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1. WO2022006292 - NEK2 PROTEOLYSIS TARGETING CHIMERAS FOR USE IN MALIGNANT DISEASE

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Publication Number WO/2022/006292
Publication Date 06.01.2022
International Application No. PCT/US2021/039923
International Filing Date 30.06.2021
IPC
A61K 31/454 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
454containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 47/54 2017.1
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
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
CPC
A61K 31/475
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
47Quinolines; Isoquinolines
475having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/704
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
7034attached to a carbocyclic compound, e.g. phloridzin
704attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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 47/55
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
55the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
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
  • BIOVENTURES, LLC [US]/[US]
Inventors
  • FRETT, Brendan
  • KENDRICK, Samantha
Agents
  • GULMEN, Tolga, S.
Priority Data
63/046,20930.06.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) NEK2 PROTEOLYSIS TARGETING CHIMERAS FOR USE IN MALIGNANT DISEASE
(FR) CHIMÈRES CIBLANT LA PROTÉOLYSE DE NEK2 DESTINÉES À ÊTRE UTILISÉES DANS UNE MALADIE MALIGNE
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Abstract
(EN) This invention describes a small molecule proteolysis targeting chimera (PROTAC) strategy to degrade the NEK2 (Never in Mitosis Related Kinase 2) protein and methods of use thereof. The NEK2 PROTAC consists of three, key regions: a NEK2 ligand to bind the NEK2 protein, a linker region to link the NEK2 ligand to a ligase ligand, and the ligase ligand.
(FR) La présente invention concerne une stratégie de chimère ciblant la protéolyse de petites molécules (PROTAC) pour dégrader la protéine NEK2 (Never in Mitosis Related Kinase 2) et ses méthodes d'utilisation. La NEK2 PROTAC est constituée de trois régions clés : un ligand NEK2 pour lier la protéine NEK2, une région lieur pour lier le ligand NEK2 à un ligand ligase, et le ligand ligase.
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