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1. (WO1998050420) SERINE PROTEASE INHIBITORS

Pub. No.:    WO/1998/050420    International Application No.:    PCT/EP1998/002587
Publication Date: Fri Nov 13 00:59:59 CET 1998 International Filing Date: Wed Apr 29 01:59:59 CEST 1998
IPC: A61K 38/00
C07K 5/02
Applicants: AKZO NOBEL N.V.
ADANG, Anton, Egbert, Peter
Inventors: ADANG, Anton, Egbert, Peter
Title: SERINE PROTEASE INHIBITORS
Abstract:
The invention relates to a compound having the formula (I): R1SO2-B-X-Z-C(O)-Y, B is a bond, an amino acid of the formula -NH-CH[(CH2)pC(O)OH]-C(O)- or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, threonine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, -NR2-CH2-C(O)- or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH¿2?, or halogen; Z is lysine or 4-aminocyclohexylglycine. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases. The variable R?1¿ and Y are defined in claim 1.