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Title:
SULPHONATED DEHYDROGENATED SYLVATE, THE PREPARATION AND USE
Document Type and Number:
WIPO Patent Application WO/2003/093225
Kind Code:
A1
Abstract:
This invention relates to sulphonated dehydrogenated sylvate, a kind of new salt useful in treating digestive canal ulcer, acute & chronic gastritis and erosive gastritis etc., as well as its preparation and use. Said compound can be represented by formula (1), in which R is Bi (OH)++, Zn++, 2BiO or 1/2Zn H. Its preparation comprises: (a) sequentially treating the industrically calcinated calcium sylvate with acid, base and extracting with organic solvent to give sylvic acid with less isomer; (b) reacting said sylvic acid with Pd/C to provide dehydrogenated sylvic acid, then converting it to pure sulphonated product, i.e. sulphonated dehydrogenated sylvic acid via sulphonation and recrystallization; (c) by use of neutralization or salt displacement reaction to convert the sulphonated product of step (b) to monozinc or bismuth salt of sulphonated dehydrogenated sylvic acid. The resultant salt can be used to prepare medicine of treating digestive canal ulcer and gastritis.

Inventors:
ZHENG LIANGYUAN (CN)
ZHANG SHIWEI (CN)
ZHENG LI (CN)
WANG MINGXIN (CN)
ZHAO YONGLI (CN)
LU XUEZHAO DI
Application Number:
PCT/CN2002/000387
Publication Date:
November 13, 2003
Filing Date:
June 04, 2002
Export Citation:
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Assignee:
SHANGHAI XINGKANG PHARMACEUTIC (CN)
NAT INST OF PHARMACEUTICAL RES (CN)
ZHENG LIANGYUAN (CN)
ZHANG SHIWEI (CN)
ZHENG LI (CN)
WANG MINGXIN (CN)
ZHAO YONGLI (CN)
International Classes:
A61P1/04; C07C309/58; (IPC1-7): C07C309/57; C07C303/02; C07C303/06; A61K31/255; A61P1/04
Domestic Patent References:
WO2001034143A12001-05-17
Foreign References:
US4529602A1985-07-16
CN1159323A1997-09-17
Other References:
DATABASE CA [online] WADA HIROSHI ET AL.: "Antiulcer activity of dehydroabietic acid derivatives", accession no. STN Database accession no. 103:47835
DATABASE CA [online] ITO YUTAKA ET AL.: "Effects of the new antiulcer drug ecabet sodium (TA-2711) on pepsin activity. I. Inactivation of enzyme protein", accession no. STN Database accession no. 119:131272
DATABASE CA [online] ITO YUTAKA ET AL.: "Metabolic fate of a new antiulcer drug (+)-(1R,4aS, 10aR)-1,2,3,4,4a,9,10,10a-octahydro-1,4a-dimethyl-7-(1-methylethyl)-6-sulfo-1-phenanthrenecarboxylic acid 6-sodium salt pentahydrate(TA-2711). I. Disposition, metabolism and protein binding in rats, dogs", accession no. STN Database accession no. 116:33863
DATABASE CA [online] ONODA Y. ET AL.: "Effects of the new antiulcer agent 12-sulfodehydroabietic acid monosodium salt on duodenal alkaline secretion in rats", accession no. STN Database accession no. 113:109064
Attorney, Agent or Firm:
CHINA SCIENCE PATENT & TRADEMARK AGENT LTD (Bldg. B Tsinghua Tongfang Hi-Tech Plaza, No. 1, Wangzhuang Rd, Haidian District Beijing 3, CN)
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