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1. WO2020112845 - PHARMACEUTICAL COMPOUNDS AND THERAPEUTIC METHODS

Publication Number WO/2020/112845
Publication Date 04.06.2020
International Application No. PCT/US2019/063356
International Filing Date 26.11.2019
IPC
A61K 31/427 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
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 2006.01
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
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
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61K 31/427
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 being nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61K 31/437
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
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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
  • RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY [US]/[US]
  • AUGERI, David J. [US]/[US]
  • SABAAWY, Hatem [US]/[US]
  • GILLERAN, John A. [US]/[US]
Inventors
  • AUGERI, David J.
  • SABAAWY, Hatem
  • GILLERAN, John A.
Agents
  • HARRIS, Robert J.
  • VIKSNINS, Ann S.
  • MALEN, Peter L.
  • MICKELSON, John W.
  • KRUEGER, Katherine A.D.
  • PADYS, Danny J.
  • ANDRUS, Alex
  • NIU, Lin
Priority Data
62/771,95627.11.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PHARMACEUTICAL COMPOUNDS AND THERAPEUTIC METHODS
(FR) COMPOSÉS PHARMACEUTIQUES ET MÉTHODES THÉRAPEUTIQUES
Abstract
(EN)
The invention provides compounds of formula (16) and (17); and salts thereof, as well as compositions comprising such compounds and salts, complexes comprising such compounds and salts, and methods for treating cancer, inhibiting BMI1 expression, or treating Huntington's disease using such compounds, salts, and complexes. The compounds, salts, and complexes have potency, permeability, and oral bioavailability that make them particularly useful, for example, for the treatment of glioblastoma.
(FR)
L'invention concerne des composés de formules (16) et (17) ; et des sels de ceux-ci, ainsi que des compositions comprenant de tels composés et sels, des complexes comprenant de tels composés et sels, et des méthodes de traitement du cancer, d'inhibition de l'expression de BMI1 ou de traitement de la maladie de Huntington au moyen de tels composés, sels et complexes. Les composés, sels et complexes présentent des propriétés d'action, de perméabilité et de biodisponibilité orale telles que celles-ci les rendent particulièrement utiles, par exemple, pour le traitement du glioblastome.
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