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Title:
BENZYLOXY-SUBSTITUTED PHENYLGLYCINOLAMIDE
Document Type and Number:
Japanese Patent JPH1059915
Kind Code:
A
Abstract:

To obtain a new compound useful for the suppression of atherosclerosis and coronary heart diseases and capable of being utilized as an antiatheroselerotic medicine.

A benzyloxy-substituted penylglycinolamide of formula I (A is a four to eight-membered carbon ring, etc.; X is a single bond or a group of formula II; D and E are each H, a 3-8C cycloalkyl, etc.; R1 is a 3-8C cycloalky, etc.; R2 is H, a 4C alkyl, etc.; R3 is H, CH2OH; R4 is hydroxy, a halogen, etc.) and its salt. The compound of formula I is obtained by activating the functional carboxyl group of a carboxylic acid of formula III and subsequently reacting the activated compound with a compound of formula IV in the presence of a base and/or an auxiliary agent in an inactive solvent (e.g. an ether compound) at a reaction temperature of 0-150°C generally in the atmospheric pressure in a protecting gas atmosphere. The base used herein is usually an inorganic or organic base, and is used in an amount of 0.6-5 moles per mole of the compound of formula III.


Inventors:
GOLDMANN SIEGFRIED DR
MUELLER ULRICH DR
CONNELL RICHARD DR
BISCHOFF HILMAR DR
DENZER DIRK DR
GRUETZMANN RUDI DR
BEUCK MARTIN DR
Application Number:
JP10682297A
Publication Date:
March 03, 1998
Filing Date:
April 10, 1997
Export Citation:
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Assignee:
BAYER AG
International Classes:
A61K31/165; A61K31/415; A61K31/4184; A61K31/44; A61K31/4402; A61K31/445; A61K31/454; A61K31/47; A61K31/535; A61K31/5355; A61K31/5375; A61P9/00; A61P9/10; C07C233/22; C07D295/16; C07C235/34; C07C235/54; C07C235/56; C07C323/50; C07D213/30; C07D213/74; C07D215/26; C07D233/84; C07D235/28; C07D295/18; C07D295/185; (IPC1-7): C07C235/34; A61K31/165; A61K31/415; A61K31/44; A61K31/445; A61K31/47; A61K31/535; C07C323/50; C07D213/30; C07D213/74; C07D215/26; C07D233/84; C07D235/28; C07D295/16
Attorney, Agent or Firm:
Heiyoshi Odashima