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-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R? is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R? is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, 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.

Abstract: Hypericin and helianthrone derivatives 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-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R? is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R? is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R? is not hydrogen when there is a C11-C12 bond and when there is a C11-C12 bond and both R? are hydroxy, both R? groups are not hydroxy.

Abstract: Novel antiviral (including antiretroviral) compounds are mono- or dicarboxylic acid esters of hypericin in which one or both of the methyl groups of hypericin are substituted by carboxylic acid ester groups of the formula COOR3 in which R3 is alkyl, the chain of which is optionally interrupted by one or more oxygen or sulphur atoms. R3 is preferably methyl, ethyl, propyl, butyl, 2-methoxyethyl or 2-(2-methoxyethoxy)ethyl. The compounds may be formulated into pharmaceutical compositions and may be used in any manner which has previously been known for hypericin.

Abstract: Hypericin, helianthrone and derivatives thereof of general formula (I) 1

Abstract: A method for treating cancer comprising administering a 1,3,4,6-tetrahydroxy-helianthrone derivative. The compounds can be used in the absence of light irradiation or for photodynamic therapy of solid tumors wherein the tumor site is subjected to light irradiation after administration of the active ingredient. A preferred compound is 10,13-dimethyl-1,3,4,6-tetrahydroxy-helianthrone.

Abstract: Disclosed herein are antiviral agents, pharmaceutical formulations comprising effective amounts of these agents and methods for treating mammals suffering from infections caused by viruses. The agents are analogs, isomers, homologs, derivatives and salts of aromatic polycyclic diones.

Abstract: Novel 3,7-disubstituted phenothiazinium salts are active in the photochemical disinfection of aqueous effluents. The novel salts are of the general formula ##STR1## wherein: either R.sub.1 is a saccharide residue;R.sub.2 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, any alkyl or alkylene chain being optionally interrupted by one or more heteroatoms, and Y is alkylene optionally substituted by alkyl, cycloalkyl, aryl or aralkyl; orR.sub.1 and R.sub.2 are each methyl and Y is a bond; and when R.sub.1 is a saccharide residue X is an anion selected from halogen, R.sub.3 CO.sub.2.sup.-, R.sub.3 SO.sub.3.sup.- and R.sub.3 OSO.sub.3.sup.-, wherein R.sub.3 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, andwhen R.sub.1 and R.sub.2 are each methyl, X is an anion selected from R.sub.3 SO.sub.3.sup.-, R.sub.3 OSO.sub.3.sup.- wherein R.sub.3 is as defined above and R.sub.4 CO.sub.2.sup.-, wherein R.sub.4 is an aldose or ketose residue, an N-protected .alpha.-amino acid residue or a .omega.-carboxy-.alpha.

Abstract: A process for preparing hypericin comprises oxidative dimerization of emodin anthrone and conversion of the intermediate protohypericin to hypericin by irradiation with visible light.

Abstract: A process for the production of 1.alpha.-hydroxy provitamin D.sub.3 which comprises treating 1.alpha., 2.alpha.-epoxy-cholesta-4,6-diene-3-one at a low temperature with liquid ammonia; with ammonium chloride and with lithium metal to produce 1.alpha.,3.beta.-dihydroxycholest-6-ene, converting this to the corresponding 1.alpha.,3.beta.-di(lower alkanoyl) derivative, reacting the latter with bromine to give 1.alpha.,3.beta.-di(lower alkanoyloxy) 6.beta.,7.alpha.-dibromocholestane, which is dehydrobrominated to give 1.alpha.,3.beta.-di(lower alkanoyloxy)-cholesta-5,7-diene, which is converted to the desired provitamin. The 1.alpha.,3.beta.-di(lower alkanoyloxy)cholest-6-ene can be oxidized to the corresponding 5-ene-7-one, which is converted to the 7-p-toluenesulfonyl hydrazone derivative, which is converted to the 1.alpha.-hydroxy provitamin D.sub.3 di(lower alkanoyloxy) derivative or to the 1.alpha.-hydroxy provitamin D.sub.3. Novel compounds are 1.alpha.,3.beta.

Abstract: Process for the production of hydroxylated derivatives of cholesterol and 7-dehydrocholesterol which comprises subjecting a saturated unsubstituted or substituted derivative of cholestane, dissolved in a suitable solvent, in the presence of peracetic acid, to irradiation with ultra-violet radiation of a wavelength below 350m.mu. , or heating in a suitable solvent, separating the reaction products, which if desired, are converted to other derivatives, and recovering the residue of the starting material. Novel derivatives are obtained and these are: 3.beta.-acetoxy,25-hydroxy,5.alpha.-cholestane; 3.beta.-acetoxy, 5.alpha.,25-dihydroxy cholestane; 3.beta.,5.alpha.,25-trihydroxy cholestane; 3-keto, 5.alpha.,25-dihydroxy cholestane; 3-keto,25-hydroxy-.DELTA..sup.4 -cholestane; 3.beta.,25-diacetoxy-5.alpha.-hydroxy-cholestane; 3.beta.-acetoxy, 25-trichloroacetoxy-5.alpha.-hydroxy-cholestane, 25-trichloroacetoxy-cholesterol and 25-acetoxy-cholesterol.