COMPOSITIONS PHARMACEUTIQUES COMPRENANT DES INHIBITEURS DE NEUROPILINE, ET LEUR UTILISATION DANS LA PRÉVENTION ET/OU LE TRAITEMENT DE TROUBLES ANGIOGÉNIQUES ET DE CANCERS
TRAGEX PHARMA;GARBAY, Christiane;HADJ-SLIMANE, Reda
发明人:
HADJ-SLIMANE, Reda,GARBAY, Christiane
申请号：
EPEP2012/058721
公开号：
WO2012/156289A1
申请日:
2012.05.11
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
The present invention relates to a compound of general formula (I), wherein Z1 is S or O, preferably S； -Z2- is -NRa-, wherein Ra is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, preferably Ra is H； -N=； O； S； -CRb=, wherein Rb is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO2, C1, Br, I, F, preferably H； -CHRC- wherein Rc is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO2, C1, Br, I, F, or -CH2-； preferably -Z2- is -NH- or -N=； each of R1 and R2 independently is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO2, C1, Br, I, F； preferably R1 and R2 together and with N and Z2 form an heterocycle eventually substituted, provided that said heterocycle is not an indole； R5 is H, OH, C1-4 alkyl, C1-4 alkoxy, C1-4 alkenyl, C1-4 alkynyl, amine, preferably R5 is NH2, NO2, C1, F, Br, I； more preferably R5 is H or CH3； even more preferably R5 is CH3； each of R8 and R9 independently is, H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO2, C1, Br, I, F； preferably R8 and R9 together form a cycle comprising 5 or 6 atoms, preferably an heterocycle comprising 5 or 6 atoms, more preferably a 1,3- dioxacyclopentene or a 1,4-dioxane； and - each of R3, R4, R6, R7, R10 and R11 independently is, H, OH, C1-4 alkyl, C1-4 alkoxy, C1-4 alkenyl, C1-4 alkynyl, amine, NO2, F, C1, Br, I； preferably H, CH3, OCH3, OH, NH2, NO2, C1, F, Br, I； more preferably is H or CH3； even more preferably is H； and to a pharmaceutical composition comprising a compound of general formula (I) or esters or salts thereof, in association with at least one pharmaceutically acceptable vehicle； and to the use thereof for inhibiting the Neuropilin pathways in the treatment of cancer and of angiogenic diseases.La présente invention concerne un composé de formule générale (I) comportant les éléments suivants : Z1, qui représente S ou O, et de préférence S ； -Z2-, qui représente -NRa-, Ra étant H, OH, un alkyle, un alkoxy, un aryle, un alcényle, un alcynyle ou une amine, et de préf
