Title:
PRODURG, MEDICINAL UTILIZATION THEREOF AND PROCESS FOR PRODUCING THE SAME
Document Type and Number:
WIPO Patent Application WO/2004/000863
Kind Code:
A1
Abstract:
A prodrug with the use of an enzyme showing different enzymatic activities between a drug target site and a site where its side effect is expressed, which has a substituent cleavable with the enzyme and is activated due by cleaving the substituent. As an example of the drug target site, a respiratory organ may be cited, while the heart may be sited as an example of the side effect expression site. As an example of the drug, a bronchodilator may be cited while a glicosidase (for example, β-glucuronidase) may be cited as an example of the enzyme. As an example of the substituent, a glycosyl group comprising a monosaccharide or an oligosaccharide may be cited. Use of the above enzyme makes it possible to lessen the side effect of a drug having a target site for exerting its effect which is different from a site where its side effect is expressed.
Inventors:
YAMASHITA SHINYA (JP)
TAKEO JIRO (JP)
OKITA TAKAAKI (JP)
TAKEO JIRO (JP)
OKITA TAKAAKI (JP)
Application Number:
PCT/JP2003/007868
Publication Date:
December 31, 2003
Filing Date:
June 20, 2003
Export Citation:
Assignee:
NIPPON SUISAN KAISHA LTD (JP)
YAMASHITA SHINYA (JP)
TAKEO JIRO (JP)
OKITA TAKAAKI (JP)
YAMASHITA SHINYA (JP)
TAKEO JIRO (JP)
OKITA TAKAAKI (JP)
International Classes:
A61P11/00; A61P11/06; A61P11/08; A61P43/00; C07H15/18; C07H15/203; (IPC1-7): C07H15/203; A61K31/7028; A61P11/00; A61P11/06; A61P11/08; A61P43/00; C07H15/18
Domestic Patent References:
| WO1997039007A1 | 1997-10-23 | |||
| WO1997044000A2 | 1997-11-27 | |||
| WO2001027132A1 | 2001-04-19 |
Foreign References:
| JPH06293665A | 1994-10-21 | |||
| JPH101495A | 1998-01-06 | |||
| EP0642799A1 | 1995-03-15 | |||
| GB2255503A | 1992-11-11 | |||
| EP0648503A1 | 1995-04-19 | |||
| JPH09202796A | 1997-08-05 | |||
| EP0940143A2 | 1999-09-08 |
Other References:
HARDMAN J.G. ET AL., 1996, GOODMAN & GILMAN'S, ISBN: 0-07-026266-7, article "The pharmacological basis of therapeutics", pages: 212 - 217, XP002971022
JOHNSON W.G. ET AL.: "Variation in ten lysosomal hydrolase enzyme activities in inbred mouse strains", BIOMED. GENET., vol. 24, no. 11/12, 1986, pages 891 - 909, XP002971023
WILLIAMS F.M. ET AL.: "The influence of the route of administration on urinary metabolites of isoetharine", XENOBIOTICA, vol. 4, no. 6, 1974, pages 345 - 353, XP002971024
MANCHEE G.R. ET AL.: "Disposition of salmeterol xinafoate in laboratory animals and humans", DRUG METAB., vol. 21, no. 6, 1993, pages 1022 - 1028, XP002971025
CLARK W. G. ET AL.: "Purification and properties of L-epinephrine glucuronide", ARZNEIM.-FORSCH (DRUG RES.), vol. 24, no. 11, 1974, pages 1769 - 1772, XP002971026
POOK K.-H. ET AL.: "Mass spectral analysis of glucuronides from sympathomimetic hydroxyphenylalkylaminoethanols", J. PHARM. SCI., vol. 65, no. 10, 1976, pages 1513 - 1518, XP002971027
D'ALONZO G.E. ET AL.: "Bambuterol in the treatment of Asthma", CHEST, vol. 107, no. 2, 1995, pages 406 - 412, XP002971028
JOHNSON W.G. ET AL.: "Variation in ten lysosomal hydrolase enzyme activities in inbred mouse strains", BIOMED. GENET., vol. 24, no. 11/12, 1986, pages 891 - 909, XP002971023
WILLIAMS F.M. ET AL.: "The influence of the route of administration on urinary metabolites of isoetharine", XENOBIOTICA, vol. 4, no. 6, 1974, pages 345 - 353, XP002971024
MANCHEE G.R. ET AL.: "Disposition of salmeterol xinafoate in laboratory animals and humans", DRUG METAB., vol. 21, no. 6, 1993, pages 1022 - 1028, XP002971025
CLARK W. G. ET AL.: "Purification and properties of L-epinephrine glucuronide", ARZNEIM.-FORSCH (DRUG RES.), vol. 24, no. 11, 1974, pages 1769 - 1772, XP002971026
POOK K.-H. ET AL.: "Mass spectral analysis of glucuronides from sympathomimetic hydroxyphenylalkylaminoethanols", J. PHARM. SCI., vol. 65, no. 10, 1976, pages 1513 - 1518, XP002971027
D'ALONZO G.E. ET AL.: "Bambuterol in the treatment of Asthma", CHEST, vol. 107, no. 2, 1995, pages 406 - 412, XP002971028
Attorney, Agent or Firm:
Shamoto, Ichio (Section 206 New Ohtemachi Bldg., 2-1,
Ohtemachi 2-chom, Chiyoda-ku Tokyo, JP)
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