公开(公告)号：DE4308096A1

公开(公告)日：1994-09-15

申请号：DE4308096

申请日：1993-03-13

Applicant: HOECHST AG

Inventor： BUDT KARL-HEINZ DR ,  STOWASSER BERND DR ,  PEYMAN ANUSCHIRWAN DR ,  KNOLLE JOCHEN DR ,  WINKLER IRVIN DR ,  BERSCHEID HANS-GERD DR

IPC: C07D295/08 ,  A61K31/215 ,  A61K31/22 ,  A61K31/27 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/66 ,  A61K38/00 ,  A61P31/12 ,  A61P37/00 ,  A61P43/00 ,  C07C317/44 ,  C07C323/52 ,  C07D207/16 ,  C07D213/40 ,  C07D215/48 ,  C07D235/14 ,  C07D277/04 ,  C07D401/12 ,  C07F9/53 ,  C07K5/02 ,  C07K7/02 ,  C07C317/50 ,  C07F9/30 ,  C07D521/00 ,  A61K37/02

Abstract: PCT No. PCT/EP94/00561 Sec. 371 Date Sep. 12, 1995 Sec. 102(e) Date Sep. 12, 1995 PCT Filed Feb. 25, 1994 PCT Pub. No. WO94/21604 PCT Pub. Date Sep. 29, 1994The invention concerns prodrugs of enzyme inhibitors in which at least one OH- group in the enzyme inhibitor has been converted into a derivative grouping of the formula III, IV or V: (III) (IV) (V) in which the groups R11 to R25 and s,l, m, o, q, and r are as defined in the description. Such prodrugs exhibit an improved solubility in water and improved pharmaco-kinetic characteristics.