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1. WO2020198055 - ALLOSTERIC BCR-ABL PROTEOLYSIS TARGETING CHIMERIC COMPOUNDS

Publication Number WO/2020/198055
Publication Date 01.10.2020
International Application No. PCT/US2020/023990
International Filing Date 20.03.2020
IPC
C07D 417/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14containing three or more hetero rings
A61K 31/506 2006.01
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
CPC
A61K 31/4439
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
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/506
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
C07D 403/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 403/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
14containing three or more hetero rings
C07D 417/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
14containing three or more hetero rings
Applicants
  • YALE UNIVERSITY [US]/[US]
Inventors
  • CREWS, Craig M.
  • BURSLEM, George
Agents
  • DOYLE, Kathryn
  • LANDRY, Brian
  • SILVA, Domingos J.
  • SIMPSON, Mark D.
  • CROTTY, Justin
  • YOUNG, Jacque
  • BROWNING, Elizabeth
  • OSTROVSKY, Dennis
Priority Data
62/822,59422.03.2019US
62/824,15426.03.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ALLOSTERIC BCR-ABL PROTEOLYSIS TARGETING CHIMERIC COMPOUNDS
(FR) PROTÉOLYSE DE BCR-ABL ALLOSTÉRIQUE CIBLANT DES COMPOSÉS CHIMÉRIQUES
Abstract
(EN)
The present invention includes novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and/or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention include an allosteric tyrosine kinase inhibitor, a linker, and a ubiquitin ligase binder. The methods of the present invention include administering to the subject an pharmaceutically effective amount of at least one compound of the invention.
(FR)
La présente invention concerne de nouveaux composés et des méthodes de prévention ou de traitement de maladies associées à et/ou causées par une surexpression et/ou une activation incontrôlée d'une tyrosine kinase chez un sujet en ayant besoin. Dans certains modes de réalisation, les composés selon la présente invention comprennent un inhibiteur de tyrosine kinase allostérique, un lieur et une liaison d'ubiquitine ligase. Les méthodes selon la présente invention comprennent l'administration au sujet d'une quantité pharmaceutiquement efficace d'au moins un composé selon l'invention.
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