PHENYLALANINE DERIVATIVE AND PROTEASE INHIBITOR

Japanese Patent JPS63238051

A

NEW MATERIAL:A compound shown by formula I [A is H2H- or group shown by formula II; B is group shown by formula II or -C(CH2)2- (n is 3W5); X is H, hydroxyl or nitro; Y is group shown by formula IV (R1 and R2 are H, phenyl or 1W4C alkyl)].

EXAMPLE: N-(5-Aminovaleryl)-L-phenylalanine 4-benzoylanilide.

USE: A protease inhibitor having extremely strong inhibitory activity against plasmin, kallikrein, trypsin and urokinase.

PREPARATION: A compound shown by formula V (Boc is t-butyloxycarbonyl) as a starting substance is successively reacted to give a compound shown by formula VI, which is then deprotected by the use of dioxane to give a compound shown by formula I.

OKAMOTO AKIYOSHI
OKADA YOSHIO
OKUMIYA AKIKO
NAITO TAKETOSHI
KIMURA YOSHIO
YAMADA MORIHIKO
ONO TOKUO
KATSUURA YASUHIRO
NOJIMA HIROSHI
SHISHIKURA TAKASHI

JP7174287A

October 04, 1988

March 27, 1987

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SHOWA DENKO KK
OKAMOTO AKIYOSHI

C12N9/99; A61K31/165; A61K31/195; A61K31/198; A61K31/22; A61K31/245; A61K31/40; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/4418; A61K31/445; A61K31/451; A61P1/00; A61P7/04; A61P29/00; A61P43/00; C07C67/00; C07C237/12; C07C237/22; C07C237/24; C07C237/36; C07C239/00; C07C257/14; C07C279/14; C07C279/18; C07D211/34; C07D213/40; C07D213/75; C07D295/18; C07K5/06; C07K14/81; (IPC1-7): A61K31/165; A61K31/195; A61K31/22; A61K31/245; A61K31/40; A61K31/44; A61K31/445; C07C103/50; C07C103/737; C07C103/76; C07C123/00; C07C129/12; C07D211/34; C07D213/40; C07D213/75; C07D295/18; C07K5/06; C12N9/99

Aoki Akira

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