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Title:
HETEROCYCLICALLY SUBSTITUTED PHENYLACETIC ACID DERIVATIVE
Document Type and Number:
Japanese Patent JP3225086
Kind Code:
B2
Abstract:

PURPOSE: To provide a novel compd. which has angiotensin II antagonism and is useful as a blood pressure lowering agent and antiatheromsclerosis agent.
CONSTITUTION: This compd. is expressed by formula I [A is a 5-membered arom. heterocycle, such as imidazole bonded via N, etc.; B is -(CH2)1-4, etc.; D is H, halogen, NO2, OH, CF3, etc.; R1, R2 are each H, OH, up to 10C alkyl, etc.; R3 is tetrazolyl, -C≡N, -CO-R18 (R18 is OH, phenoxy, etc.), etc.], for example, t-butyl 2-[4-(2-butyl-4-chloro-5-formyl-imidazol-1-ylmethyl)phenyl]2- cyclopentyl-acetate. The compd. of formula I is obtd. by bringing the compd. of formula II (X is a dissociation group; R3' is 1-6C alkoxycarbonyl, cyano) and the compd. of the formula, A-H into reaction at a temp. of -30 to 100°C in a protective gaseous atmosphere in the presence of a base (e.g. NaH) at need in at inert solvent (e.g. DMF).


Inventors:
Ulrich Michelle
Claus Morse
Jürgen Drezsel
Rudolph Hanko
Walter Hiyupusyu
Michael Matsuke
Ulrich Niebner
Siegfried Radaz
Thomas Clemmer
Matthias Miular-Greeman
Hans-Peter Bellemann
Martin Boyk
Stanislav Katsuda
Shute Juan Juan Ball Isle
Application Number:
JP13177092A
Publication Date:
November 05, 2001
Filing Date:
April 24, 1992
Export Citation:
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Assignee:
Bayer Actien Gezershyaft
International Classes:
A61K31/41; A61K31/415; A61K31/4184; A61P7/10; A61P9/00; A61P9/08; A61P9/10; A61P9/12; A61P11/08; A61P13/02; A61P13/12; A61P15/00; A61P43/00; C07D207/30; C07D231/12; C07D231/14; C07D231/56; C07D233/54; C07D233/60; C07D233/64; C07D233/68; C07D233/90; C07D235/06; A61K31/40; C07D235/08; C07D235/14; C07D235/16; C07D235/18; C07D249/04; C07D249/08; C07D249/12; C07D249/14; C07D249/18; C07D403/10; C07D405/06; C07D409/06; C07D471/04; C07D521/00; (IPC1-7): C07D207/30; C07D231/14; C07D231/56; C07D233/64; C07D233/68; C07D233/90; C07D235/06; C07D235/16; C07D249/04; C07D249/18; C07D403/10; C07D405/06; C07D409/06; C07D471/04
Domestic Patent References:
JP55313A
JP6419067A
JP4283569A
JP5504359A
Other References:
Farmaco,Ed.Sci.,Vol.43,No.7−8,p.597−611(1988)
J.Heterocycl.Chem.,Vol.16,No.7,p.1443−7(1979)
J.Med.Chem.,Vol.33,No.5,p.1312−29(1990)
Attorney, Agent or Firm:
Heikichi Odashima



 
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