PEREIRA NASCIMENTO COSTA, Gonçalo,FERREIRA GONÇALVES, Nuno Paulo,PEREIRA MONTEIRO, Carlos Jorge,REIS DE ABREU, Artur Carlos,FERRAZ CARDOSO SOARES, Hélder Tão,BORGES ROCHA, Luis Gabriel,SCHABERLE, Fabi
申请号：
IBIB2016/052606
公开号：
WO2016/178191A1
申请日:
2016.05.06
申请国别(地区):
IB
年份:
2016
代理人:
摘要：
The present invention relates to carboxamide halogenated porphyrin derivatives, in particular bacteriochlorin or chlorin, of formula (I) wherein: represents a carbon-carbon single bond or a carbon-carbon double bond, provided that at least one represents a carbon-carbon single bond； Y1, Y2 are each independently chosen from hydrogen, halogenated alkyl or halogenated cycloalkyl with 6 or less carbon atoms, or halogenated phenyl where the halogens are independently chosen from F, Cl and Br, provided that at least one position of the alkyl, cycloalkyl or phenyl is halogenated, and provided that at least one of Y1, Y2 is not hydrogen； R1 is chosen from H, I, Cl, Br or -CONR'R'', where R' and R'' are independently chosen from hydrogen, alkyl with 6 or less carbon atoms, cyclopropyl, cyclobutyl, cyclopentyl, alcohol, primary amine, secondary amine, tertiary amine, positively-charged quaternary amine, carboxylic acid, ether or ester, or pharmaceutically acceptable salts thereof. This invention also relates to the use of the above mentioned carboxamide halogenated porphyrin derivatives, in particular bacteriochlorin or chlorin, of Formula (I) or a pharmaceutically acceptable salt thereof in photodynamic therapy, where the referred derivatives are able to detect and exhibit the presence of hyperproliferative disorders and, in the presence of an adequate lighting, to treat the same. The present invention also describes a pharmaceutical composition comprising one or more of the carboxamide halogenated porphyrin derivatives, in particular bacteriochlorin or chlorin, of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of cancer and/or microbial and/or viral infections, in humans or animals.La présente invention concerne des dérivés carboxamide de porphyrines halogénées, en particulier une bactériochlorine ou une chlorine, de formule (I) où : représente une liaison simple carbone-carbone ou une double liaison carbone-carbone, à condition que l'une au m
