Title:
TRIACETYL-3-HYDROXYPHENYLADENOSINE AND ITS USE FOR REGULATING BLOOD FAT
Document Type and Number:
WIPO Patent Application WO/2010/040286
Kind Code:
A1
Abstract:
The invention discloses triacetyl-3-hydroxyphenyladenosine represented by formula (I), the preparation, the pharmaceutical composition and the use thereof. Specially, the invention discloses a new compound of 2’,3’,5’-tri-O-acetyl-N6-(3-hydroxyphenyl)adenosine. Using hypoxanthine nucleoside as starting material, the compound is prepared by acetylating with acetic anhydride, chlorinating with thionyl chloride, and being substituted with 3-hydroxy aniline. The invention also discloses the pharmaceutical composition comprising triacetyl-3-hydroxyphenyladenosine. The dosage forms of the said pharmaceutical composition include tablet, capsule, pill, injection, sustained release preparation, controlled release preparation or particulate delivery system. The medicament for treatment or precaution of hyperlipemia prepared by the compound of the invention has the advantages of significant hypolipidemic activity, less toxicity and adverse effect as well as slow metabolism in vivo.
Inventors:
ZHU HAIBO (CN)
WU SONG (CN)
HAO LINGHUA (CN)
QU KAI (CN)
ZHU PING (CN)
WANG XING (CN)
LI WEI (CN)
WU SONG (CN)
HAO LINGHUA (CN)
QU KAI (CN)
ZHU PING (CN)
WANG XING (CN)
LI WEI (CN)
Application Number:
PCT/CN2009/070725
Publication Date:
April 15, 2010
Filing Date:
March 10, 2009
Export Citation:
Assignee:
INST OF MATARIA MEDICA CHINESE (CN)
ZHU HAIBO (CN)
WU SONG (CN)
HAO LINGHUA (CN)
QU KAI (CN)
ZHU PING (CN)
WANG XING (CN)
LI WEI (CN)
ZHU HAIBO (CN)
WU SONG (CN)
HAO LINGHUA (CN)
QU KAI (CN)
ZHU PING (CN)
WANG XING (CN)
LI WEI (CN)
International Classes:
C07H19/16; A61K31/7076; A61P3/06
Foreign References:
| US20070087994A1 | 2007-04-19 | |||
| US20060276428A1 | 2006-12-07 | |||
| CN1616459A | 2005-05-18 |
Other References:
BEUKERS, MARGOT W ET AL.: "N6-Cyclopentyl-2- (3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a Very Selective Agonist with High Affinity for the Human Adenosine A1 Receptor", JOURNAL OF MEDICINAL CHEMISTRY, vol. 46, no. 8, 2003, pages 1492 - 1503, XP002479003
MATSUDA A. ET AL.: "Mutagenicity of (p-nitrophenyl)adenines in Salmonella typhimurium", MUTATION RESEARCH LETTERS, vol. 263, no. 2, 1991, pages 93 - 100, XP002931736
See also references of EP 2407474A4
MATSUDA A. ET AL.: "Mutagenicity of (p-nitrophenyl)adenines in Salmonella typhimurium", MUTATION RESEARCH LETTERS, vol. 263, no. 2, 1991, pages 93 - 100, XP002931736
See also references of EP 2407474A4
Attorney, Agent or Firm:
BEIJING SAN GAO YONG XIN INTELLECTUAL PROPERTY AGENCY CO.,LTD. (He Jing Yuan Ji Men Li, Xueyuan Road, Haidian District, Beijing 8, CN)
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