Patent ID: 6262069
Filing Date: 2001-07-17
Classification: A61K,C07D,C07K

Abstract:
A serine protease inhibitor compound of formula I ##STR23##where R.sub.1 is hydrogen, halo, cyano, nitro, hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl;R.sub.2 is hydrogen, halo, methyl, amino, hydroxy or oxo;andR is X--X--Y(R.sub.7)--L--Lp(D)nwherein each X independently is a C, N, O or S atom or a CO, CR.sub.1, C (R.sub.1).sub.2 or NR.sub.1 group, at least one X being C, CO, CR.sub.1 or a C(R.sub.1).sub.2 group;Y (the .alpha.-atom) is a nitrogen atom or a CR.sub.1 group or Y and L taken together form a cyclic group;R.sub.7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R.sub.1 ;L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group;Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl, cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R.sub.1 groups;D is a hydrogen bond donor group; and n is 0, 1 or 2;or a physiologically tolerable salt thereof.