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Title:
NEW ARGININAL DERIVATIVE
Document Type and Number:
Japanese Patent JP2000281640
Kind Code:
A
Abstract:

To obtain a new compound having an excellent inhibiting activity to many kinds of proteases and useful as a protease inhibitor.

This compound is represented by formula I [R1 is H or an amino protecting group; R2 is H, an alkyl or the like; R3 is formyl, a halogenomethyl or the like; R4 is H or an amino protecting group; A is a (substituted)1-5C alkylene], e.g. 4-(N-t-butoxycarbonyl)aminodibenzoyl-L-valyl-NG- nitroargininal semicarbazone. A starting raw material readily prepared from arginine according to a conventional method can be used to produce the above compound according to a conventional method for peptide synthesis. Specifically, the amino protecting group of a compound represented by formula II is deprotected under acidic conditions and the resultant compound is then reacted with an active derivative of an aromatic carboxylic acid represented by formula III (L is a leaving group) or the protecting group is removed according to a suitable method and the obtained compound is further formylated.


Inventors:
NUNOSAWA TETSUJI
KATSUYAMA JUNJI
ISHIZUKA MAKOTO
SANADA KUNIO
KOBASHI KYOICHI
FURUICHI YASUHIRO
Application Number:
JP8743499A
Publication Date:
October 10, 2000
Filing Date:
March 30, 1999
Export Citation:
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Assignee:
FUJI CHEM IND CO LTD
EIJIIN KENKYUSHO KK
International Classes:
C12N9/99; A61K31/00; A61K31/165; A61K31/175; A61P43/00; C07C279/12; C07C279/36; C07C281/10; (IPC1-7): C07C279/12; A61K31/00; A61K31/165; A61K31/175; C07C279/36; C07C281/10; C12N9/99