EP 0652893 A1 19950517 - KININOGENASE INHIBITORS.
Title (en)
KININOGENASE INHIBITORS.
Title (de)
KININOGENASE-INHIBITOREN.
Title (fr)
INHIBITEURS DE LA KININOGENASE.
Publication
Application
Priority
- GB 9101479 W 19910902
- GB 9019558 A 19900907
Abstract (en)
[origin: WO9204371A1] Kininogenase inhibitors, optimally not exceeding the size of a hexapeptide, represented by (II), wherein A and B = amino acyl (including amino acyl analogue) the same or different forming a dipeptide group the amino acid of A carrying a terminal group and being any amino or imino-acid residue (but preferably of D-configuration) and of B being a lipophilic amino-acid residue of D- or L-configuration but not proline or a proline analogue, or a conformational analogue of said dipeptide group wherein the peptide link is replaced by -CH2-NH- ('reduced'), -CH(OH)-CH2- ('hydroxy'), -CO-CH2 ('keto'), -CH2-CH2- ('hydrocarbon') or other conformational mimic of the peptide bond and in (III) the side chain R<1> is that of a basic amino acid or amino acid analogue (preferably of L-configuration), and R is H or lower alkyl(C1-C4) or C< alpha > or the peptide link comprising -N(R)- is replaced leading to a conformational mimic as above; Y = a binding enhancing or carbonyl activating group preferably selected from H (when A or B must be cyclohexylalanine, preferably D if at A or L if at B) or alkyl (C1-C20) or fluoroalkyl (C2-C12); substituted oxymethylene; thiomethylene; sulphoxymethylene; sulphonylmethylene; aminomethylene; hydrazino-methylene; -CH2-Het (where Het = a substituted or unsubstituted heterocycle); substituted amino (but when the resulting compound is a secondary alkylamide B must not be phenylalanine); an amino-acid group or its ester or amide; a carboxylic secondary amide or primary amide, when B must be cyclohexylalanine or adamantylalanine or other bulky lipophilic, non-aromatic amino-acid (not Ala Leu Ile Val Nva Met Nle Phe Tyr Trp Nal (1)); tertiary-carboxamide; carboxy-alkyl group or its ester or amide or amino acyl derivative.
IPC 1-7
IPC 8 full level
A61K 38/55 (2006.01); A61P 9/02 (2006.01); A61P 25/00 (2006.01); A61P 25/04 (2006.01); A61P 29/00 (2006.01); A61P 37/08 (2006.01); C07K 5/00 (2006.01); C07K 5/02 (2006.01); C07K 5/06 (2006.01); C07K 5/08 (2006.01); C07K 5/10 (2006.01); C07K 7/06 (2006.01); C07K 14/81 (2006.01)
CPC (source: EP)
A61P 9/02 (2017.12); A61P 25/00 (2017.12); A61P 25/04 (2017.12); A61P 29/00 (2017.12); A61P 37/08 (2017.12); C07K 5/02 (2013.01); C07K 5/0227 (2013.01)
Citation (search report)
See references of WO 9204371A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IT LI LU NL SE
DOCDB simple family (publication)
WO 9204371 A1 19920319; AU 8438791 A 19920330; CA 2090858 A1 19920308; EP 0652893 A1 19950517; FI 930946 A0 19930303; FI 930946 A 19930426; GB 9019558 D0 19901024; HU 9300610 D0 19930528; HU T64084 A 19931129; IE 913120 A1 19920311; JP H06501461 A 19940217; MC 2313 A1 19930927; NO 930731 D0 19930226; NO 930731 L 19930507; PT 98885 A 19920831; ZA 917096 B 19920429
DOCDB simple family (application)
GB 9101479 W 19910902; AU 8438791 A 19910902; CA 2090858 A 19910902; EP 91915557 A 19910902; FI 930946 A 19930303; GB 9019558 A 19900907; HU 61093 A 19910902; IE 312091 A 19910905; JP 51480291 A 19910902; MC 2313 D 19910902; NO 930731 A 19930226; PT 9888591 A 19910906; ZA 917096 A 19910906