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Title:
EYE SELECTIVE BETA BLOCKER AS ANTI-GLAUCOMA AGENT
Document Type and Number:
Japanese Patent JPH02243664
Kind Code:
A
Abstract:

NEW MATERIAL: A compd. represented by formula I [wherein R is H, an alkyl, a cycloalkyl, amino or a lower alkoxy, R1 is a lower alkyl, amino, cyclohexyl, phenyl, benzyl, morpholino or tetrahydrofuranyl, R2 is H or COR3 (R3 is a lower alkyl) but, when R1 is a lower alkyl or a cycloalkyl, R2 is not H] or its salt.

EXAMPLE: A compd. represented by formula II.

USE: A medicine. An eye selective beta blocker as an anti-glaucoma agent. This medicine is stably held when locally adapted to an eye and rapidly metabolized when absorbed during the circulation throughout the whole body and used in the treatment of glaucoma or the lowering of intraocular pressure.

PROCESS: For example, a compd. represented by formula III (Bz is benzyl) and a compd. represented by formula IV are reacted in the presence of pyridine to form a compd. represented by formula V, and this compd. is reacted with pivalic anhydride to obtain a compd. represented by formula VI and this compd. is hydrogenated in the presence of a Pd/C catalyst to obtain a compd. represented by formula II.


Inventors:
GAANSHIYAIAMU PATEIRU
UIRIAMU ERU MATEIA
KUUON EICHI ETSUKUSU MAI
Application Number:
JP32420489A
Publication Date:
September 27, 1990
Filing Date:
December 15, 1989
Export Citation:
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Assignee:
DU PONT
International Classes:
A61K31/16; A61K31/245; A61K31/34; A61K31/341; A61K31/35; A61K31/351; A61K31/535; A61K31/5375; A61P25/02; A61P27/02; A61K31/24; A61P27/06; C07C233/36; C07C233/37; C07C233/40; C07C233/62; C07C233/78; C07C235/50; C07C235/60; C07D295/18; C07D295/205; C07D295/215; C07D307/24; C07D307/68; C07D309/06; C07D309/08; (IPC1-7): A61K31/24; A61K31/245; A61K31/34; A61K31/35; A61K31/535; C07C233/36; C07D295/18; C07D307/24; C07D307/68; C07D309/08
Attorney, Agent or Firm:
Chika Takagi (2 outside)