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Title:
5-CARBAMOYLTHIENO(23-B)THIOPHENE-2-SULFONAMIDE AS TOPICALLY ACTIVE CARBONIC ANHYDRASE INHIBITOR
Document Type and Number:
Japanese Patent JPH02264779
Kind Code:
A
Abstract:

NEW MATERIAL: Compounds of formula I {wherein R1, R2 are H, a 1-6C alkyl [substituted with amino, a 1-6C alkylamino, (a 1-6C alkoxy-2-4C alkyl)amino, OH, a 1-3C alkylthio, a 1-3C alkylsulfonyl, morpholino, thiomorpholino, thiomorpholino-S-oxide, etc.]} or salts which can be used ophthalmologically or medicically.

EXAMPLE: 5-[N-(2,2,-Dimethylaminoethyl)carbamoyl]thieno[2,3-b]thiophene-2- sulfonamide.

USE: Drug. Carbonic anhydrase inhibitor for treatment of glaucoma and elevated intraocular pressure.

PROCESS: A compound of formula II is reacted with chlorosulfonic acid in the presence of PCl3 to prepare a compound of formula III, which is reacted with ammonium hydroxide to make a compound of formula IV. Next the compound is reacted with an amine in an alcohol solvent to obtain a compound of formula I.


Inventors:
JIYOOJI DEE HAATOMAN
JIYON DEE PURUU
Application Number:
JP2731090A
Publication Date:
October 29, 1990
Filing Date:
February 08, 1990
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
C12N9/99; A61K31/38; A61K31/535; A61K31/54; A61P27/02; A61P27/06; A61P43/00; C07D495/04; (IPC1-7): C07D495/04; A61K31/38; A61K31/535; A61K31/54; C12N9/99
Attorney, Agent or Firm:
Masao Okabe (5 others)