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Title:
NEW TYPE OF CYTIDINE DERIVATIVE DIMER AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/078399
Kind Code:
A1
Abstract:
Disclosed are a new type of cytidine derivative dimer, having the general formula (I), and an application thereof. By means of the optimized molecular design of a cytidine compound, the cytidine derivative dimer of the present invention has a significant inhibitory effect on human colon cancer HCT-116 tumor cells, while at the same time having a strong growth inhibitory effect on a transplanted human colon cancer HCT-116 tumor borne by nude mice; the new type of cytidine derivative dimer compound of the present invention has very high antitumor activity, while the toxicity of the compound is low.

Inventors:
YANG DARIA (CN)
WANG HAIDONG (CN)
WANG HUIJUAN (CN)
LIEW SIONG TERN (CN)
Application Number:
PCT/CN2015/081138
Publication Date:
May 26, 2016
Filing Date:
June 10, 2015
Export Citation:
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Assignee:
CHANGZHOU FANGYUAN PHARMACEUTICAL CO LTD (CN)
CHANGZHOU UPER BIOPHARMACEUTICAL CO LTD (CN)
International Classes:
C07H19/073; A61K31/7068; A61P35/00; A61P35/02; A61P35/04; C07H1/00
Domestic Patent References:
WO2014078295A12014-05-22
WO2004041203A22004-05-21
Other References:
KAZUHIKO KONDO ET AL.: "Studies on Biologically Active Nucleosides and Nucleotides. 5. Synthesis and Antitumor Activity of Some 2, 2'-Anhydro-1-(3', 5'-di-O-acyl- beta -D-arabinofuranosyl)cytosine Salts and 2, 2'-Anhydro-1-(3'-O-acyl- beta -D-arabinofuranosyl)cytosine 5'-Phosphates", JOURNAL OF MEDICINAL CHEMISTRY, vol. 22, no. 6, 1 June 1979 (1979-06-01), pages 639 - 646, XP000573809, DOI: doi:10.1021/jm00192a007
THEODOROS KARAMPELAS ET AL.: "GnRH-Gemcitabine Conjugates for the Treatment of Androgen-Independent Prostate Cancer: Pharmacokinetic Enhancements Combined with Targeted Drug Delivery", BIOCONJUGATE CHEMISTRY, vol. 25, no. 4, 24 March 2014 (2014-03-24), pages 813 - 823, XP055396050
See also references of EP 3216799A4
Attorney, Agent or Firm:
CHANGZHOU JIANGHAI YANGGUANG INTELLECTUAL PROPERTY AGENCY LTD. (CN)
常州市江海阳光知识产权代理有限公司 (CN)
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