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1. WO2020168170 - ISOTOPICALLY-STABILIZED TETRONIMIDE COMPOUNDS

Publication Number WO/2020/168170
Publication Date 20.08.2020
International Application No. PCT/US2020/018256
International Filing Date 14.02.2020
IPC
A61K 31/18 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
18Sulfonamides
A61K 31/351 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
351not condensed with another ring
A61K 31/381 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
CPC
A61P 35/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
04specific for metastasis
C07B 2200/05
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
05Isotopically modified compounds, e.g. labelled
C07D 307/66
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
34having two or three double bonds between ring members or between ring members and non-ring members
56with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
66Nitrogen atoms
Applicants
  • MIDWESTERN UNIVERSITY [US]/[US]
Inventors
  • OLSEN, Mark, Jon
  • SEERDEN, Jean Paul
Agents
  • LUCKOW, Verne, A.
Priority Data
62/806,32715.02.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ISOTOPICALLY-STABILIZED TETRONIMIDE COMPOUNDS
(FR) COMPOSÉS DE TÉTRONIMIDE À STABILISATION ISOTOPIQUE
Abstract
(EN)
Isotopically-stabilized tetronimide compounds comprising one or more deuterium atoms, derivatives, and intermediates, thereof, including methods for their synthesis, pharmaceutical compositions thereof, and methods of using these compounds to interact with target molecules in cell-free samples, cell- and tissue-based assays, animal models, and in a subject are disclosed. One aspect relates to molecules that modulate the expression or catalytic activity of aspartyl (asparaginyl) β-hydroxylase (ASPH) within or on the surface of a cell. Other aspects of the invention relate to use of the molecules disclosed herein to diagnose, ameliorate, or treat cell proliferation disorders and related diseases. Related aspects include uses of the compounds to modulate the activity of viruses, as anti¬ hyperlipidemia agents, and as agents to ameliorate or treat thrombosis and related cardiovascular and metabolic disorders.
(FR)
L'invention concerne des composés de tétronimide à stabilisation isotopique comprenant un ou plusieurs atomes de deutérium, des dérivés et des intermédiaires de ceux-ci, y compris des procédés pour leur synthèse, des compositions pharmaceutiques à base de ceux-ci et des procédés d'utilisation de ces composés en vue d'une interaction avec des molécules cibles dans des échantillons acellulaires, des analyses cellulaires et tissulaires, des modèles animaux et chez un sujet. Un aspect concerne des molécules qui modulent l'expression ou l'activité catalytique de l'aspartyl (asparaginyl) β-hydroxylase (ASPH) dans une cellule ou à sa surface. D'autres aspects de l'invention concernent l'utilisation des molécules décrites dans la description pour diagnostiquer, améliorer ou traiter des troubles de la prolifération cellulaire et des maladies associées. Des aspects associés comprennent des utilisations des composés pour moduler l'activité de virus, en tant qu'agents anti-hyperlipidémie et en tant qu'agents pour améliorer ou traiter la thrombose et les troubles cardiovasculaires et métaboliques associés.
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