Centre National De La Recherche Scientifique

Bernard Delpech

Joanna Bakala

Jérôme Bignon

Maria Conception Achab

Pascal Collin

Maxim Egorov

Bogdan Iorga

Franck Pelissier

Jérome Bignon

Odile Thoison

Michel Benechie

Yves-Michel Frapart-Jannuad

Fabienne Peyrot

Yves-Michel Frapart-Jannaud

Maria Achab

The present invention relates to a 3-aryl-4 catechol-pyrrole-n-propanol compound and the derivatives thereof having General Formula (I), wherein:&#x2014;Ris an aryl group, particularly a phenyl, optionally substituted by one or more (C-C)alkyl groups, one or more halogens, one or more &#x2014;OH, &#x2014;CN or CFgroups, or a combination of same, and&#x2014;Ris a (C-C)alkyl group, a hydroxy(C-C)alkyl group, a (C-C)alcoxy(C-C)alkyl group, or a pharmaceutically acceptable hydrate or solvate of same. The invention also relates to the methods for preparing said compound and derivatives, to the pharmaceutical compositions containing same, and to the use of same as a drug or in the form of a prodrug converted via dimerization, particularly via oxidative coupling in the presence of a superoxide anion, in the treatment of cancer and diseases related to excessive angiogenesis. 

Use of a novel 3-aryl-4-catechol-pyrrole-N-propanol compound and the derivatives thereof to treat cancer and diseases related to excessive angiogenesis

The present invention relates to a compound of formula (I) in which: -m is an integer from 0 to 3, preferably from 0 to 2; n is an integer from 0 to 3, preferably from 0 to 2; m+n&#x2267;1; EAG is an electro-attractive group chosen independently from among a halogen atom, an NO, CF, CCI, CN, COH, (C&#x2550;O)NR, CH&#x2550;NR, (C&#x2550;S)OR, (C&#x2550;O)SR, CSR, SOR, SONR, SOR, P(O)(OR), P(O)(R), B(OR)group where R is a (C-C) alkyl radical, a phenyl group or a hydrogen atom; A is a saturated or unsaturated, linear or branched hydrocarbon chain including 1 to 10 atoms of carbon; and Rand Reach represent independently from one another a hydrogen atom, a CO-(Ci-C6)-alkyl, (C-C) alkyl, phenyl or phenyl-(C-C)-alkyl group, in which Rand Rform, together with the nitrogen atom they carry, a 5- to 15-member heterocycle, optionally substituted by a (C-C) alkyl group; including its stereoisomers and the mixtures thereof, or a pharmaceutically acceptable salt of same. 

N-substituted 3,4-bis (catechol) pyrrole compounds, and the preparation and use thereof in the treatment of cancer

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Clamart, France

Bernard Delpech