Title:
PRODRUG OF INHIBITOR AGAINST CARBONIC ACID DEHYDRATING ENZYME
Document Type and Number:
Japanese Patent JPH03130220
Kind Code:
A
Abstract:
NEW MATERIAL: This compound is shown by formula I to formula III [Z is a water-soluble carrier; A is a group capable of maintaining carbonic anhydrase inhibiting activity and forming a bond enzymatically cleavable bond with Z when added to (a) 2-benzothiazosulfonamide, (b) hydroxy methazolamide or (c) dichlorphenamide]. EXAMPLE: 6-[β-(Glucopyranosyl)oxyethoxy-2-benzothiazolesulfonamide. USE: A prodrug for carbonic anhydrase inhibitor(CAI) useful for locally treating glaucoma, increased water solubility of CAI without exerting bad influence on CAI activity. PROCESS: Especially a water-soluble carrier containing the whole OHs protected except a reaction site with A is reacted with a CAI analog of the substance (a) to (c) under a proper reaction condition and the Z protecting group is removed to give compounds of formula I to formula III.
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Inventors:
RONARUDO DEII SHIEENBUARUTO
CHIYAARUZU EFU BARUFUKUNEHITO
CHIYAARUZU EFU BARUFUKUNEHITO
Application Number:
JP25045990A
Publication Date:
June 04, 1991
Filing Date:
September 21, 1990
Export Citation:
Assignee:
UNIV IOWA RES FOUND
International Classes:
C12N9/99; A61K31/18; A61K31/41; A61K31/425; A61K31/428; A61K31/433; A61K31/70; A61K31/7028; A61P27/02; A61P27/06; A61P43/00; C07D277/80; C07D285/135; C07H15/18; C07H15/203; C07H15/26; C07H17/00; (IPC1-7): A61K31/18; A61K31/41; A61K31/425; A61K31/70; C07D277/80; C07D285/135; C07H15/26; C12N9/99
Attorney, Agent or Firm:
Shoichi Takezawa (1 person outside)