASE (AURK) PAR CONJUGAISON D'INHIBITEURS DE L'AURK AVEC UN LIGAND DE LIGASE E3
Abstract
(EN) Provided herein are compounds, which act as protein degradation inducing moieties for aurora kinase (AURK). The present application also relates to methods for the targeted degradation of AURK through the use of the compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to AURK which can be utilized in the treatment of disorders modulated by AURK.
(FR) L'invention concerne des composés qui agissent en tant que fractions induisant la dégradation de protéines pour l'aurora kinase (AURK). La présente invention concerne également des procédés pour la dégradation ciblée de l'AURK par l'utilisation des composés qui lient une fraction de liaison à l'ubiquitine ligase à un ligand qui est capable de se lier à l'AURK qui peut être utilisé dans le traitement de troubles modulés par l'AURK.
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