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Last Updated: March 28, 2024

Claims for Patent: 9,226,912


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Summary for Patent: 9,226,912
Title:Acetyltanshinone IIA (ATA) as anticancer agent
Abstract: The present invention relates to the use of a compound of Formula I for the manufacture of a medicament for treating or preventing cancer in a subject. Formula I ##STR00001##
Inventor(s): Luo; Kathy Qian (Singapore, SG), Yu; Ting (Singapore, SG), Luo; Hou-Wei (Singapore, SG)
Assignee: Nanyang Technological University (Singapore, SG)
Application Number:14/009,431
Patent Claims:1. A method for inhibiting estrogen receptor signaling in a cell, comprising contacting said cell with an effective amount of a compound of Formula I ##STR00006##

2. The method of claim 1, wherein estrogen receptor signaling is inhibited by estrogen receptor protein degradation, reduced estrogen receptor mRNA levels and/or inhibition of estrogen receptor-responsive gene expression.

3. The method of claim 1, wherein HER2 expression is reduced in the cell after contacting said cell with an effective amount of a compound of Formula I ##STR00007##

4. The method of claim 3, wherein the cell is an estrogen receptor positive/HER2 positive (ER+/HER2+) breast cancer cell.

5. A method for inducing apoptosis in a cell, comprising contacting said cell with an effective amount of a compound of Formula I ##STR00008##

6. The method of claim 5, wherein apoptosis is induced by generation of reactive oxygen species.

7. A method for treating cancer selected from breast cancer, cervical cancer, lung cancer, liver cancer, colorectal adenocarcinoma, neuroblastoma, melanoma, and leukemia in a subject, comprising administering an effective amount of a compound of Formula I to a subject in need thereof ##STR00009##

8. The method of claim 7, wherein the cancer is estrogen receptor-positive (ER+) breast cancer.

9. The method of claim 7, wherein the cancer is HER2 positive (HER2+) breast cancer.

10. The method of claim 7, wherein the method further comprises administering a second anticancer agent to the subject.

11. The method of claim 10, wherein the second anticancer agent is administered before, together with or after the compound of Formula I.

12. The method of claim 10, wherein the second anticancer agent is selected from the group consisting of paclitaxel, doxorubicin, herceptin, lapatinib, gefitinib, erlotinib, tamoxifen, fulvestrant, anastrazole, lectrozole, exemestane, fadrozole and combinations thereof.

13. The method of claim 7, wherein the subject has prior to administration of the compound of Formula I underwent anticancer therapy with a different anticancer agent or anticancer agent combination.

14. The method of claim 7, wherein the subject has previously been treated with an anticancer agent selected from the group of selective estrogen receptor modulators, estrogen receptor down regulators, aromatase inhibitors, HER2 inhibitors, anthracyclines, and combinations thereof.

15. The method of claim 14, wherein the anticancer agent is selected from the group consisting of doxorubicine, paclitaxel, herceptin, lapatinib, gefitinib, erlotinib, tamoxifen, fulvestrant, anastrazole, lectrozole, exemestane, fadrozole and combinations thereof.

16. The method of claim 13, wherein the subject has failed the previous therapy.

17. The method of claim 13, wherein the subject has developed resistance to one or more of the previously used anticancer agents.

18. The method of claim 7, wherein the subject is a mammal.

19. The method of claim 7, wherein the subject is a human.

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