IP Library Granted Patent US 9,216,977
Granted Patent B2
US 9,216,977 · App. 13/503,113 · Granted Dec 22, 2015

Antofine and cryptopleurine derivatives as anticancer agents

Inventors: Kuo-Hsiung Lee (Chapel Hill, NC); Xiaoming Yang (Chapel Hill, NC); Qian Shi (Chapel Hill, NC); Kenneth F. Bastow (Chapel Hill, NC); Che-Ming Teng (Taipei, TW); Tse-Ming Hong (Taipei, TW); Pan-Chyr Yang (Taipei, TW); Shuenn-Chen Yang (Taipei, TW)
Assignees: The University of North Carolina at Chapel Hill; National Taiwan University
C07D471/04C07D491/04
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Quick Facts
Patent No.
US 9,216,977
App. No.
13/503,113
Granted
Dec 22, 2015
Kind
B2
Abstract

The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.

Claims (20)

1. A compound having a structure according to Formula IV:

wherein:

n is 1 or 2;

m is 1;

each R is hydroxyl;

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from the group consisting of H and alkoxy;

subject to the proviso that at least one of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 is an alkoxy;

R 18 is selected from the group consisting of H, hydroxyl, alkoxy, alkylthio, loweralkyl, loweralkenyl, loweralkynyl, alkoyl, loweralkoyl, loweralkenoyl and amino;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein R 18 is H.

3. The compound of claim 2 , selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

4. A method of treating a cancer, comprising administering to a human or animal subject in need thereof a treatment effective amount of a compound of claim 3 , or a pharmaceutically acceptable salt thereof, wherein said cancer is selected from the group consisting of breast cancer and lung cancer.

5. A composition comprising a compound of claim 3 in a pharmaceutically acceptable carrier.

6. A composition comprising a compound of claim 1 in a pharmaceutically acceptable carrier.

7. A method of treating a cancer, comprising administering to a human or animal subject in need thereof a treatment effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein said cancer is selected from the group consisting of skin cancer, lung cancer, testicular cancer, lymphoma, leukemia, Kaposi's sarcoma, esophageal cancer, stomach cancer, colon cancer, breast cancer, endometrial cancer, ovarian cancer, liver cancer and prostate cancer.

8. The method of claim 7 , wherein said cancer is breast cancer.

9. The method of claim 7 , wherein said cancer is lung cancer.

10. The method of claim 7 , wherein said cancer comprises multi-drug resistant cancer.

11. The method of claim 7 , wherein said cancer comprises etoposide resistant cancer.

Assignments (3)
CONFIRMATORY LICENSE Recorded Jan 27, 2020
From: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
To: NIH-DEITR
Reel/Frame 051708/0791 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2015
From: TENG, CHE-MING; HONG, TSE-MING; YANG, PAN-CHYR; YANG, SHUENN-CHEN
To: NATIONAL TAIWAN UNIVERSITY
Reel/Frame 035177/0652 →
CONFIRMATORY LICENSE Recorded Dec 5, 2012
From: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 029407/0658 →
Continuity (2)
Provisional Application 61253966 · Oct 22, 2009
Related Publication 20120283220A1 · Nov 8, 2012