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Last Updated: November 25, 2020

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Claims for Patent: 6,787,161

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Summary for Patent: 6,787,161
Title: Anti-cancer compounds
Abstract:This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Inventor(s): Aylward; James Harrison (Queensland, AU)
Assignee: Peplin Biotech Pty. Ltd. (Fortitude Valley, AU)
Application Number:09/888,178
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,787,161
Patent Claims: 1. A method of treating a subject with cancer, the method comprising administering to the subject in need thereof a therapeutically effective amount of at least one isolated compound selected from the group consisting of an angeloyl-substituted ingenane obtained from the sap of a Euphorbia species and an active derivative of an angeloyl-substituted ingenane obtainable from the sap of a Euphorbia species, wherein said active derivative exhibits the same anti-cancer activity as said angeloyl-substituted ingenane.

2. The method of claim 1, wherein the Euphorbia species is Euphorbia peplus.

3. The method of claim 1, wherein the Euphorbia species is Euphorbia drummondii.

4. The method of claim 1, wherein the Euphorbia species is Euphorbia hirta.

5. The method of claim 2, wherein the derivative of an angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus is an acetylated derivative.

6. The method of claim 3, wherein the derivative of an angeloyl-substituted ingenane obtained from the sap of Euphorbia drummondii is an acetylated derivative.

7. The method of claim 4, wherein the derivative of an angeloyl-substituted ingenane obtained from the sap of Euphorbia hirta is an acetylated derivative.

8. The method of any one of claims 1 to 4, wherein the at least one compound is selected from the group consisting of a 20-O-acetyl-ingenol-3-angelate and an ester derivative of a 20-O-acetyl-ingenol-3-angelate.

9. The method of any one of claims 1 to 4, wherein the compound comprises a pharmaceutically acceptable salt of the 20-O-acetyl-ingenol-3-angelate and the 20-O-acetyl-ingenol-3-angelate ester derivative.

10. The method of any one of claims 1 to 4, wherein the compound is obtained by the process of extracting said sap with 95% v/v ethanol, discarding a solid fraction and retaining a soluble fraction.

11. The method of any one of claims 1 to 4, wherein the cancer is a solid tumor.

12. The method of any one of claims 1 to 4, wherein the cancer is colon cancer.

13. The method of any one of claims 1 to 4, wherein the cancer is lung cancer.

14. The method of any one of claims 1 to 4, wherein the cancer is prostate cancer.

15. The method of any one of claims 1 to 4, wherein the cancer is cervical cancer.

16. The method of any one of claims 1 to 4, wherein the cancer is breast cancer.

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