EP 1345931 A2 20030924 - CYSTEINE PROTEASE INHIBITORS
Title (en)
CYSTEINE PROTEASE INHIBITORS
Title (de)
CYSTEIN PROTEASE INHIBITOREN
Title (fr)
INHIBITEURS DE CYSTEINE PROTEASE
Publication
Application
Priority
- US 0146486 W 20011116
- US 25284000 P 20001117
Abstract (en)
[origin: WO0240462A2] Compound s of the formula A compound of the formula IV where R1 is R'-C(=O)- or R'-S(=O)2-R´ is X, = O, S, NH, W, Y, Z = CH, N;R'' = single or multiple ring substitution combinations taken from: H, C1-7-alkyl, C3-6-cycloalkyl, OH, SH, amine, halogen; R3 = C1-7-alkyl, C2-C7 alkenyl, C3-7-cycloalkyl, Ar, Ar-C1-7-alkyl C3-6cycloalkyl; R4 = H, C1-7-alkyl, C3-7-cycloalkyl; C2-7alkenyl, Ar, Ar-C1-C7-alkyl; R5 = C1-7-alkyl, hydroxy- or halo-substituted C1-C7alkylhalogen, Ar-C1-7-alkyl, C0-3-alkyl-CONR3R4 or a bulky amine function; R6 = H, C1-7-alkyl, Ar-C1-7-alkyl, C1-3-alkyl-SO2-Rix, C1-3-alkyl-C(O)-NHRix or CH2XAr; and pharmaceutically acceptable salts thereof have utility as inhibitors of cysteine proteases such as cathepsin S and falcipain.
[origin: WO0240462A2] Compound s of the formula A compound of the formula IV where R1 is R'-C(=O)- or R'-S(=O)2-R' is X, = O, S, NH, W, Y, Z = CH, N;R'' = single or multiple ring substitution combinations taken from: H, C1-7-alkyl, C3-6-cycloalkyl, OH, SH, amine, halogen; R3 = C1-7-alkyl, C2-C7 alkenyl, C3-7-cycloalkyl, Ar, Ar-C1-7-alkyl C3-6cycloalkyl; R4 = H, C1-7-alkyl, C3-7-cycloalkyl; C2-7alkenyl, Ar, Ar-C1-C7-alkyl; R5 = C1-7-alkyl, hydroxy- or halo-substituted C1-C7alkylhalogen, Ar-C1-7-alkyl, C0-3-alkyl-CONR3R4 or a bulky amine function; R6 = H, C1-7-alkyl, Ar-C1-7-alkyl, C1-3-alkyl-SO2-Rix, C1-3-alkyl-C(O)-NHRix or CH2XAr; and pharmaceutically acceptable salts thereof have utility as inhibitors of cysteine proteases such as cathepsin S and falcipain.
IPC 1-7
IPC 8 full level
C12N 9/99 (2006.01); A61K 31/351 (2006.01); A61P 25/00 (2006.01); A61P 29/00 (2006.01); A61P 31/04 (2006.01); A61P 33/02 (2006.01); A61P 33/06 (2006.01); A61P 33/08 (2006.01); A61P 37/02 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); C07D 307/22 (2006.01); C07D 307/32 (2006.01); C07D 307/68 (2006.01); C07D 307/85 (2006.01); C07D 309/14 (2006.01); C07D 309/30 (2006.01); C07D 405/12 (2006.01); C07D 405/14 (2006.01); C07D 407/12 (2006.01); C07D 409/12 (2006.01)
CPC (source: EP)
A61P 25/00 (2017.12); A61P 29/00 (2017.12); A61P 31/04 (2017.12); A61P 33/02 (2017.12); A61P 33/06 (2017.12); A61P 33/08 (2017.12); A61P 37/02 (2017.12); A61P 37/08 (2017.12); A61P 43/00 (2017.12); C07D 307/22 (2013.01); C07D 307/32 (2013.01); C07D 307/68 (2013.01); C07D 307/85 (2013.01); C07D 309/14 (2013.01); C07D 309/30 (2013.01); C07D 405/12 (2013.01); C07D 405/14 (2013.01); C07D 409/12 (2013.01)
Citation (search report)
See references of WO 0240462A2
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR
DOCDB simple family (publication)
WO 0240462 A2 20020523; WO 0240462 A3 20030213; AU 2722202 A 20020527; CA 2428863 A1 20020523; EP 1345931 A2 20030924; IL 155961 A0 20031223; JP 2004513942 A 20040513
DOCDB simple family (application)
US 0146486 W 20011116; AU 2722202 A 20011116; CA 2428863 A 20011116; EP 01996110 A 20011116; IL 15596101 A 20011116; JP 2002543473 A 20011116