Carotene analog of porhyrins, chlorins and bacteriochlorins as therapeutic and diagnostic agents

Carotenanaloga von porphyrinen, cholrinen und bacteriochlorinen als therapeutische und diagnostische mittel

Carotenes analogues de porphyrines, chlorures et bacteriochlorures comme agents therapeutiques ou diagnostiques

Abstract

La présente invention concerne un conjugué de carotène de formule (I) dans laquelle R1 est hydrogène ou méthyle; R2 est formule (a); R?3, R4 et R5¿ sont chacun hydrogène, méthyle ou éthyle; R6 et R7 sont chacun -R?13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, ou (CH¿2?)R?14; R8 est -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, ou (CH¿2)R?14 ou, pris avec R10, est =O; R?9 est -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, ou (CH¿2)R?14 ou, pris avec R10, est une liaison chimique; R?10 est -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, ou (CH¿2)R?14 ou, pris ensemble avec R9, est une liaison chimique ou, pris avec R8, est =O, R?11 est R13¿, ou -OR13; R12 est C(R13)2C(Y)-, -C(O)O(O)C-, -C(NR13)O(O)C-, or C(O)N(R15)-C(O)-; R13 est, indépendamment et dans chaque cas, hydrogène ou alkyle inférieur de 1 à environ 10 atomes de carbone; R14 est un résidu d'acide aminé, R?15 est R13, -R14¿, ou C(O)NHR13; R16 est, indépendamment et dans chaque cas, hydrogène ou alkyle inférieur de 1 à environ 4 atomes de carbone et Y est =O, =S, ou 2H-.
A carotene conjugate of formula (I), where R1 is hydrogen or methyl; R2 is formula (a); R?3, R4 and R5¿ are independently, hydrogen, methyl or ethyl; R?6 and R7¿ are independently -R?13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, or -(CH¿2?)R?14; R8 is -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, or -(CH¿2)R?14 or taken with R10 is =O; R?9 is -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, or -(CH¿2)R?14 or taken with R10 is a chemical bond; R?10 is -R13, -OR13, -C(R16¿)(O), -C(R16)2OR13, -CH=CHR13, or -(CH¿2)R?14 or taken together with R9 is a chemical bond or taken with R8 is =O; R?11 is R13¿, or -OR13; R12 is -C(R13)2C(Y)-, -C(O)O(O)C-, -C(NR13)O(O)C-, or -C(O)N(R15)-C(O)-; R13 is, independently at each occurrence, hydrogen or lower alkyl of from 1 through about 10 carbon atoms; R14 is an amino acid residue, R?15 is -R13, -R14¿, or -C(O)NHR13; R16 is, independently at each occurrence, hydrogen or lower alkyl of 1 to about 4 carbon atoms and Y is =O, =S, or 2H-.

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