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1. WO2020115009 - LPAAT-β INHIBITORS FOR TREATMENT OF CANCER

Publication Number WO/2020/115009
Publication Date 11.06.2020
International Application No. PCT/EP2019/083405
International Filing Date 03.12.2019
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 405/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
A61K 31/53 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
53having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 405/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants
  • UNIVERSITÄT BERN [CH]/[CH]
Inventors
  • REYMOND, Jean-Louis
  • POIRIER, Marion
  • AWALE, Mahendra
  • RUDDIGKEIT, Lars
  • GIUFFREDI, Guy
  • CHARLES, Roch-Philippe
Agents
  • SCHULZ JUNGHANS PATENTANWÄLTE PARTGMBB
Priority Data
18209847.503.12.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) LPAAT-β INHIBITORS FOR TREATMENT OF CANCER
(FR) INHIBITEURS DE LPAAT-β POUR LE TRAITEMENT DU CANCER
Abstract
(EN)
The present invention relates to a compound of formula (1), wherein R1 and R4 are selected from halogen, small hydrocarbon or alkoxy moieties, R2 is a short alkyl moiety, and X is selected from -S-, -O-, -N(R5)-, wherein R5 is selected from H or a short alkyl moiety. Furthermore, the compound of formula (1) may be used as a medicament, particularly in the treatment of cancer. The invention also relates to a method of inhibiting lysophosphatidic acid acyltransferase β (LPAAT-β).
(FR)
La présente invention concerne un composé de formule (1), dans laquelle R1 et R4 sont choisis parmi un halogène, des petites fractions d'hydrocarbures ou d'alcoxy, R2 est une fraction d'alkyle courte, et X est choisi parmi-S -, -O -, -N(R5)-, dans laquelle R5 est choisi parmi H ou une fraction d'alkyle courte. En outre, le composé de formule (1) peut être utilisé en tant que médicament, en particulier dans le traitement du cancer. L'invention porte également sur un procédé d'inhibition d'acide lysophosphatidique acyltransférase β (LPAAT-β).
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