Helianthrone derivatives as anti-cancer agents

Details Helianthrone derivatives as anti-cancer agents Helianthrone derivatives as anti-cancer agents

2005-03-15

2005-03-15

Pryor, Alton N. (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

C514S680000

Reexamination Certificate

active

06867235

ABSTRACT:
Hypericin, helianthrone and derivatives thereof of general formula (I)wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10alkoxy, NH—C1-C10alkyl, and NH-hydroxy(C1-C10)alkyl; R′ is independently selected from the group consisting of hydroxy and C1-C10alkoxy; R″ is independently selected from the group consisting of hydrogen, hydroxy, C1-C10alkoxy, NH—C1-C10alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5and R6are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10alkyl, C1-C10alkoxy, and C1-C10alkoxycarbonyl, provided that R″ is not hydrogen when there is a C11-C12 bond, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrones of formula (I) can be used for the treatment of tumors in the absence of light irradiation. New compounds include those of formula I which are other than hypericin and known hypericin derivatives and there is either a C11-C12 bond or at least one R″ is other than hydrogen.

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