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Title:
SUBSTITUTED PYRIMIDINONE AS ANGIOTENSIN II ANTAGONIST
Document Type and Number:
Japanese Patent JPH03197466
Kind Code:
A
Abstract:

NEW MATERIAL: A compound of general formula I {J and K are each C(=M), CR7 [M is O or NR21 (R21 is aryl, alkyl or the like)], but only one of them is C(=M); R1 is CO2R4, SO3R5, CN [R4 is H, alkyl; R5 is H, general formula II (R4a is alkyl or the like)] or the like; R2a and R2b are H, halogen, NO2, alkyl or the like; R3a, is H, halo, alkyl or the like; R3b is H, halo, alkoxy or the like, R6 is aryl, alkyl or the like; R7 and R8 are H, alkyl, OH, SH or the like; E is single bond, O, CO or the like; X is single bond, CO, O, S or the like; r is 1, 2}, and the salt thereof.

EXAMPLE: 2-n-Butyl-1-[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl pyrimidin-4(1H)-one.

USE: Angiotensin II antagonists. Useful for medical treatments of hypertension, congestive heart failure, and high ocular internal pressure.

PROCESS: For example, a compound of general formula III and a compound of general formula IV are reacted, to obtain the corresponding compound of general formula I (general formula V).


Inventors:
ERITSUKU II AREN
UIRIAMU JIEE GURIINRII
AASAA EE PACHIETSUTO
TOMASU EFU UORUSHIYU
PURASAN KEE CHIYAKURABUAATEI
Application Number:
JP22643990A
Publication Date:
August 28, 1991
Filing Date:
August 28, 1990
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
A61K31/505; A61P9/12; A61P27/02; C07D239/36; C07D239/42; C07D239/52; C07D403/10; C07D403/12; C07F9/46; (IPC1-7): A61K31/505; C07D239/36; C07D239/42; C07D239/52; C07D403/10; C07D403/12; C07F9/46
Attorney, Agent or Firm:
Masao Okabe (6 others)