Use of extracts from aristolochia in the treatment of aids
OwnerHans Achenbach, Carlos Navarro +1inventors
InventorsHans Achenbach, Carlos Navarro, Alejandro Navarro
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Abstract
This invention relates to the use of extracts and compounds derived from the plant Aristolochia taliscana and their analogues in the treatment of AIDS.
Claims38
The use of an extract from an Aristolochia species or one or more compounds isolable therefrom, for the manufacture of a medicament for the treatment of AIDS.
The use of an extract from an Aristolochia species or one or more compounds isolable therefrom for the manufacture of a medicament for preventing or reversing cachexia in AIDS patients.
The use according to any one of the preceding claims wherein the composition contains Licarin-A.
The use according to any one of the preceding claims wherein the composition contains a cytotoxic tetralone compound.
The use according to any one of the preceding claims wherein the composition contains a 2-hydroxy-1-tetralone compound.
The use according to any one of the preceding claims wherein the composition contains at least 25% by weight of a phenolic eupomatenoid compound (such as eupomatenoid-7), at least 8% of Licarin-A and at least 8% of a non-phenolic eupomatenoid compound (such as eupomatenoid-8).
The use according to any one of the preceding claims wherein the composition contains an aristolactam.
The use according to any one of the preceding claims wherein the extract has been prepared by extraction of plant material from the Aristolochia species with an organic solvent.
The use according to claim 15 wherein the organic solvent is an alcoholic solvent such as ethanol or methanol or a mixture thereof.
A method of treating Acquired Immune Deficiency Syndrome (AIDS) in a patient suffering from AIDS, which method comprises administering to the patient an effective treatment amount of an extract from an Aristolochia species or one or more anti-AIDS active compounds isolable therefrom, as defined in any one of the preceding claims.
The use of a compound for the manufacture of a medicament for use in the treatment or alleviation of AIDS or the symptoms thereof, or the alleviation or reversal of cachexia, the compound being of the formula (I):
- 13
- wherein the dotted line signifies a single or double bond;
- n is 0, 1, 2 or 3;
- A is a monocyclic aryl ring optionally substituted by one or more substituent groups which may be the same or different and are selected from R3O, R3, R3S, halogen;
- aryl and heteroaryl, wherein R3 is hydrogen, or a hydrocarbyl group optionally substituted by a hydroxy or hydrocarbyloxy group;
- B is selected from carboxy, carboxaldehyde, hydrocarbyl and hydrocarbyloxy groups wherein the hydrocarbyl group is acyclic or cyclic, and optionally contains one or more heteroatoms, and is optionally substituted by one or more hydroxy, alkoxy, alkenyloxy, alkynyloxy, aryloxy, aldehyde, alkanoyl, acetal, hemiacetal and carboxy groups;
- R1 is hydrogen or a hydrocarbyl group optionally including one or more heteroatoms and optionally substituted by one or more substituents selected from hydroxy, hydrocarbyloxy and aryl groups;
- and R2 is hydroxy or a hydrocarbyl or hydrocarbyloxy group optionally substituted by one or more substituents selected from hydroxy, hydrocarbyloxy and aryl groups.
The use according to any one of claims 21 to 31 wherein R4 and R5 are selected from hydrogen, or C1-6 alkyl, or R4 and R5 together define an alkylene group such as —CH2—.
A compound of the formula (I) or (II) as defined in any one of the preceding claims for use in the treatment or alleviation of AIDS or the symptoms thereof, or the alleviation or reversal of cachexia;
- but provided that when R1 is 3-methyl, R2 is a single methoxy group at the 7-position, and either (i) the furan ring is unsaturated and is substituted at the 2-position with a 4-hydroxy-3-methoxyphenyl group or a 3,4-methylenedioxyphenyl group;
- or (ii) the furan ring is a 2,3-dihydrofuran ring and is substituted at the 2-position with a 4-hydroxy-3-methoxyphenyl group, then B is other than a prop-1-enyl group attached to the 5-position of the benzfuran ring.
A use, or a method of treatment as defined in any one of the preceding claims, wherein the compound is selected from the group consisting of:
- (±)-5-(1-Hydroxyallyl)-2-(4-hydroxy-3-methoxyphenyl)-7-methoxy-3-methylbenzofuran;
- 2-(4-Hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-5-(E)-propenylbenzofuran;
- 2-(4-Hydroxy-3-methoxyphenyl)-7-methoxy-3-methyl-5-[(E)-3-oxopropenyl]benzofuran;
- 5-Formyl-3-(4-hydroxy-3-methoxyphenyl)-7-methoxy-3-methylbenzofuran;
- 2-(4-Hydroxy-2-methoxyphenyl)-5-[(E)-3-hydroxypropenyl]-7-methoxy-3-methylbenzofuran;
- 2-(3,4-Dihydroxyphenyl)-7-methoxy-3-methyl-5-(E)-propenylbenzofuran;
- erythro-5-(1,2-Dihydroxypropyl)-2-(4-hydroxy-3-methoxyphenyl)-7-methoxy-3-methylbenzofuran;
- (2R,3R)-2,3-Dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-5-(E)-propenylbenzofuran;
- erythro-1-(4-Acetoxy-3-methoxyphenyl)-2-[4-(7-methoxy-3-methyl-5-(E)-propenylbenzofuran-2-yl)-2-methoxyphenoxy]propylacetate;
- threo-1-(4Acetoxy-3-methoxyphenyl)-2-[4-(7-methoxy-3-methyl-5-(E)-propenylbenzofuran-2-yl)-2-methoxyphenoxy]propyl-acetate;
- threo-1-[2-(4-Hydroxy-3-methoxyphenyl)-7-methoxy-3-methylbenzofuran-5-yl]-2-[4-(3-methyl-5-(e)-propenylbenzofuran-2-yl)-2-methoxyphenoxy]propan-1-ol;
- 2-Methoxy-4-[7-methoxy-3-methyl-5-(E)-propenylbenzofuran-2-yl]-6-[4-(7-methoxy-3-methyl-5-(E)-propenylbenzofuran-2-yl)-2-methoxyphenoxy]phenol;
- 8.2′, 9.3′-Tetrahydro-bis-eupomatenoid-7;
- 15-(Aristolactam-1-9-yl)-eupomatenoid-7;
- 14-O-α-Cadinyl-eupomatenoid-7;
- and
- (2R,4S)-2-Hydroxy-6-methoxy-4,7-dimethyl-1-tetralone.
Dependencies are inferred from the claim text.