公开(公告)号：EP0836616A1

公开(公告)日：1998-04-22

申请号：EP96924886.0

申请日：1996-07-04

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： FEHR, Theodor ,  OBERER, Lukas ,  QUESNIAUX RYFFEL, Valerie ,  SANGLIER, Jean-Jacques ,  SCHULER, Walter ,  SEDRANI, Richard

IPC分类号： C12P21 ,  A61K31 ,  A61P29 ,  A61P37 ,  C07D309 ,  C07D491 ,  C07D498 ,  C07D519 ,  C07K5 ,  C12N1 ,  A61K38 ,  C12R1

CPC分类号： C07D491/10 ,  A61K38/00 ,  C07D309/10 ,  C07D309/30 ,  C07K5/06052 ,  C12R1/465

摘要： A novel class of macrolides in which i) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/or ii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic α-amino acid residue; and/or iii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic α-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula (IX) is provided having immunosuppressant and anti-inflammatory properties and protected and ring-open forms thereof.