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Title:
PHENYLALANINE DERIVATIVE AND PROTEINASE INHIBITING AGENT
Document Type and Number:
Japanese Patent JP63233963
Kind Code:
A
Abstract:

NEW MATERIAL:A compound expressed by formula I [X is -COY (Y is lower alkyl, lower alkenyl, etc.) or -SO2Z (Z is lower alkyl or phenyl); R1 and R2 are H, alkyl, pyridyl, etc.; n is 4 or 10].

EXAMPLE: N-(trans-4-Aminomethylcyclohexylcarbonyl)-4-acetylamino-L-phenyla lanine 4-ethoxycarbonylmethylanilide hydrochloride.

USE: A proteinase inhibiting agent exhibiting very strong inhibiting action to plasmin, kallikrein, trypsin and urokinase.

PREPARATION: The compound expressed by formula I is obtained by carrying out reaction using a compound expressed by formula II (Boc is tert. butyloxycarbonyl) as a starting material one after another to afford a compound expressed by formula III (Y' is formula IV) and carrying out deprotection of the resultant compound.


Inventors:
Okamoto, Akiyoshi
Okada, Yoshio
Okumiya, Akiko
Naito, Taketoshi
Kimura, Yoshio
Yamada, Morihiko
Katsuura, Yasuhiro
Nojima, Hiroshi
Shishikura, Takashi
Application Number:
JP1987000068015
Publication Date:
September 29, 1988
Filing Date:
March 24, 1987
Export Citation:
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Assignee:
SHOWA DENKO KK
OKAMOTO AKIYOSHI
International Classes:
C12N9/99; A61K31/165; A61K31/17; A61K31/195; A61K31/198; A61K31/22; A61K31/245; A61K31/27; A61K31/44; A61K31/4402; A61K31/4418; A61K31/445; A61K31/451; A61P1/00; A61P7/04; A61P29/00; A61P43/00; C07C67/00; C07C231/00; C07C237/24; C07C239/00; C07C271/54; C07C275/42; C07C311/08; C07C311/19; C07C311/21; C07D211/34; C07D213/40; C07D213/75; C12N9/99; A61K31/165; A61K31/17; A61K31/185; A61K31/21; A61K31/44; A61K31/4402; A61K31/4418; A61K31/445; A61K31/451; A61P1/00; A61P7/00; A61P29/00; A61P43/00; C07C67/00; C07C231/00; C07C237/00; C07C239/00; C07C271/00; C07C275/00; C07C311/00; C07D211/00; C07D213/00; (IPC1-7): A61K31/165; A61K31/17; A61K31/195; A61K31/22; A61K31/245; A61K31/27; A61K31/44; A61K31/445; C07C103/76; C07C125/065; C07C127/19; C07C143/75; C07C143/79; C07D211/34; C07D213/40; C07D213/75; C12N9/99