Title:
GUANIDINE DERIVATIVE AND ENZYME INHIBITOR
Document Type and Number:
Japanese Patent JPH01139561
Kind Code:
A
Abstract:
NEW MATERIAL:A guanidine derivative shown by formula I [n is 3 or 4; R<1> and R<2> are H (with the proviso that R<1> and R<2> are not simultaneously H), 1-4C alkyl, phenyl (may be replaced with hydroxycarbonyl or alkoxycarbonyl) or R<1> and R<2> are bonded to form piperidyl (may be replaced with alkyl, benzyl or alkoxycarbonyl)] or a salt thereof. EXAMPLE:N<2>-(trans-4-Aminomethylcyclohexylcarbonyl)-L-arginine 4- methylpiperidinoamide. USE:A protease inhibitor. PREPARATION:For example, a compound shown by formula (7) is reacted with a compound shown by formula (8) to give a compound shown by formula (9), which is then reacted with a compound shown by the formula HN(R<1>)R<2> and hydrobromic acid to give a compound shown by formula (10). This compound is further reacted with a compound shown by formula (13) to give a compound shown by formula (11), which is then treated with a solution of trifluoromethanesulfonic acid-thioanisole-trifluoroacetic acid to give a compound shown by formula (12).
Inventors:
OKADA YOSHIO
OKUMIYA AKIKO
TENOU NAOKI
WANAKA KEIKO
NAITO TAKETOSHI
OKUMIYA AKIKO
TENOU NAOKI
WANAKA KEIKO
NAITO TAKETOSHI
Application Number:
JP29614987A
Publication Date:
June 01, 1989
Filing Date:
November 26, 1987
Export Citation:
Assignee:
SHOWA DENKO KK
OKAMOTO AKIYOSHI
OKAMOTO AKIYOSHI
International Classes:
C07C279/14; A61K31/16; A61P7/02; A61P29/00; A61P37/08; A61P43/00; C07C67/00; C07C239/00; C12N9/99; (IPC1-7): A61K31/16; C07C129/12; C12N9/99
Attorney, Agent or Firm:
Yaguchi flat