LUZITIN, S.A.;LUZITIN;UNIVERSIDADE DE COIMBRA; S.A.
发明人:
FERREIRA GONCALVES, NUNO PAULO,CERCA MARTINS DOS SANTOS, TANIA PATRICIA,PEREIRA NASCIMENTO COSTA, GONCALO,PEREIRA MONTEIRO, CARLOS JORGE,SCHABERLE, FABIO ANTONIO,CORREIA ALFAR, SONIA,REIS DE ABREU, AR
申请号：
CA2980251
公开号：
CA2980251A1
申请日:
2016.03.18
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
This invention relates to atroipsomers of reduced tetraphenylporphyrin derivatives with halogen atoms (F, CI, Br) in the ortho positions of the phenyl groups, particularly halogenated tetraphenylchlorins and halogenated tetraphenylbacteriochlorins, which can be used in photodynamic therapy. According to the formulae of the invention, the ortho-phenyl substituents X1, X2, X3, X4, X5, X6, X7 and X8 may be identical or different and represent halogen atoms or hydrogen atoms, provided that at least all of X2, X4, X6 and X8 are halogens, and the meta-phenyl substituents R1, R2, R3 and R4 are independently chosen from -OH, -OR or -SO2R", where R" are each independently chosen from -CI, -OH, -aminoacid, -OR, -NHR, or -NR2, where R are alkyl of 1 to 12 carbon atoms or R2 represents cycloalkyl with 2 to 12 carbon atoms. The atropisomers of this invention have the majority of the substituents R1, R2, R3 and R4 on the same side of the plane defined by the macrocycle. The invention also relates to an anticancer and/or antimicrobial and/or antiviral pharmaceutical composition where atropisomers a4 and a3ß are the main active ingredients, such that the mixture of atropisomers a4 and a3ß constitutes more than 70% of the atropisomers present in the active ingredient and/or the atropisomer a4 constitutes more than 20% of the atropisomers present in the pharmaceutical composition.
