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.

公开(公告)号：DE4030350A1

公开(公告)日：1991-04-11

申请号：DE4030350

申请日：1990-09-26

Applicant: HOECHST AG

Inventor： BUDT KARL-HEINZ DR ,  STOWASSER BERND DR ,  KNOLLE JOCHEN DR ,  RUPPERT DIETER DR ,  MEICHSNER CHRISTOPH DR ,  PAESSENS ARNOLD DR ,  HANSEN JUTTA DR

IPC: A61K38/00 ,  C07C211/27 ,  C07C237/10 ,  C07C237/22 ,  C07C271/20 ,  C07C271/22 ,  C07C317/44 ,  C07C323/60 ,  C07D211/58 ,  C07D211/96 ,  C07D213/56 ,  C07D213/70 ,  C07D215/48 ,  C07D217/26 ,  C07D333/24 ,  C07D521/00 ,  C07K5/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078 ,  C07K5/083

Abstract: Peptides of formula (I) and their salts are new, where Y = O, S, CHR5''R6'' or NR7, l = 0-1. A = D-(E)n-(F)o-(G)p-, A' = D'-(E')n'-(F')o'-(G')p'-, E,E',F,F',G,G' = natural or other amino acid, aza-amino acid or iminoacid, n,n',o,o',p,p' = 0-1. D = R1 or is a gp. R1-NR8,-CR9R10-CO-, R1'-NRT8'-CR9'R10'-CO-, R1-CHR11-CHR9-CO-, R1'-CRR11'-CHR9'-CO- or R1-O-CHR9-CO-. R1, R1' = a1) H, carboxy, alkyl (opt. substd.), mono-, bi- or tricyclic cycloalkyl or cycloalkyl alkyl (opt. substd.) aryl, aralkyl, aryloxyalkyl or aryl-cycloalkyl (in which the aryl gps. are opt. substd.), Het, Het-alkyl, Het-cycloalkyl, Het-cycloalkylalkyl, Het-cycloalkoxy-aklyl, Het-thioalkyl, Het-thiocycloalkyl, Het-thiocycloalkyl-alkyl (Het = 5-7 membered monocyclic or 8-10 membered bicyclic ring system, opt. benzyo-fused contg. 1-4 of N,O,S,NO,SO or SO2 and opt. substd. by NR12R13; a2) R1a-W or R1a'-W' (R1a, R1a' = as in a1, W, W' = CO, CS, O-CO, SO2, SO, S, NHSO2, NHCO, CHOH, NOH or CO-V where V = 1-10 unit peptide) or R1a, R1a', together with R11, R11' form a mono or bicyclic 5-12 membered ring opt. contg. 1S atom (opt. oxidised). a3) a glycosyl residue. R2, R2' = as R1, R1' in a1) and a2) or together with R4, R4' forms a 5-12 membered ring or together with R3, R3' forms a 3-12 membered ring. R3, R3' = H or 1-3C alkyl, R4,R4' = H or 1-8C alkyl, R5,R5',R5'' = H, OH, NH2 or carboxy or together with R6, R6' or R6'' form a keto gp. R6,R6',R6'' = H or 1-6C alkyl or when l = 0 they can form a bond, R7 = H, OH or 1-6C alkyl.

公开(公告)号：CZ9004711A3

公开(公告)日：2000-08-16

申请号：CZ471190

申请日：1990-09-27

Applicant: HOECHST AG

Inventor： BUDT KARL-HEINZ DR ,  STOWASSER BERND DR ,  RUPPERT DIETER DR ,  MEICHSNER CHRISTOPH DR ,  PAESSENS ARNOLD DR ,  HANSEN JUTTA DR ,  KNOLLE JOCHEN DR

IPC: A61K38/55 ,  A61K31/13 ,  A61K31/16 ,  A61K31/27 ,  A61K38/00 ,  A61K38/04 ,  A61P31/12 ,  C07C211/20 ,  C07C211/27 ,  C07C215/18 ,  C07C237/10 ,  C07C237/22 ,  C07C271/10 ,  C07C271/20 ,  C07C271/22 ,  C07C317/28 ,  C07C317/44 ,  C07C323/58 ,  C07C323/60 ,  C07D211/58 ,  C07D211/96 ,  C07D213/34 ,  C07D213/40 ,  C07D213/50 ,  C07D213/56 ,  C07D213/70 ,  C07D213/89 ,  C07D215/48 ,  C07D217/26 ,  C07D317/50 ,  C07D333/22 ,  C07D333/24 ,  C07D521/00 ,  C07F7/18 ,  C07K1/113 ,  C07K5/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K7/06 ,  C07K9/00 ,  C07K14/81

CPC classification number: C07D213/40 ,  A61K38/00 ,  C07C211/20 ,  C07C211/27 ,  C07C215/18 ,  C07C237/10 ,  C07C237/22 ,  C07C271/20 ,  C07C271/22 ,  C07C317/28 ,  C07C317/44 ,  C07C323/58 ,  C07C323/60 ,  C07C2601/14 ,  C07D211/58 ,  C07D211/96 ,  C07D213/34 ,  C07D213/50 ,  C07D213/56 ,  C07D213/70 ,  C07D213/89 ,  C07D215/48 ,  C07D217/26 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D317/50 ,  C07D333/22 ,  C07D333/24 ,  C07F7/1852 ,  C07K5/00 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06156 ,  C07K5/081 ,  C07K9/001

公开(公告)号：CZ471190A3

公开(公告)日：2000-08-16

申请号：CZ471190

申请日：1990-09-27

Applicant: HOECHST AG

Inventor： BUDT KARL-HEINZ DR ,  STOWASSER BERND DR ,  RUPPERT DIETER DR ,  MEICHSNER CHRISTOPH DR ,  PAESSENS ARNOLD DR ,  HANSEN JUTTA DR ,  KNOLLE JOCHEN DR

IPC: A61K38/55 ,  A61K31/13 ,  A61K31/16 ,  A61K31/27 ,  A61K38/00 ,  A61K38/04 ,  A61P31/12 ,  C07C211/20 ,  C07C211/27 ,  C07C215/18 ,  C07C237/10 ,  C07C237/22 ,  C07C271/10 ,  C07C271/20 ,  C07C271/22 ,  C07C317/28 ,  C07C317/44 ,  C07C323/58 ,  C07C323/60 ,  C07D211/58 ,  C07D211/96 ,  C07D213/34 ,  C07D213/40 ,  C07D213/50 ,  C07D213/56 ,  C07D213/70 ,  C07D213/89 ,  C07D215/48 ,  C07D217/26 ,  C07D317/50 ,  C07D333/22 ,  C07D333/24 ,  C07D521/00 ,  C07F7/18 ,  C07K1/113 ,  C07K5/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K7/06 ,  C07K9/00 ,  C07K14/81

Abstract: The present invention relates to a compound of the formula I in which A, Y, R , R , R , R , R , l, m and the corresponding radicals with are defined as indicated in the description, a process for the preparation thereof, and the use thereof for inhibiting retroviral proteases.