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PATENT APPLICATION PUBLICATION
INDIA
Date of filing of Application: 07/01/2005
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Application No.: 68/DEL NP/2005
Publication Date:09/06/2006
(54) Title of the Invention: “Produrg, Medicinal utilization thereof and process for producing the same.”
(51) International Classification : C07H 15/303
(31) Priority Document No. : 2002/180238
(32) Priority Date : 20/06/2002
(33) Name of priority country Japan
(86) International application No. : PCT/JP03/007868
Filing Date : 20/06/2003
(87) International Publication No. : WO/2004/000863
(61) Patent of Addition to
Application No.
: N.A.
(62) Divisional to Application No. : NIL
Filed On : N.A.
Total No. of pages : 58+07=65
(71) Name of Applicant :
NIPPON SUISAN KAISHA, LTD.
Address of the Applicant: 2-6-2, Ohtemachi,
Chiyoda-ku, , Tokyo 100-0004 (JP)
(72) Name of the Inventor:
YAMASHITA Shinya,
TAKEO Jiro,
OKITA Takaaki,
(57) Abstract: A prodrug utilizes an enzyme whose enzymatic activity is different in between the target site of the
drug and the site to express side effects, the prodrug having a substituent cleavable with the enzyme and being
activated by cleaving the substitutent with the enzyme. As the target site of the drug, for example, a respiratory organ
can be mentioned and as the site to express side effects, for example, the heart can be mentioned and as the
example of the enzyme, a glycosidase (for example,ß-glucuronidase) can be mentioned. Furthermore, the
substituent is, for example, a glycosy1 group composed of a monosaccharide or an oligosaccharide. Use of the
enzyme enables reducing the side effects of a drug of the type whose target site is different from the site to express
side effects.
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