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ATROPISOMERS OF HALOGENATED TETRAPHENYLBACTERIOCHLORINS AND CHLORINS AND THEIR USE IN PHOTODYNAMIC THERAPY
专利权人:
发明人:
申请号:
HK18101274.5
公开号:
HK1241735A
申请日:
2018.01.26
申请国别(地区):
HK
年份:
2018
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 α4 and α3β are the main active ingredients, such that the mixture of atropisomers α4 and α3β constitutes more than 70% of the atropisomers present in the active ingredient and/or the atropisomer α4 constitutes more than 20% of the atropisomers present in the pharmaceutical composition.La présente invention concerne des atropisomères de dérivés tétraphénylporphyrine réduits ayant des atomes dhalogène (F, Cl, Br) en positions ortho des groupes phényle, en particulier des tétraphénylchlorines halogénées et des tétraphénylbactériochlorines halogénées, qui peuvent être utilisées en thérapie photodynamique. Selon les formules de linvention, les substituants ortho-phényle X1, X2, X3, X4, X5, X6, X7 et X8 peuvent être identiques ou différents et représentent des atomes dhalogène ou des atomes dhydrogène, à condition quau moins tous les X2, X4, X6 et X8 soient des atomes dhalogène, et les substitu
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