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Title:
ALOE-EMODIN DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF CANCER
Document Type and Number:
WIPO Patent Application WO/2011/089602
Kind Code:
A3
Abstract:
The present invention relates to anthracycline derivatives that are based on an Aloe-emodin (AE) backbone attached to a glycoside (an amino sugar or amino carba-sugar). These derivatives are useful as chemotherapeutic agents. Advantageously, these derivatives are potent cytotoxic agents against a variety of anthracycline-resistant tumors. In addition, they may have reduced cardiotoxicity. As such, the novel compounds of the invention offer an advantage over currently available drugs. The present invention further relates to methods for preparing the novel Aloe-Emodin Glycoside (AEG) based derivatives, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.

Inventors:
FRIDMAN, Micha (12a Witsman Street, Kiryat Bialik, 27000, IL)
FLESCHER, Eliezer (6 Hageula Street, Hod Hasharon, 45272, IL)
BRINER-GOLDSTEIN, Elinor (39 Remez Street, Ness-Ziona, 74098, IL)
EVRON, Zoharia (40 Mashabim Street, Hod Hasharon, 45201, IL)
FRENKEL, Michael (26 Elisha Street, Pardes-Hanna, 37045, IL)
Application Number:
IL2011/000067
Publication Date:
December 29, 2011
Filing Date:
January 20, 2011
Export Citation:
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Assignee:
RAMOT AT TEL-AVIV UNIVERSITY LTD. (P.O. Box, 61392 Tel Aviv, 39296, IL)
FRIDMAN, Micha (12a Witsman Street, Kiryat Bialik, 27000, IL)
FLESCHER, Eliezer (6 Hageula Street, Hod Hasharon, 45272, IL)
BRINER-GOLDSTEIN, Elinor (39 Remez Street, Ness-Ziona, 74098, IL)
EVRON, Zoharia (40 Mashabim Street, Hod Hasharon, 45201, IL)
FRENKEL, Michael (26 Elisha Street, Pardes-Hanna, 37045, IL)
International Classes:
C07H15/244; A61K31/704; A61P35/00
Domestic Patent References:
WO2002090313A12002-11-14
Other References:
ABRAMSON H N ET AL: "SYNTHESIS OF ANTHRAQUINONYLGLUCOSAMINOSIDES AND STUDIES ON THE INFLUENCE OF AGLYCONE HYDROXYL SUBSTITUTION ON SUPEROXIDE GENERATION DNA BINDING AND ANTIMICROBIAL PROPERTIES", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 29, no. 9, 1 September 1986 (1986-09-01), pages 1709-1714, XP002560784, ISSN: 0022-2623, DOI: DOI:10.1021/JM00159A024
Attorney, Agent or Firm:
WEBB, Cynthia et al. (Webb & Co, P.O. Box 2189, Rehovot, 76121, IL)
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