公开(公告)号：WO9822496A3

公开(公告)日：1998-07-16

申请号：PCT/EP9706189

申请日：1997-11-07

Applicant: HOFFMANN LA ROCHE

Inventor： ATTWOOD MICHAEL RICHARD ,  HURST DAVID NIGEL ,  JONES PHILIP STEPHEN ,  KAY PAUL BRITTAIN ,  RAYNHAM TONY MICHAEL ,  WILSON FRANCIS XAVIER

IPC: C12N15/09 ,  A01N43/34 ,  A01N43/36 ,  A61K38/00 ,  A61P31/12 ,  A61P31/14 ,  C07C205/04 ,  C07C205/45 ,  C07C271/18 ,  C07D207/12 ,  C07D207/20 ,  C07D211/70 ,  C07D223/04 ,  C07D227/04 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07K7/06 ,  A61K38/08

CPC classification number: C07K7/06 ,  A01N43/34 ,  A01N43/36 ,  A61K38/00 ,  C07D207/12 ,  C07D207/20 ,  C07D211/70 ,  C07D223/04 ,  C07D227/04 ,  C07D405/10 ,  C07D409/10

Abstract: The invention provides amino acid derivatives of formula (I) wherein E represents CHO or B(OH)2; R1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl; R2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; and R3 represents hydrogen or lower alkyl; or R?2 and R3¿ together represent di- or trimethylene optionally substituted by hydroxy; R4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl; R5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl; R6 represents hydrogen or lower alkyl; R7 represents lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl; R8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; and R9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower alkoxycarbonyl, and salts of acidic compounds of formula (I) with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.