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1. WO2021058979 - THERAPY

Publication Number WO/2021/058979
Publication Date 01.04.2021
International Application No. PCT/GB2020/052335
International Filing Date 25.09.2020
IPC
A61K 41/00 2020.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
41Medicinal preparations obtained by treating materials with wave energy or particle radiation
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 41/0038
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
41Medicinal preparations obtained by treating materials with wave energy or particle radiation ; ; Therapies using these preparations
0038Radiosensitizing, i.e. administration of pharmaceutical agents that enhance the effect of radiotherapy
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07C 209/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
209Preparation of compounds containing amino groups bound to a carbon skeleton
04by substitution of functional groups by amino groups
06by substitution of halogen atoms
12with formation of quaternary ammonium compounds
C07C 65/105
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
65Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
01containing hydroxy or O-metal groups
105polycyclic
C07C 65/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
65Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
21containing ether groups, groups, groups, or groups
24polycyclic
C07C 65/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
65Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
21containing ether groups, groups, groups, or groups
24polycyclic
26containing rings other than six-membered aromatic rings
Applicants
  • VESTLANDETS INNOVASJONSSELSKAP AS [NO]/[NO]
  • GOLDING, Louise [GB]/[GB] (MG)
Inventors
  • BJØRSVIK, Hans-René
  • ENGER, Per Øyvind
  • CIRILLO, Davide
  • SAROWAR, Shahin
Agents
  • DEHNS
Priority Data
1913785.025.09.2019GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) THERAPY
(FR) THÉRAPIE
Abstract
(EN)
The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy, in one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: -C1-6 alkyl (preferably C1-3 alkyl, e.g. -CH3), -O-C1-6 alkyl (preferably -O-C1-3 alkyl, e.g, -OCH3), -S-C1-6 alkyl (preferably -S-C1-3 alkyl, e.g, -SCH3), -OH, -SH, -CO2R1 (where R1 is H or C1-6 alkyl, preferably C1-3 alkyl, e.g. -CH3), -SO2-C1-6 alkyl (preferably -SO2-C1-3 alkyl, e.g. -SO2-CH3), -SO2-NR2R3 (where R2 is H and R3 is optionally substituted phenyl), -NR4R5 (wherein R4 and R5 are independently selected from H, C1-6 alkyl (preferably C1-3 alkyl, e.g. -CH3), and -CO-C1-6 alkyl (preferably -CO-C1-3 alkyl, e.g. -CO-CH3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z double bond.
(FR)
L'invention aborde la radiorésistance dans le traitement du cancer impliquant la radiothérapie et, en particulier, les limitations associées à l'utilisation de médicament sulfasalazine. Plus précisément, elle concerne une série de composés destinés à être utilisés en tant que radiosensibilisants dans le traitement de cancers tels que les glioblastomes qui sont mortels et intrinsèquement résistants à la radiothérapie, selon un mode de réalisation, l'invention concerne des composés de formule générale (I), leurs stéréoisomères et leurs sels pharmaceutiquement acceptables destinés à être utilisés en tant que radiosensibilisants dans le traitement du cancer, le cycle A étant choisi parmi un phényle, un biphényle et un fluorényle éventuellement substitués ; chaque X étant indépendamment choisi parmi : -alkyle en C1-6 (de préférence un alkyle en C1-3, par exemple -CH3), -O-alkyle en C1-6 (de préférence -O-alkyle en C1-3, par exemple, -OCH3), -S-alkyle en C1-6 (de préférence -S-alkyle en C1-3, par exemple, -SCH3), -OH, -SH, -CO2R1 (où R1 est un H ou un alkyle en C1-6, de préférence un alkyle en C1-3, par exemple, -CH3), -SO2-alkyle en C1-6 (de préférence -SO2-alkyle en C1-3, par exemple, -SO2-CH3), -SO2-NR2R3 (où R2 est un H et R3 est un phényle éventuellement substitué), -NR4R5 (dans lequel R4 et R5 sont choisis indépendamment parmi un H, un alkyle en C1-6 (de préférence un alkyle en C1-3, par exemple, -CH3), et -CO-alkyle en C1-6 (de préférence -CO-alkyle en C1-3, par exemple, -CO-CH3), un atome d'halogène (par exemple, le F, le Cl ou le Br), et un tétrazolyle éventuellement substitué ; n est un nombre entier de 0 à 5, de préférence de 0 à 2, par exemple 1 ou 2 ; et représente une double liaison E ou Z.
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