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1. WO2020111921 - ANTI-CANCER ACTIVITIES OF A NEW FAMILY OF ETHACRYNIC ACID DERIVATIVES

Publication Number WO/2020/111921
Publication Date 04.06.2020
International Application No. PCT/MA2019/000013
International Filing Date 29.11.2019
IPC
C07F 9/6509 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6509Six-membered rings
C07D 295/185 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
18by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
182Radicals derived from carboxylic acids
185from aliphatic carboxylic acids
A61K 31/495 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
A61K 31/6615 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
661Phosphorus acids or esters thereof not having P-C bonds, e.g. fosfosal, dichlorvos, malathion
6615Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
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 31/495
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
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 295/185
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
18by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
182Radicals derived from carboxylic acids
185from aliphatic carboxylic acids
C07F 9/650952
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6509Six-membered rings
650952having the nitrogen atoms in the positions 1 and 4
Applicants
  • UNIVERSITE EUROMEDITERRANEENNE DE FES [MA]/[MA]
  • UNIVERSITE SULTAN MOULAY SLIMANE BENI MELLAL [MA]/[MA]
Inventors
  • EL KAZZOULI, Saïd
  • ZYAD, Abdelmajid
  • EL BRAHMI, Nabil
  • EL ABBOUCHI, Abdelmoula
  • BOUJDI, Khalid
  • BOUSMINA, Mostapha
  • AIT MOUSE, Hassan
  • TILAOUI, Mounir
Agents
  • BOUNOU, Salim
Priority Data
4403829.11.2018MA
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) ANTI-CANCER ACTIVITIES OF A NEW FAMILY OF ETHACRYNIC ACID DERIVATIVES
(FR) ACTIVITÉS ANTICANCÉREUSES D'UNE NOUVELLE FAMILLE DES DÉRIVÉS DE L'ACIDE ETHACRYNIQUE
Abstract
(EN)
The present invention relates to a new class of small anti-cancer molecules derived from ethacrynic acid (symbolized by AE). The invention relates to the in vitro and in vivo anti-cancer activities and to the methods for producing the new AE family. New AE analogues were synthesized and then the in vitro cytotoxic activities thereof were evaluated on the P815 tumour cell line using the MTT test. The AE derivative which exhibited the best in vitro cytotoxicity was then tested in vivo using the DBA2/P815 (H2d) mouse model. At 30 mg/kg, the effective dose, the animals showed general tolerance with a percentage survival of around 80%, and no significant weight loss was observed.
(FR)
La présente invention concerne une nouvelle classe de petites molécules anticancéreuses dérivées de l'acide éthacrynique (symbolisé par AE). L'invention concerne les activités anticancéreuses in vitro et in vivo et les procédés de préparation de la nouvelle famille de l'AE. De nouveaux analogues de l'AE ont été synthétisés puis, leurs activités cytotoxiques in vitro ont été évaluées sur la lignée cellulaire tumorale P815 en utilisant le test MTT. Le dérivé de l'AE, qui a présenté la meilleur cytotoxité in vitro, a été ensuite testé in vivo en utilisant le modèle de souries DBA2/P815 (H2d). A 30 mg/kg, la dose effective, les animaux ont montré une tolérance générale avec un pourcentage de survie aux alentours de 80%, et aucune perte de poids significative n'a été observée
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